PENSIG INJECTION

Pharmacology

Pharmacodynamics: – Pantoprazole act by selectively inhibiting the H+/K+ – ATPase enzyme in the secretory canaliculus of the stimulated parietal cell. Within this cell, the function of the enzyme is to secrete acid by forcing an exchange of H3O+ for K+ when a K+ -Cl- pathway is parallel to the pump. The result of pump turnover is the secretion of HCl into the stomach. This is the final common pathway for acid secretion. Pump inhibition blocks acid secretion regardless of whether it originates from stimulation of muscarinic, gastrin, or histamine receptors Pharmacokinetics: –

• Absorption and Distribution: – Following intravenous administration of pantoprazole, serum/plasma concentrations decline biexponentially. The terminal half-life (t½) is about 1 hour. The total serum clearance is approximately 0.1 l/h/kg and the volume of distribution is about 0,15 l/kg. The plasma kinetics for pantoprazole after both oral and intravenous administration is linear over the dose range 10 to 80 mg.

• Metabolism: – Pantoprazole is almost exclusively metabolised in the liver. The main metabolite is desmethyl-pantoprazole, which is conjugated with sulphate.

• Elimination: – Renal elimination represents the most important route of excretion (approximately 80%) for the metabolites of pantoprazole. The balance is excreted with the feces. The half-life of the main metabolite is approximately 1½ hours which is slightly longer than that of pantoprazole. A slight increase in AUC and Cmax occurs in elderly volunteers compared with younger patients.

Indications: – The FDA-labeled indication is for the short-term treatment (up to 16 weeks) of erosive oesophagitis associated with GERD. Other possible uses may include the maintenance treatment of erosive oesophagitis, acute or maintenance treatment of duodenal or gastric ulcers, treatment of pathological hypersecretory conditions, and adjunct treatment with antibiotics for Helicobacter pylori. Pantoprazole i.v. is indicated for the short-term treatment (7 to 10 days) of GERD in patients unable to take the oral formulation.