Pirlindole: a selective reversible inhibitor of monoamine oxidase A. A review of its preclinical properties.

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Bruhwyler J, Liegeois JF, Geczy J

Pirlindole: a selective reversible inhibitor of monoamine oxidase A. A review of its preclinical properties.

Pharmacol Res. 1997 Jul;36(1):23-33. doi: 10.1006/phrs.1997.0196.

PubMed ID

9368911 [ View in PubMed

]

Abstract

Pirlindole is a tetracyclic compound that has been characterized as a potential antidepressant drug. It has pharmacological characteristics in common with both tricyclic antidepressants and classical irreversible monoamine oxidase inhibitors. Its main mechanism of action consists of a selective and reversible inhibition of monoamine oxidase A. Secondarily, it exerts an inhibitory effect on noradrenaline and 5-hydroxytryptamine reuptakes. It has no effect on the dopaminergic and cholinergic systems. It has only a low potential for amplifying tyramine and noradrenaline pressor effect, which makes one expect that it will not be at the basis of a 'cheese effect'. Pirlindole has an absolute bioavailability of between 20 and 30% due to an extensive first-pass effect. Orally, the Tmax varies between 2.5 and 6 h in the rat and 0.8 and 2 h in the dog. Two phases of elimination (7.5 and 34-70 h) are measured in the rat and three phases in the dog (1.3, 10.8 and 185 h); it is extensively metabolized. The rat eliminates mainly unconjugated products while the dog eliminates mostly conjugated products. Acute and chronic toxicological studies have not revealed potentially dangerous effects of the drug at the usual doses. It does not present measurable mutagenic, clastogenic or carcinogenic properties. Thus, pirlindole shows pharmacological, pharmacokinetic and toxicological properties which make it suitable for the management of depression.

DrugBank Data that Cites this Article

Drugs

Pirlindole

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pirlindole	5-hydroxytryptamine receptor 1A	Protein	Humans	Unknown	Antagonist	Details
Pirlindole	Amine oxidase [flavin-containing] A	Protein	Humans	Unknown	Antagonist	Details