Active ingredient: Prochlorperazine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Antiemetics
• Antipsychotics
• Phenothiazines

Dosage Forms

• Tablet
• Spansule
• Capsule
• Vial
• Suppository
• Syrup

Brands / Synonyms

Bayer A 173; Buccastem; Capazine; Chlormeprazine; Chlorperazine; Combid; Compazine; Compro; Emelent; Emetiral; Eskatrol; Kronocin; Meterazin; Meterazin Maleate; Meterazine; Nipodal; Novamin; Pasotomin; Prochloroperazine; Prochlorpemazine; Prochlorperazin; Prochlorperazine; Prochlorperazine edisylate; Prochlorperazine maleate; Prochlorpromazine; Procloperazine; Proclorperazine; Stemetil; Tementil; Temetid; Vertigon

Indications

For control of severe nausea and vomiting, also used in management of the manifestations of psychotic disorders.

Pharmacology

Prochlorperazine is a piperazine phenothiazine related to high-potency neuroleptics such as perphenazine. It shares many of the actions and adverse effects of the antipsychotics.

Mechanism of Action

Prochlorperazine blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. The antiemetic effects of prochlorperazine can be attributed to dopamine blockade in the chemoreceptor trigger zone. Prochlorperazine also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha(1)-adrenergic receptors resulting in sedation, muscle relaxation, and hypotension.

Absorption

Rapidly absorbed following oral administration

Toxicity

Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus; LD₅₀=400mg/kg (orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic. Undergoes metabolism in the gastric mucosa and on first pass through the liver, CYP2D6 and/or CYP3A4.

Contraindications

Do not use in comatose states or in the presence of large amounts of central nervous system depressants (alcohol, barbiturates, narcotics, etc.).

Do not use in pediatric surgery.

Do not use in children under 2 years of age or under 20 lb.

Do not use in children for conditions for which dosage has not been established.

Drug Interactions

Thiazide diuretics may accentuate the orthostatic hypotension that may occur with phenothiazines.

Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concomitantly.

Concomitant administration of propranolol with phenothiazines results in increased plasma levels of both drugs.

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