Prochlorperazine
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| Clinical data | |
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| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682116 |
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| Routes of administration |
Oral, buccal, rectal, IM, IV |
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| Pharmacokinetic data | |
| Bioavailability | Unknown, but presumed substantial |
| Protein binding | 91–99% |
| Metabolism | Mainly hepatic (CYP2D6 and/or CYP3A4) |
| Biological half-life | 4–8 hours, differs with the method of administration |
| Excretion | Biliary, (colored) inactive metabolites in urine |
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| ChEMBL | |
| ECHA InfoCard | 100.000.345 |
| Chemical and physical data | |
| Formula | C20H24ClN3S |
| Molar mass | 373.943 g/mol |
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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.
Contents
Medical uses[edit]
Prochlorperazine is used to prevent vomiting caused by chemotherapy, radiation therapy and in the pre- and postoperative setting.[1] A 2015 Cochrane review found no differences in efficacy among drugs commonly used for this purpose in emergency rooms.[2]
IV prochlorperazine is also used to treat migraine in acute outpatient settings,[3] and in emergency rooms, and is recommended for ER use by The American Headache Society.[4]
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.[5][6]
In the UK prochlorperazine maleate has been prescribed to alleviate the symptoms of labyrinthitis, which include not only nausea and vertigo, but spatial and temporal 'jerking' and distortion[7]
Side effects[edit]
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.[8][9]
Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome (NMS). Some symptoms of NMS include high fever, stiff muscles, 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.[1]
Pharmacology[edit]
Prochlorperazine is thought to exert its antipsychotic effects by blocking dopamine receptors.[10]
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).
Marketing[edit]
Prochlorperazine is available as tablets, suppositories, and in an injectable form.[11]
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.[11][12]
It was also marketed at that time as a combination drug for humans with paracetamol as Vestil-A, as a combination drug for veterinary use, with isopropamide as Darbazine.[11]
Research[edit]
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.[13]
References[edit]
- ^ a b 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.
- ^ Patniyot, IR; Gelfand, AA (January 2016). "Acute Treatment Therapies for Pediatric Migraine: A Qualitative Systematic Review". Headache. 56 (1): 49–70. doi:10.1111/head.12746. PMID 26790849.
- ^ Orr, SL; Friedman, BW; Christie, S; Minen, MT; Bamford, C; Kelley, NE; Tepper, D (June 2016). "Management of Adults With Acute Migraine in the Emergency Department: The American Headache Society Evidence Assessment of Parenteral Pharmacotherapies". Headache. 56 (6): 911–40. doi:10.1111/head.12835. PMID 27300483.
- ^ "Buccastem M - Summary of Product Characteristics (SPC) - (eMC)". UK Electronic Medicines Compendium. 16 February 2016. Retrieved 19 September 2017.
- ^ "Medicines information". NHS Choices. Retrieved 19 September 2017.
- ^ Coatesworth AP (November 2000). "Assessment and treatment of dizziness". Journal of Neurology, Neurosurgery, and Psychiatry. 69 (5): 706. doi:10.1136/jnnp.69.5.706. PMC 1763384
. PMID 11184241. - ^ Brown, Thomas Markham; Stoudemire, Alan (1998). "Antipsychotics". Psychiatric Side Effects of Prescription and Over-The-Counter Medications. American Psychiatric Publishing. p. 1946. ISBN 9780880488686.
- ^ Drugs.com
- ^ Manuchair S. Ebadi, Desk reference of clinical pharmacology. 2007
- ^ a b c "Prochlorperazine international brands". Drugs.com. Retrieved 19 September 2017.
- ^ https://www.rxlist.com/compazine-drug/patient-images-side-effects.htm
- ^ Chua, AL; Silberstein, S (September 2016). "Inhaled drug therapy development for the treatment of migraine". Expert opinion on pharmacotherapy. 17 (13): 1733–43. doi:10.1080/14656566.2016.1203901. PMID 27416108.
External links[edit]
- 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.
