[Comparison of the new MAO-A inhibitors moclobemide, brofaromine and toloxatone with tranylcypromine in an animal experiment: significance for clinical practice].
The rat studies presented in this manuscript show that the new non-hydrazine compounds moclobemide, brofaromine and toloxatone have a profile typical of monoamine oxidase-A (MAO-A) inhibitors. These inhibitors are short-acting (16-24 h), reversible, non-hepatotoxic and have only low liability to potentiate tyramine pressor effects (cheese-effect). The present results in rats and the clinical trials provide evidence that moclobemide is an orally active MAO-A inhibitor which, due to its remarkably low tyramine potentiating pressor effects and to its lack of anticholinergic activity, has a very attractive pharmacological profile. In contrast to moclobemide, tranylcypromine is an irreversible and mixed MAO-A and MAO-B inhibitor with long-lasting effects. This hydrazine derivative is not devoid of hepatotoxic effects and markedly potentiates tyramine pressor effects. Moclobemide, being a particularly safe MAO-A inhibitor, seems to be an effective new compound for the therapy of exogenous and endogenous depressive states.
Da Prada
M
M
Pharmazeutische Forschungsabteilung, F. Hoffmann-La Roche & Co. AG, Basel.
Keller
H H
HH
Kettler
R
R
D015102:3,4-Dihydroxyphenylacetic Acid / Q000097:blood; D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D001549:Benzamides / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D020912:Moclobemide; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D010080:Oxazoles / Q000494:pharmacology; D023303:Oxazolidinones; D010880:Piperidines / Q000494:pharmacology; D051381:Rats; D012701:Serotonin / Q000097:blood; D013329:Structure-Activity Relationship; D014191:Tranylcypromine / Q000494:pharmacology*
D000928:Antidepressive Agents; D001549:Benzamides; D008996:Monoamine Oxidase Inhibitors; D010080:Oxazoles; D023303:Oxazolidinones; D010880:Piperidines; D015102:3,4-Dihydroxyphenylacetic Acid; D012701:Serotonin; D014191:Tranylcypromine; C010798:toloxatone; C038213:brofaromine; D020912:Moclobemide
Vergleich der neuen MAO-A-Hemmer Moclobemid, Brofaromin und Toloxaton mit Tranylcypromin im Tierversuch: Bedeutung für die Praxis.