Cimetidine alters the disposition kinetics of the monoamine oxidase-A inhibitor moclobemide

Marie Paula Schoerlin, Michael Mayersohn, Bettina Hoevels, Herwig Eggers, Monique Dellenbach, Jean Paul Pfefen

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

The influence of cimetidine on the absorption and disposition of moclobemide was examined in eight healthy male subjects. A single 100 mg intravenous and 100 mg oral dose of moclobemide was administered before and after 2 weeks of cimetidine administration (200 mg five times a day). The data on intravenous administration indicated that cimetidine produced a statistically significant alteration in the following disposition parameters (mean values for control versus cimetidine): systemic clearance, 46.6 versus 28.3 L/hr; mean residence time, 2.1 versus 3.2 hours; elimination half-life, 1.6 versus 2.3 hours. There was no significant difference in the steady-state volume of distribution. The absolute oral bioavailability of modobemide increased significantly after cimetidine administration (54% versus 68%), as did the maximum plasma concentration after a single oral dose (575 versus 787 ng/ml). There were no differences in the mean absorption time or time to achieve maximum concentration. The values of systemic and apparent oral clearances of mocobemide after cimetidine administration were directly related to the corresponding control values before cimetidine. In contrast, the percentage change in clearance was essentially independent of the corresponding initial control clearance value.

Original languageEnglish (US)
Pages (from-to)32-38
Number of pages7
JournalClinical Pharmacology and Therapeutics
Volume49
Issue number1
DOIs
StatePublished - Jan 1991

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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