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QuickView for Perphenazine (compound)

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
Name: Perphenazine
Name (isomeric): DB00850
Drug Type: small molecule
Description: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.
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...
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Category: Phenothiazines, Dopamine Antagonists, Antipsychotic Agents, Antipsychotics
CAS number: 58-39-9
Indication: For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults.
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...
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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...
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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
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:
GrepafloxacinIncreased risk of cardiotoxicity and arrhythmias
LevofloxacinIncreased risk of cardiotoxicity and arrhythmias
AmphetamineDecreased anorexic effect, may increase psychotic symptoms
MetrizamideIncreased risk of convulsions
TerbinafineTerbinafine 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.
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