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Cimetidine alters the disposition kinetics of the monoamine oxidase‐A inhibitor moclobemide
Author(s) -
Schoerlin MariePaule,
Mayersohn Michael,
Hoevels Bettina,
Eggers Herwig,
Dellenbach Monique,
Pfefen JeanPaul
Publication year - 1991
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1991.6
Subject(s) - moclobemide , cimetidine , volume of distribution , bioavailability , oral administration , pharmacokinetics , absorption (acoustics) , pharmacology , medicine , chemistry , physics , hippocampus , acoustics , antidepressant
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 moclobemide 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 moclobemide 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. Clinical Pharmacology and Therapeutics (1991) 49 , 32–38; doi: 10.1038/clpt.1991.6