Ethaperazine

Ethaperazine Uses, Dosage, Side Effects, Food Interaction and all others data.

An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine.

Ethaperazine 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. Ethaperazine 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.

Table Of contents

• Ethaperazine
• Uses
• Dosage
• Side Effect
• Precautions
• Interactions
• Uses during Pregnancy
• Uses during Breastfeeding
• Accute Overdose
• Food Interaction
• Half Life
• Volume of Distribution
• Clearance
• Interaction With other Medicine
• Contradiction
• Storage

Trade Name	Ethaperazine
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

Ethaperazine 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.

Ethaperazine 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 Ethaperazine 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. Ethaperazine 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. Ethaperazine may increase the effects of alcohol.

Ethaperazine 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.

Ethaperazine 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

Ethaperazine 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

Ethaperazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.

Innovators Monograph

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