| Item |
Information |
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Drug Groups
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approved |
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Description
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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 |
| • |
Humans and other mammals |
|
| 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. |
| External Links |
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