Perphenazine Tablets (Perphenazine) Drug Information: Clinical Pharmacology

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May 27, 2012

Perphenazine

Nausea and Vomiting »

Nausea and vomiting facts

Nausea and vomiting are symptoms of a disease or condition. The underlying cause of the illness causing nausea and vomiting should be identified and treated.
Nausea and vomiting symptom control is important both for comfort's sake and to prevent dehydration.
Dehydration can worsen nausea and vomiting.
Medication may be available to control symptoms of nausea and vomiting.

Introduction to nausea and vomiting

Nausea and vomiting are symptoms of an underlying illness and not a specific disease. Nausea is the sensation that the stomach wants to empty itself, while vomiting (emesis) or throwing up, is the act of forcible emptying of the stomach. The term "dry heaves" refers to an episode of vomiting where there is no food in the stomach to vomit, and only clear secretions are vomited.

Vomiting is a violent act in which the stomach almost...

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CLINICAL PHARMACOLOGY

Pharmacokinetics

Following oral administration of perphenazine (perphenazine) tablets, mean peak plasma perphenazine (perphenazine) concentrations were observed between 1 to 3 hours. The plasma elimination half-life of perphenazine (perphenazine) was independent of dose and ranged between 9 and 12 hours. In a study in which normal volunteers (n=12) received perphenazine (perphenazine) 4 mg q8h for 5 days, steady-state concentrations of perphenazine (perphenazine) were reached within 72 hours. Mean (%CV) Cmax and Cmin values for perphenazine and 7 hydroxyperphenazine (perphenazine) at steady-state are listed below:

Parameter	Perphenazine	7-Hydroxyperphenazine
Cmax (pg/mL)	984 (43)	509 (25)
Cmin (pg/mL)	442 (76)	350 (56)

Peak 7-hydroxyperphenazine (perphenazine) concentrations were observed between 2 to 4 hours with a terminal phase half-life ranging between 9.9 to 18.8 hours. Perphenazine (perphenazine) is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation. The pharmacokinetics of perphenazine (perphenazine) covary with the hydroxylation of debrisoquine which is mediated by cytochrome P450 2D6 (CYP 2D6) and thus is subject to genetic polymorphism – i.e., 7% to 10% of Caucasians and a low percentage of Asians have little or no activity and are called "poor metabolizers." Poor metabolizers of CYP 2D6 will metabolize perphenazine (perphenazine) more slowly and will experience higher concentrations compared with normal or "extensive" metabolizers.

Last reviewed on RxList: 10/21/2008
This monograph has been modified to include the generic and brand name in many instances.