The role of cytochrome P450 2D6 in the metabolism of moclobemide

doi:10.1016/0924-977X(96)00023-5

European Neuropsychopharmacology

Volume 6, Issue 3, August 1996, Pages 225-230

https://doi.org/10.1016/0924-977X(96)00023-5 Get rights and content

Abstract

The metabolic fate of moclobemide (Ro 11-1163), a new reversible and selective inhibitor of monoamine oxidase type A (MAO-A), has been assessed in a pilot study in 2 debrisoquine poor metabolizers (PM) and 4 extensive metabolizers (EM) after multiple oral dosings of moclobemide with and without co-medication of dextromethorphan. Absorption and disposition parameters were not different between PM and EM. Concurrent application of dextromethorphan, a selective substrate of CYP2D6, did not affect the pharmacokinetics of moclobemide. These results indicate that the cytochromal isoenzyme CYP2D6 does not play a major role in the metabolic degradation of moclobemide. Limited CYP2D6 activities because of a genetic defect or co-medications with CYP2D6 substrates should therefore not give rise to elevated moclobemide blood levels.

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Research paperThe role of cytochrome P450 2D6 in the metabolism of moclobemide

Abstract

Trends Pharmacol. Sci.

J. Chromatogr.

Clinical consequences of polymorphic drug oxidation

Fundam. Clin. Pharmacol.

Interactions of moclobemide with concomitantly administered medication: evidence from pharmacological and clinical studies

Psychopharmacology

Influence of food on the tyramine pressor effect during chronic moclobemide treatment of healthy volunteers

Eur. J. Clin. Pharmacol.

Relevance of genetic polymorphism in drug metabolism in the development of new drugs

Eur. J. Clin. Pharmacol.

Pharmacogenetic investigations in moclobemide (MOCL) + thioridazine (THD) vs MOCL + placebo treated depressive patients

Neuropsychopharmacology

The pharmacogenetics of the selective serotonin reuptake inhibitors

Clin. Invest.

A specific and short-acting MAO inhibitor with antidepressant properties

Neurochemical profile of moclobemide, a short-acting and reversible inhibitor of monoamine oxidase type A1

J. Pharmacol. Exp. Ther.

Debrisoquine oxidative phenotyping and psychiatric drug treatment

Eur. J. Clin. Pharmacol.

An update of recent moclobemide interaction data

Int. Clin. Psychopharmacol.

Role of cytochrome P4502D6 in the metabolism of brofaromine

Eur. J. Clin. Pharmacol.

Human cytochromes P450: problems and prospects

Trends Pharmacol. Sci.

Characterization of the common genetic defect in humans deficient in debrisoquine metabolism

Nature

Moclobemide treatment causes a substantial rise in the sparteine metabolic ratio

Br. J. Clin. Pharmacol.

Research paper
The role of cytochrome P450 2D6 in the metabolism of moclobemide

Neurochemical profile of moclobemide, a short-acting and reversible inhibitor of monoamine oxidase type A¹