Pharmacological Studies on Perazine and its Primary Metabolites

Abstract

The study served to answer the question whether metabolites possibly contribute to the clinical actions of the neuroleptic drug perazine. The primary metabolites demethylperazine and perazine sulfoxide were investigated with regard to influences on behavior in mice, to an antiemetic action in dogs, and to a modification of the pressor effect of noradrenaline in rats. In contrast to perazine, none of the metabolites exhibited effects that can be interpreted to indicate neuroleptic or antidepressive properties of the compounds.

Cytochrome P-450 enzymes and FMO3 contribute to the disposition of the antipsychotic drug perazine in vitro

“…These metabolites are also subject to secondary metabolism (Kanig and Breyer 1969;Krauss et al 1969). PSO and DMP were pharmacologically inactive at normal plasma concentrations in animal studies (Brand et al 1989). Data on the contribution of metabolic pathways to PER metabolism in vivo are limited.…”