Drug intelligence / Profile preview

Perphenazine

Development stage
Approved
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Perphenazine is a first-generation (typical) antipsychotic of the phenothiazine class, specifically a piperazinyl phenothiazine derivative. It is primarily used to treat schizophrenia and to control severe nausea and vomiting in adults. Perphenazine acts mainly by antagonizing dopamine D1 and D2 receptors in the brain, thereby reducing abnormal excitement and psychotic symptoms. Its antiemetic effect is largely due to dopamine D2 receptor blockade in the chemoreceptor trigger zone and vomiting center. Perphenazine also binds alpha-adrenergic receptor, with additional effects on histamine- and serotonin-mediated pathways[1][3][6]. The drug has been available for decades, originally marketed under the brand name Trilafon[8].

Brand names
Trilafon
Other names
perphenazine decanoate
02

Targets

HTR2A (Serotonin receptor 5-HT2A)CaM (Calmodulin)DRD1 (Dopamine D1 Receptor)DRD3 (Dopamine receptor D3)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)M1 (Muscarinic acetylcholine receptor M1)σR (Sigma receptors)DRD2 (Dopamine D2 Receptor)

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