Pantoprazole Sodium

Pantoprazole Sodium

40mg for Injection IV

Drug Category: Proton Pump Inhibitor

Pharmacological Action:

Mechanism of action:

Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production by covalently binding to the (H⁺, K⁺)-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⁺, K⁺)-ATPase results in a duration of antisecretory effect that persists longer than 24 hours for all doses tested.

Pharmacokinetics:

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_max) 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.

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.

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.

Indications:

Pantoprazole for injection is indicated for the treatment of gastric ulcer, duodenal ulcer, moderate and severe reflux esophagitis.

Contraindications:

Pantoprazole for injection is contraindicated in known hypersensitivity to the formulation.

Dosage and Administration:

Dosage:

The recommended dose is intravenous administration of the content of one vial (40mg pantoprazole) once daily for 7 days.

Duodenal Ulcer: 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.

Gastric Ulcer and Gastro-esophageal reflux: 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.

Elderly: No dose adjustment is necessary in the elders.

Patient with impaired renal function: No dose adjustment is necessary in patients with impaired renal function.

Patient with impaired hepatic function: 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.

Administration:

The content of the vial needs to be reconstituted with 10 ml of sodium chloride injection 0.9%w/v before injection.

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.

The duration of administration should be 2 to 15 minutes. The reconstituted solution must be used within 12 hours of preparation.

Warnings and precautions:

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.

Anaphylaxis has been reported with the use of intravenous pantoprazole. This may require emergency medical treatment.

The diagnosis of an inflammation of the esophagus should be endoscopically confirmed.

Pantoprazole does not affect the ability to drive and use machines.

Pregnancy and Lactation:

Pregnancy: During pregnancy, pantoprazole should be used unless the benefit exceeds the potential risk.

Lactation: 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.

Adverse Effects:

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.

Drug Interactions:

No clinically significant interactions were observed with carbamazepine, caffeine, diazepan, diclofena, digoxin, ethanol, glibenclamide, metoprolol, phenytoin, warfarin and concomitantly administered antacids.

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.

Overdosage and its treatment:

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.

Storage Conditions:

Store in a dry place at a temperature not exceeding 30^oC.

Keep away from direct sunlight.

Keep out reach of children.