QuickView for Perphenazine (compound)

Summary
General Info

PubChem

PubChem Compound 10319251

Name:	Perphenazine
PubChem Compound ID:	10319251
Description:	An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.
Molecular formula:	C₂₁H₂₆ClN₃OS
Molecular weight:	407.994 g/mol

DrugBank

Identification

Name:	Perphenazine
Name (isomeric):	DB00850
Drug Type:	small molecule
Description:	An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.
Synonyms:	Perphenazin; Chlorperphenazine; Etaperazine; Perfenazine; PZC; Ethaperazine; Perfenazina; Etaperazin
Brand:	Decentan, Fentazin, Trilifan, Triphenot, Apo-Perphenazine, Trilafon, Etrafon-Forte, Thilatazin, Trifaron, Etrafon-A, F-Mon, Perphenan, Emesinal
Brand name mixture:	Pms-Levazine 3/15 Tab(Amitriptyline Hydrochloride + Perphenazine), Proavil Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon F Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon a Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon D Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon 2 10(Amitriptyline Hydrochloride + Per... show more » Pms-Levazine 3/15 Tab(Amitriptyline Hydrochloride + Perphenazine), Proavil Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon F Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon a Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon D Tab(Amitriptyline Hydrochloride + Perphenazine), Etrafon 2 10(Amitriptyline Hydrochloride + Perphenazine), Apo Peram Tab 3-15(Amitriptyline Hydrochloride + Perphenazine), Apo Peram Tab 2-25(Amitriptyline Hydrochloride + Perphenazine), Pms-Levazine 2/25 Tab(Amitriptyline Hydrochloride + Perphenazine), Elavil Plus Tab(Amitriptyline Hydrochloride + Perphenazine), Triavil Tab(Amitriptyline Hydrochloride + Perphenazine), Pms-Levazine 4/25 Tab(Amitriptyline Hydrochloride + Perphenazine) show less «
Category:	Phenothiazines, Dopamine Antagonists, Antipsychotic Agents, Antipsychotics
CAS number:	58-39-9

Pharmacology

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 po... show more » 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. show less «
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 as... show more » 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. show less «
Absorption:	Absolute bioavailability is 40% following oral administration.
Biotransformation:	Hepatic.
Route of elimination:	Perphenazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.
Half Life:	8-12 hours, but ranges up to 20 hours.
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

Interactions

Food interaction:

Avoid alcohol.

Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.

Take with food.

Drug interaction:

Grepafloxacin	Increased risk of cardiotoxicity and arrhythmias
Levofloxacin	Increased risk of cardiotoxicity and arrhythmias
Amphetamine	Decreased anorexic effect, may increase psychotic symptoms
Metrizamide	Increased risk of convulsions
Terbinafine	Terbinafine may reduce the metabolism and clearance of Perphenazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Perphenazine if Terbinafine is initiated, discontinued or dose changed.

Grepafloxacin	Increased risk of cardiotoxicity and arrhythmias
Levofloxacin	Increased risk of cardiotoxicity and arrhythmias
Amphetamine	Decreased anorexic effect, may increase psychotic symptoms
Metrizamide	Increased risk of convulsions
Terbinafine	Terbinafine may reduce the metabolism and clearance of Perphenazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Perphenazine if Terbinafine is initiated, discontinued or dose changed.
Sparfloxacin	Increased risk of cardiotoxicity and arrhythmias
Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Phentermine	Decreased anorexic effect, may increase psychotic symptoms
Phenylpropanolamine	Decreased anorexic effect, may increase psychotic symptoms
Bromocriptine	The phenothiazine decreases the effect of bromocriptine
Donepezil	Possible antagonism of action
Guanethidine	Perphenazine may decrease the effect of guanethidine.
Dextroamphetamine	Decreased anorexic effect, may increase psychotic symptoms
Methamphetamine	Decreased anorexic effect, may increase psychotic symptoms
Mazindol	Decreased anorexic effect, may increase psychotic symptoms
Benzphetamine	Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Perphenazine, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
Atomoxetine	The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Terfenadine	Increased risk of cardiotoxicity and arrhythmias
Trimethobenzamide	Trimethobenzamide and Perphenazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Phendimetrazine	Decreased anorexic effect, may increase psychotic symptoms
Galantamine	Possible antagonism of action
Trospium	Trospium and Perphenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine	The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Perphenazine. Monitor for symptoms of ventricular arrhythmias. Additive anticholinergic and CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Fenfluramine	Decreased anorexic effect, may increase psychotic symptoms
Gatifloxacin	Increased risk of cardiotoxicity and arrhythmias
Phenmetrazine	Decreased anorexic effect, may increase psychotic symptoms
Rivastigmine	Possible antagonism of action
Cisapride	Increased risk of cardiotoxicity and arrhythmias
Diethylpropion	Decreased anorexic effect, may increase psychotic symptoms
Dexfenfluramine	Decreased anorexic effect, may increase psychotic symptoms

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Targets

D(2) dopamine receptor

D(1A) dopamine receptor

Enzymes