Prochlorperazine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Cyprus: Stemetil; Denmark: Stemetil; Finland: Stemetil; Ireland: Buccastem, Prochlorperazine, Stemetil; Italy: Stemetil; Poland: Chloropernazinum; Romania: Emetiral, Proclorperezina; Sweden: Stemetil; UK: Buccastem, Prochlorperazine, Stemetil.

North America

Canada: Prochlor, Prochlorperazine; USA: Compro, Prochlorperazine.

Asia

Japan: Novamin.

Drug combinations

Chemistry

Prochlorperazine Edisylate: C~20~H~24~ClN~3~S C~2~H~6~O~6~S~2~. Mw: 564.14. (1) 10H-Phenothiazine, 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-, 1,2-ethanedisulfonate (1:1); (2) 2-Chloro-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazine 1,2-ethanedisulfonate (1:1). CAS-1257-78-9; CAS-58-38-8 (prochlorperazine).

Prochlorperazine Maleate: C~20~H~24~ClN~3~S 2C~4~H~4~O~4~. Mw: 606.09. 10H-Phenothiazine, 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-, (Z)-2-butenedioate (1:2). CAS-84-02-6.

Pharmacologic Category

Antiemetics; Antihistamines. Antipsychotics; Phenothiazines. (ATC-Code: N05AB04).

Mechanism of action

Blocks postsynaptic mesolimbic dopaminergic D~1~ and D~2~ receptors in brain, including chemoreceptor trigger zone. Exhibits strong α-adrenergic- and anticholinergic-blocking effect and depresses release of hypothalamic and hypophyseal hormones. Believed to depress reticular activating system, thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone and emesis.

Therapeutic use

Management of nausea and vomiting. Psychotic disorders including schizophrenia. Anxiety.

Pregnancy and lactiation implications

Crosses placenta. Jaundice, extrapyramidal signs, hyper-/hyporeflexes noted in newborns. Available evidence with use of occasional low doses suggests safe use during pregnancy. Excretion of prochlorperazine not known.

Unlabeled use

Behavioral syndromes in dementia. Psychosis/agitation related to Alzheimer’s dementia.

Contraindications

Hypersensitivity to prochlorperazine or any component of the formulation (cross-reactivity between phenothiazines may occur). Severe CNS depression. Coma. Pediatric surgery. Reye’s syndrome. Should not be used in children <2 years of age or <9 kg.

Warnings and precautions

May alter cardiac conduction (life-threatening arrhythmias occurred with therapeutic doses of phenothiazines). May cause anticholinergic effects (use with caution in decreased GI motility, paralytic ileus, urinary retention, benign prostatic hypertrophy, xerostomia, or visual problems). Antipsychotic use associated with esophageal dysmotility and aspiration (use with caution in risk of pneumonia). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Risk of dystonia (and possibly other extrapyramidal symptoms) may be greater with increased doses, use of conventional antipsychotics, males, and younger patients. Hypotension may occur following administration, particularly when parenteral form used, or high dosages. May be associated with neuroleptic malignant syndrome (risk may be increased in Parkinson’s disease or Lewy body dementia). May cause orthostatic hypotension (use with caution in cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). May be associated with pigmentary retinopathy. May cause sedation. Impaired core body temperature regulation may occur. Use with caution in bone marrow suppression (blood dyscrasias occurred), and in severe cardiovascular disease. Prochlorperazine not approved for dementia-related psychosis (increased incidence of cerebrovascular adverse events, including fatalities). Use with caution in narrow-angle glaucoma (may be exacerbated by cholinergic blockade), in hepatic impairment, in myasthenia gravis (may be exacerbated by cholinergic blockade), and in Parkinson’s disease (may be more sensitive to adverse effects). Use with caution in breast cancer or other prolactin-dependent tumors (elevates prolactin levels), in renal impairment, in respiratory disease, and in risk of seizures, including patients with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects. Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in the elderly (increased risk for developing tardive dyskinesia). Children with acute illness or dehydration are more susceptible to neuromuscular reactions (e.g. dystonias).

Information

Legal

Legal Notice
Privacy Policy
Cookie Policy

Contact

Phone: +34-981-780505
Email: genomicmedicine@wagem.org
Location: Sta Marta de, C. P. Babío, S/N, 15165 Bergondo, A Coruña

Copyright © 2023 WAGEM

Add to cart