Disposition kinetics of moclobemide, a monoamine oxidase-A enzyme inhibitor: Single and multiple dosing in normal subjects

M. P. Schoerlin, Michael Mayersohn, A. Korn, H. Eggers

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Abstract

The absorption and disposition kinetics of moclobemide (Ro 11-1163), a new reversible and preferential monoamine oxidase-A enzyme inhibitor, were examined in 12 normal male subjects. An intravenous infusion was administered before and after a 15-day multiple oral dosing regimen (100 mg t.i.d.). Plasma concentration-time data were obtained after each intravenous infusion, after the first oral dose, during two dosing intervals at steady state, and before the second daily dose on several days. The disposition values (percent coefficient of variation in parentheses) after the first and second intravenous infusions, respectively, were: clearance, 39.4 (15%) and 29.1 (12%) L/hr; elimination half-life, 1.60 (15%) and 2.00 (18%) hours; and volume of distribution at steady state, 84.3 (11%) and 80.7 (15%) L. The absolute oral bioavailability increased from 0.56 after the first oral dose to 0.86 and 0.90 after the first and second weeks of administration, respectively. The reduced metabolic, presumably hepatic, clearance may be the result of self-inhibition or metabolite inhibition of moclobemide clearance.

Original languageEnglish (US)
Pages (from-to)395-404
Number of pages10
JournalClinical Pharmacology and Therapeutics
Volume42
Issue number4
Publication statusPublished - 1987
Externally publishedYes

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ASJC Scopus subject areas

  • Pharmacology

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