|Oral, buccal, rectal, IM, IV|
|Bioavailability||Unknown, but presumed substantial|
|Metabolism||Mainly hepatic (CYP2D6 and/or CYP3A4)|
|Elimination half-life||4–8 hours, differs with the method of administration|
|Excretion||Biliary, (colored) inactive metabolites in urine|
|Chemical and physical data|
|Molar mass||373.943 g/mol|
|3D model (JSmol)|
Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly potent typical antipsychotic, 10–20 times more potent than chlorpromazine. It is also used to treat migraine headaches. Intravenous administration can be used to treat status migrainosus.
Prochlorperazine (Compazine) is used to prevent vomiting caused by chemotherapy, radiation therapy and in the pre- and postoperative setting. A 2015 Cochrane review found no differences in efficacy among drugs commonly used for this purpose in emergency rooms.
In the UK, prochlorperazine is available for the treatment of nausea caused by migraine as a tablet dissolved in the mouth; it is sold as a "pharmacy medicine", meaning it does not require a prescription but is only available after talking with a pharmacist.
Sedation is very common, and extrapyramidal side effects are common and include restlessness, dystonic reactions, pseudoparkinsonism, and akathisia; the extrapyramidal symptoms can affect 2% of people at low doses, whereas higher doses may affect as many as 40% of people.
Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome (NMS). Some symptoms of NMS include high fever, stiff muscles, neck muscle spasm,confusion, irregular pulse or blood pressure, fast heart rate (tachycardia), sweating, abnormal heart rhythms (arrhythmias). VA and FDA research show injection site reactions.
Adverse effects are similar in children.
Prochlorperazine is analogous to chlorpromazine, both of these agents antagonize dopaminergic D2 receptors in various pathways of the central nervous system. This D2 blockade results in antipsychotic, antiemetic and other effects. Hyperprolactinaemia is a side effect of dopamine antagonists as blockade of D2 receptors within the tuberoinfundibular pathway results in increased plasma levels of prolactin due to increased secretion by lactotrophs in the anterior pituitary.
Following intramuscular injection, the antiemetic action is evident within 5 to 10 minutes and lasts for 3 to 4 hours. Rapid action is also noted after buccal treatment. With oral dosing, the start of action is delayed but the duration somewhat longer (approximately 6 hours).
Prochlorperazine is available as tablets, suppositories, and in an injectable form.
As of September 2017 it was marketed under the trade names Ametil, Antinaus, Antinaus, Buccastem, Bukatel, Chlormeprazine, Chloropernazine, Compazine, Compro, Daolin, Dhaperazine, Emedrotec, Emetiral, Eminorm, Lotamin, Mitil, Mormal, Nautisol, Novamin, Novomit, Proazine, Procalm, Prochlorperazin, Prochlorperazine, Prochlorpérazine, Prochlorperazinum, Prochlozine, Proclorperazina, Promat, Promin, Promtil, Roumin, Scripto-metic, Seratil, Stemetil, Steremal, Vergon, Vestil, and Volimin.
Alexza Pharmaceuticals studied an inhaled form of prochlorperazine for the treatment of migraine through Phase II trials under the development name AT-001; development was discontinued in 2011.
- Lau Moon Lin, M; Robinson, PD; Flank, J; Sung, L; Dupuis, LL (June 2016). "The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis". Drug safety. 39 (6): 509–16. doi:10.1007/s40264-016-0398-9. PMID 26884326.
- Furyk, JS; Meek, RA; Egerton-Warburton, D (28 September 2015). "Drugs for the treatment of nausea and vomiting in adults in the emergency department setting". The Cochrane Database of Systematic Reviews (9): CD010106. doi:10.1002/14651858.CD010106.pub2. PMID 26411330.
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- Manuchair S. Ebadi, Desk reference of clinical pharmacology. 2007
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- Prochlorperazine. MedlinePlus. U.S. National Library of Medicine. National Institutes of Health.
- Prochlorperazine. Hazardous Substances Data Bank (HSDB). U.S. National Library of Medicine. National Institutes of Health.
- "Suspicious Behavior". Snap Judgment. Episode 405. Public Radio Exchange and NPR. Retrieved May 19, 2014. The segment "Hands Up" relates an anecdote about the side effects of prochlorperazine.