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Clinical pharmacology of moclobemide, a new reversible monoamine oxidase inhibitor

Charterhouse Clinical Research Unit, London EC1, UK

P. Turner

St Bartholomew's Hospital Medical College, London EC1, UK

T.G.K. Mant

Guys Drug Research Unit, London SE1, UK

P. Morrison

Guys Drug Research Unit, London SE1, UK

G. Haywood

Guys Drug Research Unit, London SE1, UK

V. Glover

q Queen Charlotte's and Chelsea Hospital, London W6, UK

B.L. Goodwi

q Queen Charlotte's and Chelsea Hospital, London W6, UK

M. Sandler

q Queen Charlotte's and Chelsea Hospital, London W6, UK

P. St. John-Smith

Roche Products Limited, Welwyn Garden City, Herts, UK

G.R. McClelland

Roche Products Limited, Welwyn Garden City, Herts, UK

The clinical pharmacology of the new reversible monoamine oxidase (MAO) inhibitor, moclobemide, was examined in three separate studies in healthy male volunteers. In a single oral dose study, moclobemide (25-150 mg) was rapidly absorbed from the gastrointestinal tract and had a relatively short plasma half-life (mean 1.3 h after 150 mg). A decrease in the plasma concentrations of the noradrenaline metabolite 4- hydroxy-3-methoxyphenylglycol (HMPG), however, indicated a longer time to peak pharmacodynamic effect and longer duration of activity. Assay of platelet MAO activity did not reveal any evidence of irreversible inhibition of the B form of the isoenzyme. Single oral doses of moclobemide (150 and 300 mg) significantly lowered the threshold to the cardiovascular effects ('cheese reaction') of intravenous tyramine. However, after repeated administration of 100 mg three times daily for over 2 weeks, moclobemide caused significantly less potentiation than did phenelzine (15 mg three times per day) on the cardiovascular effects of oral tyramine, a clinically more relevant model. The MAO-B inhibitor, selegiline (5 mg once daily), also lowered the oral tyramine threshold significantly. Moclobemide was generally well tolerated by these healthy volunteers.

Journal of Psychopharmacology, Vol. 5, No. 1, 82-91 (1991)
DOI: 10.1177/026988119100500112


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