Prochlorperazine: Difference between revisions
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== Medical uses == |
== Medical uses == |
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Prochlorperazine is used to [[antiemetic|prevent vomiting]] caused by [[chemotherapy]], [[radiation therapy]] and [[Postoperative nausea and vomiting|in the pre- and postoperative setting]].<ref name=Lin2016>{{cite journal|last1=Lau Moon Lin|first1=M|last2=Robinson|first2=PD|last3=Flank|first3=J|last4=Sung|first4=L|last5=Dupuis|first5=LL|title=The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis.|journal=Drug safety|date=June 2016|volume=39|issue=6|pages=509-16|doi=10.1007/s40264-016-0398-9|pmid=26884326}}</ref> |
Prochlorperazine is used to [[antiemetic|prevent vomiting]] caused by [[chemotherapy]], [[radiation therapy]] and [[Postoperative nausea and vomiting|in the pre- and postoperative setting]].<ref name=Lin2016>{{cite journal|last1=Lau Moon Lin|first1=M|last2=Robinson|first2=PD|last3=Flank|first3=J|last4=Sung|first4=L|last5=Dupuis|first5=LL|title=The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis.|journal=Drug safety|date=June 2016|volume=39|issue=6|pages=509-16|doi=10.1007/s40264-016-0398-9|pmid=26884326}}</ref> A 2015 Cochrane review found no differences in efficacy among drugs commonly used for this purpose in emergency rooms.<ref>{{cite journal|last1=Furyk|first1=JS|last2=Meek|first2=RA|last3=Egerton-Warburton|first3=D|title=Drugs for the treatment of nausea and vomiting in adults in the emergency department setting.|journal=The Cochrane database of systematic reviews|date=28 September 2015|issue=9|pages=CD010106|doi=10.1002/14651858.CD010106.pub2|pmid=26411330}}</ref> |
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IV prochlorperazine is also used to treat migraine in emergency rooms, and is recommended for this use by the The American Headache Society.<ref name=AHS2016>{{cite journal|last1=Orr|first1=SL|last2=Friedman|first2=BW|last3=Christie|first3=S|last4=Minen|first4=MT|last5=Bamford|first5=C|last6=Kelley|first6=NE|last7=Tepper|first7=D|title=Management of Adults With Acute Migraine in the Emergency Department: The American Headache Society Evidence Assessment of Parenteral Pharmacotherapies.|journal=Headache|date=June 2016|volume=56|issue=6|pages=911-40|doi=10.1111/head.12835|pmid=27300483}}</ref> |
IV prochlorperazine is also used to treat migraine in emergency rooms, and is recommended for this use by the The American Headache Society.<ref name=AHS2016>{{cite journal|last1=Orr|first1=SL|last2=Friedman|first2=BW|last3=Christie|first3=S|last4=Minen|first4=MT|last5=Bamford|first5=C|last6=Kelley|first6=NE|last7=Tepper|first7=D|title=Management of Adults With Acute Migraine in the Emergency Department: The American Headache Society Evidence Assessment of Parenteral Pharmacotherapies.|journal=Headache|date=June 2016|volume=56|issue=6|pages=911-40|doi=10.1111/head.12835|pmid=27300483}}</ref> |
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Revision as of 21:55, 18 September 2017
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| Clinical data | |
|---|---|
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682116 |
| Pregnancy category | |
| Routes of administration | Oral, buccal, rectal, IM, IV |
| ATC code | |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | Unknown, but presumed substantial |
| Protein binding | 91–99% |
| 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 |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.000.345 |
| Chemical and physical data | |
| Formula | C20H24ClN3S |
| Molar mass | 373.943 g/mol g·mol−1 |
| 3D model (JSmol) | |
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| (verify) | |
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.
Medical uses
Prochlorperazine is used to prevent vomiting caused by chemotherapy, radiation therapy and in the pre- and postoperative setting.[2] A 2015 Cochrane review found no differences in efficacy among drugs commonly used for this purpose in emergency rooms.[3]
IV prochlorperazine is also used to treat migraine in emergency rooms, and is recommended for this use by the The American Headache Society.[4]
To alleviate the symptoms of vertigo[5]
In the UK, prochlorperazine maleate is available as Buccastem M in buccal form as an over-the-counter treatment for migraine.[6] In this indication it blocks the chemoreceptor trigger zone (CTZ) in the brain, which is responsible for causing severe nausea and vomiting. Its over the counter (OTC) use is strictly restricted to a maximum of 2 days, because of the potentially severe side effects of prochlorperazine, which mandate supervision by a health care provider.
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
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.[2]
Pharmacology
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).
Society and culture
Prochlorperazine is available as an oral liquid, tablets, cream for transdermal (compounding pharmacy), and suppositories, as well as in an injectable form. It is marketed under the trade names Buccastem, Compazine, Phenotil, Stemetil, and Stemzine.[citation needed]
Research
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.[11]
References
- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
- ^ 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.
- ^ 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.
- ^ Benson AJ (June 1969). "Effect of diphenidol and prochlorperazine on semicircular canal function in man". Aerospace Medicine. 40 (6): 589–95. PMID 4891872.
- ^ Siow HC, Young WB, Silberstein SD (April 2005). "Neuroleptics in headache". Headache. 45 (4): 358–71. doi:10.1111/j.1526-4610.2005.05074.x. PMID 15836574.
- ^ 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
- ^ 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
- 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.
{{cite episode}}: Unknown parameter|serieslink=ignored (|series-link=suggested) (help) The segment "Hands Up" relates an anecdote about the side effects of prochlorperazine.