Pharmacokinetics of oral moclobemide in healthy human subjects and effects on MAO-activity in platelets and excretion of urine monoamine metabolites.

The plasma concentrations of the MAO-inhibitor moclobemide (Ro 11-1163) were determined in six healthy male subjects after oral (tablets) administration. Effects on MAO activity in platelets and excretion of monoamine metabolites in urine were investigated. The design of the study was a double-blind cross-over study with single oral doses of placebo, 50, 100 and 200 mg of moclobemide.

Single-dose pharmacokinetics of the MAO-inhibitor moclobemide in man.

The single-dose kinetics of the MAO-inhibitor p-chloro-N-(2-morpholinoethyl)-benzamide (moclobemide, Ro 11-1163) following oral and i.v. administration to six healthy subjects is described.

[The use of the concepts of "half-life" and "clearance" in practice and in pharmacokinetics].

The elimination of drugs from the body and the different modes of dealing with this process on a quantitative scale are discussed. The concepts of half-life and clearance are briefly reviewed. It is shown that with the term "half-life" the investigator focuses upon the elimination of the drug from the whole of the body.

[The bioavailability of orally administered drugs with special regard to the liver as a filter for foreign matter].

A survey of the various aspects of the concept of bioavailability of orally administered drugs is presented. Oral bioavailability may be less than complete as a result of one of three main situations: incomplete absorption due to very slow and/or incomplete dissolution of the drug in the gastrointestinal tract, incomplete absorption due to poor permeability of the drug through the intestinal epithelia, and biotransformation of the drug during its first passage through the liver. This latter so-called first-pass effect is discussed in details.