tag:blogger.com,1999:blog-34657622493528108712024-03-06T12:00:43.775-08:00Drug LiteratureAll About DrugsUnknownnoreply@blogger.comBlogger42125tag:blogger.com,1999:blog-3465762249352810871.post-42161729512975685102016-12-08T23:35:00.001-08:002016-12-08T23:35:43.766-08:00Lactulose<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Lactulose<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">3.3g/5ml
Syrup<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Drug
Category:</span></b><span style="font-family: "Arial","sans-serif";"> Stimulant
Laxative / Osmotically acting laxatives.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Brand
Name:</span></b><span style="font-family: "Arial","sans-serif";"> Duphalac<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Pharmaceutical
Form and Composition<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Lactulose
is an oral solution. It is a clear, viscous liquid, colorless to brownish
yellow. Lactulose oral solution does not contain any excipients, but may
contain small amounts of related sugars (e.g. lactose, galactose, epilactose, and
fructose) derived from the route of synthesis.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Pharmacodynamics
<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">In
the colon lactulose is broken down by colonic bacteria into low-molecular
organic acids. These acids lead to a lowering of pH in the colonic lumen and
via an osmotic effect to an increase of the volume of the colonic contents.
These effects stimulate the peristalsis of the colon and return consistency of
the stools. The constipation is cleared and the physiological rhythm of the
colon is reinstated.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">In
hepatic encephalopathy (HE), the effect has been attributed to suppression of
proteolytic bacteria by an increase of acidophilic bacteria (e.g.
lactobacillus) trapping of ammonia in the ionic form by acidification of the
colonic contents, catharsis due to the low pH in the colon as well as osmotic
effect, and alteration of the bacterial nitrogen metabolism by stimulating the
bacteria to utilize ammonia for bacterial protein synthesis.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Within
this context, however, it should be realized that hyperammonemia alone cannot
explain the neuropsychiatric manifestation of HE. The ammonia however might
serve as a model compound for other nitrogenous substances.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Lactulose
as a prebiotic substance strengthens the growth of health promoting bacteria,
like Bifidobacterium and Lactobacillus, whereas potentially pathogenic
bacteria, like Clostridium and Escherichia coli may be suppressed. This may
lead to a more favorable balance of the intestinal flora.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Pharmacokinetic
Properties<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Lactulose
is poorly absorbed after oral administration and it reaches the colon
unchanged. There it is metabolized by the colonic bacterial flora. Metabolism
is complete at doses up to 25 – 50g or 40 -75ml; at higher dosages, a
proportion may be excreted unchanged.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Preclinical
Safety Data<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">The
results of acute, sub-chronic and chronic toxicity studies in various species
indicate that the compound has very low toxicity. The effects observed, appear
to be more related to the effect of bulk in the gastrointestinal tract than to
a more specific toxic activity.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">In
reproduction and teratology experiments in rabbits, rats or mice no adverse
effects were found.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Therapeutic
Indications<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<i><span style="font-family: "Arial","sans-serif";">For Constipation:</span></i><span style="font-family: "Arial","sans-serif";"> regulation of the physiological
rhythm of the colon. Indicated where a soft stool is considered of medical
benefit (hemorrhoids, post colonic/anal surgery). Hepatic <i>Encephalopathy (HE):</i> treatment and prevention of hepatic coma or
precoma.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Administration
and Dosage<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Lactulose
solution may be administered diluted or undiluted. <o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">A
single dose of lactulose should be swallowed in one and should not be kept in
mouth for an extended period of time. The dose should be adjusted according to
the individual needs of the patient. In case of single daily dose, this should
be taken at the same time, e.g. during breakfast. During the therapy with
laxatives it is recommended to drink sufficient amounts of fluids (1.5 – 2 liters,
equal to 6 – 8 glasses) during the day. <u>Dosing in constipation or where a
soft stool is considered of medical benefit. </u>It may be given as a single
daily dose or is two divided doses; in bottles the measuring cup may be used. After
a few days the starting dosage may be adjusted to the maintenance dose based
upon treatment response. Several days (2 – 3 days) of treatment may be needed
before treatment effect occurs.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">The
following dose is given: <o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<i><span style="font-family: "Arial","sans-serif";">Adult and adolescents:</span></i><span style="font-family: "Arial","sans-serif";"> Starting daily dose 15 – 45ml.
Maintenance daily dose 15 – 30ml. <o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<i><span style="font-family: "Arial","sans-serif";">Children (7 – 14years):</span></i><span style="font-family: "Arial","sans-serif";"> Starting daily dose 15ml. Maintenance
daily dose 10 - 15ml.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<i><span style="font-family: "Arial","sans-serif";">Children (1 – 6years):</span></i><span style="font-family: "Arial","sans-serif";"> Starting daily dose 5 – 10ml.
Maintenance daily dose 5 - 10ml.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<i><span style="font-family: "Arial","sans-serif";">Infants under 1 year</span></i><span style="font-family: "Arial","sans-serif";">: Starting daily dose up to 5ml.
Maintenance daily dose up to 5ml.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Dosing
in HE (for adults only)<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Starting
dose: 3 to 4 times daily 20 – 30g or 30 – 45ml. This dose may be adjusted to
the maintenance dose to achieve 2 to 3 soft stools per day.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Pediatric
population<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">The
safety and efficacy in children (newborn to 18years of age) with HE have not
been established. No data are available.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Elderly
patients and patients with renal or hepatic insufficiency<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">No
special dosage recommendations exist, since systemic exposure to lactulose is
negligible.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Contraindications<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">- Hypersensitivity to the active substance or
to any of the ingredients.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">-
Galactosemia<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">-
Gastrointestinal obstruction, digestive perforation or risk of digestive
perforation.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Special
Warnings and Precautions for use<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Consultation
of a physician is advised in case of:<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">-
Painful abdominal symptoms of undetermined cause before the treatment are
started.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">-
Insufficient therapeutic effect after several days.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Lactulose
should be administered with care to patients who are intolerant to lactose. <o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">The
dose normally used in constipation should not pose a problem for diabetics. The
dose used in the treatment of HE is usually much higher and may need to be
electrolyte balance. <o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Chronic
use of unadjusted doses and misuse can lead to diarrhea and disturbance of the
electrolyte balance.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">This
product contains lactose, galactose and small amounts of fructose. Therefore,
patients with the rate hereditary problem of galactose or fructose intolerance,
the Lapp lactase deficiency or glucose-galactose malabsorption should not take
this medicine.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Pediatric
Population<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Use
of laxatives in children should be exceptional and under medical supervision.
It should be taken into account that the defecation reflex could be disturbed
during the treatment.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Pregnancy<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">No
effects during pregnancy are anticipated, since systemic exposure to lactulose
is negligible.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Lactation<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">No
effects on the breastfed newborn/infant are anticipated, since the systemic
exposure of the breast-feeding woman to lactulose is negligible. Lactulose can
be used during breast-feeding.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Fertility<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">No
effects are to be expected, since systemic exposure to lactulose is negligible.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><i><span style="font-family: "Arial","sans-serif";">Effects
on ability to drive and use machines<o:p></o:p></span></i></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Lactulose
has no or negligible influence on the ability to drive and use machines.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Undesirable
Effects<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Flatulence
may occur during the first few days of treatment. As a rule it disappears after
a few days. Abdominal pain and vomiting may occur, as well as, nausea.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">When
dosages higher than instructed are used, abdominal pain and diarrhea may occur.
In such a case the dosage should be decreased.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">If
high doses (normally only associated with hepatic encephalopathy, HE) are used
for an extended period of time, the patient may experience an electrolyte
imbalance due to diarrhea.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Drug
Interaction<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Do
not use with any other gastrokinectic drugs or other laxatives. Concomitant use
may lead to severe diarrhea.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Overdose<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">If
the dose is too high, the following may occur:<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Symptom:
diarrhea and abdominal pain.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Treatment:
cessation of treatment or dose reduction. Extensive fluid loss by diarrhea or
vomiting may require correction of electrolyte disturbances.<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Shelf
life<o:p></o:p></span></b></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">3
years<o:p></o:p></span></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<br /></div>
<div class="MsoNoSpacing" style="text-align: justify;">
<b><span style="font-family: "Arial","sans-serif"; font-size: 14.0pt;">Storage
condition<o:p></o:p></span></b></div>
<br />
<div class="MsoNoSpacing" style="text-align: justify;">
<span style="font-family: "Arial","sans-serif";">Store
at temperatures not exceeding 25<sup>o</sup>C<o:p></o:p></span></div>
Unknownnoreply@blogger.com1tag:blogger.com,1999:blog-3465762249352810871.post-8534679994984189982014-12-27T01:45:00.000-08:002014-12-27T01:45:49.336-08:00Clopidogrel<div style="text-align: justify;">
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Clopidogrel</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">75mg
Tablet</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">300mg
Tablet</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Anti-Thrombotic
Agent</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGY:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Clopidogrel
is an inhibitor of ADP-induced platelet aggregation acting direct
inhibition of adenosine diphosphate (ADP) binding to its receptor and
of the subsequent ADP-mediated activation of the glycoprotein
GPIIb/IIIa complex.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Clopidogrel
is an inhibitor of platelet aggregation. A variety of drugs that
inhibit platelet function have been shown to decrease morbid events
in people with established atherosclerotic cardiovascular disease as
evidence by stroke or transient ischemic attacks, myocardial
infarction, or need for bypass or angioplasty. This indicates that
platelets participate in the initiation and/or evolution of these
events and that inhibiting them can reduce the event rate.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Clopidogrel
selectively inhibits the binding of adenosine diphosphate (ADP) to
its platelet receptor and the subsequent ADP mediated activation of
the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet
aggregation. Biotransformation of Clopidogrel is necessary to produce
inhibition of platelet aggregation, but as active metabolite
responsible for the activity of the drug has not been isolated.
Clopidogrel also inhibits platelet activation by released ADP.
Clopidogrel are affected for the remainder of their lifespan. Dose
dependent inhibition of platelet aggregation can be seen 2 hours
after oral single doses of Clopidogrel. Repeated doses of 75mg
Clopidogrel per day inhibit ADP induced platelet aggregation on the
first day, and inhibition reaches steady state between Day 3 and Day
7. At steady state, the average inhibition level observed with a dose
of 75 mg Clopidogrel per day was between 40% and 60%. Platelet
aggregation and bleeding time gradually return to baseline values
after treatment is discontinued, generally in about 5 days.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Absorption
and Distribution:</b> Clopidogrel is rapidly absorbed after oral
administration of repeated doses 75mg Clopidogrel (base), with peak
plasma levels (≡ 3mg/l)
of the main circulating metabolite occurring approximately 1 hour
after dosing. The pharmacokinetics of the main circulating metabolite
are linear (plasma concentrations increased in proportion to dose) in
the dose range of 50mg to 150mg of Clopidogrel. Absorption is at
least 50% based on urinary excretion of Clopidogrel-related
metabolites. Clopidogrel and the main circulating metabolite bind
reversibly in vitro to human plasma protein (98% and 94%,
respectively). The binding is nonsaturable in vitro up to a
concentration of 100mcg/ml.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Metabolism
and Elimination:</b> In vitro and in vivo, Clopidogrel undergoes
rapid hydrolysis into its carboxylic acid derivative. In plasma and
urine, the glucuronide of the carboxylic acid derivative is also
observed.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Clopidogrel
is indicated for the reduction of atherosclerotic events (myocardial
infarction, stroke, and vascular death) in patients with
atherosclerosis documented by recent stroke, recent myocardial
infarction, or established peripheral arterial disease.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<ul style="text-align: justify;">
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
use of Clopidogrel is contraindicated in the following conditions:</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Hypersensitivity
to the drug substance or any component of the product. </span>
</div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Active
pathological bleeding such as peptic ulcer or intracranial
hemorrhage.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Severe
liver impairment.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Pregnancy
and Breast Feeding</span></div>
</li>
</ul>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>For
prophylaxis of Thromboembolic events:</b> The usual dose is
Clopidogrel 75mg once daily.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>For
the management of acute coronary syndrome, including unstable angina
and non-Q wave myocardial infarction:</b> Clopidogrel is given as
single 300mg loading dose, followed by 75mg once daily. Or as
prescribed by physician. Drug is not approved for use in children.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">No
dosage adjustment is necessary for elderly patients or patients with
renal disease. </span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Clopidogrel
can be taken with or without the food. If you forget to take a dose
of Clopidogrel take it as soon as you remember. If it is almost time
for your next dose, skip the forgotten dose and continue with your
regular schedule.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PRECAUTION
AND WARNING:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Thrombotic
Thrombocytopenic Purpura (TTP): TTP has been reported rarely
following the use of Clopidogrel, sometimes after a short exposure
(<2 weeks). TTP is a serious condition requiring prompt treatment.
It is characterized by thrombocytopenia, microangiopathic hemolytic
anemia (schistocytes (fragmented RBC) seen on peripheral smear),
neurological findings, renal dysfunctions, and fever.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>General:
</b>As with other antiplatelet agents, Clopidogrel should be used
with caution in patients who may be at risk of increased bleeding
from trauma, surgery or other pathological conditions. If a patient
is to undergo elective surgery and an antiplatelet effect is not
desired. Clopidogrel should be discontinued 7 days prior to surgery.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Gastrointestinal
Bleeding:</b> Clopidogrel can prolong the bleeding time. In CAPRIE,
Clopidogrel was associated with a rate of gastrointestinal bleeding
of 2.0% vs 2.7% of aspirin. Clopidogrel should be used with caution
in patients who have lesions with a propensity to bleed (such as
ulcers). Drugs that might induce such lesions (such as aspirin and
other non-steroidal anti-inflammatory (NSAIDs) should be used with
caution in patients taking Clopidogrel.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Use
in Hepatically Impaired Patients: </b>Experience is limited in
patients with severe hepatic disease, who may have bleeding
diathesis. Clopidogrel should be used with caution in this
population.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Information
for Patients:</b> Patients should be told that is may take them
longer than usual to stop bleeding when they take Clopidogrel, and
that they should report any unusual bleeding to their physician.
Patients should inform physicians and dentists that they are taking
Clopidogrel before any surgery is scheduled and before any new drug
is taken.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Pregnancy:
</b>Clopidogrel should be used during pregnancy only if clearly
needed.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Nursing
Mothers:</b> Studies in rats have shown that Clopidogrel and/or its
metabolites are excreted in the milk. It is not known whether this
drug is excreted in human milk. Because many drugs are excreted in
human milk and because of the potential for serious adverse reactions
in nursing or to discontinue the drug, taking into account the
importance of the drug to the nursing woman.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Pediatric
Use:</b> Safety and effectiveness in the pediatric population have
not been established.]</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>SIDE
EFFECTS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
side effects from Clopidogrel are not common but in few cases any of
the following symptoms may occur. Upset stomach, fatigue, muscle
aches (flu-like symptoms), stomach pain, headaches, diarrhea,
constipation, rash or purple areas on skin. If you experience any of
the following symptoms, consult physician immediately: i.e. chest
pain, unusual bleeding or bruising, bloody vomit, dark urine, bloody
diarrhea, tarry stools, fever, constipation, rash or purple areas on
skin.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Other
side effects, reported rarely, include serum sickness, interstitial
pneumonitis, erythema multiforme, Stevens-Johnson syndrome, lichen
planus, and myalgia.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<ol style="text-align: justify;">
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
did not modify the Clopidogrel-mediated inhibition of ADP-induced
platelet aggregation. Concomitant administration of 500mg of Aspirin
twice a day for 1 day did not significantly increase the
prolongation of bleeding time induced by Clopidogrel. Clopidogrel
potentiated the effect of Aspirin on collagen-induced platelet
aggregation. The safety of chronic concomitant administration of
Aspirin and Clopidogrel has not been established.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
a study in healthy volunteers, Clopidogrel did not necessitate
modification of the Heparin dose or alter the effect of heparin on
coagulation. Co-administration of heparin had no effect on
inhibition of platelet aggregation induced by Clopidogrel. The
safety of this combination has not been established, however,
concomitant use should be undertaken with caution.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
healthy volunteers receiving Naproxen, concomitant administration of
Clopidogrel was associated with increased occult gastrointestinal
blood loss. Non-steroidal Anti-inflammatory Drugs (NSAIDs) and
Clopidogrel should be coadministered with caution.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
safety of the coadministration of Clopidogrel with Warfarin has not
been established. Consequently concomitant administration of these
two agents should be undertaken with caution.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">No
clinically significant pharmacodynamic interactions were observed
when Clopidogrel was coadministered with Atenolol, or both Atenolol
and Nifedipine. The pharmacodynamic activity of Clopidogrel was also
not significantly influenced by the coadministration of
phenobarbital, Cimetidine or estrogen. The pharmacokinetics of
Digoxin or Theophylline were not modified by the coadministration of
Clopidogrel.</span></div>
</li>
</ol>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE
CONDITION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Store
at a temperatures not exceeding 30<sup>o</sup>C.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Protect
from light and moisture. Keep out of the reach of children.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-9435425962416793302014-12-23T19:27:00.000-08:002014-12-23T19:27:04.655-08:00Atorvastatin<div style="text-align: justify;">
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">10mg
Tablet</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">20mg
Tablet</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">40mg
Tablet</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">80mg
Tablet</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dyslipidemic
Agent</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>MECHANISM
OF ACTION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
is a selective, competitive inhibitor of HMG-CoA reductase, the
rate-limiting enzyme that converts
3-hydroxy-3methyl-glutaryl-coenzyme A to mevalonate, a precursor of
steroids, including cholesterol. Cholesterol and triglycerides
circulate in the bloodstream (intermediate-density lipoprotein), LDL
(low-density lipoprotein), and VLDL (very-low-density lipoprotein)
fractions. Triglycerides (TG) and cholesterol in the liver are
incorporated into VLDL and released into the plasma for delivery to
peripheral tissues. LDL is formed from VLDL and is catabolized
primarily through the high-affinity LDL receptor. Clinical and
phathologic studies show that elevated plasma levels of total
cholesterol (total-C), LDL-cholesterol (LDL-C), and apolipoprotein B
(apo B) promote human atherosclerosis and are risk factors for
developing cardiovascular disease, while increased levels of HDL-C
are associated with a decreased cardiovascular risk.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
animal models, Atorvastatin lowers plasma cholesterol and lipoprotein
levels by inhibiting HMG-CoA reductase and cholesterol synthesis in
the liver and by increasing the number of hepatic LDL receptors on
the cell-surface to enhance uptake and catabolism of LDL;
Atorvastatin also reduces LDL production and the number of LDL
particles. Atorvastatin reduces LDL-C in some patients with
homozygous familial hypercholesterolemia (FH), a population that
rarely responds to other lipid-lowing medication(s).</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">A
variety of clinical studies have demonstrated those elevated levels
of total-C, LDL-C and apo B (a membrane complex for LDL-C) promote
human atherosclerosis. Similarly, decreased levels of HDL-C (and its
transport complex, apo A) are associated with the development of
atherosclerosis.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Epidemiological
investigations have established that cardiovascular morbidity and
mortality very directly with level of total-C and LDL-C, and
inversely with the level of HDL-C. Although frequently found in
association with low HDL-C, elevated plasma TG has not been
established as an independent risk factor for coronary heart disease.
The independent effect of raising HDL-C or lowering TG on the risk
for coronary and cardiovascular morbidity and mortality has not been
established.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
reduces total-C, and apo B in patients with homozygous and
heterozygous FH, Nonfamilial forms of hypercholesterolemia, and mixed
Dyslipidemia. Atorvastatin also reduces VLDL-C and TG and produces
variable increases in HDL-C and apolipoprotein A-1. This effect of
Atorvastatin on cardiovascular morbidity and mortality has not been
determined.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
is rapidly absorbed from the gastrointestinal tract. It has absolute
bioavailability of about 12% due to pre-systemic clearance in the
gastrointestinal mucosa and/or first-pass metabolism in the liver,
its primary site of action. Atorvastatin is metabolized by the
cytochrome P450 3A4 to a number of compounds which are also active
inhibitors of HMG CoA reductase. The mean plasma elimination half
life of Atorvastatin is about 14 hours, although the half-life of
inhibitory activity of HMG CoA reductase is approximately 20-30 hours
due to the contribution of the active metabolites. It is 98% bound to
plasma proteins. Atorvastatin is excreted as metabolites, primarily
in the bile.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
is indicated as an adjunct to diet for the reduction of cholesterol,
LDL-Cholesterol ApolipoproteinEB and triglycerides and to increase
HDL-cholesterol in patients with primary hypecholesterlemia,
heterozygous familial and non-familial hypercholesterolemia, and
combined (mixed) hyperlipidemia. Atorvastatin is indicated as an
adjunct to diet for the treatment of patients with elevated serum
triglycerides level, and for the treatment of patients with
dysbetalipoproteinemia, who do not respond adequately to the diet.
Atorvastatin is also indicated or the reduction of total cholesterol
and LDL-cholesterol in patients with homozygous familial
hypercholesterolemia when response to diet and other
non-pharmacological measures are inadequate.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
patient should be placed on a standard cholesterol-lowering diet
before receiving Atorvastatin and should continue on this diet during
treatment with Atorvastatin.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Hypercholesterolemia
(Heterozygous Familial and Nonfamilial) and Mixed Dyslipidemia
(Frederickson Types IIa and IIb):</b></i></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
recommended starting dose of Atorvastatin is 10mg once daily. The
dosage range is 10 to 80mg once daily. Atorvastatin can be
administered as single dose at any time of the day, with or without
food. Therapy should be individualized according to goal of therapy
and response. After initiation and/or upon titration of Atorvastatin,
lipid levels should be analyzed within 2 to 4 weeks and dosage
adjusted accordingly. Since the goal of treatment is to lower LDL-C,
the NCEP recommends that LDL-C levels be used to initiate and assess
treatment response. Only if LDL-C levels are not available, should
total-C be used to monitor therapy.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Homozygous
Familial Hypercholesterolemia:</b></i></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
dosage of Atorvastatin in patients with homozygous FH 10 to 80 mg
daily. Atorvastatin should be used as an adjunct to other
lipid-lowering treatments (eg. LDL apheresis) in these patients or if
such treatments are unavailable.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Concomitant
Therapy:</b></i></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
may be used in combination with a bile acid binding resin for
additive effect. The combination of HMG-CoA reductase inhibitors and
fibrates should generally be avoided </span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Dosage
in Patients with Renal Insufficiency:</b></i></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Renal
disease does not affect the plasma concentrations nor LDL-reduction
of Atorvastatin; thus, dosage adjustment in patients with renal
dysfunction is not necessary.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Body
as a Whole:</b> Chest pain, face edema, fever, neck rigidity,
malaise, photosensitivity reaction, generalized edema. </span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Digestive
System:</b> Nause, gastroentiritis, liver function tests abnormal,
colitis, vomiting, gastritis, dry mouth, rectal hemorrhage,
esophagitis, eructation, glossitis, mouth ulceration, anorexia,
increased appetite, stomatitis, biliary pain, chellitis, duodenal
ulcer, dysphagia, enteritis, melena, gum hemorrhage, stomach ulcer,
tenesmus, ulcerative stomatitis, hepatitis, pancreatitis, cholestatic
jaudice.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Respiratory
System: </b>Bronchitis, rhinitis, pneumonia, dyspnea, asthma and
epistaxis.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Nervous
System:</b> Insomnia, dizziness, paresthesia, somnolence, amnesia,
abnormal dreams, libido decreased, emotional ability, incoordination,
peripheral neuropathy, torticollis, facial paralysis, hyperkinesia,
depression, hypersthesia, hypertonia.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Musculoskeletal
System: </b>Arthritis, leg cramps, bursitis, tenosynovitis,
myasthenia, tendinous contracture, myositis.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Skin
and Appendages:</b> Pruritus, contact dermatitis, alopecia, dry skin,
sweating, acne, urticaria, eczema, seborrhea, skin ulcer.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Urogenital
System: </b>Urinary tract infection, urinary frequency, cystitis,
hematuria, impotence, dysuria, kidney calculus nocturia,
epididymitis, librocystic breast, vaginal hemorrhage, albuminuria,
breast enlargment, metorrhagia, nephritis, urinary incontinence,
urinary retention, urinary urgency, abnormal ejaculation, uterine
hemorrhage.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Special
Senses: </b>Amblyopia, tinnitus, dry eyes, refraction disorder, eye
hemorrhage, deafness, glaucoma, parosmia, taste loss, taste
perversion.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Cardiovascular
System:</b> Palpitation, vasodilator, syncope, migraine, postural
hypotension, phlebitis, arrhythmia, angina pectoris and hypertension.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Metabolic
and Nutritional Disorder:</b> Peripheral edema, hyperglycemia,
creatine phosphokinase increased, gout, weight gain, hypoglycemia.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Contraindicated
in patients who are hypersensitive to any component of this
medication, who have active liver disease or persistent elevation of
serum transaminase exceeding three times the upper limit of normal,
who are pregnant since there is a possibility that it could interfere
with fetal sterol synthesis, who are breast feeding, or in women of
childbearing potential who are not using adequate contraceptive
measures.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PRECAUTIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Before
instituting therapy with Atorvastatin, an attempt should be made to
control hypercholesterolemia with appropriate diet, exercise, and
weight reduction in obese patients, and to treat other underlying
medical problems. Patients should be advised to report promptly
unexplained muscle pain tenderness, or weakness, particularly if
accompanied by malaise or fever.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<ol style="text-align: justify;">
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">When
Atorvastatin and antacid suspensions were coadministered, plasma
concentrations of Atorvastatin decreased approximately 35%. However,
LDL-C reduction was not altered.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Because
Atorvastatin does not affect the pharmacokinetics of Antipyrine,
interactions with other drugs metabolized via the same cytochrome
isoenzymes are not expected.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Plasma
concentrations of Atorvastatin decreased approximately 25% when
Colestipol and Atorvastatin were coadministered. However, LDL-C
reduction was greater when Atorvastatin and Colestipol were
coadminstered than when either drug was given alone.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
plasma concentrations and Ldl-C reduction were not altered by
coadministration of Cimetidine.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">When
multiple doses of Atorvastatin and Digoxin were coadministered,
steady-state plasma Digoxin concentrations increased by
approximately 20%. Patients taking Digoxin should be monitored
appropriately.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
healthy individuals, plasma concentrations of Atorvastatin increased
approximately 40% with coadministration of Atorvastatin and
Erythromycin, a known inhibitor o cytochrome P450 3A4.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Coadministration
of Atorvastatin and an oral contraceptive increased AUC values of
norethindrone and ethinyl estradiol by approximately 30% and 20%.
These increases should be considered when selecting an oral
contraceptive for a woman taking Atorvastatin.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Atorvastatin
had no clinically significant effect of prothrombin time when
administered to patients receiving chronic Warfarin treatment.</span></div>
</li>
</ol>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE
CONDITIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Store
ad temperatures not exceeding 30<sup>o</sup>C. Protect from light and
excessive heat.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-7568189436840850412014-12-22T07:29:00.000-08:002014-12-22T07:29:28.382-08:00Dicyclomine / Dicycloverine
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dicyclomine
/ Dicycloverine</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">10mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">10mg/5ml
Syrup</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Anticholinergic
Drug/ Antispasmodic Drug</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>BRAND
NAME:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Bentyl</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGICAL
ACTION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dicycloverine
in hydrochloride as its salt, is tertiary amine with antimuscarinic
effects similar to but weaker than those atropine. It also has a
direct antispasmodic action.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dicycloverine
is readily absorbed from the gastrointestinal tract; it is also
absorbed from mucous membranes, the eye, and to some extent through
intact skin. It is rapidly cleared from the blood and is distributed
throughout the body. It crosses the blood-brain barrier. It is
incompletely metabolized in the liver and is excreted in the urine as
unchanged drug and metabolites. A half-life of about 4 hours has been
reported. It crosses the placenta and traces appear in breast milk.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:
</b></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">For
the treatment of functional gastrointestinal conditions including
smooth muscle spasms, e.g. irritable colon (mucous colitis, spastic
colon, irritable bowel syndrome) and spastic constipation. Adjunctive
therapy in organic gastrointestinal conditions to relieve associated
smooth muscle spasms (e.g. diverticulitis, regional enteritis,
gastric, and peptic ulcers).</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Adults:</b>
10mg to 20mg 3 to 4 times a day.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Children:</b>
6 mos to 2 years – 5mg to 10mg 3 to 4 times daily. Dose does not
exceed 40m<span style="font-weight: normal;">g. 2yrs to 12 years –</span>
10mg 3 times a day.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Elderly:</b>
older adults should begin with the lowest possible dose and increase
their dosage only as needed.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Child
(under 6 months):</b> not recommended</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Or
as prescribed by a physician.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dose
is usually given 15 minutes before meals. If you forget to take a
dose of Dicycloverine (Dicyclomine, in USA), take it as soon as you
remember. If it is almost time for your nest dose, skip the forgotten
dose and continue with your regular schedule.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">It
is contraindicated in patients with prostatic enlargement in whom it
may lead to urinary retention, and in those with paralytic ileus or
pyloric stenosis. In patients with ulcerative colitis its use may
lead to ileus or megacolon, and its effects on the lower esophageal
sphincter may exacerbate reflux. Caution is generally advisable in
any patient with diarrhea. Its should not be given to patients with
myasthenia gravis except to reduce adverse muscarinic effects of an
anticholinesterase.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Antimuscarinic
should not be given to patients with angle-closure glaucoma or with a
narrow angle between the it is and the cornea, since it may raise
intra-ocular pressure and precipitate an acute attack. Acute
angle-closure glaucoma has been reported in patients receiving
nebulized atropine. Some recommend that atropine eye drops should not
be used in infants aged less than 3 months due to the possible
association between the induced cycloplegia and the development of
amblyopia. Systemic reactions have followed the absorption of
atropine from eyes drops; overdosage is less likely if the eye
ointment is used. In the event of blurred vision following topical
administration of atropine to the eye patients should not drive or
operate machinery. Systemic administration of antimuscarinics may
also cause blurred vision, dizziness, and other effects that may
impair a patients ability to perform skilled tasks such as driving.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Because
of the risk of provoking hyperthermia, antimuscarinic should not be
given to patients, especially children, when the ambient temperature
is high. It should also be used cautiously in patients with fever.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Antimuscarinics
need to be used with caution in conditions characterized by
tachycardia such as thyrotoxicosis, heart failure, and in cardiac
surgery, where they may further accelerate the heart rate. Care is
required in patients with acute myocardial infarction, as ischemia
and infarction may be made worse, and in patients with hypertension.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Antimuscarinics
may cause confusion, especially in the elderly, Reduced bronchial
secretion caused by systemic administration of antimuscarinic may be
associated with the formation of mucous plugs.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
the treatment of parkinsonism, increases in dosage and transfer to
other forms of treatment should be gradual and antimuscarinic should
not be withdrawn abruptly. Minor reactions may be controlled by
reducing the dose until tolerance has developed.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Persons
with Down's syndrome appear to have an increased susceptibility to
some of the actions of antimuscarinic, whereas those with albinism
may have reduced susceptibility.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
pattern of adverse effects seen with atropine and other
antimuscarinics can mostly be related to their pharmacological
actions at muscarinic and, at high doses, nicotinic receptors. These
effects are dose-related and are usually reversible when therapy is
discontinued. The peripheral side-effects of antimuscarinic
are a consequence of their inhibitory effects include dryness of the
mouth with difficulty in swallowing and talking, thirst, reduced
bronchial secretions, dilatation of the pupils (mydriasis) with loss
of accommodation (cyclopegia) and photophobia, flushing and dryness
of the skin, transient bradycardia followed by tachycardia, with
palpitation and arrhythmias, and difficulty in micturition, as well
as reduction in the tone and motility of the gastrointestinal tract
leading to constipation.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PRECAUTIONS AND
WARNINGS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">It should be given with
caution to children and geriatric patients, who may be more
susceptible to its adverse effects. It is contraindicated in
patients, who may be more susceptible to its adverse effects. It is
contraindicated in patients with prostatic enlargement and in those
with paralytic ileus or pyloric stenosis. In patients with ulcerative
colitis, myasthenia gravis, and closed-angle glaucoma and in patients
taking antimuscarinic agents in conditions characterized by
tachycardia such as thyrotoxcosis, cardiac insufficiency, or failure
and in cardiac surgery.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Pregnancy and
Lactation:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">A few cases of human
malformation were linked to Dicycloverine, but studies have shown
that the drug has not effect on the developing baby. As with all
other drug products, Dicycloverine should be used during pregnancy
only when absolutely necessary.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dicycloverine or
Dicyclomine should not be used by nursing mothers because like other
drugs in is group, it may reduce the amount of milk produced. Also, a
few infants less than 3 months o age who were given Dicycloverine
drops developed breathing difficulty that went away on its own after
20 to 30 minutes.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Use in Elderly:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Older adults may be more
susceptible to the side effects of the drug, especially memory loss,
mental changes, and glaucoma, and may need less medicine to get a
beneficial effect than a younger adult. Report any problems to your
doctor at once.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Effects
on ability to drive and operate machinery:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Oral
administration of antimuscarinics such as Dicycloverine may cause
blurred vision, dizziness, and other effects that may impair a
patients ability to perform skilled tasks such as driving and
operating machinery.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Never
mix Dicycloverine with other anticholinergic drugs, including
Atropine, Belladonna, Clidinium, Glycopyrrolate, Hyoscyamine,
Isopropamide, Propantheline, Scopolamine, and others because of the
possibility of intensifying drug adverse effects.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dicycloverine
can reduce stomach acidity and reduce the amount of Ketoconazole
absorbed into the blood after it is taken by mouth.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Antacids
containing calcium and/or magnesium citrates, sodium bicarbonate,
and carbonic anhydrase inhibitor drugs may slow the rate at which
Dicycloverine is released from the blood, increasing its therapeutic
effect and possible side-effects.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Taking
Dicycloverine may counteract the effect of Metoclopramide in
reducing nausea and vomiting when taken together.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dicycloverine
together with narcotic pain reliever can increase the chances of
severe constipation.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Taking
this drug or any other drug that slows the movement of stomach and
intestinal muscles together with a potassium chloride supplement
(especially one that comes in wax-matrix tablet form) can lead to
excessive irritation of the stomach.</span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>OVERDOSAGE:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
principal signs of overdose are blurred vision; clumsiness;
confusion; difficulty breathing; dizziness; drowsiness; dry mouth,
nose, or throat; rapid heartbeat; fever; hallucinations; weakness;
slurred speech; excitement, restlessness, or irritability; warmth;
and dry or flushed skin. Overdose victims should be taken to a
hospital emergency room at once for treatment. Always bring the
medicine with you.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE
CONDITIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Store
at temperatures not exceeding 30<sup>o</sup>C. Protect from light.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com1tag:blogger.com,1999:blog-3465762249352810871.post-56412915888091960222014-12-21T04:50:00.000-08:002014-12-21T04:50:07.277-08:00Erythromycin
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
</span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">100mg/ml
Suspension Oral Drops</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">125mg/5ml
Suspension</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">200mg/5ml
Suspension</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">250mg/5ml
Suspension</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">250mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">500mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Macrolide
Antibacterial Drug</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>MECHANISM
OF ACTION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
and other macrolides bind reversibly to the 50s sub units of the
ribosome, resulting in blockage of the transpeptidation or
translocation reactions in inhibition of protein synthesis, and hence
inhibition of cell growth. Its action is predominantly bactericidal
against the more sensitive strains.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
base is destroyed by stomach acid and must be administered with
enteric coating. Stearates and esters are fairly acid-resistant and
relatively well absorbed. The lauryl salt of propionyl ester of
Erythromycin (Erythromycin estolate) is among the best-absorbed oral
preparations. Oral doses of 2 g/d result in serum levels of up to
2μg/ml. Large amounts are
lost in feces. Absorbed drug is distributed widely except to the
brain and cerebrospinal fluid. It traverses the placenta and reaches
the fetus.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycins
are excreted largely in the bile, where levels may be 50 times higher
than in the blood. A portion of the drug excreted into bile is
reabsorbed from the intestines. Only 5% of the administered dose is
excreted in the urine.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Streptococcus
pyogenes: </b></i>Upper and lower respiratory tract, skin, and
soft-tissue infections of mild to moderate severity.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Staphylococcus
aureus:</b></i> Acute infections of skin and soft tissue that are
mild to moderately severe. Resistant organisms may emerge during
treatment.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Streptococcus
pneumoniae: </b></i>Infections of the upper respiratory tract (e.g.
otitis media, pharyngitis) and lower respiratory tract (e.g.
pneumonia) of mild to moderate severity.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Mycoplasma
pneumoniae:</b></i> In the treatment of respiratory tract infections
due to this organism.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Hemophilus
influenzae:</b></i> For upper respiratory tract infections of mild to
moderate severity when used concomitantly with adequate doses of
sulfonamides. The concomitant use of sulfonamides is necessary since
not all strains of Hemophilus influenzae are susceptible to
Erythromycin at the concentrations of the antibiotic achieved with
usual therapeutic doses.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Chlamydia
trachomatis: </b></i>Erythromycin is indicated for treatment of the
following infections caused by Chlamydia trachomatis: conjunctivitis
of the new born, pneumonia of infancy and urogenital infections
during pregnancy. When tetracyclines are contraindicated or not
tolerated, Erythromycin is indicated for the treatment of
uncomplicated urethral, endocervical, or rectal infections in adults
due to Chlamydia trichomatis.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Treponema
pallidum: </b></i>Erythromycin is an alternate choice o treatment for
primary syphilis in penicillin-allergic patients. In treatment of
primary syphilis, spinal fluid examinations should be done before
treatment and as part of follow-up after therapy.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Corynebacterium
diphtheriae: </b></i>As an adjunct to antitoxin, to prevent
establishment of carriers, and to eradicate the organisms in
carriers.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Corynebacterium
minutissimum:</b></i> In the treatment of erythema.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Estamoeba
histolytica: in the treatment of intestinal amoebiasis only.
Extra-enteric amoebiasis requires treatment with other agents.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Listeria
monocytogenes: </b></i>Infections due to this organism.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Bordetella
pertussis:</b></i> Erythromycin is effective in eliminating the
organisms from the nasopharynx of infected individuals.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
may be given as the base or its salts or esters; doses are expressed
in terms of the base. The usual oral dose is the equivalent of
Erythromycin 1 to 2 g daily in 2 to 4 divided doses; for severe
infections, this may be increased to up to 4g daily in divided doses.
For children the dose is usually about 30 to 50mg per Kg body-weight
daily although it may be doubled in severe infections; a recommended
dose for children aged 2 to 8 years 1g daily in divided doses, and
for infants and children up to 2 years of age, 500mg daily in divided
doses.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
the patient who is unable to take Erythromycin by mouth and in
severely ill patients in whom it is necessary to attain an immediate
high blood concentration, Erythromycin maybe given intravenously in
the form of one its more soluble salts such as gluceptate or the
lactobionate, in doses equivalent to those by mouth.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
is contraindicated in patients with known hypersensitivity to this
antibiotic and in those with liver disorders.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PRECAUTION
AND WARNING:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">There
have been a few reports of hepatic dysfunction, with or without
jaundice, occurring in patients receiving oral Erythromycin products.
All forms of Erythromycin should be used with care in patients with
existing liver disease or hepatic impairment.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
use in patients who are receiving high doses of Theophylline may be
associated with an increase in serum Theophylline levels and
potential Theophylline toxicity. In case of Theophylline toxicity
and/or elevated serum Theophylline levels, the dose of Theophylline
should be reduced while the patient is receiving concomitant
Erythromycin therapy.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Concomitant
administration of Erythromycin and Digoxin has been reported to
result in elevated Digoxin serum levels.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">There
have been reports of increased anticoagulant effects when
Erythromycin and oral anticoagulant were used concomitantly.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Concurrent
use of Erythromycin and Ergotamine or dihydroergotamine has been
associated in some patients with acute ergot toxicity characterized
by severe peripheral vasospasm and dysesthesia.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
has been reported to decrease the clearance of triazolam and thus
may increase the pharmacologic effect of triazolam.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
use of Erythromycin in patients concurrently taking drugs
metabolized by the cytochrome P450 system may be associated with
elevations in serum Erythromycin with carbamazepine, cycloporine,
hexobarbital and phenytoin.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Serum
concentrations of drugs metabolized by the cytochrome P450 system
should be monitored closely in patients concurrently receiving
Erythromycin. </span>
</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Troleandomycin
significantly alters the metabolism of terfenadine when taken
concomitantly; therefore, observe caution when Erythromycin and
terfenadine are used concurrently. </span>
</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Patients
receiving concomitant Lovastatin and Erythromycin should be
carefully monitored: cases of rhabdomyolysis have been reported in
seriously ill patients.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Concomitant
use of CYP3A inhibitors like nitroimidazole antifungals can cause
increased serum levels of Erythromcyin and probably increase the
risk of cardiac arrhythmia. </span>
</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Concurrent
use of diltiazem or verapamil with Erythromycin should be avoided by
persons at risk for heart irregularities or those with long QT
manifestations.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Erythromycin
may interfere with some diagnostic tests including measurement of
urinary catecholamines and 17 – hydroxycorticosteroids.</span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
most frequent side effects of oral Erythromycin preparations are
gastrointestinal and are dose-related. They include nausea, vomiting,
abdominal pain, diarrhea and anorexia. Symptoms of hepatic
dysfunction and/or abnormal liver function test results may occur.
Pseudomembranous colitis has been rarely reported in association with
Erythromycin therapy. There have been isolated reports of transient
central nervous system side effects including confusion,
hallucinations, seizures, and vertigo; however, a cause and effect
relationship has not been established.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Occasional
case reports of cardiac arrhythmias such as ventricular tachycardia
have been documented in patients receiving Erythromycin therapy.
There have been isolated reports of other cardiovascular symptoms
such as chest pain, dizziness, and palpitations; however, a cause and
effect relationship has not been established.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allergic
reactions ranging from urticaria and mild skin eruptions to
anaphylaxis have occurred.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">There
have been isolated reports of reversible hearing loss occurring
chiefly in patients with renal insufficiency and in patients
receiving high doses of Erythromycin.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>OVERDOSAGE:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
case of overdosage, Erythromycin should be discontinued. Overdosage
should be handled with the prompt elimination of unabsorbed drug and
all other appropriate measures. Erythromycin is not removed by
peritoneal dialysis or hemodialysis.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE
CONDITION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Store
at a temperatures not exceeding 30<sup>o</sup>C.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-1811022598419030732014-12-20T05:21:00.000-08:002014-12-20T05:21:26.959-08:00Tramadol
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">50mg Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">100mg Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">50mg/ml i.v. Injection</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">100mg/2ml i.v. Injection</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Opioid Analgesic</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>BRAND
NAME:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramal</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Tramadol
is a centrally acting analgesic with binding to specific opioid
receptors. It is a nonselective, pure agonist at mu (μ), delta (d),
and kappa (k) opioid receptors with a higher affinity for the μ
receptor. Other mechanisms, which may contribute to its analgesic
effect, are inhibition of neuronal re-uptake of noradrenaline and
serotonin. Tramadol does not promote the release of histamine.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Tramadol
is well absorbed after oral or rectal administration, with an
absorption half-life (t</span></span><sub><span style="text-decoration: none;"><span style="font-weight: normal;">1/2ka</span></span></sub><span style="text-decoration: none;"><span style="font-weight: normal;">)
of 0.38 ± 0.18 hours, leading to an analgesic effect lasting for up
to 9 hours. The parenteral form of Tramadol has more rapid onset of
action. The mean systemic bioavailability is 68%.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Tramadol
hydrochloride crosses the blood-brain and placental barrier. Only
very small amounts are excreted in breast milk unchanged or as the
metabolite M1 (Tramadol hydrochloride approximately 0.1%, M1
approximately 0.02% of the i.v. dose. The elimination half-life is 5
to 7 hours. Tramadol is mainly metabolized in the liver (90%).
Tramadol hydrochloride and its metabolites are almost completely
excreted by the renal route (95%). Biliary excretion of these
component is quantitatively insignificant and is therefore subject to
hepatic metabolism and renal elimination. The terminal half-life
(t</span></span><sub><span style="text-decoration: none;"><span style="font-weight: normal;">1/2β</span></span></sub><span style="text-decoration: none;"><span style="font-weight: normal;">)
is likely to be prolonged in the (t</span></span><sub><span style="text-decoration: none;"><span style="font-weight: normal;">1/2β</span></span></sub><span style="text-decoration: none;"><span style="font-weight: normal;">)
values is relatively low if at least one of these organs is
functioning normally. In patients with liver cirrhosis, the mean of
t</span></span><sub><span style="text-decoration: none;"><span style="font-weight: normal;">1/2β
</span></span></sub><span style="text-decoration: none;"><span style="font-weight: normal;">of
Tramadol was 13.3 ± 4.9h, t</span></span><sub><span style="text-decoration: none;"><span style="font-weight: normal;">1/2β</span></span></sub><span style="text-decoration: none;"><span style="font-weight: normal;">/m1
18.5 ± 9.4 h; in patients with renal insufficiency (creatinine
clearance ≤5ml/min) the values were 11.0 ± 3.2h (Tramadol) and
16.9 ± 3.0h (M1) respectively.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">There are six differences in the
pharmacokinetic parameters of Tramadol. The absolute bioavailability
was 73% in males and 79% in females. Plasma clearance was 6.4
ml/min/kg in males and 5.73 ml/min/kg in females following a 100mg
i.v. dose. Following a single oral dose and after adjusting for body
weight, females had 12% higher peak concentration and a 35% higher
area under the concentration time curve compared to males. The
clinical significance of these differences is unknown.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Management of moderate to
moderately severe pain.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol is contraindicated in
known hypersensitivity to Tramadol hydrochloride, or opioids, in
acute intoxication with alcohol, hypnotics, analgesics or
psychotropic medicines. It should not be administered to patients who
are receiving monoamine oxidase inhibitors or within two weeks of
their withdrawal. Tramadol must not be used for narcotic withdrawal
treatment. </span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol should not be given to
patients with increased intracranial pressure or central nervous
system depression due to head injury or cerebral disease.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PRECAUTIONS
AND WARNINGS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-style: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Rapid intravenous use:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Rapid intravenous administration
may be associated with higher incidence of adverse events and should
therefore be avoided.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Liver
and kidney impairment:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol should be used with
caution in patients with severe impairment of hepatic and renal
function and in patients prone to convulsive disorders or in shock.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Seizures:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Seizures have been reported in
patients receiving Tramadol at dosages within the recommended dosage
range. The risk of seizures is enhanced in patients exceeding the
recommended dose, or in patients taking tricyclic antidepressants or
other tricyclic compounds e.g. promethazine, selective serotonin
re-uptake inhibitors. MAO-inhibitors and neuroleptics. The risk of
seizures may also be increased in patients with epilepsy, with a
history of seizures or in patients with a recognized risk for
seizures e.g. drug and alcohol withdrawal and intracranial
infections, head trauma, metabolic disorders and naloxone treatment
with Tramadol overdose. Patients known to suffer from cerebral
convulsions should be carefully monitored during treatment with
Tramadol.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Drug
abuse and dependence: </b></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Although
Tramadol has a low dependence potential, tolerance psychic and
physical dependence of the morphine-type (μ opioid) may develop with
long-term use. The drug has been associated with craving,
drug-seeking behavior and tolerance development. Cases of abuse and
dependence on Tramadol have been reported. Tramadol should not be
used in opioid-dependent patients. Tramadol can re-initiate physical
dependence in patients who have been previously dependent on or
chronically using other opioids. In patients with a tendency to drug
abuse, a history of drug dependence or who are chronically using
opioids, treatment with Tramadol is not recommended.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Respiratory
Depression:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol should not be given to
patients with respiratory depression especially in the presence of
cyanosis and excessive bronchial secretions.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Pregnancy
and Lactation:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol is toxic to animal
fetuses at doses only 3 to 15 times the maximum adult dose. In
people, Tramadol passes into the blood circulation of the developing
fetus. Pregnant women should not take this drug unless it is
absolutely necessary. This drug should not be taken by nursing
mothers.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Elderly:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">In people age 75 and older, blood
concentrations are somewhat higher than in younger adults. Older
adults can also be expected to be more sensitive to the side effects
of this drug. Older adults should not take more than 300mg a day.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Effects
on ability to drive and operate machinery:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol may affect reactions to
the extent that driving ability and the ability to operate machinery
may be impaired. This applies particularly in conjunction with other
psychotropic medicines including alcohol.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINSTRATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The dosage should be adjusted to
the intensity of pain and the individual's response to the analgesic
action of Tramadol. It should not be used to treat minor pain. In
general a total daily dose should not exceed 400mg of Tramadol.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">For post-operative pain,
administer an initial bolus of 100mg. During the 90 minutes following
the initial bolus further doses of 50mg may be given every 30
minutes, up to a total dose of 250mg including the initial bolus.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Subsequent doses should be 50mg
or 100mg 4 to 6 hourly up to a total daily dose of 600mg. For less
severe pain administer 50mg or 100mg 4 to 6 hourly.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><b>Elderly:
</b></span><span style="text-decoration: none;"><span style="font-weight: normal;">The
usual dosages may be used except in patients 75 years of age and over
where a downward adjustment of the dose and/or prolongation of the
interval between doses are recommended.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Renal
impairment/renal dialysis:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The elimination of Tramadol may
be prolonged. It is recommended that the usual initial dosage be
used. For patients with a creatinine clearance <30 ml/min, the
dosage interval should be increased to 12 hours. As Tramadol is
removed very slowly by hemodialysis or hemofiltration, postdialysis
administration to maintain analgesia is not usually necessary.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Hepatic
impairment:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The elimination of Tramadol may
be prolonged. The usual initial dosage should be used but in severe
hepatic impairment, the dosage interval should be increased to 12
hours.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol may be taken without
regard to food or meals. If you forget a dose of Tramadol, take it as
soon as you remember. If it is almost time for your next dose, skip
the one you forgot and continue with your regular schedule. Do not
take a double dose.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The following side-effects have
reported:</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><span style="text-decoration: none;"><b>Gastrointestinal
system:</b></span></i><span style="text-decoration: none;"><span style="font-weight: normal;">
Nausea, vomiting, dry mouth, heartburn, constipation.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><span style="text-decoration: none;"><b>Central
nervous system and psychiatric:</b></span></i><span style="text-decoration: none;"><span style="font-weight: normal;">
Fatigue, sedation, drowsiness, dizziness, confusion, hallucinations,
seizures.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><span style="text-decoration: none;"><b>Others:</b></span></i><span style="text-decoration: none;"><span style="font-weight: normal;">
Sweating (especially when intravenous administration is too rapid),
skin rashes, bradycardia, tachycardia, flushing, bronchospasm,
angioedema, syncope, anaphylaxis and anaphylactic reactions have been
reported.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The reactions may occur after the
first dose. Postural hypotension or cardiovascular collapse has been
observed, potential for Toxic Epidermal Necrolysis and
Stevens-Johnson syndrome. Tramadol should not be use for the
treatment of minor pain.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol must not be combined
with a MAO-inhibitor, or within 14 days of discontinuation of it, as
potentiation of serotonergic and noradrenergic effects may result.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Simultaneous administration with
Cimetidine is associated with clinically insignificant changes in
serum concentrations of Tramadol. Therefore, no alternation of the
Tramadol dosage regimen is recommended for patients receiving
chronic Cimetidine therapy.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Animal studies have shown that
the duration of anesthesia is prolonged when Tramadol is combined
with barbiturates. </span>
</div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The analgesic effect and
duration of action may be reduced on concomitant or previous use of
Carbamazipine. People taking this combination may need twice the
usual dose of Tramadol.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The concomitant administration
of Tramadol tablet with centrally acting depressants may produce
intensified effects.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">On the other hand combining
Tramadol with tranquilizer may produce favorable effects on pain
sensation and management.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Quinidine may slow the breakdown
of Tramadol because it affects the liver enzyme that breaks down
Tramadol. The full impact of this interaction is not known.</span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>OVERDOSAGE:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The most serious effects of
Tramadol are usually difficulty breathing and seizures. Some people
have died from Tramadol overdose; it is estimated that they took
between 3000 and 5000 mg (3 to 5 grams)of the drug. The lowest fatal
dose was thought to be between 500 and 1000mg in an 40kg (88 pound)
woman. </span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Respiratory depression can be
antagonized with a pure opiate antagonist (naloxone). If naloxone is
to be administered, use cautiously because it may precipitate
seizures. Treatment of restlessness and/or convulsions is symptomatic
and supportive (benzodiazepines/barbiturates).</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tramadol is minimally eliminated
from the serum by hemodialysis or hemofiltration. Treatment of acute
intoxication with hemodialysis or hemofiltration alone is therefore
not suitable for detoxification.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE
CONDITION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Store
in a dry place at temperatures not exceeding 30</span></span><sup><span style="text-decoration: none;"><span style="font-weight: normal;">o</span></span></sup><span style="text-decoration: none;"><span style="font-weight: normal;">C.
Protect from light. Keep out of reach of children.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-18803518444298280612014-12-19T00:40:00.000-08:002014-12-19T00:40:17.859-08:00Omeprazole
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Omeprazole</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">20mg Capsule</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">40mg Capsule</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Proton Pump Inhibitor</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>BRAND
NAME: </b></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Prilosec</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole is a substituted
benzimidazole which suppresses gastric acid secretion. Omeprazole is
activated at an acidic pH to a sulphenamide derivative that binds
irreversibly to H<sup>+/</sup>K<sup>+ </sup>ATPase, an enzyme system
found at the secretory surface of parietal cells. It hereby inhibits
the final transport of hydrogen ions to the gastric lumen. Therefore,
Omeprazole has been referred to as an acid or proton pump inhibitor.
Omeprazole inhibits basal and stimulated gastric acid secretion. The
degree of inhibition of gastric acid secretion is related to the dose
and duration of therapy.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole is rapidly but
variably absorbed after oral doses. Absorption is not significantly
affected by food. Omeprazole is acid-labile and the pharmacokinetics
of the various formulation develop to improve oral bioavailability
may vary. The absorption of Omeprazole also appears to be
dose-dependent; increasing the dosage above 40mg has been reported to
increase the plasma concentrations in non-linear fashion because of
saturable first-pass hepatic metabolism. In addition, bioavailability
is higher after long-term use. Bioavailability of Omeprazole may be
increased in elderly patients, in some ethnic groups such as Chinese,
and in patients with hepatic impairment, but is not markedly affected
in patients with renal impairment. On absorption, Omeprazole is
almost completely metabolized in the liver, primarily by the
cytochrome P450 isoenzyme CYP2C19 to form hydroxyl-omeprazole, and to
a small extent by CYP3A4 to form omeprazole sulfone. The metabolites
are inactive, and are excreted mostly in the urine and to a lesser
extent in bile. The elimination half-life from plasma is reported to
be about 0.5 to 3 hours. Omeprazole is about 95% bound to plasma
proteins.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">For treatment of benign gastric
and duodenal ulcers including NSAID gastric and duodenal ulcers or
gastroduodenal erosions, gastroesophageal reflux disease (GERD), acid
related dyspepsia or disorders associated with hyper secretion of
gastric acid, such as the ZollingerEllison Syndrome. It is also use
in combination with antibiotics for eradication of Helicobacter
pylori in peptic ulcer disease as triple therapy.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>For
the relief of Acid-related Dyspepsia</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole is given in usual
doses of 10 or 20 mg daily orally for 2 to 4 weeks.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Gastroesophageal
Reflux Disease (GERD)</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The usual dose is 20 mg orally
once daily for 4 weeks, followed by a further 4 to 8 weeks if not
fully healed.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Refractory
Esophagitis</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">A dose of 40mg daily may be used.
Maintenance therapy after healing of esophagitis is 20 mg once daily,
and for acid reflux is 10 mg daily.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Peptic
Ulcer Disease</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">A single dose of 20mg daily, or
40 mg in severe cased, is give. Treatment is continued for 4 weeks
for duodenal ulcer and 8 weeks for gastric ulcer.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>For
eradication of Helicobacter pylori in Peptic Ulceration</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole may be combined with
antibacterials in dual or triple therapy. Effective triple therapy
regimens include Omeprazole 20mg twice daily or 40mg once daily
combined with: Amoxicillin 500mg and Metronidazole 500mg, both three
times daily; Clarithromycin 250mg and Metronidazole 500mg (or
Tinidazole 500mg) both twice daily; or with Amoxicillin 1 g and
Clarithromycin 500mg, both twice daily. These regimens are given 1
week. Dual therapy regimens such as Omeprazole 20mg twice daily or
40mg daily with either Amoxicillin 750mg to 1 gram twice daily or
Clarithromycin 500mg three times daily, are less effective and must
be given for 2 weeks. Omeprazole alone may be continued for a further
4 to 8 weeks.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Treatment
of NSAID-associated Ulceration</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Doses of 20mg dialy orally are
used; a dose of 20mg daily may also be used for prophylaxis in
patients with a history of gastroduodenal lesions who require
continued NSAID treatment.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Zollinger-Ellison
Syndrome</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">The initial recommended dosage is
60mg orally once daily, adjusted as required. The majority of
patients are effectively controlled by doses in range 20 to 120mg,
but doses up to 120mg three times daily have been used. Daily doses
above 80mg should be given as divided doses (usually 2).</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Prophylaxis
of acid aspiration during general anesthesia</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole is also used for the
prophylaxis of acid aspiration during general anesthesia, in a dose
of 40mg the evening before surgery and a further 40mg two to six
hours before the procedure.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Dosage
for Children</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">For the treatment of
gastroesophageal reflux disease in children 1 year of age and over
are determined by body-weight as follows: 10 to 20kg: 10 mg once
daily; over 20mg once daily. These doses may be doubled if necessary.
Treatment may be given for 4 to 12 weeks.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole should be taken
immediately before a meal, preferably in the morning. If you forget
to take a dose of Omeprazole, take it as soon as you remember. If it
is almost time for your next dose, skip the one you forgot and
continue with your regular schedule. Do not take a double dose.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Omeprazole should not be used to
patients who are/have:</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Chronic, current or history of
hepatic disease;</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Presence of gastric malignancy;</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Pregnancy
and lactation;</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Sensitive
to Omeprazole or any component of the capsules;</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Children:
Safety and efficacy for children are not established.</span></span></span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">ADVERSE
DRUG REACTIONS:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Omeprazole
has a very favorable tolerability profile. Generally, Omeprazole
causes few side effects such as:</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">Most
Common:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Headache,
diarrhea, abdominal pain, nausea, sore throat, upper respiratory
infections, fever, vomiting, dizziness, rash, constipation, muscle
pain, unusual tiredness, cough, and back pain.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">Rare:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Abdominal
swelling, a feeling of ill health, angina pain, appetite loss, stool
discoloration, irritable bowel, fungal infection in the esophagus,
dry mouth, low blood sugar, weight gain, muscle cramps, joint and leg
pains, dizziness, fainting, nervousness, sleeplessness, apathy,
anxiety, unusual dreams, tingling in the hands or feet, nosebleeds,
itching and inflammation of the skin, dry skin, hair loss, sweating,
frequent urination, and testicle pain.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">DRUG
INTERACTIONS:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Omeprazole
and other proton pump inhibitors are metabolized by cytochrome P450
system, primarily by isoenzyme CYP2C19, and to a smaller extent by
CYP3A4. Inhibitors or inducers of these isoenzymes may affect
exposure to Omeprazole and other proton pump inhibitors. In turn,
proton pump inhibitors may alter the metabolism of some drugs
metabolized by these enzymes.</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Omeprazole
may prolong the elimination of diazepam, phenytoin, and warfarin by
slowing the breakdown of these drugs by liver. It may also interact
with other drugs broken down by the liver.</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Omeprazole
and other proton pump inhibitors can reduce the absorption of drugs
such as dasatinib, ketoconazole, itraconazole, ampicillin and iron,
whose absorption is dependent on the acid gastric pH.</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">With
voriconazole, the plasma concentration of both drugs may be
increased. </span></span></span>
</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Omeprazole
and other proton pump inhibitors should be used with atazanavir, as
it substantially reduces exposure to atazanavir.</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">The
use of Omeprazole with drugs that reduce the production of blood
cells by the bone marrow may increase their effect.</span></span></span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Exclude
the presence of gastric malignancy, as treatment with Omeprazole may
delay diagnosis by alleviating symptoms.</span></span></span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">PRECAUTIONS
AND WARNINGS:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">Pregnancy
and Lactation</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Animal
studies with Omeprazole have shown toxic effects in developing
fetuses, but no such problems have been reported in humans. However,
as with most drugs, pregnant women, and those who might become
pregnant, should not use Omeprazole unless its advantages clearly
outweigh its possible dangers.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Because
of tumorigenic potential of Omeprazole in animals at high doses, a
decision should be made on whether nursing should be discontinued or
the medicament withdrawn taking into account the importance of
Omeprazole to the mother.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">Elderly
</span></b></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Elderly
exhibit the same side effects seen in younger adults. However, older
adults are likely to have age-related reduction in kidney and/or
liver function, which could account or increased amounts of drug in
the bloodstream. Report any unusual side effects to your doctor.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">OVERDOSAGE:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">No
specific antidote for Omeprazole overdosage is known. The drug is
extensively protein bound and is, therefore, not readily dialyzed.
Overdose symptoms are likely to be similar to Omeprazole's side
effects. In the event of overdosage; treatment should be symptomatic
and supportive. Call you local poison control center or hospital
emergency room for additional information.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b><span style="text-decoration: none;">STORAGE
CONDITIONS:</span></b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Store
at temperatures not exceeding 30</span></span><sup><span style="text-decoration: none;"><span style="font-weight: normal;">o</span></span></sup><span style="text-decoration: none;"><span style="font-weight: normal;">C.</span></span></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-51912535603983341462014-12-13T22:40:00.000-08:002014-12-13T22:40:19.229-08:00Allopurinol<div style="text-align: justify;">
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>100mg
Tablet</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>300mg
Tablet</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Antigout
Drug</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>BRAND
NAME:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Zyloprim</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGY:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol
is used in gout and hyperuricemia to inhibit the enzyme xanthine
oxidase, thus preventing the oxidation of hypoxanthine to xanthine
and xanthine to uric acid. The urinary purine load, normally almost
entirely uric acid, is thereby divided between hypoxanthine,
xanthine, and uric acid, each with its independent solubility. This
results in the reduction of urate and uric acid concentrations in
plasma and urine, ideally to such an extent that deposits of
monosodium urate monohydrate or uric acid are dissolved or prevented
from forming. At low concentrations Allopurinol acts as a competitive
inhibitor of xanthine oxidase and at higher concentrations as a
non-competitive inhibitor. However, most of its activity is due to
the metabolite oxipurinol which is a non-competitive inhibitor of
xanthine oxidase.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol
is used in patients with chronic gout to correct hyperuricemia
thereby reducing the likelihood of acute attacks and preventing the
sequel of chronic gout.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">In
the initial stages of Allopurinol therapy the release of urate and
uric acid from deposits may increase concentrations of these
compounds circulating in plasma. This may trigger or exacerbate acute
attacks, hence Allopurinol should not be started until an acute
attack has completely subsided. In addition, it is recommended that
treatment should be started with a low dose increased gradually and
that an NSAID or Colchicine should also be given during the first few
months.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Up
to 90% of a dose of allopurinol is absorbed from the gastrointestinal
tract after oral administration; its plasma half-life is about 1 to 2
hours. Allopurinol's major metabolite is oxipurinol (alloxanthine)
which is also an inhibitor of xanthine oxidase with a plasma
half-life of about 15 or more hours in patients with normal renal
function, although this greatly prolonged by renal impairment. Both
Allopurinol and oxipurinol are conjugated to form their respective
ribonucleosides. Allopurinol and oxipurinol are not bound to plasma
proteins.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">For
the treatment of hyperuricemia associated with chronic gout, acute
uric acid nephropathy, recurrent uric acid stone formation, enzyme
disorders, and cancer chemotherapy. It is also used in the management
of renal calculi caused by the deposition of calcium oxalate.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">A
suggested starting dose of Allopurinol is 100mg daily by mouth,
gradually increased by 100mg for example at weekly intervals until
the concentration of urate in plasma is reduced to 0.36 mmol per
liter (6mg per 100ml) or less. A daily dose range of 100 to 300 mg
may be adequate for those with mild to moderate gout and up to 600mg
for those with moderately severe tophaceous gout. The maximum
recommended daily dose is 800mg in the USA and 900mg in the UK. Up to
300mg may be taken as single daily dose; larger amounts should be
taken in divided doses to reduce the risk of gastric irritation.
Taking Allopurinol after food will also minimize gastric irritation.
Patients should maintain an adequate fluid intake to prevent renal
xanthine deposition. Or as prescribed by a physician.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">If
you forget to take your regular dose of Allopurinol, take the missed
dose as soon as possible. If it is time for your next regular dose,
double this dose. For example, if your regular dose is 300 mg and you
miss a dose, take 600mg at the next usual dose time.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATION:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol
is contraindicated to patients with hypersensitivity reactions. If
Allopurinol has taken and developed a rash or any other adverse
effects, stop taking the medication immediately and contact your
doctor.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Liver
toxicity have been associated with Allopurinol; they improved when
the drug was stopped. Periodic liver and kidney test should be
performed while taking this medicine. People with severely
compromising kidney function should take a reduced dose of this
medicines.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
<b>most common</b> adverse drug reaction of Allopurinol is skin rash.
Rashes are generally maculopapular or pruritic, but more serious
hypersensitivity reactions may occur and include exfoliative rashes,
the Stevens-Johnson Syndrome, and toxic epidermal necrolysis. It is
therefore recommeded that Allopurinol be withdrawn immediately if a
rash occurs.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Less
common: </b>Nausea, vomiting diarrhea, intermittent stomach pains,
effects on blood components, and drowsiness or lack of ability to
concentrate.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Rare:
</b><span style="font-weight: normal;">E</span>ffects on the eyes,
loss of hair, fever, chills, difficulty breathing or asthma-like
symptoms, arthritis-like symptoms, itching, loosening of the
fingernails, pain in the lower back, unexplained nosebleeds,
cataracts, conjunctivitis and other eye conditions, numbness,
tingling or pain in the hands or feet, confusion, dizziness,
fainting, depression, memory loss, ringing or buzzing in the ears,
weakness, sleeplessness, and feelings of ill health.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<ol style="text-align: justify;">
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Drugs
that can increase uric acid concentrations may decrease the efficacy
of Allopurinol. Aspirin and the salicylates possess this activity
and should generally be avoided in hyperuricemia and gout.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Large
doses of drugs that make your urine more acid, like megadoses of
vitamin C, may increase the possibility of kidney stone formation.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">An
increase in hypersensitivity reactions, and possibly also other
adverse effects, has been reported to patients with Allopurinol with
ACE inhibitors or thiazide diuretics, particularly to patients with
impaired renal function. </span>
</div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Alcohol,
Diazoxide, Mecamylamine, or Pyrazinamide can increase the amount of
uric acid in your blood, requiring a possible increase in your
Allopurinol dose.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Large
doses of Allopurinol (more than 600mg per day) may increase the
effects of and chances for toxic reactions to Theophylline by
interfering with its clearance from the body.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
metabolism of Azathioprine, Mercaptopurine, or Cyclophosphamide and
other anticancer medicines is inhibited by Allopurinol and their
doses should be reduced to one-quarter to one-third of the usual
dose when either of them is given with Allopurinol to avoid serious
bleeding, or infection, and potentially life-threatening toxicity.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dacarbazine,
Probenecid, or Sulfinpyrazone may cause additive reductions in uric
acid when taken with Allopurinol.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol
may interact with anticoagulant (blood-thinning) medications,
reducing the rater at which the anticoagulant is broken down in the
body. Dosage reduction is necessary.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Using
Vidarabine and Allopurinol together can increase the risk of
neurotoxic effects and anemia, nausea, pain and itching.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol
can reduce the breakdown of Chlorpropamide (for diabetes), causing
an increase in antidiabetic effect. Dosage adjustment may be
necessary.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">People
who are susceptible to Ampicillin, Amoxicillin, Bacampicillin, or
Hetacillin rash are more likely to have that problem while also
taking Allopurinol.</span></div>
</li>
</ol>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>SPECIAL
PRECAUTIONS:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="font-style: normal; margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Liver
and Kidneys Impairment:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">Dosage
should be reduced in renal impairment and in hepatic impairment;
extra monitoring may be necessary. Care is advised in patients being
treated for hypertension or cardiac insufficiency, who may have
concomitant renal impairment.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Pregnancy
and Lactation:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">This
drug may cause birth defects or interfere with your baby's
development. Check with your doctor before taking it if you are, or
might be, pregnant. A nursing mother should not take this medication,
since it will pass through the mother's milk to the child.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Elderly:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">No
special precautions are required. Be sure to follow your doctor's
directions and report any side effects at once.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Effects
on ability to drive and use machines:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="font-weight: normal; margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Allopurinol can make you drowsy
or make it difficult for you to concentrate. Take care while driving
a car or operating hazardous equipment.</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="font-weight: normal; margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="font-weight: normal; margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE:</b></span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="font-weight: normal; margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Arial,Helvetica,sans-serif;">Store at temperatures not
exceeding 30<sup>o</sup>C</span></div>
<div style="text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;">
</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-23876583415047010062014-12-11T23:46:00.000-08:002014-12-11T23:46:05.542-08:00Acetaminophen / Paracetamol
<div align="JUSTIFY" style="margin-bottom: 0in;">
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
/ Paracetamol</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>325mg
Tablet</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;"><b>
</b></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>500mg
Tablet</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;"><b>
</b></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>100mg/ml
Suspension or Syrup</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;"><b>
</b></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>120mg/ml
Suspension or Syrup</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;"><b>
</b></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>125mg/ml
Suspension</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;"><b>
</b></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>250mg/ml
Suspension or Syrup</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Analgesic
and Antipyretic Drug</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>BRAND
NAMES:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Tylenol;
Tempra; Panadol; Biogesic</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
produces analgesia by raising the threshold of the pain in the brain
and by obstructing impulses at the pain mediating chemoreceptors. The
drug produces antipyresis by an action on the hypothalamus; heat
dissipation is increased as a result of vasodilation and increased
peripheral blood flow.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
is readily absorbed from the gastrointestinal tract with peak plasma
concentrations occurring about 10 to 60 minutes after oral doses.
Acetaminophen is distributed into most body tissues. It crosses the
placenta and is present in breast milk. Plasma-protein binding is
negligible at usual therapeutic concentrations but increases with
increasing concentrations. The elimination half-life of Acetaminophen
varies from about 1 to 3 hours.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Paracetamol,
other name of Acetaminophen, is metabolized predominantly in the
liver and excreted in the urine mainly as the glucoronide and sulfate
conjugates. Less than 5% is excreted as unchanged acetaminophen. A
minor hydroxylated metabolite (N-acetyl-p-benzoquinoneimine) is
usually produced in very small amounts by cytochrome P450 isoenzymes
(mainly CYP2E1 and CYP3A4) in the liver and kidney. It is usually
detoxified by conjugation with glutathione but may accumulate
following acetaminophen overdosage and cause tissue damage.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
has analgesic and antipyretic properties and therefore commonly used
for the symptomatic management of pain and fever associated with
common childhood disorders, tonsillitis, upper respiratory tract
infections, post immunization reaction and other conditions including
prevention of febrile convulsions. Acetaminophen is also effective in
the short-term management of osteoarthritis of the knee, and is
suitable for patients sensitive to aspirin.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
<b>usual adult dose</b> by mouth is 0.5 to 1g every 4 to 6 hours up
to maximum dose of 4g daily. Avoid taking more than 2.6g (eg. 8
pieces of 325mg tablets) per day for long periods of time.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Usual
doses in children</b> under 3 months is 10mg per kg body weight; 3
months to 1 year is 60 to 120mg; 1 to 5 years is 120mg to 250mg; 6 to
12 years is 250mg to 500mg. The doses may be given every 4 to 6 hours
when necessary up to a maximum 4 doses in 24 hours. Or as prescribed
by the physician.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
may be taken without regard of food.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Avoid
alcoholic beverages when taking acetaminophen. Alcoholic beverages
will worsen the liver damage that acetaminophen can cause. </span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">If
you forget to take a dose of Acetaminophen, take it as soon as you
remember. If it is within an hour of your next dose, skip the
forgotten dose and continue with your regular schedule. Do not take a
double dose.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
is contraindicated in patients who are hypersensitive to it. Do not
take Acetaminophen for more than 10 days in a row unless directed by
your doctor. Do not take more than is prescribed or recommended on
the package.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">This
drug is also contraindicated to patients who have kidney or liver
disease or viral infections of the liver. Large amounts of alcohol
increases the liver toxicity of large doses or overdoses of
Acetaminophen. Avoid alcohol if you regularly use large doses of
Acetaminophen.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen
has rarely been found to produce any side effects in therapeutic
doses and is usually well tolerated by aspirin sensitive patients.
Adverse effects may result from a single toxic dose of the drug or
from long-term ingestion. The following adverse reactions have been
reported; liver damage, rash, itching, fever, lowered blood sugar,
stimulation, yellowing of the skin (cyanosis) or eyes, and/or
hematological toxicity such as thrombocytopenia, methemoglobinemia,
and renal damage.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Absorption
of Acetaminophen may be accelerated by drugs such as
Metoclopraminde.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Excretion
may be affected and plasma concentrations altered when given with
Probenecid.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Cholestyramine
reduces the absorption of Paracetamol if given within 1 hour.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Acetaminophen's
effects may be reduced by long-term use or large doses of
barbiturate drugs, Carbamazepine, Phenytoin (and similar drugs),
Rifampin, and Sulfinpyrazone. These drugs are possible hepatotoxic
drugs or drugs that induce liver microsomal enzymes also, which may
increase liver toxicity if taken with Acetaminophen.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Avoid
alcoholic beverages when taking Acetaminophen. Alcoholic beverages
can increase the chances for liver toxicity and possible liver
failure with Acetaminophen.</span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PRECAUTION</b>:</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Paracetamol
should be given with care to patients with impaired kidney or liver
function. It should also be given with care to patients with alcohol
dependence.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Pregnancy
and Lactation:</b></i></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">This
drug is considered safe for use during pregnancy when taken in usual
doses. Taking continuous high doses of the drug may cause birth
defects or interfere with your baby's development. Three cases of
congenital hip dislocation appear to have been associated with taking
Acetaminophen. Check with your doctor before taking it if you are, or
might be, pregnant.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Elderly:</b></i></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Elderly
may take Acetaminophen as directed by a doctor.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>OVERDOSAGE</b>:</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Symptoms
of overdosage may include nausea, vomiting, abdominal pain,
diaphoresis, generalized weakness and lethargy. If overdosage of
Acetaminophen is suspected, blood should be withdrawn immediately for
Acetaminophen plasma assay, without regard to the presence or absence
of symptoms. The acute hepatotoxicity and nephrotoxicity of
Acetaminophen can be overcome by the administration of sulphydryl
donors (eg. N-acetylcysteine) which should be given as soon as
possible after ingestion. Treatment after 12 hours is not effective.
Paracetamol overdosage should be treated with gastric lavage if the
patient is seen within 24 hours of ingestion of the drug. The patient
should be taken to the hospital emergency room for further evaluation
and treatment. Always bring the medication bottle or the drug itself.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>STORAGE:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Store
at temperatures not exceeding 30<sup>o</sup>C.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-12100593306001420902014-12-10T21:28:00.000-08:002014-12-10T21:28:47.366-08:00Aspirin
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Aspirin</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">80mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">100mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">300mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">500mg
Tablet</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
CATEGORY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Analgesic;
Anti-inflammatory agent; Anticoagulant agent</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOLOGY:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>General
Pharmacology:</b></i></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
action o aspirin is vastly due to its capacity to inhibit
prostaglandin biosynthesis. It does this by irreversibly blocking the
enzyme cyclooxygenase (prostaglandin synthase), which catalyzes the
conversion of arachidonic acid to endoperoxide compounds. At
appropriate doses, the drug decreases the formation of both the
prostaglandins and thomboxane A<sub>2 </sub>but not the leukotrienes.
Most of an anti-inflammatory dose of aspirin is rapidly deacetylated
to form salicylate as the active metabolite. Salicylate reversibly
inhibits prostaglandin synthesis.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Analgesic
Action:</b></i></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
acts peripherally through its effects on inflammation but probably
also inhibit pain stimuli at a subcortical site.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Antipyretic
Action:</b></i></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
alleviates fever by causing blood vessels in the skin to open,
allowing heat to leave the body more rapidly.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Platelet
Action:</b></i></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
inhibit platelet aggregation secondary to inhibition of thromboxane
synthesis. Because its action is irreversible, aspirin inhibits
platelet aggregation for up to 8 days until new platelets are formed.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>PHARMACOKINETICS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">The
salicylates are rapidly absorbed from the stomach and upper small
intestines, yielding a peak plasma salicylate level within 1 to 2
hours. The acid medium in the stomach keeps a large fraction of the
salicylate in the nonionized from, promoting absorption. However,
when high concentration of salicylate enter the mucosal cell, the
drug may damage the mucosal barrier. If the gastric pH is raised by a
suitable buffer to 3.5 or higher, gastric irritation is minimized.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
is absorbed as such and is hydrolyzed to acetic acid and salicylate
by esterases in tissue and blood. Salicylate is bound to albumin,
but, as the serum concentration of salicylate increases, a greater
fraction remains unbound and available to tissues. Ingested
salicylate and that generated by the hydrolysis converted to
water-soluble conjugates that are rapidly cleared by the kidney. When
this pathway becomes saturated, a small increase in plasma levels.
Alkalinization of the urine increases the rate of excretion of free
salicylate. When aspirin is used in low doses (600mg), elimination is
in accordance with first order kinetics and the serum half-life is 3
to 5 hours. With higher dosage, zero-kinetics prevail; at
anti-inflammatory dosage (≥4
g/d), the half-life increase to 15 hours or more. This effect occurs
in about a week and is related to saturation of hepatic enzymes that
catalyze the formation of salicylate metabolites,
salicylphenylglucuronide and salicyluric acid.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>INDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Quick
relief of mild to moderate pain such as headache, neuralgia and
periodic pains. It reduces fever discomfort in colds and flu. It is
also use for prophylaxis of patients who suffer from thromboembolic
disorders in preventing myocardial infarction and transient ischemic
attacks. Aspirin in a long term effect may reduce cataract formation
according to some studies.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Adult:</b>
100mg tablet once a day for prophylaxis of thromboembolic disorders.
Headache, rheumatism, muscular pains, toothache, neuralgia, periodic
pains, fever and discomfort in colds and flu: 1 to 2 tablets. Repeat
3 to 4 hours if necessary.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>Children:
</b>5 yrs old 1 tab; 3 to 5 ½ tab. Repeat if necessary but not
greater than 3 times daily. Caution when given to children age 16 and
under, Reye's syndrome may can acquire.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Take
aspirin immediately after meals, because it can cause upset stomach
or bleeding. If you forget to take a dose of Aspirin, take it as soon
as you remember. If it is almost time for your next dose, skip the
forgotten dose and continue with your regular schedule. Do not take a
double dose.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>CONTRAINDICATIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
is contraindicated to individuals who have history of
salicylate-induced asthma. It is also contraindicated to patients who
are suffering from active peptic ulcers, hemorrhagic diathesis,
severe renal or cardiac failure and those taking methotrexate at
doses of ≥15mg/wk. Aspirin
should not be used by
patients who are hypersensitive to this medication.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>ADVERSE
DRUG REACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Most
Common:</b></i> Nausea,
upset stomach, heartburn, loss of appetite, and loss of small amounts
of blood in the stool.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><i><b>Rare:</b></i>
Hives, rashes, liver damage, fever, thirst, and difficulties with
vision. Aspirin may develop dizziness, hearing loss, or
ringing or buzzing in your ears. Aspirin
may contribute to the formation of stomach ulcers and bleeding.
People who are allergic to Aspirin and those with a history of nasal
polyps, asthma, or rhinitis may experience breathing difficulty and a
stuffed nose.</span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><br /></span>
</div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;"><b>DRUG
INTERACTIONS:</b></span></div>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span><ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Patients
who are taking other anticoagulant drugs (such as clopidogrel,
warfarin) should avoid Aspirin. The effect of anticoagulant will be
augmented.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Do
take aspirin concomitantly with adrenal corticosteroids,
phenylbutazone, or alcoholic beverages.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Aspirin
may increase blood levels of Methotrexate and of Valproic Acid when
taking with either of these drugs, leading to increased chances of
drug toxicity. Aspirin and Nitroglycerin tablets may lead to an
unexpected drop in blood pressure.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Avoid
taking Aspirin with a NSAID. There is no benefit to the combination,
and the chance o side effects, especially stomach irritation, is
vastly increased.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Large
Aspirin doses (2000mg per day or more) can lower blood sugar. This
can be a problem in diabetics who take insulin or oral antidiabetes
drugs to control their condition.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Do
not take aspirin with carbonated drinks or acidic beverages. Doing
so may lead to increased stomach acidity leading to severe stomach
irritation or bleeding.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Arial,Helvetica,sans-serif;">Milk
or other basic food can slower Aspirin absorption, because aspirin
can be absorbed faster in an acidic environment. When aspirin is
taken with these food ionization will occur and aspirin will not be
absorbed.</span></div>
</li>
</ol>
<span style="font-family: Arial,Helvetica,sans-serif;">
</span>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-27499872930438268252014-12-08T21:21:00.001-08:002014-12-08T21:21:46.954-08:00LORATADINE<div style="text-align: justify;">
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>LORATADINE</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">10mg
Tablet</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">5mg/5ml
Syrup</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>BRANDNAME:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Claritin;
Loraday; Allerta</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>DRUG
CATEGORY:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Antihistamine
( H1-receptor antagonist)</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>INDICATION:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Loratadine
is prescribed for relief signs and symptoms of chronic urticaria and
other allergic dermatologic disorders. Relief of symptoms associated
with allergic rhinitis especially sneezing, nasal discharge and
itching, as well as ocular itching and burning. Loratadine is also
used for asthmatics whose asthma may be triggered by an allergic
reaction. Prescribed also to patient with throat itchiness or
irritation that lead to simultaneous coughing.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>PHARMACOLOGY:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Loratadine
is a long-acting trycyclic antihistaminic with selective peripheral
histamine H1-receptor antagonistic activity. Loratadine, a piperidine
derivative related to azatidine, is a long-acting, non-sedating
antihistamine with no significant sedative or antimuscarinic
activity. It is used for the symptomatic relief of allergic
conditions including rhinitis and chronic urticaria.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>PHARMACOKINETICS:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Loratadine
is rapidly absorbed from the gastrointestinal tract after oral
administration, peak plasma concentrations being attained in about
one hour. Bioavailability is increased and time to peak plasma
concentration is delayed when administered with food. Loratadine
undergoes extensive metabolism. The major metabolite,
descarboethoxyloratadine (desloratadine) has potent antihistamine
activity. Reported mean elimination half-life for Loratadine and
descarboethoxyloratadine are 8.4 and 28 hours respectively.
Loratadine is about 98% bound to plasma proteins;
descarboethoxyloratadine is less extensively bound.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Loratadine
and its metabolites have been detected in breast milk, but do not
appear to cross the blood-brain barrier to significant extent. Most
of a dose excreted equally in the urine and feces, mainly in the form
o metabolite. The pharmacokinetic profile of Loratadine is children
is the 6 – 12 years age group is similar to that of adults. In a
single – dose pharmacokinetic study of 13 pediatric volunteers (age
8 – 12 years) given 10ml of Loratadine syrup containing 10mg
Loratadine , the ranges of individual subject values or
pharmacokinetic parameters (AUC and C<sub>max</sub>) were comparable
to those following administration of 10mg tablet or syrup to adult
volunteers.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>DOSAGE
AND ADMINISTRATION:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Adult
and children over 12 years: </b>1 tablet or 2 tsp once a day.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Children:
2 – 12 years over 66lbs (30kg) 2 tsp once a day, 2 – 12 year <span style="font-family: Times New Roman, serif;">≤
66lbs (30kg) 1 tsp, 1 – 2 yr ½ syrup once a day</span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;">Patient
with </span><span style="font-family: Times New Roman, serif;"><b>liver or kidney
disease</b></span><span style="font-family: Times New Roman, serif;"> should take
10mg every other day.</span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;">Dosage
may also depend on your doctor's order.</span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;">Loratadine
should be taken on an empty stomach 1 hour before or 2 hours after
meals. It may be taken with food or mild if it upsets your stomach.
If you forget to take a dose of Loratadine, take it as soon as you
remember. If its is almost time for your nest regularly scheduled
dose, skip the one you forgot and continue with your regular
schedule. Do not take a double dose.</span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b><span style="font-family: Times New Roman, serif;">CONTRAINDICATION:</span></b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;">Loratadine
is contraindicated in patients who are hypersensitive to this
medication.</span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b><span style="font-family: Times New Roman, serif;">SPECIAL
PRECAUTION:</span></b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;"><b>Liver
Dysfunction:</b></span><span style="font-family: Times New Roman, serif;"> People
with liver disease should receive smaller doses of Loratadine that
others because they are unable to clear the drug as rapidly from
their bodies. </span></span>
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;"><b>Renal
Impairment: </b></span><span style="font-family: Times New Roman, serif;">The
disposition of Loratadine does not appear to be significant altered
in patients with severe renal insufficiency and hemodialysis does not
appear to be an effective means o removing Loratadine or its
metabolite descarboethoxyloratadine from the body.</span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>ADVERSE
DRUG REACTION:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Most
Common:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Headache,
dry mouth, and drowsiness or fatigue.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Less
Common:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Eyes,
Ears and Nose:</b></i> Tearing, blurred vision, conjunctivitis,
earache, eye pain, ringing or buzzing in the ears, dizziness, rapid
eye-muscle spasms, dry nose, stuffed nose, runny nose and nosebleeds.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Skin:</b></i>
Sweating, flushing, itching, rash, dry hair or skin, unusual
sensitivity to the sun, black and blue marks.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Urogenital
System:</b></i> Male impotence, loss of sex drive, breast pain,
vaginal irritation, menstrual changes, altered urination, and urine
discoloration.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Gastrointestinal
System:</b></i> Thirst, nausea and vomiting, abdominal distress,
stomach irritation or upset, constipation, diarrhea, taste changes,
sore throat and vomiting blood.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Musculoskeletal
System: </b></i><span style="font-style: normal;"><span style="font-weight: normal;">B</span></span>ack
pain, leg cramps, toothache and joint or muscle aches or pains.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Respiratory
System:</b></i> Respiratory infection, breathing difficulty,
coughing, sneezing, bronchitis, bronchial spasm and laryngitis.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Circulatory
System:</b></i> Blood pressure changes and heart palpitation.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Nervous
System:</b></i> Migraine</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Psychological:
</b></i>Hyperactivity, appetite changes, anxiety, depression,
agitation, sleeplessness, memory lapse, loss of concentration,
paranoia, confusion and nervousness.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Extremities:</b></i>
Tingling in the hands or feet and tremors.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><i><b>Others:</b></i>
Fever, chills, feelings of ill health, weakness, worsening of
allergic symptoms and fainting.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Rare:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Breast
enlargement, yellowing of the skin or eyes; hepatitis; hair loss;
swelling in the legs, ankles, or feet; seizures and erythema
multiforme ( a very specific skin reaction).</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Dizziness
or fainting may be the first sign of serious drug side effects. Call
your physician at once if this happens to you. Report sore throat;
unusual bleeding, bruising, tiredness, or weakness; or any other
unusual side effects to your doctor.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>SPECIAL
PRECAUTION:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Pregnancy
and Nursing Mothers:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Animal
studies of Loratadine have not revealed any adverse effect on the
developing fetus. Nevertheless, you should not take any antihistamine
without your doctor's knowledge if you are pregnant. Loratadine
should be used during pregnancy only if clearly needed or after
judging the risk-benefit ratio.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Loratadine
and its metabolite, discard descarboethoxydesloratadine, easily pass
in to breast milk and achieve concentration that are equivalent to
plasma levels, and may effect a nursing infant. Nursing mothers
should avoid Loratadine or use an alternative feeding method while
taking the medicine.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Elderly:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Elderly
are unlikely to experience nervous-system effects with Loratadine, as
opposed to some of the older, more sedating antihistamines. However,
older adults, especially those with liver disease, will be more
likely to experience drug side effects than their younger
counterparts. Report nay unusual side effects to your doctor..</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Effects
on ability to drive and use machines:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><span style="font-family: Times New Roman, serif;"><span style="text-decoration: none;"><span style="font-weight: normal;">Patients
should be advised that they may experience undesirable effects such
as dizziness, sedation and accommodation disorder during treatment
with Loratadine. Therefore, caution should be recommended when
driving a car or operating machinery. If patients experience the
above mentioned side effects they should avoid potentially hazardous
tasks such as driving or operating machinery.</span></span></span></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b><span style="font-family: Times New Roman, serif;"><span style="text-decoration: none;">DRUG
INTERACTION:</span></span></b></span></div>
<ol style="text-align: justify;">
<li><div style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Loratadine
does not interact with alcohol or other nervous-system depressant to
produce drowsiness or loss of coordination.</span></div>
</li>
<li><div style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Loratadine
may possible interact with Ketoconazole, Erythromycin, Cimetidine,
Ranitidine or Theophylline and can increase plasma concentration of
Loratadine. Co-administration with these drugs are known to inhibit
hepatic metabolism of Loratadine.</span></div>
</li>
</ol>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>OVERDOSAGE:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Loratadine
overdose is likely to cause drowsiness, headache, and rapid heartbeat
as general symptoms. Exaggerated drug side effects may also occur.
Overdose victim should be given Syrup of Ipecac to make them vomit
and be taken to a hospital emergency room for treatment. Supportive
measures should instituted and maintained for as long as necessary.
Call your local poison center or hospital emergency room for
instructions. Always bring the prescription order or bottle with you.
Loratadine is not eliminated by hemodialysis. It is not known if
Loratadine is eliminated by peritoneal dialysis.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>STORAGE:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 25<sup>o</sup>C. Protect from light.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Keep
out of reach of children.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
Unknownnoreply@blogger.com2tag:blogger.com,1999:blog-3465762249352810871.post-7269000699019804632014-12-08T00:45:00.000-08:002014-12-08T00:48:19.062-08:00Acarbose<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>ACARBOSE</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">50mg
Tablet</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">100mg
Tablet</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
<b>BRAND NAMES:</b><br />
Glucobay; Precose<b> </b><br />
<b> </b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>DRUG
CATEGORY: </b> </span><br />
<span style="font-family: Times New Roman, serif;">Antidiabetic (Type II)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>PHARMACODYNAMICS:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Acarbose
works against diabetes in a way different from all other antidiabetes
medicines. It interferes with enzymes in the intestine responsible
for breaking the complex carbohydrates found in starchy foods down
into simple sugars, including glucose, and lowers blood sugar by
delaying the absorption of glucose into the blood. Because it works
by a different method than the sulfonylurea-type oral antidiabetes
drugs and Metformin, the blood-sugar-lowering effect of Acarbose is
additive to that of other antidiabetes drugs. Acarbose may also be
used by people who are unable to control their blood sugar by diet
alone. Half of each dose of Acarbose remains unchanged in the
intestines and passes out of the body in the stool, and about 2% is
absorbed into the blood, and the rest is broken down in the
intestines. Most of Acarbose's side effects are directly related to
the fact that it leaves undigested carbohydrate in the lower
intestines. In studies of Acarbose, both black and white patients
responded similarly, but a better response was seen in Hispanic
patients.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>DOSAGE
AND ADMINISTRATION</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Adult
Additional Therapy in patients with Diabetes Mellitus:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Initially
3 times 1 tab 500mg/day or 3 times ½ tab 100mg/day up to 3 times 1
tab 100mg/day. Further increase to 3 times 200mg acarbose/day may
occasionally necessary.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Impaired
glucose tolerance:</b> 100mg 3 times a day.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">It
is not recommended for children.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>SPECIAL
PRECAUTION:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">It
is essential to take each dose of Acarbose at the beginning of each
meal. Since the drug works in the intestines, it has to be there at
the same time as the food you are digesting.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
with all antidiabetes medicines, people taking Acarbose must follow
their physician's instructions for diet and exercise. Read product
labels carefully or check with your pharmacist before buying any
nonprescription medicine to be sure it is safe for diabetics to take
with Acarbose.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">If
you forget a dose of Acarbose, skip it and continue with your regular
schedule. Taking a missed dose later on will not provide any benefit.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>SIDE
EFFECTS:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Gastrointestinal:
</i>Stomach gas (which 75% of the people who take it experience it),
abdominal pains, and diarrhea. But these side effects tend to improve
or go away after a few weeks. </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Liver
and other organs:</i> Liver irritation and some minor abnormalities
in blood tests.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>CONTRAINDICATION:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Acarbose
should not be used if you are hypersensitive to it. People should not
use Acarbose if they have diabetic ketoacidosis, cirrhosis, severe
kidney disease, inflammatory bowel disease, ulcers of the colon,
intestinal obstruction, severe digestive disease, or absorption
disease, or if intestinal gas will be a severe problem. It is also
contraindicated to patient with hepatic impairment such as CrCl <25
ml/min/1.73ml and liver inflammation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>DRUG
INTERACTIONS:</b></span></div>
<ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Augments
blood-sugar-lowering effect of sulfonylurea and other antidiabetes
drugs.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Drugs
such as diuretics, thyroid hormones, corticosteroids,
phenothiazines, estorgens, oral contraceptives, phenytoin, nicotinic
acid stimulants and decongestants, calcium channel blockers, and
isoniazid which can raise blood sugar can decrease effects of
Acarbose.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Activated
charcoal, antacids, and other drugs intended to absorb stomach
contents, and digestive enzyme preparations may reduce the
effectiveness of Acarbose. Separate these drugs from Acarbose by at
least 2 hours.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Cholestyramine,
intestinal absorbents and digestive enzymes may attenuate its
effect.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Acarbose
must be taken at the beginning (with the first bite) of each meal.</span></div>
</li>
</ol>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>USE
IN ELDERLY:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Blood
levels of Acarbose are higher in older adults, but this is not
considered important. Older adults with severe kidney disease should
avoid this medicine.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>USE
IN PREGNANCY AND LACTATING:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Animal
studies of Acarbose showed no effects on the developing fetus. There
is no information available on the effects of Acarbose in pregnant
women. As with all medicines, Acarbose should be taken during
pregnancy only if absolutely necessary and only if the potential
risks have been completely discussed with your doctor. </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">It
is not known if Acarbose passes into breast milk. Nursing mothers who
must take this medicine should consider bottle-feeding their babies.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>OVERDOSAGE:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
has no reported with Acarbose overdosage, but diarrhea, abdominal
pains, and intestinal gas can expected. Excess blood-sugar-lowering
should not occur. Call your local poison center for more information.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>STORAGE
CONDITION:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 30<sup>o</sup> C.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-37387569801897556952013-08-04T06:56:00.000-07:002013-08-04T06:56:05.311-07:00Bupivacaine Hydrochloride<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Bupivacaine
Hydrochloride</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>5mg/ml
Solution for Spinal Injection</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Drug
Category: </b>Local Anesthetic</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Brand
Name:</b> Sensorcaine 0.5% Heavy</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Clinical
Particulars</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Therapeutic
Indications:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Spinal
anesthesia for surgery, e.g. urological surgery and surgery on the
lower limbs lasting 2-3 hours, abdominal surgery lasting 45-60
minutes.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Dosage
and method of administrations:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
hydrochloride Spinal Heavy should only be used by clinicians with
experience of regional anesthesia or under their supervision. The
lowest possible dose for adequate anesthesia should be used.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">The
doses given below are guides for adults and the dosage should be
adjusted to the individual patients.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">The
dose should be reduced in elderly patients and patients in late
stages of pregnancy.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><span style="font-size: small;">
</span><span style="font-size: small;">
</span><span style="font-size: small;">
</span><span style="font-size: small;">
</span><table border="0" cellpadding="2" cellspacing="0" style="width: 567px;">
<colgroup><col width="142"></col></colgroup><colgroup><col width="78"></col></colgroup><colgroup><col width="82"></col></colgroup><colgroup><col width="129"></col></colgroup><colgroup><col width="115"></col>
</colgroup><tbody>
<tr valign="TOP">
<td height="60" width="142">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Indication</span></span></div>
</td>
<td width="78">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Dose mL</span></span></div>
</td>
<td width="82">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Dose mg</span></span></div>
</td>
<td width="129">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Time to onset of
effect in minutes (approx.)</span></span></div>
</td>
<td width="115">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Duration of
effect in hours (approx.)</span></span></div>
</td>
</tr>
<tr valign="TOP">
<td height="60" width="142">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Urological
surgery<br /><br />Surgery on lower limbs, including hip
surgery<br /><br />Abdominal surgery (including cesarean section)</span></span></div>
</td>
<td width="78">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">1.5-3 ml<br /><br />2-4
ml<br /><br /><br /><br />2-4 ml</span></span></div>
</td>
<td width="82">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">7.5-15 mg<br /><br />10-20
mg<br /><br /><br /><br />10-20 mg</span></span></div>
</td>
<td width="129">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">5-8 min<br /><br />5-8
min<br /><br /><br /><br />5-8 min</span></span></div>
</td>
<td width="115">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">2-3 hours<br /><br />2-3
hours<br /><br /><br /><br />45-60 min</span></span></div>
</td>
</tr>
</tbody></table>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">The
recommended injection site is the L<sub>3</sub>-L<sub>4</sub>
intervertebral space. There is currently no experience of doses
higher than 20 mg. A spinal injection is given only after the
subarachnoid space has been clearly identified by means of lumbar
puncture (clear cerebrospinal fluid runs out via the spinal needle or
is seen on aspiration). In the event of unsuccessful anesthesia, a
new attempt to administer the drug should only be made by injecting
at a different level and with a smaller volume. One cause of lack of
effect may be poor intrathecal distribution of the drug, and this can
be helped by altering the patient's position.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Contraindications:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Hypersensitivity
to local anesthetics of the amide type or to other components of the
product. Diseases of the central nervous system (e.g. meningitis,
poliomelitis, intracranial hemorrhage). Local pyogenic infection at
or adjacent to the injection site. Spinal stenosis and active disease
(e.g. spondylitis, tumor) or trauma (e.g. fracture of the spine).
Septicemia, pernicious anemia with subacute degeneration of the
spinal cord. Spinal anesthesia should not be given to patients in
shock. Nor should spinal anesthesia be given to patients with
coagulation disorders or to patients receiving ongoing
anticoagulation treatment. </span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Special
warning and precaution for use: </b></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">One
should be aware that spinal anesthesia can sometimes lead to major
blocks, with paralysis of intercostal muscles and the diaphragm,
especially in pregnant women.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Caution
should be exercised in patients with degree II or III-AV block since
local anesthetics can lower the conduction capacity of the
myocardium. Elderly patients and patients with severe hepatic
disease, severely impaired renal function or in generally reduced
general condition also require special attention.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Patients
treated with class III anti-arrhythmic drugs (e.g. amiodarone) should
be closely observed and ECG monitoring should be considered, since
the cardiac effects of bupivacaine and class III anti-arrhythmic
drugs can be addictive.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Like
all local anesthetic drugs, bupivacaine can cause acute central
nervous and cardiovascular toxic effects in cases of use leading to
high concentrations in the blood. This applies particularly after
inadvertent intravascular administration.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Ventricular
arrhythmia, ventricular fibrillation, sudden cardiovascular collapse
and death have been reported in association with high systemic
concentrations of bupivacaine. However, with doses normally used for
spinal anesthesia high systemic concentrations are uncommon.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">An
uncommon, but dangerous, side effect in spinal anesthesia is
extensive or total spinal blockade, which results in cardiovascular
depression and respiratory depression. The cardiovascular depression
is caused by extensive sympathetic blockade, which can result in
hypotension and bradycardia, or even cardiac arrest. Respiratory
depression can be caused by blockade of the innervation of the
respiratory muscles, including the diaphragm. There is an increased
risk of extensive or total spinal blockade in elderly patients and
patients in late stages of pregnancy. The dose should therefore be
reduced for these patients.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Spinal
anesthesia can lead to a fall in blood pressure and bradycardia. The
risk can be reduced by means of intravenous administration of
crystalloid or colloid solution. A fall in blood pressure should be
treated immediately, for example with ephedrine 5-10mg intravenously,
repeated as required.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">In
rare cases spinal anesthesia can cause neurological damage, resulting
in paresthesia, anesthesia, motor weakness and paralysis.
Neurological disorders, such as multiple sclerosis, hemiplegia,
paraplegia and neuromuscular disturbances are not thought to be
adversely affected by spinal anesthesia, but caution should be
exercised.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Interactions
with other medical products and other forms of interactions:</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
should be use with caution with other local anesthesia or drugs that
are structurally similar to local anesthetics, i.e. class IB
anti-arrhythmic drugs, as the toxic effects are additive.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">No
specific interaction studies with local anesthesia and class III
anti-arrhythmic drugs (e.g. amiodarone) have been carried out, but
caution is recommended (see Special warning and special precautions
for use).</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Pregnancy
and Lactation:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><i>Pregnancy</i></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">No
known risks for the fetus from use during pregnancy. However, note
that the dose should be reduced for patients in late stages of
pregnancy (see Special warning and special precautions for use).</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><i>Lactation</i></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
passes into breast milk, but the risk of this affecting the child
appears unlikely with therapeutic doses.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Effects
on ability to drive and use machines:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Depending
on the dose and method of administration, bupivacaine can have a
transient effect on movement and coordination.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Undesirable
effects:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><span style="font-style: normal;"><span style="font-weight: normal;">Undesirable
effects caused by the product itself can be difficult to distinguish
form </span></span>the physiological effects of the nerve block (e.g.
fall in blood pressure, bradycardia, temporary urinary retention),
events caused directly by the needle puncture (e.g. spinal hematoma)
or caused indirectly by the needle puncture (e.g. meningitis,
epidural abscess) or events associated with leakage of cerebrospinal
fluid ( e.g. post lumbar puncture headache).</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><span style="font-size: small;">
</span><table border="0" cellpadding="2" cellspacing="0" style="width: 564px;">
<colgroup><col width="181"></col></colgroup><colgroup><col width="375"></col>
</colgroup><tbody>
<tr valign="TOP">
<td height="60" width="181">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Very
common<br />(>1/10)</span></span></div>
</td>
<td width="375">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">General:
Nausea<br />Circ.: Hypotension, bradycardia</span></span></div>
</td>
</tr>
<tr valign="TOP">
<td height="60" width="181">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Common<br />(>1/100)</span></span></div>
</td>
<td width="375">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">CNS: Post lumbar
puncture headache<br />GI: Vomiting<br />Genitourinary: Urinary
retention, urinary incontinence</span></span></div>
</td>
</tr>
<tr valign="TOP">
<td height="60" width="181">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Uncommon<br />(1/100-1/1000)</span></span></div>
</td>
<td width="375">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">CNS:
Paresthesia, paresia, dysesthesia<br />Musculoskel.: Muscle
weakness, back pain</span></span></div>
</td>
</tr>
<tr valign="TOP">
<td height="60" width="181">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Rare<br />(<1/1000)</span></span></div>
</td>
<td width="375">
<div align="LEFT">
<span style="font-family: inherit;"><span style="font-size: small;">Circ.: Cardiac
arrest<br />General: Allergic reactions, anaphylactic shock<br />CNS:
Accidental total spinal blockade, paraplegia, paralysis,
neurophathy, arachnoiditis<br />Airways: Respiratory depression</span></span></div>
</td>
</tr>
</tbody></table>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Overdose:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
can cause acute toxic effects of a central nervous and cardiovascular
nature if it is given in high doses, especially if it is administered
intravascularly. However, the dose used in spinal anesthesia is low
(≤ 20% of the dose used for epidural anesthesia) and thus the risk
of overdosage is unlikely. In cases of concomitantly administration
with other local anesthetics, however, systemic toxic effects may
occur, ass the toxic effects are additive.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><i>Treatment
of complications</i></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">In
cases of total spinal blockade adequate ventilation must be ensured
(patent airways, oxygen, intubation and controlled ventialtion if
necessary). If there is a fall in blood pressure a vasopressor
(preferably with an inotropic effect) should be given, e.g. ephedrine
5-10mg intravenously.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">If
signs of acute systemic toxicity occur the administration of local
anesthesia must be stopped immediately. Treatment must be given to
maintain good ventilation, oxygenation and circulation. Oxygen must
always be given, and assisted ventilation if necessary. If
convulsions do not cease spontaneously within 15-20 seconds,
theopentone sodium 1-3 mg/kg should be given intravenously to
facilitate ventilation or diazepam 0.1 mg/kg intravenously ( acts
rather more slowly). Prolonged seizures jeopardize the patient's
respiration and oxygenation. Injection of muscle relaxants (e.g.
suxamethonium 1mg/kg) creates more favourable conditions for
ventilation and oxygenation of the patient, but requires experience
of tracheal intubation and controlled ventilation. In cases of a fall
in blood pressure/bradycardia, a vasopressor should be given (e.g.
ephedrine 5-10 mg intravenously, which may be repeated after 2-3
minutes). In the event of circulatory arrest, cardiopulmonary
resuscitation should be instituted immediately. It is important to
maintain good oxygenation, respiration and circulation, and to treat
acidosis.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Children
must be given doses in proportion to their age and body weight for
treatment of systemic toxicity.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Pharmacological
Properties</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Pharmacodynamic
Properties</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
hydrochloride spinal heavy contains bupivacaine, which is a
long-acting local anesthetic of the amide type. Bupivacaine
reversibly blocks impulse conduction in the nerves by inhibiting the
transport of sodium ions through the nerve membrane. Similar effects
can also be seen on excitatory membranes in the brain and myocardium.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
hydrochloride spinal heavy is intended for hyperbaric spinal
anesthesia. The relative density of the solution for injection is
1.026 at 20<sup>o</sup>C (equivalent to 1.021 at 37<sup>o</sup>C) and
the initial distribution into the subarachnoid space is markedly
influenced by gravity.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">For
administration into the spine, a small dose is given, which gives a
relatively low concentration and short duration of effects.
Bupivacaine hydrochloride spinal (without glucose) produces a less
predictable block, but with a longer duration of effects than
bupivacaine hydrochloride spinal heavy (with glucose).</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Pharmacokinetic
Properties:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
is very liposoluble with an oil/water distribution coefficient of
27.5.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
displays complete and bi-phasic absorption from the subarachnoid
space, with half-lives for the two phases of approx. 50 and approx.
400 minutes, with large variations. The slow absorption phase is the
rate-determining factor in the elimination of bupivacaine, which
explains why the apparent half-life is longer than after intravenous
administration.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Absorption
form the subarachnoid space is relatively slow, which, in combination
with the low dose required a spinal anesthesia, gives relatively low
plasma concentration (approx. 0.4 mg/mL per 100 mg injected).</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">After
intravenous administration, total plasma clearances is approx. 0.58
L/min, the volume of distribution in steady state is approx. 73 L,
the elimination half-life is 2.7 hours, and the hepatic extraction
ration is approx. 0.40. Bupivacaine is metabolized almost completely
in the liver, predominantly through aromatic hydroxylation to
4-hydorxybupivacaine and N-dealkylation to PPX, both of which are
mediated by cytochrome P450 3A4. Clearance is thus depended on
hepatic perfusion and the activity of the metabolizing enzyme.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Bupivacaine
crosses the placenta and the concentration of free bupivacaine is the
same in the the mother and the fetus. However, the total plasma
concentration is lower in the fetus, which has a lower degree of
protein binding.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Pharmaceutical
Particulars</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Incompatibilities:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Additions
to spinal solutions are not recommended.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Shelf-Life:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Please
refer to the expiration date.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">The
solution must be used as soon as possible after the container has
been opened.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><b>Storage:</b></span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="line-height: 0.14in; margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;">Store
at a temperature not exceeding above 25<sup>o</sup>C. Do not freeze.</span></span></div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: inherit;"><span style="font-size: small;"><br /></span></span>
</div>
<span style="font-family: inherit;"><span style="font-size: small;">
</span></span>Unknownnoreply@blogger.com1tag:blogger.com,1999:blog-3465762249352810871.post-46830583220862263312013-08-02T06:05:00.001-07:002013-08-02T06:14:19.176-07:00MEFENAMIC ACID<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>MEFENAMIC
ACID</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>500mg
Capsule</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>250mg
Capsule</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>50mg/5ml
Suspension</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>DRUG
CATEGORY: </b><span style="font-weight: normal;">Analgesic/Antipyretic,
Non Steroidal Anti-inflammatory</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>BRAND
NAME: </b><span style="font-weight: normal;">Ponstan®</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>DESCRIPTION:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is
N-(2,3,-xylyl)-anthranilic acid. It is an orally active analgesic
agent. It is a white powder with a melting point of 230-231<sup>o</sup>C,
molecular weight of 241.28, and water solubility of 0.0004% at pH
7.1.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>THERAPEUTIC
INDICATIONS</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is indicated for:</span></div>
<ol>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The symptomatic relief of
rheumatoid arthritis (including Still's Disease), osteoarthritis,
and pain including muscular, traumatic and dental pain, headaches of
most etiology, post-operative and postpartum pain.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The symptomatic relief of
primary dysmenorrhea.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Menorrhagia due to dysfunctional
causes or the presence of an intrauterine device (IUD) when organic
pelvic pathology has been excluded.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Premenstrual syndrome.</span></div>
</li>
<li><div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The relief of pyrexia in
pediatric patients over 6 months of age.</span></div>
</li>
</ol>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>DOSAGE
AND METHOD OF ADMINISTRATION</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Undesirable effects may be
minimized by using the minimum effective dose for shortest duration
necessary to control symptoms.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The oral dosage form of mefenamic
acid may be taken with food if gastrointestinal upset occurs.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mild to moderate pain/rheumatoid
arthritis/osteoarthritis in adults and adolescents over 14 years of
age: 500mg three times daily.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Dysmenorrhea: 500mg three times
daily, to be administered at the onset of menstrual pain and
continued while symptoms persist according to the judgment of the
physician.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Menorrhagia: 500mg three times
daily, starting with the onset of bleeding and associated symptoms
and continued according to the judgment of the physician.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Premenstrual syndrome: 500mg
three times daily, starting with the onset of symptoms and continued
until the anticipated cessation of symptoms according to the judgment
of the physician.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">For Still's Disease or
antipyretic action in infants and children over 6 months to 14 years:
19.5mg/kg to 25mg/kg of body weight daily in divided doses three
times daily.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Pediatric Use</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is reported to be
effective for pyrexia in pediatric patients over 6 months of age, and
for pain in adolescents over 14 years of age.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Use in the Elderly</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Impairment of renal function,
sometimes leading to acute renal failure, has been reported. Elderly
or debilitated patients seem unable to tolerate ulceration of
bleeding as well as some other individuals; most spontaneous reports
of fatal gastrointestinal events are in this patient population. (See
Special Warnings and Special Precautions for Use – Gastrointestinal
Effects)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>CONTRAINDICATIONS</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Because the potential exists for
cross-sensitivity to aspirin or other nonsteroidal anti-inflammatory
drugs, mefenamic acid should not be given to patients in whom these
drugs induce symptoms of bronchospasm, allergic rhinitis, or
urticaria.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is contraindicated
in patients with active ulceration or chronic inflammation of either
the upper or lower gastrointestinal tract and should be avoided in
patients with pre-existing renal disease.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid should not be used
in patients with known hypersensitivity or any of the components of
this drug.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Treatment of peri-operative pain
in the setting of coronary artery bypass graft (CABG) surgery.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Patients with severe renal and
hepatic failure.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Patients with severe heart
failure.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>SPECIAL
WARNINGS AND SPECIAL PRECAUTIONS FOR USE</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The use of mefenamic acid with
concomitant NSAIDs including COX-2 inhibitors should be avoided.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Cardiovascular Effects</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">NSAIDs may cause an increased
risk of serious cardiovascular thrombotic events, myocadial
infarction, and stroke which can be fatal. This risk may increase
with duration risk. Patients with known cardiovascular disease may be
at greater risk. To minimize the potential risk for an adverse
cardiovascular event in patients treated with mefenamic acid, the
lowest effective dose should be used for the shortest duration
possible. Physicians and patients should remain alert for the
development of such events, even in the absence of previous
cardiovascular symptoms. Patients should be informed about the signs
and/or symptoms of serious cardiovascular toxicity and the steps to
take if they occur (see Contraindications).</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Hypertension </span>
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">As with all NSAIDs, mefenamic
acid can lead to the onset of new hypertension or worsening of
pre-existing hypertension, either of which may contribute to the
increased incidence of cardiovascular events. NSAIDs, including
mefenamic acid, should be used with caution in patients with
hypertension. Blood pressure should be monitored closely during
initiation of therapy with mefenamic acid and throughout the course
of therapy.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Fluid Retention and Edema</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">As with other drugs known to
inhibit prostaglandin synthesis, fluid retention and edema have been
observed in some patients taking NSAIDs, including mefenamic acid.
Therefore, mefenamic acid should be used with caution in patients
with compromised cardiac function and other conditions predisposing
to, or worsened by, fluid retention. Patients with pre-existing
congestive heart failure or hypertension should be closely monitored.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Gastrointestinal Effects</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">If diarrhea occurs, the dosage
should be reduced or temporarily suspended. Symptoms may recur in
certain patients following subsequent exposure. NSAIDs including
mefenamic acid, can cause serious gastrointestinal (GI) adverse
events including inflammation, bleeding, ulceration, and perforation
of stomach, small intestine, or large intestine, which can be fatal.
When GI bleeding or ulceration occurs in patients receiving mefenamic
acid, the treatment should be withdrawn. Patients most at risk of
developing these types of GI complications with NSAIDs are the
elderly, patients with cardiovascular disease, patients using
concomitant aspirin, or patients with a prior history of, or active
gastrointestinal disease, such as ulceration, GI bleeding or
inflammatory conditions. Therefore, mefenamic acid should be used
with caution in the patients (see Contraindications)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Skin Reaction</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Serious skin reactions, some of
them fatal including exfoliative dermatitis, Stevens Johnson
syndrome, and toxic epidermal necrolysis, have been reported very
rarely in association with the use of NSAIDs including mefenamic
acid. Patients appear to be at highest risk for these events early in
the course of therapy, the onset of the event occurring in the
majority of cases within the first month of treatment. Mefenamic acid
should be discontinued at the first appearance of skin rash, mucosal
lesions, or any other sign of hypersensitivity.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Laboratory Tests</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">A false-positive reaction for
urinary bile, using the diazo tablet test, may result following
mefenamic acid administration. If biliuria is suspected, other
diagnostic procedures, such as the Harrison spot test, should be
performed.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Renal Effects</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">In rare cases, NSAIDs, including
mefenamic acid, may cause interstitial nephritis, glomerulitis,
papillary necrosis and the nephrotic syndrome. NSAIDs inhibit the
synthesis of renal prostaglandin which plays a supportive role in the
maintenance of renal perfusion in patients whose renal blood flow and
blood volume are decreased. In these patients, administration of an
NSAID may precipitate overt renal decompensation, which is typically
followed by recovery to pretreatment state upon discontinuation of
NSAID therapy. Patients at greatest risk of such a reaction are those
with congestive heart failure, liver cirrhosis, nephrotic syndrome,
overt renal disease and the elderly. Such patients should be
carefully monitored while receiving NSAID therapy.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Discontinuation of nonsteroidal
anti-inflammatory drug (NSAID) therapy is typically followed by
recovery to the pretreatment state. Since mefenamic acid metabolites
are eliminated primarily by the kidneys, the drug should not be
administered to patients with significantly impaired renal function.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Hematologic Effects</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid, like other
nonsteroidal anti-inflammatory agents, can inhibit platelet
aggregation and may prolong prothrombin time in patients on warfarin
therapy. (see Interactions with other Medicinal Products and Other
Forms of Interaction)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Hepatic effects</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Borderline elevations of one or
more liver function tests may occur in some patients receiving
mefenamic acid therapy. These elevations may progress, may remain
essentially unchanged, or may be transient with continued therapy. A
patient with symptoms and/or signs suggesting liver dysfunction, or
in whom an abnormal liver test has occurred, should be evaluated for
evidence of the development of more severe hepatic reaction while on
therapy with mefenamic acid. If abnormal liver tests persist or
worsen, if clinical signs and symptoms consistent with liver disease
develop, or if systematic manifestations occur, mefenamic acid should
be discontinued.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>INTERACTIONS
WITH OTHER MEDICINAL PRODUCTS AND OTHER FORMS OF INTERACTION</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Anticoagulants: Mefenamic acid
has been shown to displace warfarin from protein binding sites, and
may enhance the response to oral anticoagulants. Therefore,
concurrent administration of mefenamic acid with oral anticoagulant
drugs requires frequents prothrombin time monitoring.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Anti-hypertensives including
diuretics, angiotensin-converting enzyme (ACE) inhibitors and
angiotensin II antagonist (AII): NSAIDs can reduce the efficacy of
diuretics and other antihypertensive drugs.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">In patients with impaired renal
function (e.g. dehydrated patients or elderly patients with
compromised renal function), the co-administration of an ACE
inhibitor or an AIIA with a cyclo-oxygenase inhibitor can increase
the deterioration of the renal function, including the possibility of
acute renal failure, which is usually reversible. The occurrence of
these interactions should be considered in patients taking mefenamic
acid with an ACE inhibitor or an AIIA.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Therefore, the concomitant
administration of these drugs should be done with caution, especially
in elderly patients. Patients should be adequately hydrated and the
need to monitor the renal function should be assessed in the
beginning of the concomitant treatment and periodically thereafter.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Corticosteroids: Increased risk
of gastrointestinal ulceration or bleeding.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Cyclosporine: Because of their
effect on renal prostaglandins, cyclo-oxygenase inhibitors such as
diclofenac can increase the risk of nephrotoxicity with cyclosporine.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Hypoglycemic agents: There have
been reports of changes in the effects of oral hypoglycemic agents in
the presence of NSAIDs. Therefore, mefenamic acid should be
administered with caution in patients receiving insulin or oral
hypoglycemic agents.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Lithium: Nonsteroidal
anti-inflammatory drugs (NSAIDs), including mefenamic acid have
produced an elevation of plasma lithium levels and a reduction in
renal lithium clearance. Thus, when mefenamic acid and lithium are
administered concurrently, patients should be observed carefully for
signs of lithium toxicity.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Methotrexate: Caution is advised
when methotrexate is administered concurrently with NSAIDs, including
mefenamic acid, because NSAID administration may result in increased
plasma levels of methotrexate. </span>
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Tacrolimus: Possible increased
risk of nephrotoxicity when NSAIDs are given with tacrolimus.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>PREGNANCY
AND LACTATION</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Pregnancy</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">(see Preclinical Safety)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Since there are no adequate and
well-controlled studies in pregnant women, this drug should be used
only if the potential benefits to the mother justify the possible
risk to the fetus. It is known if mefenamic acid or its metabolites
cross the placenta. However, because of the effects of drugs in this
class (i.e., inhibitors of prostaglandin synthesis) on the fetal
cardiovascular system (e.g., premature closure of the ductus
arteriosus), the use of mefenamic acid in pregnant women is not
recommended. Mefenamic acid inhibits prostaglandin synthesis which
may result in prolongation of pregnancy and interference with labor
when administered late in the pregnancy. Women on mefenamic acid
therapy should consult their physician if they decide to become
pregnant.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Lactation</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Trace amounts of mefenamic acid
may be present in breast milk and transmitted to the nursing infant.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Therefore, mefenamic acid should
not be taken by nursing mothers.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>EFFECTS
ON ABILITY TO DRIVE AND USE MACHINE</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The effects of mefenamic acid on
the ability to drive or use machinery has not been systematically
evaluated.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>UNDESIRABLE
EFFECTS</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Blood and lymphatic system
disorders: agranulocytosis, aplastic anemia, autoimmune hemolytic
anemia, bone marrow hypoplasia, decreased hematocrit, eosinophilia,
leukopenia, pancytopenia, and thrombocytopenic purpura.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Immune system disorders:
anaphylaxis</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Metabolism and nutrition
disorder: glucose intolerance in diabetic patients, hyponatremia</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Psychiatric disorders:
nervousness</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Nervous system disorders: aseptic
meningitis, blurred vision, convulsions, dizziness, drowsiness,
headache, and insomnia.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Eye disorders: eye irritation,
reversible loss of color vision</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Ear and labyrinth disorders: ear
pain</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Cardiac disorders: palpitation</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Vascular disorders: hypotension</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Respiratory, thoracic and
mediastinal disorders: asthma, dyspnea</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Gastrointestinal disorders:</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The most frequently reported side
effects associated with mefenamic acid involve the gastrointestinal
tract. Diarrhea appears to be the most common side effect and is
usually dose-related. It generally subsides on dosage reduction, and
rapidly disappears on termination of therapy. Some patients may not
be able to continue therapy.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">The following are the most common
gastrointestinal side effects: abdominal pain, diarrhea and nausea
with or without vomiting.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Less frequently reported
gastrointestinal/hepatobiliary side effects include: anorexia,
cholestatic jaundice, colitis, constipation, enterocolitis,
flatulence, gastric ulceration with and without hemorrhage, mild
hepatic toxicity, hepatitis, hepatorenal syndrome, pyrosis,
pancreatitis and steatorrhea.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Skin and subcutaneous tissue
disorders: angioedema, edema of the larynx, erythema multiforme,
facial edema, Lyell's syndrome (toxic epidermal necrolysis),
perspiration, pruritus, rash, Stevens-Johnson syndrome and urticaria.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Renal and urinary disorders:
dysuria, hematuria, renal failure including papillary necrosis.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>OVERDOSE</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Following accidental overdosage,
the stomach should be emptied immediately by inducing emesis, or by
gastric lavage, followed by administration of activated charcoal.
Vital functions should be monitored and supported. Hemodialysis is of
little value since mefenamic acid and its metabolites are firmly
bound to plasma proteins.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Seizures, acute renal failure,
and coma have been reported with mefenamic acid overdoses. Overdose
has led to fatalities.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>PHARMACODYNAMIC
PROPERTIES</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Mechanism
of Action</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is a nonsteroidal
agent with demonstrated anti-inflammatory, analgesic, and antipyretic
activity in laboratory animals. It is not a narcotic. Mefenamic acid
was found to inhibit prostaglandin synthesis and to compete for
binding at the prostaglandin receptor sites in animal models.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>PHARMACOKINETICS
PROPERTIES</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Absorption</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is rapidly
absorbed from the gastrointestinal tract. Following administration of
a one gram dose to adult, peak plasma levels of 10mcg/ml occur in 1
to 4 hours, with a half-life of 2 hours. Plasma levels are
proportional to dose, following multiple doses, with no drug
accumulation. One gram of mefenamic acid administered four times
daily produces peak blood levels of 20mcg/ml by the second day of administration.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Distribution</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid is extensively
bound to plasma proteins.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Metabolism</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Mefenamic acid metabolism is
predominantly mediated via cytochrome P450 CYP 2C9 in the liver.
Patients who are known or suspected to be poor CYP2C9 metabolizers
based on previous history/experience with other CYP2C9 substrates
should be administered mefenamic acid with caution as they may have
abnormally high plasma levels due to reduced metabolic clearance.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>Elimination</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Following a single oral dose,
52-67% of the dose was recovered from the urine as unchanged drug or
one of two metabolites. Assay of stools over 3 days accounted for
20-25% of the dose, chiefly as unconjugated metabolite II.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>PRECLINICAL
SAFETY</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Rats given up to 10 times the
human dose showed decreased fertility delay in parturition, and a
decreased rate of survival to weaning. No fetal abnormalities were
observed in this study and in another study in dogs receiving 10
times the human dose.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;"><b>SPECIAL
PRECAUTIONS FOR STORAGE</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in; text-decoration: none;">
<span style="font-family: Times New Roman, serif;">Store at temperature not
exceeding 30<sup>o</sup>C. </span>
</div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-27814689610886383352013-07-27T02:52:00.000-07:002013-07-27T02:52:02.401-07:00Etoricoxib
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Etoricoxib</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>30mg Tablet</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>60mg Tablet</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>90mg Tablet</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>120mg Tablet</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Drug Category: </b>COX-2
Specific Inhibitor</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Brand Name:</b>
Arcoxia/Arcoxia Ac</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Product Description:</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib is a member of
a class arthritis/analgesia medications called, coxibs. Etoricoxib is
a highly selective inhibitor of cycloxygenase-2 (COX-2). Etoricoxib
tablets contain etoricoxib, which is described chemically as
5-chloro-6-methyl-3-[4-9methylsulfony)phenyl],-2,3`-bipyridine. The
empirical formula is C<sub>18</sub>H<sub>15</sub>CIN<sub>2</sub>OS.
The molecular weight is 358.84.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib is a white to
off-white powder. Etoricoxib is free soluble in methanol,
tetrahydrofuran, dimethyl sulfoxide, methyl ethyl ketone, dimethyl
formamide, and chloroform. Etoricoxib is soluble in isopropyl
acetate, ethanol and toluene, sparingly soluble in 2-propanol, and
practically insoluble in water.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Pharmacokinetics:</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i><b>Absorption</b></i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Orally administered
etoricoxib is well absorbed. The mean oral bioavailability is
approximately 100%. Following 12mg once daily dosing to steady-state,
the peak plasma concentration (geometirc mean C<sub>max</sub> =
3.6mcg/ml) was observed at approximately 1 hour (T<sub>max</sub>)
after administration to fasted adults. The</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
geometric mean AUC<sub>0-24hr</sub>
was 37.8 mcg<span style="font-size: x-large;"><b>.</b></span>hr/ml.
The pharmacokinetics of etoricoxib are linear across the clinical
dose range.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The standard meal had no
clinically meaningful effect on the extent or rate of absorption of a
dose of etoricoxib 120mg. In clinical trials, etoricoxib was
administered without regard to food.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The pharmacokinetics of
etoricoxib in 12 healthy subjects were similar (comparable AUC, C<sub>max</sub>
within approximately 20%) when administered alone, with a
magnesium/aluminum hydroxide antacid, or a calcium carbonated antacid
(approximately 50 mEq acid-neutralizing capacity).</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i><b>Distribution</b></i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib is
approximately 92% bound to human plasma protein over the range of
concentration of 0.05 to 5mcg/ml. The volume of distribution at
steady-state (V<sub>dss</sub>) is approximately 120L in humans.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib crosses the
placenta in rats and rabbits, and the blood-brain-barrier in rats.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i><b>Metabolism</b></i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib is extensively
metabolized with <1% of a dose recovered in urine as the parent
drug. The major route of metabolism to form the 6`-hydroxymethyl
derivative is catalyzed by cytochrome P450 (CYP) enzymes.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Five metabolites have
been identified in man. The principal metabolite in the 6`-carboxylic
acid derivative of etoricoxib formed by further oxidation of the
6`-hydroxymethyl derivative. These principal metabolites either
demonstrate no measurable activity or are only weakly active as COX-2
inhibitors. None of these metabolites inhibit COX-1.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i><b>Elimination</b></i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Following administration
of single 25mg radio labeled intravenous dose of etoricoxib to
healthy subjects, 70% of radioactivity was recovered in urine and 20%
in feces, mostly as metabolites. Less than 2% was recovered as
unchanged drug.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Elimination of etoricoxib
occurs almost exclusively through metabolism followed by renal
excretion. Steady-state concentration of etoricoxib are reached
within seven days of once-daily administration of 120mg, with an
accumulation ration of approximately 2, corresponding to an
accumulation half-life of approximately 22 hours. The plasma
clearance is estimated to be approximately 50ml/min.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Characteristic in
Patients (Special Populations)</b></div>
<div align="JUSTIFY" style="font-style: normal; margin-bottom: 0in;">
<b>Gender</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The pharmacokinetics of
etoricoxib are similar between men women. (See recommended dose.)</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Elderly</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Pharmacokinetics in
elderly (65years of age and older) similar to those in the young. No
dosage adjustment is necessary for elderly patients. (See recommended
dose).</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Race</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
There is no clinically
important effect of race on the pharmacokinetics of etoricoxib. (See
recommended dose).</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Hepatic Insufficiency</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Patients with mild
hepatic insufficiency (Child-Pugh score 5-6) administered etoricoxib
60mg once daily had an approximately 16% higher mean AUC as compared
to healthy subjects given the same regime. Patients with moderate
hepatic insufficiency (Child-Pugh score 7-9) administered etoricoxib
60m once daily; etoricoxib 30mg once daily has not been studied in
this population. There are no clinical or pharmacokinetic data in
patients with severe hepatic insufficiency (Child-Pugh score >9).
(See recommended dose, Hepatic Insufficiency).</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Renal Insufficiency</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The pharmacokinetics of a
single dose of etoricoxib 120mg in patients with moderate-to-severe
renal insufficiency and patients with end-stage renal disease on
hemodialysis were not significantly different from those in healthy
subjects. Hemodialysis contributed negligibly to elimination
(dialysis clearance approximately 50ml/min).</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Pediatric Patients</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The pharmacokinetic study
(N=16) conducted in adolescents (aged 12 to 17) the pharmacokinetics
in adolescents weighing 40 to 60 kg given etoricoxib 60mg once daily
and in adolescents >60kg given etoricoxib 90mg once daily were
similar to the pharmacokinetics in adults given etoricoxib 90mg once
daily. Safety and effectiveness of etoricoxib in pediatric patients
have not been established.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Drug Interactions with
additional pharmacokinetic data:</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The main pathway of
etoricoxib biotransformation is CYP-dependent oxidation to produce
6`-hydroxymethyl etoricoxib, which can undergo further metabolism to
the corresponding carboxylic acid or O-glucuronide. In vitro data
indicate that CYP3A4 plays a major role (approximately 60%) in the
hydroxylation of etoricoxib and that the remainder of the activity
(approximately 40%) is shared among CYP2C9, and 2D6. Administration
of a potent inhibitor of CYP3A (ketoconazole) did not increase
etoricoxib plasma concentrations to a clinically meaningful extent
(approximately 43% increase in AUC). Administration of a potent
inducer of CYP enzymes (rifampin) produced a 65% decrease in
etoricoxib plasma AUC.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The potential for
etoricoxib to inhibit or induce CYP3A4 activity was investigated in
human studies using the intravenous erythromycin breath test.
Compared to placebo, etoricoxib (120mg daily for 11 days) did not
produce any significant effect on erythromycin N-demethylation,
indicating no effect on hepatic CYP3A4 activity. Based on in vitro
studies, etoricoxib does not inhibit cytochromes P4501A2, 2C9, 2C19,
2D6, or 2E1.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Indications:</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib is indicated
for:</div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Acute and chronic
treatment of the signs and symptoms of osteoarthritis (OA) and
rheumatoid arthritis (RA)</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Treatment of
ankylosing spondylitis (AS)</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Treatment of acute
gouty arthritis</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Relief of acute pain</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Treatment of primary
dysmenorrhea.</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Treatment of
moderate to sever acute post-operative pain associated with dental
surgery.</div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
Treatment of
moderate to sever acute post-operative pain associated with
abdominal gynecological surgery</div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The decision to prescribe
a selective COX-2 inhibitor should be based on an assessment of the
individual patient's overall risks (See Warnings and Precautions).</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Recommended Dose:</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Etoricoxib is
administered orally. Etoricoxib may be taken with or without food.
Etoricoxib should be administered for the shortest duration possible
and the lowest effective daily dose should be used.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Arthritis</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Osteoarthritis</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
30mg or 60mg once daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Rheumatoid Arthritis</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
90mg once daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Ankylosing Spondylitis
</i>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
90mg once daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Acute Pain</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
For acute pain
conditions, the recommended dose is 90mg or 120mg once daily.
Etoricoxib should be used only for the acute symptomatic period,
limited to a maximum of 8 days treatement.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Acute Gouty Arthritis</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
120mg once daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Primary Dysmenorrhea</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
120mg once daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Post-operative Dental
Pain</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
90mg once daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i>Post-operative
Gynecological Pain</i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The recommended dose is
90mg once daily. The initial dose should be administered shortly
before surgery. The dose can be increased to a maximum 120mg once
daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
Doses greater than those
recommended for each indication have either no demonstrated
additional efficacy or have not been studied. Therefore:</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for OA should
not exceed 60mg daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for RA should
not exceed 90mg daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for ankylosing
spondylitis should not exceed 90mg daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for acute gout
should not exceed 120mg daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for acute pain
and primary dysmenorrhea should not exceed 120mg daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for
post-operative acute dental surgery pain should not exceed 90mg
daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
The dose for
post-operative acute gynecological surgery pain should not exceed
120mg daily.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
As the cardiovascular
risks of selective COX-2 inhibitors may increase with dose and
duration of exposure, the shortest duration possible and the lowest
effective daily dose should be used. The patient's need for
symptomatic relief and response to therapy should be re-evaluated
periodically. (See Warnings and Precautions)</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Elderly, Gender, Race</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
No dosage adjustment in
etoricoxib is necessary for the elderly or based on gender or race.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Hepatic Insufficiency</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
In patients with mild
hepatic insufficiency (Child-Pugh score 5-6), a dose of 60mg once
daily should not be exceeded. In patients with moderate hepatic
insufficiency (Child-Pugh score 7-9), the dose should be reduced; a
dose of 60mg <b>every other day </b><span style="font-weight: normal;">should
not be exceeded, administration of 30mg once daily can also be
considered. There are no clinical or pharmacokinetic data in patients
with severe hepatic insufficiency (Child-Pugh score >9). (See
WARNINGS AND PRECAUTIONS.)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b>Renal Insufficiency</b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-weight: normal;">In
patients with advanced renal disease (creatinine clearance <30
ml/min), treatment with etoricoxib is not recommended. No dosage
adjustment is necessary for patients with lesser degrees of renal
insufficiency (creatinine clearance </span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">≥</span></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">30ml/min).
(See WARNINGS AND PRECAUTIONS.)</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Mode
of Administrations:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Etoricoxib
is administered orally. Etoricoxib may be taken with or without food.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindications:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Hypersensitivity
to the active substance or to any of the excipients.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Active
peptic ulceration or active gastrointestinal (GI) bleeding.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Patients
who have experienced bronchospasm, acute rhinitis, nasal polyps,
angioneurotic edema, urticaria, or allergic-type reactions after
taking acetylsalicylic acid or NSAIDS including COX-2
(cyclooxygenase-2) inhibitors.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pregnancy
and lactation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">Severe
hepatic dysfunction (serum albumin <25g/l or Child-Pugh score
</span></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">≥10).</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Estimate
renal creatinine clearance <30ml/min.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Children
and adolescents under 16 years of age.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Inflammatory
bowel disease.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Congestive
heart failure (NYHA II-IV)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Patients
with hypertension whose blood pressure has not been adequately
controlled.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Established
ischemic heart disease, peripheral arterial disease and/or
cerebrovascular disease.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Warnings
and Precautions:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Clinical
trials suggest that the selective COX-2 inhibitors class of drugs may
be associated with an increased risk of thrombotic events (especially
MI and stroke), relative to placebo and some NSAIDs (naproxen). As
the cardiovascular risks of selective COX-2 inhibitors may increase
with dose and duration of exposure, the shortest duration possible
and the lowest effective daily dose should be used. The patient's
need for symptomatic relief and response to therapy should be
re-evaluated periodically.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Patients
with significant risk factors for cardiovascular events (e.g.
hypertension, hyperlipidemia, diabetes mellitus, smoking) should only
be treated with etoricoxib after careful consideration.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Selective
COX-2 inhibitors are not a substitute for aspirin for cardiovascular
prophylaxis because of their lack of effect on platelets. Because
etoricoxib, a member of this class, does not inhibit platelet
aggregation, antiplatelet therapies should not be discontinued.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
is a further increase in the risk of gastrointestinal adverse effects
(gastrointestinal ulceration or other gastrointestinal complications)
for etoricoxib, other selective COX-2 inhibitors and NSAIDs, when
taken concomitantly with acetylsalicylic acid (even at low doses).
The relative difference in gastrointestinal safety between selective
COX-2 inhibitors + acetylsalicylic acid vs. NSAIDs + acetylsalicylic
acid has not been adequately evaluated in long-term clinical trials.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Long-term
administration of NSAIDs has resulted in renal papillary necrosis and
other renal injury. Renal prostaglandins may play a compensatory role
in the maintenance of renal perfusion. Therefore, under conditions of
compromised renal perfusion, administration of Etoricoxib may cause a
reduction in prostaglandin formation and, secondarily, in renal blood
flow, and thereby impair renal function. Patients at greatest risk of
this response are those with preexisting significantly impaired renal
function, uncompensated heart failure, or cirrhosis. Monitoring of
renal function in such patients should be considered.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Caution
should be used when initiating treatment with etoricoxib in patients
with considerable dehydration. It is advisable to rehydrate patients
prior to starting therapy with etoricoxib.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
with other drugs known to inhibit prostaglandin synthesis, fluid
retention, edema and hypertension have been observed in some patients
taking etoricoxib. The possibility of fluid retention, edema or
hypertension should be taken into consideration when etoricoxib is
used in patients with preexisting edema, hypertension or heart
failure. All Nonsteroidal Antiinflammatory Drugs (NSAIDs), including
etoricoxib, can be associated with the new onset or recurrent
congestive heart failure. (see Undesirable effects). Etoricoxib may
be associated with more frequent and severe hypertension than some
other NSAIDs and selective COX-2 inhibitors, particularly at high
doses. Therefore, special attention should be paid to blood pressure
monitoring during treatment with etoricoxib. If blood pressure rises
significantly, alternative treatment should be considered.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">Physicians
should be aware that individual patients may develop upper
gastrointestinal (GI) ulcers/ulcer complications irrespective of
treatment. Although the risk of GI toxicity is not eliminated with
etoricoxib, the results of the MEDAL Program demonstrate that in
patients treated with etoricoxib, the risk of GI toxicity with
etoricoxib 60mg or 90mg once daily is significantly less than with
diclofenac 150mg daily. In clinical studies with ibuprofen and
naproxen, the risk of endoscopically detected upper GI ulcers was
lower in the patients treated with etoricoxib 120mg once daily than
in patients treated with non-selective NSAIDs. While the risk of
endoscopically detected ulcers was low in patients treated with
etoricoxib. These events can occur at any time during use and without
warning symptoms. Independent of treatment, patients with a prior
history of GI perforation, ulcers and bleeding (PUB) and patients
greater than 65 years of age are known to be at a higher risk for a
PUB.</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Elevations
of alanine aminotransferase (ALT) and/or aspartate aminotransferase
(AST) (approximately three or more times the upper limit of normal)
have been reported in approximately 1% of patients in clinical trials
treated for up to one year with etoricoxib 30, 60, and 90 mg daily.
In active comparator portions of clinical trials, the incidence of
elevated AST and/or ALT in patients treated with etoricoxib 60 and 90
mg daily was similar to that of patients treated with naproxen 1000mg
daily, but notably less than the incidence in the diclofenac 150mg
daily group. These elevations resolved in patients treated with
etoricoxib, with approximately half resolving while patients remained
on therapy. In controlled clinical trials of etoricoxib 30mg daily
versus ibuprofen 2400mg daily or celecoxib 200mg daily, the incidence
of elevations of ALT or AST was similar.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">A
patient with symptoms and/or signs suggesting liver dysfunction, or
in whom an abnormal liver function test has occurred, should be
evaluated for persistently abnormal liver function tests. If
persistently abnormal liver function test (three times the upper
limit of normal) are detected, etoricoxib should be discontinued.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">When
using etoricoxib in the elderly and in patients with renal, hepatic,
or cardiac dysfunction, medically appropriate supervision should be
maintained. If these patients deteriorated during treatment
appropriate measures should be taken, including discontinuation of
therapy.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Serious
skin reactions, some of them fatal, including exfoliative
dermintitis, Stevens-Johnson syndrome, and toxic epidermal
necrolysis, have been reported very rarely in association with the
use of NSAIDs and some selective COX-2 inhibitors during
post-marketing surveillance (see Undesirable effects). These serious
events may occur without warning. Patients appear to be at highest
risk for these reactions early in the course of therapy: the onset of
the reaction occurring in the majority of cases within the first
month of treatment. Serious hypersensitivity reactions (such as
anaphylaxis and angioedema) have been reported in patients receiving
etoricoxib (see Undesirable effects). Some selective COX-2 inhibitors
have been associated with an increased risk of skin reactions in
patients with a history of any drug allergy. Etoricoxib should be
discontinued at the first appearance of skin rash, mucosal lesions,
or any other sign of hypersensitivity.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Etoricoxib
may mask fever, which is a sign of infection. The physician should be
aware of this when using etoricoxib in patients being treated for
infection.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Interactions
with other medicaments:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Warfarin:</b></i>
In subjects stabilized on chronic warfarin therapy, the
administration of etoricoxib 120mg daily was associated with an
approximate 13% increase in prothrombin time International Normalized
Ration (INR). Standard monitoring of INR values should be conducted
when therapy with etoricoxib is initiated or changed, particularly in
the first few days, in patients receiving warfarin or similar agents.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="text-decoration: none;"><b>Rifampin:</b></span></i>
Co-administration of etoricoxib with rifampin, a potent inducer of
hepatic metabolism, produced a 65% decrease in etoricoxib plasma area
under the curve (AUC). This interaction should be considered when
etoricoxib is co-administered with rifampin.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Methotrexate:</b></i>
Two studies investigated the effects of etoricoxib 60, 90, or 120mg
administered once daily for seven days in patients receiving
once-weekly methotrexate doses of 7.5 to 20mg for rheumatoid
arthritis. Etoricoxib at 60 and 90 mg had no effect on methotrexate
plasma concentrations (as measured by AUC) or renal clearance. In one
study, etoricoxib 120mg had no effect on methotrexate plasma
concentrations (as measured by AUC) or renal clearance. In the other
study, etoricoxib 120mg increased methotrexate plasma concentrations
by 28% (as measured by AUC) and reduced renal clearance of
methotrexate by 13%. Monitoring for methotrexate-related toxicity
should be considered when etoricoxib at doses greater than 90 mg
daily and methotrexate are administered concomitantly.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Diuretics,
Angiotensin Converting Enzyme (ACE) Inhibitors and Angiotensin II
Antagonists (AIIAs): Reports suggest that NSAIDs including selective
COX-2 inhibitors may diminish the anti-hypertensive effect of
diuretics, ACE inhibitors and AIIAs. This interaction should be given
consideration in patients taking etoricoxib concomitantly with these
products.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
some patients with compromised renal function (e.g. elderly patients
or patients who are volume-depleted, including those on diuretic
therapy) who are being treated with non-steroidal anti-inflammatory
drugs, including selective COX-2 inhibitors, the co-administration of
ACE inhibitors or AIIAs may result in a further deterioration of
renal function, including possible acute renal failure. These effects
are usually reversible. Therefore, the combination should be
administered with caution especially in the elderly.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Lithium:
</b></i>Reports suggest that non-selective NSAIDs and selective COX-2
inhibitors may increase plasma lithium levels. This interaction
should be given consideration in patients taking etoricoxib
concomitantly with lithium.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Aspirin:</b></i>
Etoricoxib can be used concomitantly with low-dose aspirin at doses
for cardiovascular prophylaxis. At steady state, etoricoxib 120 mg
once daily had no effect on the anti-platelet activity of low-dose
aspiring with etoricoxib increased rate of GI ulceration or other
complications compared to use of etoricoxib alone. (See Warnings and
Precautions.)</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Oral
Contraceptives:</b></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
Etoricoxib 60mg given concomitantly with an oral contraceptive
containing 35mcg ethinyl estradiol (EE) and 0.5 to 1mg norethindrone
for 21 days increased the steady sate AUC</span></span><sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">0-24hr</span></span></sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
of EE by 37%. Etoricoxib 120mg given with the same oral contraceptive
concomitantly or separated by 12 hours, increased the steady state
AUC</span></span><sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">0-24hr
</span></span></sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">of
EE by 50% to 60%. This increase in EE concentration should be
considered when selecting an oral contraceptive for use with
etoricoxib. An increase in EE exposure can increase the incidence of
adverse events associated with oral contraceptives (e.g. venous
thromboembolic events in women at risk).</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">Hormone
Replacement Therapy: Administration of Etoricoxib 120mg with hormone
replacement therapy consisting of conjugated estrogens (0.625mg
Premarin) for 28 days, increased the mean steady state AUC</span></span><sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">0-24hr</span></span></sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
of unconjugated estrone (41%), equilin (76%), and 17-β-estradiol
(22%).</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">The
effects o the recommended chronic doses of etoricoxib (30, 60, and
90mg) has not been studied. The effects of etoricoxib 120mg on the
exposure ( AUC</span></span><sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">0-24hr</span></span></sub><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">)
to these estrogenic components of Premarin were less than half of
those observed when Premarin was administered alone and the dose was
increased from 0.625 to 1.25mg. The clinical significance of these
increases is unknown, and higher doses of Premarin were not studied
in combination with etoricoxib. These increases in estrogenic
concentration should be taken into consideration when selecting
prost-menopausal hormone therapy for use with etoricoxib.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Other:</b></i>In
drug-interaction studies etoricoxib did not have clinical important
effects on the pharmacokinetics of prednisone/prednisolone or
digoxin.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Antacids
and ketoconazole (a potent inhibitor of CYP3A4) did not have
clinically important effects on the pharmacokinetics of etoricoxib.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pregnancy
and Lactation:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
use of etoricoxib, as with any drug substances known to inhibit
COX-2, is not recommended in women attempting to conceive.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">No
clinical data on exposed pregnancies are available for etoricoxib.
Studies in animals have shown reproductive toxicity. The potential
for human risk in pregnancy in unknown. Etoricoxib, as with other
medicinal products inhibiting prostaglandin synthesis, may cause
uterine inertia and premature closure o the ductus arteriosus during
the last trimester. Etoricoxib is contraindicated in pregnancy. If a
woman becomes pregnant during treatment, etoricoxib must be
discontinued.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Reproductive
studies conducted in rats have demonstrated no evidence of
developmental abnormalities at doses up to 15mg/kg/day (approximately
1.5 times the human dose [90mg] based on systemic exposure). At doses
approximately 2 times the adult human exposure (90mg) based on
systemic exposure, a low incidence of cardiovascular malformations
and increases in post implantation loss were observed in
etoricoxib-treated rabbits. No developmental effects were seen at
systemic exposure of approximately equal to or less than the daily
human dosage (90mg). However, animal reproduction studies are not
always predictive of human response. There are no adequate and
well-controlled studies in pregnant women.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">It
is not known whether etoricoxib is excreted in human milk. Etoricoxib
is excreted in the milk of lactating rats. Women who use etoricoxib
should not breast feed.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pediatric
Use:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Safety
and effectiveness of etoricoxib in pediatric patients have not been
established.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in the Elderly:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pharmacokinetics
in the elderly (65 years of age and older) are similar to those in
the young. In clinical studies, a higher incidence of adverse
experiences was seen in older patients, compared to younger patients:
the relative differences between etoricoxib and control groups were
similar in the elderly and the young. Greater sensitivity of some
older individuals cannot be ruled out.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Undesirable
Effects:</b></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
clinical trials, etoricoxib was evaluated for safety in 7152
individuals, including 4488 patients with OA, RA or chronic low back
pain (approximately 600 patients with OA or RA were treated for one
year or longer).</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">The
following drug-related adverse experiences were reported in clinical
studies in patients with OA, RA or chronic low back pain treated for
up to 12 weeks. These occurred in ≥1% of patients treated with
etoricoxib and at an incidence greater than placebo:
asthenia/fatigue, dizziness, lower extremity edema, hypertension,
dyspepsia, heartburn, nausea headache, ALT increased, AST increased.</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
adverse experience profile was similar in patients with OA or RA
treated with etoricoxib for one year or longer.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
the MEDAL Study, an endpoint driven CV outcomes trial involving
23,504 patients, the safety of etoricoxib 60 or 90 mg daily was
compared to diclofenac 150mg daily in patients with OA or RA (mean
duration of treatment was 20 months). In this large trial, only
serious adverse events and discontinuations due to any adverse events
were recorded. The rates of confirmed thrombotic cardiovascular
serious adverse events were similar between etoricoxib and
diclofenac. The incidence of discontinuations for
hypertension-related adverse events was less than 3% in each
treatment group; however, etoricoxib 60 and 90mg demonstrated
significantly higher rates of discontinuations for these events than
diclofenac. The incidence of congestive heart failure adverse event
(discontinuations and serious events) and the incidence of
discontinuations due to edema occurred at similar rate on etoricoxib
60mg compared to diclofenac; however, the incidences for these events
were higher for etoricoxib 90mg compared to diclofenac. The incidence
of discontinuations due to atrial fibrillation was higher for
etoricoxib compared to diclofenac.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
EDGE and EDGE II studies compared the GI tolerability of etoricoxib
90mg daily (1.g to 3 times the doses recommended for OA) and
diclofenac 150mg daily in 7111 patients with OA (EDGE Study; mean
duration of treatment 9 months) and 4086 patients with RA (EDGE II;
mean duration of treatment 19 months). In each of these studies, the
adverse experience profile of etoricoxib was generally similar to
that reported in the phase IIb/III placebo-controlled clinical
studies; however, hypertension and edema-related adverse experiences
occurred at a higher rate on etoricoxib 90 mg than on diclofenac 150
mg daily. The rate of confirmed thrombotic cardiovascular serious
adverse events occurring in the two treatment groups was similar.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">In
combined analysis of phase IIb to V clinical studies 4 weeks duration
or longer (excluding the MEDAL Program Studies), there was no
discernible difference in the rate of confirmed thrombotic
cardiovascular serious adverse events between patients receiving
etoricoxib ≥30mg or non-naproxen NSAIDs. The rate of these events
was higher in patients receiving etoricoxib compared with those
receiving with those of naproxen 500mg twice daily.</span></span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
a clinical study for ankylosing spondilitis, patients were treated
with etoricoxib 90mg once daily for up to 1 year (N=126). The adverse
experience profile in this study was generally similar to that
reported in chronic studies in OA, RA and chronic low back pain.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
a clinical study for acute gouty arthritis, patients were treated
with etoricoxib 120mg once daily for eight days. The adverse
experience profile in these studies was generally similar to that
reported in chronic studies in OA, RA and chronic low back pain.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
initial clinical studies for acute analgesia, patients were treated
with etoricoxib 120mg once daily for one to sever days. The adverse
experience profile in these studies was generally similar to that
reported in chronic studies in OA, RA and chronic low back pain.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
the additional clinical studies for acute post-operative pain
associated with dental and abdominal gynecological surgeries
including 1222 patients treated with etoricoxib (90 or 120mg), the
adverse experience profile was generally similar to that reported in
the combined OA, RA, and chronic low back pain studies.</span></div>
<div align="JUSTIFY" style="font-weight: normal; margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">In
the combined studies for acute post-operative dental pain, the
incidence of post-dental extraction alveolitis (dry socket) reported
in patients treated with etoricoxib was similar to that of patients
treated with active comparators.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<i><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">Post-marketing
experiences</span></span></i></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">The
following adverse reactions have been reported in post-marketing
experience.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Blood
and lymphatic systems disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
thrombocytopenia.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Immune
system disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
hypersensitivity reactions, including anaphylactic/anaphylactoid
reactions including shock.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Metabolism
and nutrition disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
hyperkalemia.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Psychiatric
disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
anxiety insomnia, confusion, hallucinations, depression,
restlessness.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Nervousness
system disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
dysgeusia, somnolence.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Eye
disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
blurred vision.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Cardiac
disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
congestive heart failure, palpitation, angina, arrhythmia.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Vascular
disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
hypersensitive crisis.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Respiratory,
thoracic and mediastinal disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
bronchospasm.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Gastrointestinal
disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
abdominal pain, oral ulcers, peptic ulcers including perforation and
bleeding (mainly in elderly patients) vomiting, diarrhea.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Hepatobiliary
disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
hepatitis, jaundice, hepatic failure.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Skin
and subcutaneous tissue disorders:</span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">
angioedema, pruritus, erythema, rash, Stevens-Johnson syndrome, toxic
epidermal necrolysis, urticaria, fixed drug eruption.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><span style="font-weight: normal;">Renal
and urinary disorders: </span></i></span><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">renal
insufficiency, including renal failure (see Warnings and
precautions).</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Overdosage
and Treatment:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">In
clinical studies, administration of etoricoxib at single doses up to
500mg and multiple doses up to 150mg/day for 21 days did not result
in significant toxicity. There have been reports of acute overdosage
with etoricoxib, although adverse experiences were not reported in
the majority of cases. The most frequently observed adverse
experiences were consistent with the safety profile for etoricoxib
(e.g. gastrointestinal events, renovascular events).</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">In
the event of overdosage, it is reasonable to employ the usual
supportive measures, e.g. remove unabsorbed material from the
gastrointestinal tract, employ clinical monitoring and institute
supportive therapy, if required.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">Etoricoxib
is not dialyzable by hemodialysis; it is not known whether etoricoxib
is dialyzable by peritoneal dialysis.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Storage
Condition:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">Store
ate temperatures not exceeding 30</span></span><sup><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">o</span></span></sup><span style="font-family: Times New Roman, serif;"><span style="font-weight: normal;">C.
Protect from light. Store in the original package.</span></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-42522380970694360862013-07-04T07:08:00.001-07:002013-07-04T07:08:26.459-07:00Ketorolac Trometamol
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Ketorolac
Trometamol</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>30mg/ml
Solution for Injection (IM/IV)</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category: </b>Non-Opioid Analgesic</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Mode
of Actions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ketorolac
Trometamol is a non-narcotic analgesic. It inhibits synthesis of
prostaglandins and is considered a peripherally acting analgesic
since it does not have any known effects on opiate receptors. No
evidence of respiratory depression has been observed after
administration of Ketorolac Trometamol. It did not cause pupil
constriction. It caused no more drowsiness than placebo and less
drowsiness than morphine in postoperative patients. It is a
non-steroidal anti-inflammatory agent that exhibits anti-inflammatory
and antipyretic activity.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetics:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ketorolac
Trometamol is rapidly and completely absorbed following intramuscular
administration with a mean peak plasma concentration of 2.2mcg/ml
occurring an average 50minute after a single 30 mg dose. The terminal
plasma half-life is 5.3 hours in young adults and 7 hours in elderly
subjects (mean age 72). Intravenous administration of a single 10 mg
dose of ketorolac trometamol results in a terminal plasma elimination
intravenous administration of a single 10 mg dose of ketorolac
trometamol results in a terminal plasma elimination half-life of 5.1
hours, an average volume of distribution of 0.15L/kg and a total
plasma clearance of 0.35 ml/min/kg. More than 99% of the ketorolac in
plasma is protein-bound over a wide concentration range. The
pharmacokinetics of ketorolac in a man following single or multiple
intramuscular (IM) doses are linear. Steady-state plasma levels are
achieved after dosing every 6 hours of 1 day. No changes in
clearances occur with chronic dosing. The primary route of excretion
of ketorolac and its metabolites (conjugates and a para-hydroxyl
metabolites) is in the urine (mean 91.4%) and the remainder (mean
6.1%) is excreted in the feces (see table).</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<table border="1" cellpadding="4" cellspacing="0" style="width: 100%px;">
<colgroup><col width="104*"></col>
<col width="78*"></col>
<col width="74*"></col>
</colgroup><tbody>
<tr>
<td colspan="3" valign="TOP" width="100%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Influence
of Age Liver and Kidney Function on the Clearance </b></span>
</div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>and
Terminal Half-life of Ketorolac Trometamol</b></span></div>
</td>
</tr>
<tr valign="TOP">
<td width="41%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Type Of
Subjects</b></span></div>
</td>
<td width="30%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Total
clearance (L/Hr/Kg)</b></span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Mean
(range)</b></span></div>
</td>
<td width="29%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Terminal
Half-life (hrs)</b></span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Mean
(range)</b></span></div>
</td>
</tr>
<tr valign="TOP">
<td width="41%">
<div align="JUSTIFY">
<span style="font-family: Times New Roman, serif;">Normal
subjects (n=54)</span></div>
</td>
<td width="30%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">0.023</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(0.010-0.045)</span></div>
</td>
<td width="29%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">5.3</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(3.5-9.2)</span></div>
</td>
</tr>
<tr valign="TOP">
<td width="41%">
<div align="JUSTIFY">
<span style="font-family: Times New Roman, serif;">Patients with
hepatic dysfunction (n=7)</span></div>
</td>
<td width="30%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">0.029</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(0.013-0.066)</span></div>
</td>
<td width="29%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">5.4</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(2.2-6.9)</span></div>
</td>
</tr>
<tr valign="TOP">
<td width="41%">
<div align="JUSTIFY">
<span style="font-family: Times New Roman, serif;">Patients with
renal impairment (n=10) (serum creatinine) (1.9-5mg/dl)</span></div>
</td>
<td width="30%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">0.016</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(0.007-0.043)</span></div>
</td>
<td width="29%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">9.6</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(3.2-15.7)</span></div>
</td>
</tr>
<tr valign="TOP">
<td width="41%">
<div align="JUSTIFY">
<span style="font-family: Times New Roman, serif;">Renal
dialysis (n=9)</span></div>
</td>
<td width="30%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">0.016</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(0.003-0.036)</span></div>
</td>
<td width="29%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">13.6</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(8-39.1)</span></div>
</td>
</tr>
<tr valign="TOP">
<td width="41%">
<div align="JUSTIFY">
<span style="font-family: Times New Roman, serif;">Healthy
elderly subjects (n=13) </span>
</div>
<div align="JUSTIFY">
<span style="font-family: Times New Roman, serif;">(mean age 72)</span></div>
</td>
<td width="30%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">0.019</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(0.013-0.034)</span></div>
</td>
<td width="29%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">7</span></div>
<div align="CENTER">
<span style="font-family: Times New Roman, serif;">(4.7-8.67)</span></div>
</td>
</tr>
<tr>
<td colspan="3" valign="TOP" width="100%">
<div align="CENTER">
<span style="font-family: Times New Roman, serif;"><b>Estimated
from 30mg single doses of Ketorolac Trometamol IM/IV</b></span></div>
</td>
</tr>
</tbody></table>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Hemodynamics
of patients are not altered by parenteral administration of Ketorolac
Trometamol.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Indications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">For
short term management of moderate to severe acute post-operative pain
following surgical procedures associated with low risk of hemorrhage.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindications:
</b></span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ketorolac
Trometamol should not be used:</span></div>
<ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
patients who have previously exhibited allergy to it.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
suspected or confirmed cerebrovascular bleeding or hemophilia in
other bleeding problems including coagulation or platelet function
disorders due to increased risk of bleeding because ketorolac
inhibits platelet aggregation and may also cause gastrointestinal
ulceration or hemorrhage.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
active, recent or history of gastrointestinal bleeding or recent
gastrointestinal perforation or active or history of peptic
ulceration, ulceration colitis or other ulcerative gastrointestinal
disease due to increased risk of gastrointestinal ulceration,
perforation and/or hemorrhage.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
aspirin induced nasal polyps associated with bronchospasm, or
angioedema, anaphylaxis or history of other severe allergic
reactions of cross-sensitivity.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
severe renal function impairment, due to increased risk of renal
failure.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">During
pregnancy labor, delivery or lactation.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">A
history of asthma.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Hypovolemia
or dehydration from any cause.</span></div>
</li>
</ol>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Adverse
Effects:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
following adverse reactions were reported to be probably related to
patients who receive up to 20 doses for 5 days of intramuscular
administered Ketorolac Trometamol and in patients who receive up to 8
doses for 2 days, of intravenously administered ketorolac trometamol.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Incidence
between 3 and 9%:</b></i></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Gastrointestinal:
</b></u>Nausea, dyspepsia, gastrointestinal pain.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Central
nervous system:</b></u> Drowsiness</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Incidence
between 1 and 3%:</b></i> </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Gastrointestinal:
</b></u>Diarrhea</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Central
Nervous system: </b></u></span>Dizziness, headache, sweating</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Body
as a whole: </b></u></span>Edema</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Injection
site pain was reported by 2% of patient</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i><b>Incidence
1% or less:</b></i></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Gastrointestinal:</b></u></span>
Constipation, flatulence, gastrointestinal fullness, liver function
abnormalities, melena, peptic ulcer, rectal bleeding, stomatitis,
vomiting.</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Body
as a whole: </b></u></span>Asthenia, myalgia</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Cardiovascular:
</b></u></span>flushing, pallor</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Hemic
and lymphatic: </b></u></span>purpura</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Nervous
system: </b></u></span>Dry mouth, nervousness, paresthesia, abnormal
thinking, depression, euphoria, excessive thirst, inability to
concentrate, insonmia, stimulation, vertigo</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Respiratory:</b></u></span>
Dyspnea, asthma</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Urogenital:
</b></u></span>Increased urinary frequency, oliguria</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><b>Dermatologic:
</b></u></span>Pruritus, urticaria</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Special
senses: Abnormal taste, abnormal vision</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Precautions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
with other non-steroidal anti-inflammatory analgesic agents,
ketorolac trometamol can cause gastrointestinal irritation, ulcers or
bleeding with or without previous symptoms and should be given under
close supervision to patients with history of gastrointestinal tract
disease. Elderly and debilitated individuals are most susceptible to
these complications, the incidence of which increased with dose and
duration of treatment.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Renal
Effects:</b> As with other non-steroidal anti-inflammatory drugs that
inhibits prostaglandin biosynthesis, elevations of serum urea
nitrogen and creatinine have been reported with ketorolac trometamol.
Since ketorolac trometamol and its metabolites are excreted primarily
by the kidney, patients with significance impairment or renal
functions should not receive ketorolac trometamol unless the expected
benefits out weight the risks. If used in patients with impaired
renal function, ketorolac trometamol dosage should be reduced and
renal status should be closely monitored. In patients with serum
creatinine values ranging from 1.9-5mg/dl, the rate of ketorolac
clearance was reduced to approximately half of normal. The total
daily dose of ketorolac should be reduced by half in such patients.
With more severe degrees of renal impairment, ketorolac is not
recommended for patients with serum creatinine serum levels above 5
mg/dl. Patients who are volume-depleted because of blood loss or
severe dehydration may be dependent on renal prostaglandin production
to maintain renal perfusion and therefore, glomerular filtration
rate. In such situation, the use of drugs which inhibit prostaglandin
synthesis might be expected to further decrease renal blood flow.
Caution is advised if ketorolac trometamol is used in such
circumstances. Close monitoring of urine output, serum urea and serum
creatinine is recommended until the patient is normo-volemic. As with
other drugs that inhibit prostaglandin biosynthesis, the following
renal abnormalities may be associated with the use of ketorolac
trometamol: Glomerular nephritis, interstitial nephritis, renal
papillary necrosis, nephrotic syndrome and acute renal failure. Other
renal disease is possible.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Fluid
retention and edema:</b> Fluid retention and edema have been reported
with use of ketorolac trometamol; therefore ketorolac trometamol
should be used with caution in patients with cardiac decompensation,
hypertension or similar conditions.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Hematological
Effects: </b>Ketorolac trometamol inhibits platelet aggregation and
may prolong bleeding time. Patients on full anticoagulation therapy
(e.g. Heparin or dicumarol derivatives) may be at increased risk of
bleeding, if given ketorolac trometamol concurrently. Thus, the
benefits should be weighed against the risk. Low-dose heparin (5000
units SC 2 times a day) appears to be associated with less risk.
Patients who have coagulation disorders or are receiving drug therapy
that interferes with homeostasis should be carefully observed if
ketorolac trometamol is administered. Unlike the prolonged effects
from aspirin, the inhibition of platelet function by ketorolac
disappears within 24-48 hours after the drug is discontinued.
Ketorolac does not affect platelet count, prothrombin time (PT) or
partial thromboplastin similar to control groups i.e. 5/11750 (0.4%)
with ketorolac trometamol compared to 1/570 (0.2%) with opiates.
Postoperative wound hemorrhage has been reported rarely in
association with the immediate perioperative use of ketorolac
trometamol. Therefore caution should be used where strict homeostasis
is critical. Specifically in cosmetic plastic surgery, hematomas and
other other signs of wound hemorrhage have been reported with the use
of ketorolac trometamol. Physicians should be alert to the
pharmacologic similarity of ketorolac to other non-steroidal
anti-inflammatory drugs that inhibits cyclooxygenase.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Hepatic
effects: </b>Borderline elevation of one or more liver tests may
occur. These abnormalities may progress, may remain unchanged or may
be transient with continued therapy. Meaningful elevations (>3
times normal) of serum glutamic oxaloacetic transaminase (SGOT or
AST) occurred in <1% of patients. If clinical signs and symptoms
consistent with liver disease develop or if systemic manifestation
occur (e.g. eosinophilia, rash, etc.) ketorolac trometamol should be
discontinued. Patients with impaired hepatic functions from cirrhosis
do not have any clinical important changes in ketorolac clearance.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ketorolac
trometamol is not an anesthetic agent and possesses no sedative or
anxiolytic properties: therefore it is not recommended as an
preoperative medication when these effects are required. Ketorolac is
not recommended in obstetric analgesia.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Carcinogenicity,
mutagenicity, and impairment of fertility: </b>In animal ketorolac
was not associated with tumourigenicity or mutagenicity and did not
demonstrate teratogenic potential.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in pregnancy and lactation: </b>Ketorolac trometamol is not
recommended during pregnancy, labor or delivery. Ketorolac trometamol
is not recommended for treatment of nursing mothers. Secretion of
ketorolac in human milk after ingestion of ketorolac trometamol is
limited. The milk to plasma ration of ketorolac concentrations ranged
between 0.015 and 0.037. </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in children: </b>Safety and efficacy in children have not been
established. Therefore, it is not recommended for use in children
under 16 years.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in the Elderly: </b>Because ketorolac is cleared somewhat more slowly
by the elderly who are also more sensitive to the renal effects of
NSAIDs (see Renal effects), extra caution and the lowest effective
dose should be given when treating the elderly with ketorolac
trometamol.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
abuse and Physical dependence: </b>Ketorolac is not a narcotic
agonist or antagonist. No subjective symptoms or objective signs of
drug withdrawal upon abrupt discontinuation of IV or IM dosing.
Patients receiving Ketorolac Trometamol for 6 months or longer have
not developed tolerance to the drug and there is no pharmacological
basis to expect addition. Ketorolac Trometamol did not exhibit
activity in classical animal which are reasonable predictors of
opiate analgesic action (hot plate and tail withdrawal test). In
vitro, ketorolac does not bind to opiate receptors. These demonstrate
that ketorolac trometamol does not have opiate-like activity.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Warnings:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Risk
of GI ulceration, bleeding and perforation with NSAID</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Serious
GI toxicity such bleeding, ulceration and perforation can occur at
any time, with or without symptoms, in patients treated with NSAID
therapy. Although minor upper GI problems (e.g. dyspepsia) are
common, usually developing early in therapy, prescribers should
remain alert for ulceration and bleeding in patients treated with
NSAID even in the absence of previous GI tract symptoms.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Studies
to date have not identified any subset of patients not at risk of
developing peptic ulceration and bleeding. Patients with prior
history of serious adverse events and other risk factors associated
with peptic ulcer disease (e.g. alcoholism, smoking, and
corticosteroid therapy) are at increased risk. Elderly or
debilitated patients seem to tolerate ulceration or bleeding less
then other individuals and account for most spontaneous for fatal GI
events.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Interactions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Given
10 mg orally for 6 days prior to coadministration of single dose of
warfarin 25mg, no significant changes in pharmacokinetics of the
warfarin enantiomers were detected. Ketorolac is highly bound to
plasma proteins (mean 99.2%) and binding is independent of
concentration. The in-vitro binding of warfarin to plasma proteins is
only slightly reduced by ketorolac. Ketorolac does not alter digoxin,
protein binding. In vitro at therapeutic concentration of salicylate
(300mcg/ml). The binding of ketorolac was reduced from approximately
99.2%-97.5%. Therapeutic concentrations of digoxin, warfarin,
acetaminophen, phenytoin and tolbutamine did not alter ketorolac
protein-binding. Because ketorolac is highly potent drug and present
in low concentrations in plasma, it would be expected to displace
other protein bound drugs significantly. There is no evidence that
ketorolac induces or inhibits the hepatic enzymes capable of
metabolizing itself or other drugs. Hence ketorolac would not be
expected to alter the pharmacokinetics of other drugs due to enzyme
induction of inhibition mechanisms. Concomitant administration of
ketorolac trometamol and probenecid results in the decreased
clearance of ketorolac and a significant increase in ketorolac plasma
levels and terminal half-life of ketorolac. Ketorolac trometamol
reduces the diuretic response to furosemide in normo-volemic healthy
subjects by approximately 20%. Inhibition of renal lithium clearance
leading to an increase in plasma lithium concentrations and potential
lithium toxicity has been reported with some prostaglandin synthesis
inhibiting drugs. Concomitant administration of ketorolac trometamol
and methotrexate should be done with caution, since some
prostaglandin synthesis inhibiting drugs have been reported to reduce
the clearance of methotrexate, and thus possibly enhance the toxicity
of methotrexate. Ketorolac trometamol has been administered
concurrently with morphine in postoperative pain without evidence of
adverse interactions. There are no clinical data available dealing
with the safety or efficacy of concomitant use with other
non-steroidal anti-inflammatory drugs. It is not recommended that
ketorolac trometamol be routinely used with other non-steroidal
anti-inflammatory drugs because of potential for additive side
effects.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Cautions
for Usage:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Incompatibilities:
This product should not be mixed in a small volume (e.g. in a
syringe) with Morphine Sulfate, Pethidine hydrochloride, Promethazine
hydrochloride or Hydroxyzine hydrochloride as precipitation of
ketorolac trometamol will occur. It is compatible with normal saline,
5% dextrose, Ringer's solution, Ringer's Lactate Solution or
Plasmalyte solution.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Recommended
Dosage, Dosage Schedule and Route of Administration:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administration: </b>Dosage should be adjusted according to the
severity of the pain and the patient response. The recommended usual
initial dose of ketorolac trometamol is 30mg followed by 10-30 mg
every 4-6 hours as needed to control pain. A lower initial dose is
recommended for patients under 50kg for patients over 65 years and
for patients with reduced renal function. In the initial
postoperative period, ketorolac trometamol may be given as often as
every 2 hours if needed. A total daily dose >120mg/day is not
recommended. Intravenous injections should be administered over at
least 15 seconds.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Opiates
analgesic (e.g. Morphine, Pethidine) may be concomitantly used if
further pain relief, anxiolytic effects and/or sedative effects of
opiates are desired. Supplemental opiates may be most appropriate in
the early postoperative period when pain is most severe. The
administration of continuous multiple daily intramuscular doses of
ketorolac trometamol should not exceed 2 days because adverse events
may increase with prolonged usage.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Symptoms
and treatment for overdosage and antidotes:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Overdosage:
</b>The absence of experience with acute overdosage precludes
characterization of sequalae and assessment of antidotal efficacy at
this time. In gastroscopic uses, daily doses of 360mg given over an 8
hour interval for each of 5 consecutive days (3 times the highest
recommended dose) caused abdominal pain and peptic ulcers which
healed after discontinuation of dosing.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Storage
Conditions: </b></span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 30<sup>o</sup>C. Protect from light.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-63067088586231583462013-06-28T23:17:00.001-07:002013-06-28T23:17:14.380-07:00Hydralazine <div style="text-align: justify;">
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Hydralazine
</b></span>
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>20mg/ml</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Solution
for Injection (IM/IV)</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category:</b> Direct Vasodilator</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Description:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">A
clear colorless solution to pale yellow solution in USP.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetics:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Hydralazine
given orally is rapidly absorbed from the gastrointestinal tract but
undergoes considerable first pass metabolism by acetylation in the
gastrointestinal mucosa and liver. The rate of metabolism is
genetically determined and depends upon the acetylator status of the
individual. The bioavailability of hydralazine has been reported to
be about 35% in slow acetylators and less in fast acetylators; thus
plasma concentrations after a given dose are higher in slow
acetylators. Peak plasma concentrations have been reported to occur
after about one hour. Hydralazine is chiefly present in plasma as
hydrazone conjugate with pyruvic acid. Plasma protein binding is
about 90%. The drug is widely distributed, notably into arterial
walls. Systemic metabolism in the liver is by hydroxylation of the
ring system and conjugation with glucuronic acid; most sources
suggest that N-acetylation is not of major importance in systemic
clearance and that therefore acetylator status does not affect
elimination. Hydralazine is excreted mainly in urine as metabolites.
The apparent average half-life for hydralazine has been reported to
vary from about 45 minutes to about 8 hours, with a number of sources
giving the average as about 2 to 4 hours. Some of the variation may
be due to problems with analytical procedures. The half-life is
prolonged in renal impairment and may be up to 16 hours in patients
with a creatinine clearance of less than 20 ml/minute. Hydralazine
crosses the placenta and is distributed into breast milk.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Indications:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Hydralazine
is used for the treatment of hypertension usually with a beta blocker
and a thiazide diuretic. It is also used with isosorbide dinitrate in
the management of heart failure.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administration</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">In
hypertensive crises, hydralazine hydrochloride is given in doses of 5
to 10 mg by slow intravenous injection, repeated if necessary after
20 to 30 minutes. Alternatively, it may be given by continuous
intravenous infusion in an initial dose of 200 to 300 micrograms per
minute. The usual maintenance dose range is 50 to 150 micrograms per
minute. Hydralazine hydrochloride can be also given by intramuscular
injection.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Adverse
Effects:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Adverse
effects are common with hydralazine, particularly tachycardia,
palpitations, angina pectoris, sever headache, and gastrointestinal
disturbances such as anorexia, nausea, vomiting, and diarrhea. These
adverse effects, and flushing, dizziness, and nasal congestion, which
occur less often, may be seen at the start of treatment, especially
if the dose is increased quickly. They generally subside with
continued treatment. Other less common adverse effects include
orthostatic hypotension, fluid retention with edema and weight gain,
conjunctivitis, lachrymation, tremor, and muscle cramps. Hydralazine
may deplete pyridoxine in the body, and can produce peripheral
neuropathy with numbness and tingling of the extremities.
Occasionally, hepatotoxicity, blood dyscrasia, hemolytic anemia,
difficulty in urinating, glomerulonephritis, constipation, paralytic
ileus, depression, and anxiety occur. Hypersensitivity reactions
including fever, chills, pruritus, and rashes have been reported, and
eosinophilia may occur. Antinuclear antibodies may develop after
prolonged use of large doses, and a condition resembling Systemic
Lupus Erythematosus may occur. The incidence is greater in slow
acetylators, patients with renal impairment, women, and patients
taking more than 100mg of hydralazine daily. The symptoms usually
disappear when the drug is withdrawn; some patients may require
treatment with corticosteroids. Acute overdosage may produce
hypotension, tachycardia, myocardial ischemia, arrhythmias, shock and
coma.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Carcinogenicity.
</b>Although earlier reports suggested that hydralazine might be
carcinogenic, there was no evidence from a survey of 1978 patients
with lung or colorectal carcer and 6807 controls that there was an
increased risk o these neoplasms.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Effects
on the blood. </b>Three cases of thrombocytopenia were reported in
neonates whose mothers had been treated with hydralazine for some
months before deliver. The thrombocytopenia and bleeding was
transient with full recovery occurring within a few weeks. No adverse
effects were noticed in the mothers.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Effects
on the cardiovascular system.</b> Paradoxical sever hypertension
developed after oral or intramuscular hydralazine on 3 occasions in a
patient with renal artery stenosis.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Effects
on the kidney. </b>Rapidly progressive glomerulonephritis with focal
and segmental lesions, usually accompanied by necrosis and crescents
formation, has been reported in patients given hydralazine. The
condition is reported to be associated with the presence of
antinuclear antibodies and slow acetylator status, factors associated
with the development of hydralazine induced lupus erythematosus.
However, renal involvement is much less common in drug-induced lupus,
and in a report of 15 such cases men and women and fast and slow
acetylators were equally affected. In addition the criteria for
Systemic Lupus Erythematosus were not usually fulfilled in these
patients and it was suggested withdrawal of hydralazine generally
results in some improvement in renal function but complete recovery
is uncommon; sever cases may require immunosuppressive therapy.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Effects
on the skin.</b> Pruritus and skin rashes have been reported with
hydralazine use. A 59-year-old woman who had been taking hydralazine
2t5mg three times daily for 6 months developed sysmtoms of Sweet's
syndrome (erythematosus plaques and nodules and hemorrhagic
blisters). Symptoms began to subside on withdrawal of the drug but
recurred on rechallenge. The condition resolved on discontinuation of
hydralazine and treatment with prednisolone.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Lupus
erythematosus. </b>Lupus erythematosus is a well-documented adverse
effects of hydralazine. Onset is typically delayed from 1 month to 5
years from the start of treatment, and the most common symptoms are
arthralgia or arthritis, usually non-deforming, in up to 95% of
patients, fever and myalgia in about 50%, and pleuropulmonary
involvemnt, manifesting as pleurisy, pleural effusions, or pulmonary
infiltrates in up to 30%. Renal involvement is reported to be less
common than idiopathic Systemic Lupus Erythematosus and there is some
uncertainty as to whether the glomerulonephritis sometimes seen in
patients receiving hydralazine should be considered lupus nephritis
(see Effects on the Kidneys). Nonetheless, a 20% incidence of renal
involvement has been reported. Other complications and symptoms
associated with lupus erythematosus in patients taking hydralazine
include cutaneous ulceration, bilateral retinal vasculitis, reactive
hypoglycemia (although the attribution is uncertain),
life-threatening cardiac tamponade, and hoarseness and stridor
secondary to vocal cord palsy, which progressed to respiratory
arrest. Skin rashes are reported to be less prominent than with the
idiopathic from of the disease. Fatalities have occurred, but appear
to be rare. Estimates of the overall incidence of
hydralazine-associated lupus erythematosus vary from about 1.2 to 5%
or more. Th syndrome appear to occur only in patients who develop
antinuclear antibodies while receiving hydralazine, but the incidence
of positive antinuclear antibody tests is much higher than that of
lupus, at up to 60%, so the presence of antinuclear antibodies alone
is not diagnostic. There is a strong relationship with drug dose,
acetylator status, and patient gender, the syndrome being more common
in slow acetylators and women, and in patients receiving 100mg daily
or more. Although it has been reported that hydralazine-associated
lupus was more frequent in patients with HLA-DR4 antigen this was not
confirmed by others and subsequent work has suggested that the
association is rather with the non-expressing or null forms of the
adjacent complement C4 in vitro and might exacerbate complement
deficiency (which is known to be associated with idiopathic Systemic
Lupus Erythematosus) in patients with an already low lever of C4 due
to a null allele.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Overdosage
and Treatment of Adverse Effects</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Withdrawal
of hydralazine or dosage reduction reverses many of the adverse
effects. Peripheral neuropathy has been reported to be alleviated by
pyridoxine. If overdose occurs the benefit of gastric decontamination
is uncertain, but activated charcoal may be given, If the patient
presents within 1 hour of ingestion. Symptomatic and supportive
treatment, including plasma expanders for shock and a beta blocker
for tachycardia, should be given as necessary. Hypotension may
respond to placing the patient in the supine position with the feet
raised. If possible, pressor drugs should be avoided. If a pressor is
necessary, one should be chosen that will not cause tachycardia or
exacerbate arrhythmias; adrenaline should not be used.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Precaution:</b><br />Hydralazine
is contraindicated in patients with sever tachycardia, dissecting
aortic aneurysm, heart failure with high output, cor pulmonale, or
myocardial insufficiency due to mechanical obstruction, for example
aortic or mitral stenosis or constrictive pericarditis. Hydralazine
is also contraindicated in patients with idiopathic Systemic Lupus
Erythematosus and related disorders. Hydralazine-induced vasodilation
produces myocardial stimulation. It should therefore be used with
caution in patients with ischemic heart disease since it can increase
angina and it should not be given after myocardial infarction until
the patient's condition has stabilized. Patients with suspected or
confirmed ischemia heart disease should be given hydralazine under
cover of a beta blocker, which should be started a few days before
hydralazine, in order to prevent myocardial stimulation. If given to
patients with heart failure they should be monitored for orthostatic
hypotension and tachycardia during the initial stages of therapy,
preferably in hospital. If treatment with hydralazine is to be
stopped in patients with heart failure it should generally be
withdrawn gradually. Hydralazine should be used with caution in
patients with cerebrovascular disorders. The dose of hydralazine
should be reduced or the dosage interval prolonged in patients with
hepatic or renal impairment. Complete blood counts and antinuclear
antibody determinations should be carried out about every 6 months
during long term therapy. Urine analysis (for microhematuria and
proteinuria) is also recommended. Hydralazine is teratogenic in some
species of animals and should therefore be avoided during the first
tow trimesters of pregnancy. Patients may experience impaired,
especially at the start of therapy, and should not drive or operate
machinery if affected.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Breastfeeding.</b>
Hydralazine is distributed into mild in small amounts (see Pregnancy)
but no adverse effects have been seen in infants and the American
Academy of Pediatrics therefore considers hydralazine to be usually
compatible with breastfeeding.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Pregnancy.</b>
Hydralazine should be avoided during first two trimesters of
pregnancy.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Interactions:</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">The
hypotensive effect on hydralazine may be enhanced by other drugs with
hypotensive action. Severe hypotension may occur if hydralazine and
diazoxide are given together. However, some interactions with an
antihypertensive may be beneficial: thiazide diuretics also
counteract the fluid retention caused by hydralazine, and
beta-blockers diminish the cardiac accelerating effects.</span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<br />
</div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;"><b>Storage
Condition</b></span></div>
<div style="margin-bottom: 0in; text-align: justify;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 25<sup>o</sup>C. Protect from light and
moisture. The injection should be discharge if any visible article
appears.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-74494745538693172052013-06-04T05:57:00.002-07:002013-06-04T05:57:39.810-07:00Pantoprazole Sodium
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pantoprazole
Sodium</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">40mg
for Injection IV</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category:</b></span><span style="font-family: Times New Roman, serif;"> Proton Pump
Inhibitor</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pharmacological
Action:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Mechanism
of action:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pantoprazole
is a proton pump inhibitor (PPI) that suppresses the final step in
gastric acid production by covalently binding to the (H</span><sup><span style="font-family: Times New Roman, serif;">+</span></sup><span style="font-family: Times New Roman, serif;">,
K</span><sup><span style="font-family: Times New Roman, serif;">+</span></sup><span style="font-family: Times New Roman, serif;">)-ATPase
enzyme system at the secretory surface of the gastric parietal cell.
This effect leads to inhibition of both basal and stimulated gastric
acid secretion irrespective of the stimulus. The binding to the (H</span><sup><span style="font-family: Times New Roman, serif;">+</span></sup><span style="font-family: Times New Roman, serif;">,
K</span><sup><span style="font-family: Times New Roman, serif;">+</span></sup><span style="font-family: Times New Roman, serif;">)-ATPase
results in a duration of antisecretory effect that persists longer
than 24 hours for all doses tested.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pharmacokinetics:
</span></b>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pantoprazole
does not accumulate and its pharmacokinetics are unaltered with
multiple daily dosing. Following the administration of pantoprazole
for injection, the serum concentration of pantoprazole declines
biexponentially with a terminal elimination half-life of
approximately one hour. In extensive metabolizers with normal liver
function receiving a 40mg dose of pantoprazole for injection by
constant rate over 15 minutes, the peak concentration (C</span><sub><span style="font-family: Times New Roman, serif;">max</span></sub><span style="font-family: Times New Roman, serif;">)
is 5.52 mcg/ml and the total area under the plasma concentration
versus time curve (AUC) is 5.4 mcg.hr/ml. The total clearance is
7.6-14.0 L/h and the apparent volume of distribution is 11.0-23.6 L.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
serum protein binding of pantoprazole is about 98%, primarily to
albumin. Pantoprazole is extensively metabolized in the liver through
the cytochrome P450 (CYP) system.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">After
administration of a single intravenous dose of Pantoprazole to
healthy, normal metabolizer subjects, approximately 71% of the dose
was excreted in the urine with 18% excreted in the feces through
biliary excretion. There was no renal excretion of unchanged
pantoprazole.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Indications:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pantoprazole
for injection is indicated for the treatment of gastric ulcer,
duodenal ulcer, moderate and severe reflux esophagitis.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Contraindications:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pantoprazole
for injection is contraindicated in known hypersensitivity to the
formulation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Dosage
and Administration:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Dosage:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
recommended dose is intravenous administration of the content of one
vial (40mg pantoprazole) once daily for 7 days.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Duodenal
Ulcer:</i></span><span style="font-family: Times New Roman, serif;"> Duodenal ulcers
generally heal within 2 weeks. If a 2-week period of treatment is not
sufficient, healing will be achieved in almost all cases within a
further 2 weeks.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Gastric
Ulcer and Gastro-esophageal reflux:</i></span><span style="font-family: Times New Roman, serif;">
A 4 week period is usually required for the treatment of gastric
ulcers and gastro-esophageal reflux. If this is not sufficient,
healing will usually be achieved within a further 4 weeks.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Elderly:</i></span><span style="font-family: Times New Roman, serif;">
No dose adjustment is necessary in the elders.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Patient
with impaired renal function:</i></span><span style="font-family: Times New Roman, serif;">
No dose adjustment is necessary in patients with impaired renal
function.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Patient
with impaired hepatic function: </i></span><span style="font-family: Times New Roman, serif;">In
patients with severe liver impairments, the daily dose should be
reduced to 20 mg pantoprazole. Also, in these patients the liver
enzymes should be monitored during pantoprazole therapy. In cases of
a liver enzymes, it should be discontinued.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Administration:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
content of the vial needs to be reconstituted with 10 ml of sodium
chloride injection 0.9%w/v before injection.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">This
freshly prepared solution should be administered intravenously over 2
to 15 minutes, either as a slow injection or it may be further
diluted with 100ml of sodium chloride injection 0.9%w/v or 5% glucose
injection and administered as a short term infusion.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
duration of administration should be 2 to 15 minutes. The
reconstituted solution must be used within 12 hours of preparation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Warnings
and precautions:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Prior
to the treatment of gastric ulcer, the possibility of malignancy
should be excluded before treatment with pantoprazole is instituted,
as treatment may alleviate symptoms and delay diagnosis.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Anaphylaxis
has been reported with the use of intravenous pantoprazole. This may
require emergency medical treatment.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
diagnosis of an inflammation of the esophagus should be
endoscopically confirmed. </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pantoprazole
does not affect the ability to drive and use machines.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pregnancy
and Lactation:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pregnancy:</b></span><span style="font-family: Times New Roman, serif;">
During pregnancy, pantoprazole should be used unless the benefit
exceeds the potential risk.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Lactation:
</b></span><span style="font-family: Times New Roman, serif;">There is no
information about the safety of pantoprazole during breast feeding in
humans. During breast feeding, pantoprazole should not be used unless
the benefit exceeds the potential risk.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="font-style: normal; margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Adverse
Effects:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Treatments
with pantoprazole can occasionally lead to headache or diarrhea.
Rarely nausea/vomiting, abdominal pain, flatulence, constipation,
allergic reactions such as skin rash and pruritus may occur.
Individual cases of edema, blurred vision, fever, dizziness,
thrombophlebitis, depression or myalgia subsiding after termination
of therapy have been reported.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Drug
Interactions:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">No
clinically significant interactions were observed with carbamazepine,
caffeine, diazepan, diclofena, digoxin, ethanol, glibenclamide,
metoprolol, phenytoin, warfarin and concomitantly administered
antacids.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
with other acid secretions inhibitors, changes in absorption may be
observed when drugs whose absorption is pH dependent, e.g.
ketoconazole are taken concomitantly.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Overdosage
and its treatment:</b></span><span style="font-family: Times New Roman, serif;"> </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
is no known symptoms of overdosage in human. Doses of up to 240mg IV
were administered without adverse effects. Apart from symptomatic and
supportive treatment, no specific therapeutic recommendations can be
made.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Storage
Conditions: </span></b>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
in a dry place at a temperature not exceeding 30</span><sup><span style="font-family: Times New Roman, serif;">o</span></sup><span style="font-family: Times New Roman, serif;">C.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Keep
away from direct sunlight.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Keep
out reach of children.</span></div>
Unknownnoreply@blogger.com2tag:blogger.com,1999:blog-3465762249352810871.post-28010909319906380432013-06-03T07:07:00.001-07:002013-06-03T07:07:54.568-07:00Tranexamic Acid
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Tranexamic
Acid </b></span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>100mg/ml
Injection (I.V.)</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category:</b> Antifibrinolytic agent</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Chemical
Name and Molecular Formula:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Trans-4-(Aminomethyl)
cyclohexanecarboxylic acid. C<sub>8</sub>H<sub>15</sub>NO<sub>2</sub></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacology:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Tranexamic
acid is an antifibrinolytic drug, which inhibits breakdown of fibrin
clots. It acts primarily by blocking the binding of plasminogen and
plasmin to fibrin; direct inhibition of plasmin occurs only to a
limited degree. Tranexamic acid is a competitive inhibitor of
plasminogen activation, and at much higher concentrations, a
noncompetitive inhibitor of plasmin, i.e., actions similar to
aminocaproic acid. Tranexamic acid binds more strongly than
aminocaproic acid to both the strong and weak receptor sites of the
plasminogen molecule in a ration corresponding to the difference in
potency between the compounds.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetics:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Absorption:</i>
Tranexamic acid can be administered by slow intravenous injection or
continuous infusion. After an intravenous dose of 1 g, the plasma
half-life is about 2 hours for the terminal elimination phase. The
plasma protein binding of tranexamic acid is about 3% at therapeutic
plasma levels.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Distribution:
</i>Tranexamic acid is widely distributed throughout the body.
Tranexamic acid diffuses rapidly into joint fluid, the synovial
membrane, CSF, aqueous humor and semen. If diffuses across the
placenta and is distributed into breast milk. The concentration in
cord blood after an intravenous injection of 10mg/kg to pregnant
women is about 30mg/liter, as high as in the maternal blood.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Metabolism:
</i>Only a small fraction of the drug is metabolized.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Excretions:</i>
It is excreted in the urine mainly in unchanged drug. Excretion of
tranexamic acid is about 90% at 24 hours after intravenous
administration of 10mg/kg body weight.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Indications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
the treatment and prophylaxis of hemorrhage associated with excessive
fibrinolysis. In patients with hemophilia for short term use 2-8 days
to reduce or prevent hemorrhage and reduce the need for replacement
therapy during and following tooth extraction.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Tranexamic
acid is contraindicated in patients with acquired defective color
vision, subarachnoid hemorrhage and active intravascular clotting.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Precautions
and Warnings:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
dose of tranexamic acid injection should be reduced in patient with
renal insufficiency because of the risk of accumulation. Caution
should be exercised in the patients with upper urinary tract bleeding
which may cause the ureteral obstruction due to clot formation.
Venous and arterial thrombosis or thromboembolism has been reported
in patients treated with tranexamic acid. In addition, cases of
central retinal artery and central retinal vein obstruction have been
reported.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Used
with caution in patients with a previous history of thromboembolic
disease which may be at increased risk for venous or arterial
thrombosis. Strict supervision by physician should be done while
administrating tranexamic acid to the patients with disseminated
intravascular coagulation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">An
ophthalmic examination, including visual acuity, color vision,
eye-ground and visual fields, is advised for patients who are to be
treated continually for longer than several days and drug should be
discontinued if changes in examination results are found.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Dosage
adjustment should be done in the patients with moderate to severe
impaired renal function.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in Pregnancy and Lactation:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
are no adequate and well-controlled studies in pregnant women.
However, tranexamic acid is known to pass the placenta and appears
in cord blood at concentrations approximately equal to maternal
concentration. Therefore, drug should be used during pregnancy only
if clearly needed.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Tranexamic
acid is present in the mother's milk at a concentration of about a
hundredth of the corresponding serum levels. Caution should be
exercised when tranexamic acid is administered to a nursing woman.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Interactions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Caution
should be exercised when concomitant administration of drugs with
actions on homeostasis is given in the patient with antifibrinolytic
therapy. Care should be taken while concurrently administrating of
estrogen, because it may increase the potential for thrombus
formation. Tranexamic acid should not be administered concomitantly
with Factor IX Complex concentrates or Anti-inhibitor Coagulant
concentrates, as the risk of thrombosis may be increased.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Adverse
Effects:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Gastrointestinal
disturbances (nausea, vomiting, diarrhea) may occur but disappear
when the dosage is reduced. Orthostatic symptoms and hypotension have
been reported occasionally. Hypersensitivity skin reactions have also
been reported. Hypotension has been observed when intravenous
injection is too rapid.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administration:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Adults:</i></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Parenteral
Therapy: 10mg/kg 3-4 times daily.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Immediately
before dental extraction in patients with hemophilia: 10mg/kg
intravenous together with replacement therapy; following surgery,
25mg/kg given orally 3 or 4 times daily for 2-8 days.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><i>Children:
</i></span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Intravenous
therapy: 10mg/kg 2-3 times daily.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Note:</b></span></div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">For
intravenous infusion, tranexamic acid injection may be mixed with
most solutions for infusion such as electrolyte solutions,
carbohydrate solutions, amino acid solutions and dextran solutions.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
mixture should be prepared the same day the solution is to be used.
Heparin may be added to tranexamic acid injection.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Tranexamic
acid injection should NOT be mixed with blood.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
drug is a synthetic amino acid, and should NOT be mixed with
solutions containing penicillin.</span></div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Overdosage:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
is no known case of overdosage of tranexamic acid injection. Symptoms
of overdosage may be nausea, vomiting, orthostatic symptoms and/or
hypotension. In the event of an overdose, the patient should be
treated symptomatically, and supportive measures instituted as
required.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Shelf-Life:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">36
months from the date of manufacturing.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Storage
Conditions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at a temperatures not exceeding 30</span><sup><span style="font-family: Times New Roman, serif;">o</span></sup><span style="font-family: Times New Roman, serif;">C.
Protect from direct sunlight. Keep out of reach of children.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-45307141815497905672013-06-02T06:09:00.000-07:002013-06-02T06:09:57.609-07:00Glimepiride
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Glimepiride</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>1mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>2mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>3mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category: </b>Oral Hypoglycemic (Sulfonylurea group)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Description:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Glimepiride
is an oral blood-glucose-lowering drug of the sulfonylurea class.
Chemically, Glimepiride is identified as
1-[{p[2-(3-ethyl-4-methyl-2-oxo-3-pyrolline-1-carboxamido)ethyl]phenyl]-sulfonyl-3-(trans-4-methylcyclhexyl)urea.
Its molecular formula is C<sub>24</sub>H<sub>34</sub>N<sub>4</sub>O<sub>5</sub>S
and its molecular weight is 490.62.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Mechanism
of Action:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
primary mechanism of action of glimepiride in lowering blood glucose
appears to be dependent on stimulating the release of insulin from
functioning pancreatic beta cells. In addition, extrapancreatic
effects may also play a role in the activity of sulfonylureas such as
glimepiride. This is supported by both preclinical and clinical
studies demonstrating that glimepiride administration can lead to
increased sensitivity of peripheral tissues to insulin.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetics:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">After
oral administration, glimepiride is completely (100%) absorbed from
the GI tract. Peak levels (Cmax) occur at 2 to 3 hours. When
glimepiride was given with meals, the mean Tmax (time to reach Cmax)
was slightly increased (12%) and the mean Cmax and AUC (area under
curve) were slightly decreased (8% and 9%, respectively). Protein
binding was greater than 99.5%. Glimepiride is completely metabolized
by oxidative biotransformation. The major metabolites are the
cyclohexyl hydroxy methyl derivative (M1) and the carboxy derivative
(M2). Cytochrome P450 II C9 has been shown to be involved in the
biotransformation of glimepiride to M1. M1 is further metabolized to
M2, by one or several cytosolic enzymes. M1, but no M2, possesses
about 1/3 of the pharmacological activity as compared to its parent
in an animal model; however, whether the glucose-lowering effect of
M1 is clinical meaningful is not clear. When <sup>14</sup>C-glimepiride
was given orally, approximately 60% of the total radioactivity was
recovered in the urine in 7 days and M1 (predominant) and M2
accounted for 80-90% of the recovered in the urine. Approximately 40%
of the total radioactivity was recovered in feces and M1 and M2
(predominant) accounted for about 70% of that recovered in feces. No
parent drug was recovered from urine or feces.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Indications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Glimepiride
is indicated as an adjunct to diet and exercise to lower the blood
glucose in patients with non-insulin-dependent (Type II) diabetes
mellitus (NIDDM) whose hyperglycemia cannot be controlled by diet and
exercise alone.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindications</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Glimepiride
is not suitable for the treatment of type I diabetes mellitus (eg for
the treatment of diabetics with history of ketoacidosis), of diabetic
ketoacidosis, or of diabetic precoma or coma.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Glimepiride
is contraindicated in patients with known hypersensitivity to
glimepiride, other sulfonylureas, other sulfonamides or any of the
excipients.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
is insufficient data concerning the use of Glimaryl in patients with
severe renal or hepatic impairment. A changeover to insulin is
indicated.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Precautions
and Warnings:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
administration of oral hypoglycemic drugs has been reported to be
associated with increased cardiovascular mortality as compared to
treatment with diet alone or diet plus insulin. The patient should be
informed of the potential risks and advantages of glimepiride and of
alternative modes of therapy.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">All
sulfonylurea drugs are capable of producing severe hypoglycemia.
Proper patient selection, dosage, and instructions are important to
avoid hypoglycemic episodes. Patients with impaired renal function
may be more sensitive to the glucose-lowering effect of glimepiride.
A starting dose of 1mg once daily followed by appropriate dose
titration is recommended in those patients. Debilitated or
malnourished patients, and those with adrenal, pituitary, or hepatic
insufficiency are particularly susceptible to the hypoglycemic action
of glucose-lowering drugs. Hypoglycemia may be difficult to recognize
in the elderly and in people who are taking beta-adrenergic blocking
drugs or other sympatholytic agents. Hypoglycemia is more likely to
occur when caloric intake is deficient, after severe or prolonged
exercise, when alcohol is ingested, or when more than one
glucose-lowering drugs is used. Combined use of glimepiride with
insulin or metformin may increase the potential for hypoglycemia.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">When
a patient stabilized on any diabetic regimen is exposed to stress
such as fever, trauma, infection, or surgery, a loss of control may
occur. At such times, it may be necessary to add insulin in
combination with glimepiride or even use insulin monotherapy. The
effectiveness of any oral hypoglycemic drug, including in many
patients over a period of time, which may be due to progression of
the severity of the diabetes or to diminished responsiveness to the
drug. The phenomenon is known as secondary failure to distinguish if
from primary failure in which the drug is ineffective in an
individual patient when first given. Should secondary failure occur
with glimepiride or metformin monotherapy, combined therapy with
glimepiride and metformin or glimepiride and insulin may result in a
response. Should secondary failure occur with glimepiride/metformin
therapy, it may be necessary to initiate insulin therapy.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Usage
in pregnancy, lactation and children:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
are no adequate and well-controlled studies in pregnant women. On
basis of results from animal studies, Glimepiride should not be used
during pregnancy. Prolonged severe hypoglycemia (4 to 10 days) has
been reported in neonates born to mothers who were receiving a
sulfonylurea drug at the time of delivery. This has been reported
more frequently with the use of agents with prolonged half-lives.
Patients who are planning a pregnancy should consult their physician,
and it is recommended that they change over to insulin for the entire
course of pregnancy and lactation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Because
of the potential for hypoglycemia in nursing infants may exist, and
because of the effects on nursing animals, glimepiride should be
discontinued in nursing mothers. Safety and effectiveness of the drug
in pediatric patients have not been established.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Adverse
Reactions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
incidence of hypoglycemia with glimepiride, as documented by blood
glucose values ,60mg/dhl, has ranged from 0.9-1.7% in most of the
clinical trials carried out with the drug. Adverse events, other than
hypoglycemia, considered to be possible or probably related to study
drug that occurred in more than 1% patients treated with glimepiride
are dizziness, asthenia, headache and nausea. </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Vomiting,
gastrointestinal pain, and diarrhea have been reported, but the
incidence in placebo-controlled trials was less than 1%. In rare
cases, there may be an elevation of liver enzymes levels. In isolated
instances impairment of liver function (e.g. with cholestasis and
jaundice), as well as hepatitis, which may also lead to liver failure
have been reported with sulfonylureas including glimepiride.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Allergic
skin reactions, e.g., pruritus, erythema, urticaria, and morbiliform
or maculopapular eruptions, occur in less than 1% of treated
patients. These may be transient and may disappear despite continued
use of glimepiride. If these hypersensitivity reactions persist, the
drug should be discontinued. Porphyria cutanea tarda,
photosensitivity reactions, and allergic vasculitis have been
reported with sulfonylurea.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Interactions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
hypoglycemic action of sulfonylurea may be potentiated by certain
drugs, including nonsteroidal anti-inflammatory drugs and other drugs
that are highly protein bound, such as salicylates, sulfonamides,
chloramphenicol, coumarins, probenecid, monoamine oxidase inhibitors,
and beta adrenergic blocking agents. When these drugs are
administered to a patient receiving glimepiride, the patient should
be observed closely for hypoglycemia. When these drugs are withdrawn
from a patient receiving glimepiride, the patient should be observed
closely for loss of glycemic control.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Certain
drugs tend to produce hyperglycemia and may lead to loss of control.
These drugs include the thiazides and other diuretics,
corticosteroids, phenothiazines, thyroid products, estrogens, oral
contraceptives, phenytoin, nicotinic acid, sympathomimetics and
isoniazid. When these drugs are administered to a patient receiving
glimepiride, the patient should be closely observed for loss of
control. When these drugs are withdrawn from a patient receiving
glimepiride, the patient should be observed for hypoglycemia.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administration:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
usual starting dose of glimepiride as initial therapy is 1-2mg once
daily, administered with breakfast of the first main meal. Those
patients who may be more sensitive to hypoglycemic drugs should be
started at 1 mg once daily, and should be titrated carefully. The
maximum starting dose of glimepiride should be no more than 2mg.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
usual maintenance dose is 1 to 4 mg once daily. The maximum
recommended dose is 8 mg once daily. After reaching a dose of 2 mg,
dosage increases should be made in increments of no more than 2 mg at
1-2 week intervals based upon the patients blood glucose response.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">If
patients do not respond adequately to the maximal dose of glimepiride
monotherapy, addition of metformin may be considered. Combination
therapy with glimepiride and insulin may also be used in secondary
failure patients.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Glimepiride
is not recommended for use in pregnancy, nursing mother, or children.
In elderly, debilitated, or malnourished patients, or in patients
with renal or hepatic insufficiency, the initial dosing, dose
increments, and maintenance dosage should be conservative to avoid
hypoglycemic reactions.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
with other sulfonylurea hypoglycemic agents, no transition period is
necessary when transferring patients to glimepiride. Patients should
be observed carefully (1-2 weeks) for hypoglycemia when being
transferred from longer half-life sulfonylureas (e.g. chlorpropamide)
to glimepiride due to potential overlapping of drug effect. Or as
prescribed by a physician.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Overdosage:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Overdosage
of sulfonylureas, including glimepiride, can produce hypoglycemia.
Mild hypoglycemia symptoms without loss of consciousness or
neurologic findings should be treated aggressively with oral glucose
and adjustments in drug dosage and/or meal patterns. Close monitoring
should continue until the physician is assured that the patient is
out of danger. Severe hypoglycemic reactions with coma, seizure or
other neurological impairment occur infrequently, but constitute
medical emergencies requiring immediate hospitalization. If
hypoglycemic coma is diagnosed or suspected, the patient should be
given rapid intravenous injection of concentrated (50%) glucose
solution. This should be followed by a continuous infusion of a more
dilute (10%) glucose solution at a rate that will maintain the blood
glucose at a lever above 100mg/dL. Patients should be closely
monitored for a minimum of 24 to 48 hours, because hypoglycemia may
recur after apparent recovery.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Storage
condition:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 30<sup><span style="text-decoration: none;">o</span></sup>C.
Protect from moisture. Store away from heat and direct light.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-13440567021464754892013-05-12T08:13:00.000-07:002013-05-12T08:13:28.371-07:00Ranitidine Hydrochloride
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Ranitidine
Hydrochloride</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>75mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>150mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>300mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category: </b></span><span style="font-family: Times New Roman, serif;">H</span><sub><span style="font-family: Times New Roman, serif;">2
</span></sub><span style="font-family: Times New Roman, serif;">Receptor Antagonist</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Structure
and Chemical Name:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">N[2-[[[5-[9dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-N-methyl-2-nitro-1,1-ethenediamine,
hydrochloride. C</span><sub><span style="font-family: Times New Roman, serif;">13</span></sub><span style="font-family: Times New Roman, serif;">H</span><sub><span style="font-family: Times New Roman, serif;">22</span></sub><span style="font-family: Times New Roman, serif;">N</span><sub><span style="font-family: Times New Roman, serif;">4</span></sub><span style="font-family: Times New Roman, serif;">S.HCl</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacology:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
is a specific rapidly acting histamine H</span><sub><span style="font-family: Times New Roman, serif;">2</span></sub><span style="font-family: Times New Roman, serif;">-antagonist.
It inhibits basal and stimulated secretions of gastric acid, reducing
both the volume and the acid and pepsin content of the secretion.
Ranitidine has a long duration of action and a single 75-mg dose
suppresses gastric acid secretion for up to twelve hours.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Clinical
studies have shown that Ranitidine can relieve the symptoms of excess
acid production for up to twelve hours.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetics:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
HCl is 50% absorbed after oral administration. Absorption is not
significantly impaired by the administration of food or antacids.
Following a single dose of 150mg, serum concentrations of ranitidine
HCl are in this range up to 12 hours. However, blood levels bear no
consistent relationship to dose or degree of acid inhibition.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
principal route of excretion is the urine, with approximately 30% of
the orally administered dose collected in the urine as unchanged drug
in 24 hours. Renal clearance is about 410ml per minute, indicating
active tubular excretion.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
man, the N-oxide is the principal metabolite in he urine; however,
this amounts to <4% of the dose. Other metabolites are the S-oxide
(1%) and the desmethyl ranitidine (1%). The remainder of the
administered dose is found in the stool.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
volume of distribution is about 1.4L/kg. Serum protein binding
averages 15%.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Indications:</b></span></div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Short-term
treatments of active duodenal ulcer</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Maintenance
therapy for duodenal ulcer patients at reduced dosage after healing
of acute ulcers</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
treatment of pathological hypersectory conditions (e.g.
Zollinger-Ellison syndrome and systemic mastocytosis)</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Short-term
treatment of active, benign gastric ulcer</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Maintenance
therapy for gastric ulcer patients at reduced dosage after healing
of acute ulcers</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Treatment
of GERD</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Treatment
of endoscopically diagnosed erosive esophagitis</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Maintenance
of healing of erosive esophagitis</span></div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
is contraindicated for patients known to be hypersensitivity to the
drug or any of the </span><span style="font-family: Times New Roman, serif;">ingredients
of the product.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Precautions
and Warnings:</b></span></div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
excreted via the kidney and so plasma levels of the drug are
increased in patients with severe renal impairment. Ranitidine is
not suitable for these patients.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Patients
who are taking non-steroidal anti-inflammatory drugs especially in
the elderly should be referred to their doctor before taking
ranitidine.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Although
clinical reports of acute intermittent porphyria associated with
ranitidine administration have been rare and inconclusive;
ranitidine should be avoided in patients with a history of this
conditions.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Treatment
with histamine H</span><sub><span style="font-family: Times New Roman, serif;">2</span></sub><span style="font-family: Times New Roman, serif;">-antagonist
may mask symptoms associated with carcinoma of the stomach and may
therefore delay diagnosis of the condition.</span></div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in Pregnancy and Lactation:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
crosses the placenta but therapeutic doses administered to obstetric
patients in labor or undergoing cesarean section have been without
any adverse effect in labor, delivery or subsequent neonatal
progress. Therefore, ranitidine should not be taken during pregnancy
without consulting a doctor.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
is also excreted in human breast milk and women who are breast
feeding will be advised to speak to their doctor before taking
Ranitidine.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Interactions:</b></span></div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Although
ranitidine has been reported to bind weakly to cytochrome P-450 in
vitro, recommended doses of the drug do not inhibit the action of
the cytochrome P-450-linked oxygenase enzymes in the liver. However,
ranitidine may affect the bioavailability of certain drugs by some
mechanism.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Increased
or decreased prothrombin times have been reported during concurrent
use of ranitidine and warfarin. However, in human pharmacokinetic
studies with dosages of ranitidine up to 400mg per day, no
interaction occurred; ranitidine had no effect on warfarin clearance
or prothrombin time.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Reduced
gastric acidity due to ranitidine may result in an increase in the
availability of triazolam, when used concurrently. The clinical
significance of triazolam and ranitidine pharmacokinetic interaction
is unknown.</span></div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Adverse
Effects:</b></span></div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Transient
and reversible changes in liver function tests can occur. There have
been occasional reports of reversible hepatitis (hepatocellular,
hepatocanalicular or mixed) with or without jaundice.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Leucopenia
and thrombocytopenia have occurred rarely in patients. The are
usually reversible.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Rare
cases of agranulocytosis or of pancytopenia, sometimes with marrow
hypoplasia, or aplasia have been reported.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Hypersensitivity
reactions (urticaria, angioneurotic edema, fever, bronchospasm,
hypotension, anaphylactic shock) have been seen rarely following
oral administration of ranitidine. These reactions have occasionally
occurred after a single dose.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
with other H</span><sub><span style="font-family: Times New Roman, serif;">2</span></sub><span style="font-family: Times New Roman, serif;">
receptor antagonist there have been rare reports of bradycardia and
AV block.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Headache,
sometimes severe and dizziness have been reported in a very small
proportion of patients. Rare cases of vasculitis and alopecia have
been reported rarely.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Reversible
impotence has been reported rarely.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Musculoskeletal
symptoms such as arthralgia and myalgia have been reported rarely.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
have been a few reports of breast symptoms (swelling and/or
discomfort) in men taking ranitidine; some cases have resolved on
continued ranitidine treatment.</span></div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administration:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Usual
dosage of Ranitidine is 150mg twice daily. Alternatively, it can be
given as a single bedtime dose of 300mg. Treatment should be
continued for up to 4-8 weeks in most cases of duodenal ulcer,
gastric ulcer and post operative ulcer and reflux esophagitis. In
cases of NSAIDs induced ulceration, 150mg twice daily at bedtime
should be given. In patient with Zollinger-Ellison syndrome, the
starting dose is 150m twice or three times daily and this may be
increased as necessary. Patients with this syndrome have been given
increasing doses up to 6g/day and these doses have been well
tolerated; or as prescribed by the physician.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Overdosage:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Ranitidine
is very specific in action and accordingly no particular problems are
expected following overdosage with the drug. Symptomatic and
supportive therapy should be given as appropriate. However, in case
of overdose, symptomatic treatment with gastric lavage should
employed. If need be, the drug may be removed form the plasma by
hemodialysis.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Storage
Condition:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 30</span><sup><span style="font-family: Times New Roman, serif;">o</span></sup><span style="font-family: Times New Roman, serif;">C.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Protect
from direct sunlight.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Keep
out or reach of children.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-44716609832644052322013-05-11T05:33:00.001-07:002013-05-11T05:33:44.567-07:00Amlodipine besilate
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Amlodipine
besilate</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>5mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>10mg
Tablet</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category:</b> Anti-hypertensive / Calcium Channel Blocker</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacodynamic
Properties</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Mechanism
of Action:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
is a calcium ion influx inhibitor of the dihydropyridine group (slow
channel blocker or calcium ion antagonist) and inhibits the
transmembrane influx of calcium ions into cardiac and vascular smooth
muscle.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
mechanism of the antihypertensive action of amlodipine is due to a
direct relaxant effect on vascular smooth muscle. The precise
mechanism by which amlodipine relieves angina has not been fully
determined but amlodipine reduces total ischemic burden by the
following two actions.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<ol>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
dilates peripheral arterioles and thus, reduces the total peripheral
resistance (afterload) against which the heart works. Since the
heart rate remains stable, this unloading of the heart reduces
myocardial energy consumption and oxygen requirements.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
mechanism of action of amlodipine also probably invovles dilation of
the main coronary arteries and coronary arterioles, both in normal
and ischemic regions. This dilation increases myocardial oxygen
delivery in patients with coronary artery spasm (Prinzmetal's or
variant angina).</span></div>
</li>
</ol>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
patients with hypertension, once daily dosing provides clinical
significant reductions of blood pressure in both the supine and
standing positions throughout the 24 hour interval. Due to the slow
onset of action, acute hypotension is not a feature of amlodipine
administration.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
patients with angina, once daily administration of amlodipine
increases total exercise time, time to angina onset, and time to 1mm
ST segment depression, and decreases both angina attack frequency and
glyceryl trinitrate tablet consumption.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
has not been associated with any adverse metabolic effects or changes
in plasma lipids and is suitable for use in patients with asthma,
diabetes and gout.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Use
in Patients with Heart Failure: Hemodynamic studies and exercise
based controlled clinical trials in NYHA Class II-IV heart failure
patients have shown that amlodipine did not lead to clinical
deterioration as measured by exercise tolerance, left ventricular
ejection fraction and clinical symptomatology.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">A
placebo controlled study designed to evaluate patients in NYHA Class
III-IV heart failure receiving digoxin, diuretics and ACE inhibitors
has shown that amlodipine did not lead to an increase in risk of
mortality or combined mortality and morbidity with heart failure.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
a follow-up, long term, placebo controlled study of amlodipine in
patients with NYHA III and IV heart failure without clinical symptoms
or objective finding suggestive or underlying ischemic disease, on
stable doses of ACE inhibitors, digitalis and diuretics, amlodipine
had no effect on total cardiovascular mortality. In this same
population amlodipine was associated with increased reports of
pulmonary edema despite no significant difference in the incidence of
worsening heart failure as compared to placebo.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
long-term effects of amlodipine on growth, puberty and general
development have not been studied. The long-term efficacy of
amlodipine on therapy in childhood to reduce cardiovascular morbidity
and mortality in adulthood have also not been established.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetic
Properties:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
is well absorbed following oral administration with peak plasma blood
concentrations occurring after 6 12 hours. It has prolonged terminal
elimination half-life of 35 to 50 hours and steady state plasma
concentrations are not achieved until 7 to 8 days of administration.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
is extensively metabolized; metabolites are mostly excreted in urine
together with less than 10% of a dose as unchanged drug.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
is reported to be about 97.5% bound to plasma protein.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in the elderly: </b></span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
time to reach peak plasma concentrations of amlodipine is similar in
elderly and younger subjects. Amlodipine clearance tends to be
decreased with resulting increases in AUC and elimination half-life
in elderly patients. Increases in AUC and elimination half-life in
patients with congestive heart failure were as expected for the
patient age group studied.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Indication</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Management
of Hypertension.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Management
of stable and vasopastic angina pectoris.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administration</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>For
Adults:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">For
both hypertension and angina the usual initial dose is 5mg amlodipine
once daily which may be increased to a maximum dose of 10mg depending
on the individual patient's response.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">No
dose adjustment of amlodipine is required upon concomitant
administration of thiazide diuretics, beta blockers, and
angiotensin-converting enzyme inhibitors.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Use
in the elderly:</b> Amlodipine is used at similar doses in elderly or
younger patients, is equally well tolerated. Therefore normal dosage
regimens are recommended.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Patients
with renal impairment:</b> Changes in amlodipine plasma
concentrations are not correlated with degree of renal impairment,
therefore the normal dosage is recommended. Amlodipine is not
dialysable.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>For
Children and infants by age groups:</b> Not recommended.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindication</b></span></div>
<ul>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
is contraindicated in patients with known sensitivity to
dihydropyridines, amlodipine or any of the excipients.</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
should not be used in cardiogenic shock, clinically significant
aortic stenosis, unstable angina (excluding Prinzmetal's angina)</span></div>
</li>
<li><div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pregnancy
and lactation</span></div>
</li>
</ul>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Warning
and Precautions</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Use
in patients with Heart Failure: In a long-term, placebo controlled
study of amlodipine in patients with NYHA III and IV heart failure or
non-ischemic etiology, amlodipine was associated with increased
reports of pulmonary edema despite no significant difference in the
incidence of worsening heart failure as compared to placebo.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Use
in patients with impaired hepatic function: As with all calcium
antagonists, amlodipine's half-life is prolonged in patients with
impaired liver function and dosage recommendations have not been
established. The drug should therefore be administered with caution
in these patients.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
are no data to support the use of amlodipine alone, during or within
one month of myocardial infarction.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
safety and efficacy of amlodipine in hypertensive crisis has not been
established.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pregnancy
and Lactation</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Although
some dihydropyridine compounds have been found to be teratogenic in
animals, data in the rat and rabbit for amlodipine provide no
evidence for a teratogenic effect. There is, however, no clinical
experience with the preparation in pregnancy or lactation.
Accordingly, amlodipine should not be administered during pregnancy,
or lactation, or to women of childbearing potential unless effective
concentration is used.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Adverse
Drug Reactions</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
most commonly reported side effects of amlodipine are headache,
edema, rash, fatigue, nausea, flushing, and dizziness.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Other
reported side effects are:</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Blood
and lymphatic system disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: thrombocytopenia, leucocytopenia</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Immune
system disorders</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: allergic reaction</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Metabolic
and nutrition disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: hyperglycemia</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Psychiatric
disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
mood changes, insomnia</span></div>
<div align="JUSTIFY" style="font-style: normal; margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Nervous
system disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Common:
somnolence</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
tremor, taste pervesion, syncope, hypoaesthesia, paresthesia</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: peripheral neuropathy</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Eye
disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
visual disturbances</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Ear
and Labyrinth disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
tinnitus</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Cardiac
disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Common:
palpitations</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Rare:
syncope</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: Myocardial infarction, arrhythmia, ventricular tachycardia and
atrial fibrillation</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Vascular
disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
hypotension</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: vasculitis</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Respiratory,
thoracic and mediastinal disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
Dyspnea, rhinitis</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: coughing</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Gastrointestinal
disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Common:
Abdominal pain</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
Vomiting, dyspnea, altered bowel habits, dry mouth</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: Pancreatitis, gastritis, gingival hyperplasia</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Hepato-biliary
disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: Abnormal liver function tests, hepatitis, jaundice</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Skin
and subcutaneous tissue disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
alopecia, pruritus, perpura, skin discoloration, increased sweating</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Very
rare: erythema multiforme, angioedema and urticaria</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Musculoskeletal,
connective tissue and bone disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
Myalgia, arthralgia, muscle cramps and back pain</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Renal
and urinary disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
Increased urinary frequency, micturition disorder, nocturia</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Reproductive
system and breast disorders</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
Impotence, gynecomastia</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">General
disorders and administration site conditions</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Uncommon:
Chest pain, asthenia, pain, malaise, increase or decrease in weight</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Drug
Interactions</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Amlodipine
has been safely administered with thiazide diuretics, alpha blockers,
beta blockers, angiotensin-converting enzyme inhibitors, long acting
nitrates, sublingual glyceryl trinitrate, non-steroidal
anti-inflammatory drugs (NSAIDs), antibiotics and oral hypoglycemic
drugs.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Special
Studies:</b></span><span style="font-family: Times New Roman, serif;"> Effect of
Other agents on amlodipine</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u>Cimetidine:</u></span><span style="font-family: Times New Roman, serif;">
Co-administration of amlodipine with cimetidine did not alter the
pharmacokinetics of amlodipine.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u>Grapefruit
Juice: </u></span><span style="font-family: Times New Roman, serif;">Co-administration
of 240ml of grapefruit juice with a single oral dose of amlodipine
10mg in 20 healthy volunteers had no significant effect on the
pharmacokinetics of amlodipine.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u>Sildenafil:</u></span><span style="font-family: Times New Roman, serif;">
When amlodipine and sildenafil were used in combination, each agent
independently exerted its own blood pressure lowering effect.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Special
Studies: </b></span><span style="font-family: Times New Roman, serif;">Effect of
amlodipine on other agents</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u>Atorvastatin:</u></span><span style="font-family: Times New Roman, serif;">
Co-administration of multiple 10mg doses of amlodipine with 80mg of
atorvastatin resulted in no significant change in the steady state
pharmacokinetics parameters of atorvastatin.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u>Digoxin:</u></span><span style="font-family: Times New Roman, serif;">
Co-administration of amlodipine with digoxin did not change serum
digoxin levels or digoxin renal clearance in normal volunteers.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u>Warfarin:
</u></span><span style="font-family: Times New Roman, serif;">In healthy male
volunteers, the co-administration of amlodipine does not
significantly alter the effect of warfarin on prothrombin response
time. Co-administration of amlodipine with warfarin did not change
the warfarin prothrombin response time.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><u><span style="font-weight: normal;">Ciclosporin:
</span></u></span><span style="font-family: Times New Roman, serif;">Pharmacokinetics
studies with ciclosporin have demostrated that amlodipine does not
significantly alter the pharmacokinetics of ciclosporin.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug/Laboratory
test Interactions: </b></span><span style="font-family: Times New Roman, serif;">None
known.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Known
symptoms of overdosage and particular of its treatment:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">There
is no documented experience with amlodipine overdosage. Gastric
lavage may be of benefit. Gross overdosage could result in excessive
peripheral vasodilation, resulting in marked and probably prolonged
systemic hypotension. Clinically significant hypotension due to
amlodipine over-dosage requires active cardiovascular support.
Intravenous calcium gluconate may be of benefit in reversing the
effects of calcium channel blockade. Since amlodipine is highly
protein-bound, dialysis is not likely to be of benefit. TREATMENT IS
SYMPTOMATIC AND SUPPORTIVE.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Storage
Conditions:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at temperatures not exceeding 30</span><sup><span style="font-family: Times New Roman, serif;">o</span></sup><span style="font-family: Times New Roman, serif;">C.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-58477636230441815632013-05-09T05:53:00.000-07:002013-05-09T05:53:11.314-07:00Terbutaline Sulfate
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Terbutaline
Sulfate</span></b></div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">2.5mg
Tablet</span></b></div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">1.5mg/5ml
Syrup</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category:</b> <span style="font-family: Times New Roman, serif;"><i>β</i></span>-adrenergic
Receptor Agonist (Anti-asthma)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pharmacologic
Action:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Terbutaline
sulfate contains a sympathomimetic substance which stimulates
<span style="font-family: Times New Roman, serif;"><i>β</i></span>-adrenergic
receptors of the sympathetic nervous system. Its main effect is
relaxation of smooth muscles of the bronchial tree and peripheral
vaculature.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Indications:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">For
the relief of reversible bronchospasm in patients with obstructive
airway disease, e.g., asthma, bronchitis, and emphysema.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Dosage
and Administration:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Adults:
2.5mg three times daily to be increased to 5mg three times daily as
necessary.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Pediatric
Dose: Children's doses may be calculated on the basis of the body
weight: a dose of 75mcg per kg three times daily. For children over 7
years of age 2.5mg two or three times daily or as prescribed by the
physicians.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Contraindications:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Patients
who are known to be hypersensitive to sympathomimetic agents.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Precaution:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Terbutaline
sulfate should be used with caution in patients with diabetes
mellitus, hypertension, hyperthyroidism or cardiac disease especially
those with associated arrhythmias. Discontinue use and consult a
physician if decreased effectiveness and bronchoconstriction occurs.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Use
in pregnancy and lactation:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Although
no teratogenic effects have been observed in animals or in patients,
caution is recommended during the first trimester of pregnancy. It
passes into the maternal milk but the risk of influence on the child
is unlikely with therapeutic doses.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Adverse
Effect:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
most common observed adverse effects are tremor and nervousness. The
frequency of side effects appear to diminish with continual therapy.
Other reported reactions are headache, drowsiness, vomiting, nausea,
sweating and muscle cramps. There are usually transient and do not
require treatment.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><br /></b>
</div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Interactions:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Other
sympathomimetic bronchodilators or epinephrine should not be used
concomitantly with terbutaline sulfate, since their combined effects
may be deleterious to the patients. It should be used with caution in
patients being treated with MAOI or tricyclic antidepressants, since
the action of terbutaline on the cardiovascular system may be
potentiated.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><br /></b>
</div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Storage
Condition:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
at temperature not exceeding 30<sup>o</sup>C.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-3465762249352810871.post-90453573768315588582013-05-09T05:51:00.000-07:002013-05-09T05:51:25.544-07:00Rosuvastatin
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Rosuvastatin</span></b></div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">10mg
Tablet</span></b></div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">20mg
Tablet</span></b></div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">40mg
Tablet</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Drug
Category: </b>Antihyperlipidemic</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Pharmacokinetics:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Rosuvastatin
is incompletely absorbed from the gastrointestinal tract, with
bioavailability of about 20%. Peak plasma concentration are achieved
about 5 hours after an oral dose. It is taken up extensively by the
liver, its primary site of action, and undergoes limited metabolism,
mainly by the cytochrome P450 isoenzyme CYP2C9. It is abut 90% bound
to plasma proteins. The plasma elimination half-life of rosuvastatin
is about 19 hours. About 19% of oral dose of rosuvastatin is excreted
in the feces, including absorbed and non-absorbed drug, and the
remainder is excreted in the urine; about 5% of a dose is excreted
unchanged in urine.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><br /></b>
</div>
<b>
</b><div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Indication:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">For
primary hypercholesterolemia (Type IIa including heterozygous
familial hypercholesterolemia), mixed dyslipidemia (Type IIb), or
homozygous familial hypercholesterolemia in patients who have not
responded adequately to diet and other appropriate measure.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Contraindication:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Rosuvastatin
is contraindicated in patients with a known hypersensitivity. It is
contraindicated in patients with active liver disease or with
unexplained persistent elevations of serum transaminases.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Drug
Interaction:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Rosuvastatin
undergoes limited metabolism, principally by the cytochrome P450
isoenzyme CYP2CP, and may not have the same interactions with enzyme
inhibitors as simvastatin. However, increased rosuvastatin plasma
concentrations have been reported with ciclosporin and, to a lesser
extent, with gemfibrozil, and such combination should be avoided. If
they must be given together, lower doses of rosuvastatin should be
used.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Adverse
Effects:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
most common adverse effects of therapy with rosuvastatin and other
statins are gastrointestinal disturbances. Other adverse effects
reported include headache, skin rashes, dizziness, blurred vision,
insomnia, dysgeusia. Reversible increases in serum-aminotransferase
concentration may occur and liver function should be assessed before
treatment is initiated and then monitored periodically until one year
after the last elevation in dose. Hepatitis and pancreatitis have
been reported. Myopathy, characterized by myalgia, and muscle
weakness and associated with increased creatinine phosphokinase
concentration has been reported, especially in patients taking
rosuvastatin concurrently with ciclosporin, fibric acid and
derivatives or nicotinic acid. Rarely, rhabdomyolysis with acute
renal failure may develop.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Precaution:
</span></b>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Rosuvastatin
should not be given to patients with acute liver disease and
unexplained persistently raised serum-aminotransferase
concentrations. It should be avoided during pregnancy since there is
a possibility that it could interfere with fetal sterol synthesis;
there have been few reports of congenital abnormalities associated
with statins. It should be discontinued if marked or persistent
increases in serum-aminotranferase or creatine phosphokinase
concentrations occur. It should be used with caution in patients with
severe renal impairment.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<b><span style="font-family: Times New Roman, serif;">Dosage
and Administration:</span></b></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Usual
initial dose is 10mg once daily. However, a lower initial dose of 5mg
once daily may be adequate is also recommended for patients at risk
of myopathy. Patients with marked hypercholesterolemia, may be
started on 20mg once daily. Or prescribed by the physicians.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br /></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Storage Condition:</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store at temperatures not exceeding </span><span style="font-family: Times New Roman, serif;">30<sup>o</sup>C.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"> </span></div>
Unknownnoreply@blogger.com1tag:blogger.com,1999:blog-3465762249352810871.post-74973101412611992372013-05-06T07:27:00.000-07:002013-05-06T07:27:49.758-07:00Phospholipids
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Phospholipids</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>300mg
Hard Gel Capsule</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Category:
Hepatoprotector</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Composition:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Phospholipids
as active ingredient. is from soya-bean 300mg </span>
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Indications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Nutritional
support in the management of damaged liver (due to chronic liver
disease, liver cirrhosis, fatty liver and intoxication by hepatotoxic
substances).</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Dosage
and Administrations:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Age
and/or Body Weight : Children from 12 years (approx. 43 kg),
Adolescents and adults</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Single
dose: 2 hard capsules (600mg of soya-bean phospholipids)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Total
daily dose: 3 times daily 2 hard capsules (1800mg of soya-bean
phospholipids)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Phospholipids
300mg hard gel capsule is taken unchewed with meals with plenty of
liquid (e.g. with a glass of water).</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Basically,
the duration of the application is not limited.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Contraindications:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Known
hypersensitivity to soya-bean preparations or to any of the
excipients.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Special
warnings and precautions for use:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">This
drug therapy is not a substitute for the avoidance of the noxious
agent causing liver damage (e.g. alcohol). In chronic hepatitis the
adjuvant therapy with soya-bean phospholipids is justified only when
improved subjective well-being becomes manifest during therapy.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Consult
your doctor when complaints aggravate or when other unclear
complaints occur.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Children:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">As
information about the administration in children is insufficient,
Phospholipids 300mg hard gel capsule should not be given to children
under 12 years of age.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Due
to the content in soya-bean oil the medicinal product may provoke
severe allergic reactions.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Interaction
with other medicinal products and other forms of interaction:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">An
interaction of Phospholipids 300mg hard gel capsule with
anti-coagulants cannot be excluded. For this reason, dose adjustment
of the anti-coagulants might be necessary.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Consult
a doctor in the case of simultaneous application.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pregnancy
and lactation:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Preparation
from soya-bean are largely used in human food and so for no clue has
appeared that would suggest any risk during pregnancy. Results from
investigation are insufficient. For this reason, the use of
Phospholipids 300mg hard gel capsule is not recommended during
pregnancy and lactation.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Effects
on ability to drive and use machines:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Phospholipids
300mg hard gel capsule has no effect on the ability to drive and to
use machines.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Side
Effects:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">For
the evaluation of any adverse effects the following incidences are
considered:</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">very
frequent (≥1/10)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">frequent
(≥1/100 to ≥1/10)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">occasional
(≥1/1,000 to ≥1/1,00)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">rare
(≥1/10,000 to ≥1/1,000)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">very
rare (<1/10,000)</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Occasionally
the administration of Phospholipids 300mg hard gel capsule may
provoke gastrointestinal disorders, such as stomach complaints, soft
stools and diarrhea. On very rare occasions allergic reactions may
occur, such as exanthema and urticaria. The doctor or pharmacist
should be informed about any undesirable effect not listed.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
administration of Phospholipids 300mg hard gel capsule should be
discontinued in the event of one of the above mentioned undesirable
effects, especially in hypersensitivity reactions. The patient should
consult who may decide the severity and any measures that might be
necessary.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Overdose:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">No
overdose reaction nor symptom of intoxication has been reported to
date with Phospholipids 300mg hard gel capsule.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
listed undesirable effects may be reinforced.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">The
patient should consult the doctor who may decide about the severity
and any measures that might be necessary.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Clinical
Pharmacology</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacodynamic:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Among
the pharmacodynamic properties reported were hepatoprotective effects
found in numerous experimental models in acute liver damage (induced
by ethanol, alcyl alcohol, carbon tetrachloride, paracetamol and
galactosamine). Furthermore, it was also seen to inhibit steatosis
and fibrosis in chronic liver damage models (induced by ethanol,
thioacetamide, and organic solvents). Its suggested principal actions
have been through accelerated membrane regeneration and
stabilization, inhibited lipid peroxidation and inhibited collagen
synthesis.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Pharmacokinetic:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Animal
experiments into the pharmacokinetics showed that more than 90% of
the orally applied soya-bean phospholipids are absorbed in the small
intestines. Most of it is split by phospholipase A to
1-acyl-lysophosphatidylcholine, 50% of which reacylated immediately
into polyunsaturated phosphotidylcholine still during the process of
absorption in the intestinal mucosa. This polyunsaturated
phosphatidylcholine reaches the blood via the lymph pathway and from
there – mainly bound to HDL – it passes in particular to the
liver.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Tests
into human pharmacokinetics were performed with radioactively labeled
dilinoleoyl-phosphatidlcholine (<sup>3</sup>H and <sup>14</sup>C).
The choline moiety was <sup>3</sup>H-labeled and the linoleic acid
had the <sup>14</sup>C-label. The maximum <sup>14</sup>C
concentration was achieved after 4 to 12 hours and amounted to 27.9%
of the dose. The half-life for this component was 32 hours.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">In
the feces were found 2% of the <sup>3</sup>H and 4.5% of the <sup>14</sup>C
label,in the urine 6% of the <sup>3</sup>H and only minor amounts of
the <sup>14</sup>C label.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">These
results show that both isotopes are absorbed to over 90% in the
intestines.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Storage
Conditions:</b></span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
in the original container, not above 25<sup>o</sup>C</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Store
in the original container in order to protect from humidity.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;">Do
not use after the expiry date.</span></div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<br />
</div>
<div align="JUSTIFY" style="margin-bottom: 0in;">
<span style="font-family: Times New Roman, serif;"><b>Shelf
life:</b> 2 years</span></div>
Unknownnoreply@blogger.com0