U. Breyer, H. Gaertner, A. Prox
Jan 15, 1974
Citations
1
Influential Citations
27
Citations
Quality indicators
Journal
Biochemical pharmacology
Abstract
Abstract Degradation of the piperazine ring in the phenothiazine drugs perazine, trifluoperazine, fluphenazine, prochlorperazine and perphenazine in vivo leads to the formation of γ-(phenothiazinyl-10)-propylamine (PPA) and of its ring-substituted analogues CF 3 -PPA and Cl-PPA. The sulfoxides of these metabolites have been identified as urinary biotransformation products in patients ingesting perazine or fluphenazine, in rats treated chronically with perazine, trifluoperazine, prochlorperazine or perphenazine, and in a dog given fluphenazine. The structures of the compounds have been confirmed by mass spectrometry. The primary amines are also known metabolites of dimethylamino-substituted phenothiazines, since PPA results from didemethylation of promazine, and CF 3 -PPA and Cl-PPA (= nor 2 -chlorpromazine) are formed from triflupromazine and chlorpromazine, respectively.