Drug Groups

approved

Description

An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine. [PubChem]

Indication

For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults.

Pharmacology

Perphenazine is a piperazinyl phenothiazine, acts on the central nervous system, and has a greater behavioral potency than other phenothiazine derivatives whose side chains do not contain a piperazine moiety. It is a member of a class of drugs called phenothiazines, which are dopamine D1/D2 receptor antagonists. Perphenazine is 10 to 15 times as potent as chlorpromazine; that means perphenazine is a highly potent antipsychotic. In equivalent doses it has approximately the same frequency and severity of early and late extrapypramidal side-effects compared to Haloperidol.

Toxicity

Symptoms of overdose include stupor or coma, and children may have convulsive seizures. Signs of arousal may not occur for 48 hours. Oral LD₅₀=318 mg/kg (rat); IPR LD₅₀=64 mg/kg (mouse)

Affected Organisms

Biotransformation

Hepatic.

Absorption

Absolute bioavailability is 40% following oral administration.

Half Life

8-12 hours, but ranges up to 20 hours.

Elimination

Perphenazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.

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