Dose linearity of the pharmacokinetics of the new H+/K(+)-ATPase inhibitor pantoprazole after single intravenous administration

• Published in: International journal of clinical pharmacology and therapeutics Vol. 34; no. 1 Suppl; p. S18
• Main Authors: Bliesath, H, Huber, R, Hartmann, M, Lühmann, R, Wurst, W
• Format: Journal Article
• Language: English
• Published: Germany 01-05-1996
• Subjects: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Area Under Curve; Benzimidazoles - administration & dosage; Benzimidazoles - adverse effects; Benzimidazoles - pharmacokinetics; Enzyme Inhibitors - administration & dosage; Enzyme Inhibitors - adverse effects; Enzyme Inhibitors - pharmacokinetics; Half-Life; Humans; Injections, Intravenous; Male; Omeprazole - analogs & derivatives; Proton Pump Inhibitors; Regression Analysis; Single-Blind Method; Sulfoxides - administration & dosage; Sulfoxides - adverse effects; Sulfoxides - pharmacokinetics
• ISSN: 0946-1965

Pantoprazole is a specific inhibitor of the H+/K(+)-ATPase of the gastric parietal cell. The dose-dependency of a range of pantoprazole pharmacokinetic characteristics was studied. Twelve healthy male subjects were given 10, 20, 40 and 80 mg pantoprazole intravenously according to a randomized, single blind, 4-period change-over scheme. The area under the concentration vs time curve (AUC) and the maximum serum concentration (Cmax) showed a linear increase in line with the dose. Apparent volume of distribution (Vd area), clearance (Cl) and terminal half-life (t1/2) were independent of the dose. The dose-independent elimination of pantoprazole was attributed to the lack of interaction of the drug with cytochrome P450. In clinical practice, a good predictable response, as well as a low potential for interaction with other drugs might be expected.