Indication: For the treatment of schizophrenia, nusea, vomiting
Pharmacology: Perphenazine is a piperazinyl phenothiazine indicated for the treatment of patients with moderate to severe anxiety and/or agitation and depressed mood; patients with depression in whom anxiety and/or agitation are moderate or severe; patients with anxiety and depression associated with chronic physical disease; patients in whom depression and anxiety cannot be clearly differentiated. Perphenazine is also used to treat schizophrenia and symptoms such as hallucinations, delusions, and hostility. It can also be used to treat nausea and vomiting. Perphenazine 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 phenthiazines, which are dopamine D1/D2 receptor antagonists.
Mechanism Of Action: Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone and vomiting centre. Perphenazine also binds the alpha andrenergic receptor. This receptor's action is mediated by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Drug Category: Antipsychotics; Phenothiazines; Dopamine Antagonists; ATC:N05AB03
Interactions:
DrugBank: Interactions for Perphenazine
Interactions for Perphenazine:
Metabolism of a number of medications, including antipsychotics, antidepressants, b- blockers, and
antiarrhythmics, occurs through the cytochrome P450 2D6 isoenzyme (debrisoquine hydroxylase). Approximately 10% of
the Caucasian population has reduced activity of this enzyme, so-called poorî metabolizers. Among other
populations the prevalence is not known. Poor metabolizers demonstrate higher plasma concentrations of antipsychotic
drugs at usual doses, which may correlate with emergence of side effects. In one study of 45 elderly patients
suffering from dementia treated with perphenazine, the 5 patients who were prospectively identified as poor P450 2D6
metabolizers had reported significantly greater side effects during the first 10 days of treatment than the 40
extensive metabolizers, following which the groups tended to converge. Prospective phenotyping of elderly patients
prior to antipsychotic treatment may identify those at risk for adverse events.
The concomitant administration of other drugs that inhibit the activity of P450 2D6 may acutely increase plasma
concentrations of antipsychotics. Among these are tricyclic antidepressants and selective serotonin reuptake
inhibitors, e.g.fluoxetine, sertraline and paroxetine. When prescribing these drugs to patients already receiving
antipsychotic therapy, close monitoring is essential and dose reduction may become necessary to avoid toxicity. Lower
doses than usually prescribed for either the antipsychotic or the other drug may be required.
Chemical IUPAC Name: 2-[4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
Chemical Formula: C21H26ClN3OS
Half Life: Not Available
Drug Type: Approved Drug
# Accession No: APRD00429
CAS Registry Number: 58-39-9
Perphenazine News (When available)
CATIE Phase I Helps Clinicians Tailor Schizophrenia TreatmentJan 12, 2006 Psychiatric Times, ...olanzapine [Zyprexa], quetiapine [Seroquel], risperidone [Risperdal] and ziprasidone [Geodon]) and one first-generation antipsychotic, perphenazine (Trilafon). ...
We need more studies like CATIE - says Principal InvestigatorJan 11, 2006 Pharma Times (subscription), ...olanzapine (Zyprexa), quetiapine (Seroquel), risperidone (Risperdal), and ziprasidone (Geodon); or to the older, 'typical' medication, perphenazine (Trilafon). ...
Study briefs, 1/03: Antipsychotics, kidney disease, foot soresJan 3, 2006 Lincoln Journal Star, The drugs included the conventional antipsychotics Tindal, Thorazine, Prolixin, Permitil, Serentil, Trilafon, Mellaril, Stelazine, Vesprin, Taractan, Haldol ...
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