APO-PERPHENAZINE TABLET 4mg

Perphenazine

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

2-(4-[3-(2-chloro-10H-Phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol | 2-chloro-10-(3-(4-(2-Hydroxyethyl)piperazin-1-yl)propyl)phenothiazine | 4-[3-(2-chloro-10H-Phenothiazin-10-yl)propyl]-1-piperazineethanol | 4-[3-(2-Chlorophenothiazin-10-yl)propyl]-1-piperazineethanol | Chlorpiprazine | Etaperazin | Etaperazine | Ethaperazine | gamma-(4-(beta-Hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine | Perfenazina | Perfenazine | Perphenazin | Perphénazine | Perphenazinum | Perphenazine |

Description

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.

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.

Pharmacodynamics

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.

Pharmacokinetics

Absorption:

Absolute bioavailability is 40% following oral administration.

Distribution:

Not Available

Metabolism:

Hepatic.

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.

Clearance

Not Available

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)

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

APO-PERPHENAZINE TABLET 4mg was registered with Health Science Authority of Singapore by PHARMAFORTE SINGAPORE PTE LTD. It is marketed with the registration number of SIN00444P with effective from 1988-04-27.

This product contains 4mg of Perphenazine in the form of TABLET, FILM-COATED.

The medicine was manufactured by APOTEX INC in CANADA

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N05AB03

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44APO-DIAZEPAM TABLET 5mgDiazepamPOMPHARMAFORTE SINGAPORE PTE LTDActive
45APO-DIAZEPAM TABLET 10mgDiazepamPOMPHARMAFORTE SINGAPORE PTE LTDActive
46APO-PROPRANOLOL TABLET 10mgPropranololPOMPHARMAFORTE SINGAPORE PTE LTDActive
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Products Containing as Mixture Ingredient

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400FAKTU SUPPOSITORYCinchocaine|PolicresulenP OnlyTAKEDA PHARMACEUTICALS (ASIA PACIFIC) PTE LTDActive
407TRIMAXAZOLE TABLETSulfamethoxazole|TrimethoprimPOMBEACONS PHARMACEUTICALS PTE LTDActive
435APO-SULFATRIM TABLETSulfamethoxazole|TrimethoprimPOMPHARMAFORTE SINGAPORE PTE LTDActive
508APO-SULFATRIM PEDIATRIC TABLETSulfamethoxazole|TrimethoprimPOMPHARMAFORTE SINGAPORE PTE LTDActive
526B.S. SUSPENSIONSulfamethoxazole|TrimethoprimPOMAPEX PHARMA MARKETING PTE LTDActive
583CO-TRIMEXAZOLE SUSPENSIONSulfamethoxazole|TrimethoprimPOMBEACONS PHARMACEUTICALS PTE LTDActive
676BANEOCIN OINTMENTBacitracin|NeomycinPOMNOVARTIS (SINGAPORE) PTE LTDActive
678BANEOCIN POWDERBacitracin|NeomycinPOMNOVARTIS (SINGAPORE) PTE LTDActive