Perphenan
Perphenan Uses, Dosage, Side Effects, Food Interaction and all others data.
An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine.
Perphenan 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. Perphenan 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.
Trade Name | Perphenan |
Availability | Prescription only |
Generic | Perphenazine |
Perphenazine Other Names | Chlorpiprazine, Etaperazin, Etaperazine, Ethaperazine, Perfenazina, Perfenazine, Perphenazin, Perphénazine, Perphenazine, Perphenazinum |
Related Drugs | hydroxyzine, lorazepam, ondansetron, Zofran, meclizine, promethazine, haloperidol, prochlorperazine, Haldol, Compazine |
Type | |
Formula | C21H26ClN3OS |
Weight | Average: 403.969 Monoisotopic: 403.148510866 |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Perphenan is a phenothiazine used to treat schizophrenia as well as nausea and vomiting.
For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults.
Perphenan is also used to associated treatment for these conditions: Anxiety, Depression, Schizophrenia, Moderate Agitation, Moderate Anxiety, Moderate Depressed mood, Severe Anxiety, Severe Depressed mood, Severe Nausea and vomiting, Severe agitation
How Perphenan works
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. Perphenan 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.
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)
Food Interaction
- Avoid alcohol. Consuming alcohol may increase hypotension. Perphenan may increase the effects of alcohol.
Perphenan Alcohol interaction
[Moderate] GENERALLY AVOID:
Concurrent use of ethanol and phenothiazines may result in additive CNS depression and psychomotor impairment.
Also, ethanol may precipitate dystonic reactions in patients who are taking phenothiazines.
The two drugs probably act on different sites in the brain, although the exact mechanism of the interaction is not known.
Patients should be advised to avoid alcohol during phenothiazine therapy.
Perphenan Drug Interaction
Major: ziprasidone, escitalopram, topiramateModerate: aripiprazole, amphetamine / dextroamphetamine, lorazepam, duloxetine, divalproex sodium, clonazepam, lamotrigine, lurasidone, lithium, fluoxetine, mirtazapine, quetiapine, alprazolam, sertralineUnknown: omega-3 polyunsaturated fatty acids, levothyroxine, cholecalciferol
Perphenan Disease Interaction
Major: dementia, liver damage, acute alcohol intoxication, cardiovascular disease, CNS depression, head injuryModerate: anticholinergic effects, breast cancer, dystonic reactions, hematologic toxicity, NMS, parkinsonism, renal dysfunction, respiratory disorders, seizure disorders, tardive dyskinesia
Elimination Route
Absolute bioavailability is 40% following oral administration.
Half Life
8-12 hours, but ranges up to 20 hours.
Elimination Route
Perphenan is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.
Innovators Monograph
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