Chemical formula: C₂₁H₂₆ClN₃OS Molecular mass: 403.969 g/mol PubChem compound: 4748
Perphenazine (4-[3-(2-chlorophenothiazin-10-yl)propyl]-1-piperazineethanol), a piperazinyl phenothiazine, having the chemical formula, C21H26CIN3OS.
Perphenazine is a depressant which blocks dopamine receptors in the central nervous system.
Perphenazine is absorbed readily from the gastro-intestinal tract. It is distributed widely throughout the body, and crossesthe placenta. Following oral administration of perphenazine tablets, mean peak plasma perphenazine concentrations were observed between 1 to 3 hours.
Perphenazine is metabolised extensively by sulphoxidaction, demethylation, hydroxylation, N-oxidation, glucuronic acid conjugation, and possible ring fission. The pharmacokinetics of perphenazine covary with the hydroxylation of debrisoquine which is mediated by cytochrome P450 2D6 (CYP 2D6) and thus is subject to genetic polymorphism – i.e. 7% to 10% of Caucasians and a low percentage of Asians have little or no activity and are called “poor metabolizers.” Poor metabolizers of CYP 2D6 will metabolize perphenazine more slowly and will experience higher concentrations compared with normal or “extensive” metabolizers.
20 to 70% is excreted in the urine, very little is unchanged. 5% is excreted in the faeces.
No further relevant data.
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