Monday, December 8, 2014

LORATADINE

LORATADINE
10mg Tablet
5mg/5ml Syrup

BRANDNAME:
Claritin; Loraday; Allerta

DRUG CATEGORY:
Antihistamine ( H1-receptor antagonist)

INDICATION:
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.

PHARMACOLOGY:
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.

PHARMACOKINETICS:
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.
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 Cmax) were comparable to those following administration of 10mg tablet or syrup to adult volunteers.

DOSAGE AND ADMINISTRATION:
Adult and children over 12 years: 1 tablet or 2 tsp once a day.
Children: 2 – 12 years over 66lbs (30kg) 2 tsp once a day, 2 – 12 year ≤ 66lbs (30kg) 1 tsp, 1 – 2 yr ½ syrup once a day
Patient with liver or kidney disease should take 10mg every other day.
Dosage may also depend on your doctor's order.

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.

CONTRAINDICATION:
Loratadine is contraindicated in patients who are hypersensitive to this medication.

SPECIAL PRECAUTION:
Liver Dysfunction: 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.

Renal Impairment: 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.

ADVERSE DRUG REACTION:
Most Common:
Headache, dry mouth, and drowsiness or fatigue.

Less Common:
Eyes, Ears and Nose: 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.
Skin: Sweating, flushing, itching, rash, dry hair or skin, unusual sensitivity to the sun, black and blue marks.
Urogenital System: Male impotence, loss of sex drive, breast pain, vaginal irritation, menstrual changes, altered urination, and urine discoloration.
Gastrointestinal System: Thirst, nausea and vomiting, abdominal distress, stomach irritation or upset, constipation, diarrhea, taste changes, sore throat and vomiting blood.
Musculoskeletal System: Back pain, leg cramps, toothache and joint or muscle aches or pains.
Respiratory System: Respiratory infection, breathing difficulty, coughing, sneezing, bronchitis, bronchial spasm and laryngitis.
Circulatory System: Blood pressure changes and heart palpitation.
Nervous System: Migraine
Psychological: Hyperactivity, appetite changes, anxiety, depression, agitation, sleeplessness, memory lapse, loss of concentration, paranoia, confusion and nervousness.
Extremities: Tingling in the hands or feet and tremors.
Others: Fever, chills, feelings of ill health, weakness, worsening of allergic symptoms and fainting.

Rare:
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).

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.

SPECIAL PRECAUTION:
Pregnancy and Nursing Mothers:
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.
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.

Elderly:
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..

Effects on ability to drive and use machines:
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.

DRUG INTERACTION:
  1. Loratadine does not interact with alcohol or other nervous-system depressant to produce drowsiness or loss of coordination.
  2. 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.

OVERDOSAGE:
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.

STORAGE:
Store at temperatures not exceeding 25oC. Protect from light.
Keep out of reach of children.

2 comments:

  1. Loratadine is a histamine H1 receptor antagonist, used to treat allergies. It also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM. Loratadine

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  2. 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.
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