[Comparison of the new MAO-A inhibitors moclobemide, brofaromine and toloxatone with tranylcypromine in an animal experiment: significance for clinical practice]

Psychiatr Prax. 1989 Aug:16 Suppl 1:18-24.
[Article in German]

Abstract

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.

Publication types

  • Comparative Study
  • English Abstract

MeSH terms

  • 3,4-Dihydroxyphenylacetic Acid / blood
  • Animals
  • Antidepressive Agents / pharmacology*
  • Benzamides / pharmacology
  • Blood Pressure / drug effects
  • Heart Rate / drug effects
  • Moclobemide
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Oxazoles / pharmacology
  • Oxazolidinones*
  • Piperidines / pharmacology
  • Rats
  • Serotonin / blood
  • Structure-Activity Relationship
  • Tranylcypromine / pharmacology*

Substances

  • Antidepressive Agents
  • Benzamides
  • Monoamine Oxidase Inhibitors
  • Oxazoles
  • Oxazolidinones
  • Piperidines
  • 3,4-Dihydroxyphenylacetic Acid
  • Serotonin
  • Tranylcypromine
  • toloxatone
  • brofaromine
  • Moclobemide