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'{{Drugbox | Watchedfields = changed | verifiedrevid = 464214968 | IUPAC_name = 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-10''H''-phenothiazine | image = Prochlorperazine.svg | width = 250 <!--Clinical data--> | tradename = | Drugs.com = {{drugs.com|monograph|prochlorperazine}} | MedlinePlus = a682116 | pregnancy_category = C <small>([[Australia|Au]], [[United States|U.S.]])</small> | legal_AU = S3 | legal_US = Rx-only | legal_UK = POM | legal_UK_comment = but packs of 8 buccal tablets for nausea/vomiting associated with migraine are sold as [[pharmacy medicines]] | routes_of_administration = Oral, [[Cheek|buccal]], [[Suppository|rectal]], [[Intramuscular injection|IM]], [[Intravenous injection|IV]] <!--Pharmacokinetic data--> | bioavailability = Unknown, but presumed substantial | protein_bound = 91–99% | metabolism = Mainly [[Liver|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--> | IUPHAR_ligand = 7279 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 58-38-8 | ATC_prefix = N05 | ATC_suffix = AB04 | PubChem = 4917 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00433 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4748 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = YHP6YLT61T | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D00493 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 8435 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 728 <!--Chemical data--> | C=20 | H=24 | Cl=1 | N=3 | S=1 | molecular_weight = 373.943 g/mol | SMILES = Clc2cc1N(c3c(Sc1cc2)cccc3)CCCN4CCN(C)CC4 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C20H24ClN3S/c1-22-11-13-23(14-12-22)9-4-10-24-17-5-2-3-6-19(17)25-20-8-7-16(21)15-18(20)24/h2-3,5-8,15H,4,9-14H2,1H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = WIKYUJGCLQQFNW-UHFFFAOYSA-N |drug_name=|alt=|caption=|type=|legal_status=|licence_EU=|pregnancy_AU=|pregnancy_US=|licence_US=}} '''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 (medical)|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 [[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> IV prochlorperazine is also used to treat migraine in acute outpatient settings,<ref>{{cite journal|last1=Patniyot|first1=IR|last2=Gelfand|first2=AA|title=Acute Treatment Therapies for Pediatric Migraine: A Qualitative Systematic Review.|journal=Headache|date=January 2016|volume=56|issue=1|pages=49–70|doi=10.1111/head.12746|pmid=26790849}}</ref> and in emergency rooms, and is recommended for ER use by 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> In the UK, prochlorperazine is available for the treatment of nausea caused by migraine as a [[Buccal administration|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]].<ref>{{cite web|title=Buccastem M - Summary of Product Characteristics (SPC) - (eMC)|url=https://www.medicines.org.uk/emc/medicine/22797|publisher=UK Electronic Medicines Compendium|accessdate=19 September 2017|language=en|date=16 February 2016}}</ref><ref>{{cite web|title=Medicines information|url=http://www.nhs.uk/conditions/Medicinesinfo/Pages/Introduction.aspx|publisher=NHS Choices|accessdate=19 September 2017|language=en}}</ref> 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<ref>{{cite journal | vauthors = Coatesworth AP | title = Assessment and treatment of dizziness | journal = Journal of Neurology, Neurosurgery, and Psychiatry | volume = 69 | issue = 5 | pages = 706 | date = November 2000 | pmid = 11184241 | pmc = 1763384 | doi = 10.1136/jnnp.69.5.706 }}</ref> == Side effects == Sedation is very common, and [[Extrapyramidal symptoms|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.<ref name=Brown1998>{{cite book | last1 = Brown | first1 = Thomas Markham | last2 = Stoudemire | first2 = Alan | title = Psychiatric Side Effects of Prescription and Over-The-Counter Medications | chapter = Antipsychotics | publisher = American Psychiatric Publishing | year = 1998 | pages = 1946 | url = https://books.google.com/books?id=K7kevbILCuQC&pg=PA1946| isbn = 9780880488686 }}</ref><ref>[http://www.drugs.com/sfx/procot-side-effects.html Drugs.com]</ref> 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.<ref name=Lin2016/> == Pharmacology == Prochlorperazine is thought to exert its [[antipsychotic]] effects by blocking [[dopamine receptor]]s.<ref>Manuchair S. Ebadi, Desk reference of clinical pharmacology. 2007</ref> Prochlorperazine is analogous to [[chlorpromazine]], both of these agents antagonize dopaminergic [[dopamine receptor D2|D₂ receptor]]s 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 antagonist]]s 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 tablets, suppositories, and in an injectable form.<ref name=brands/> As of September 2017 it was marketed under the trade names Ametil, Antinaus, Antinaus, Buccastem, Bukatel, Chlormeprazine, Chloropernazine, 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, Stemetil, Stemetil, Steremal, Vergon, Vestil, and Volimin.<ref name=brands>{{cite web|title=Prochlorperazine international brands|url=https://www.drugs.com/international/prochlorperazine.html|publisher=Drugs.com|accessdate=19 September 2017}}</ref> 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.<ref name=brands/> ==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.<ref>{{cite journal|last1=Chua|first1=AL|last2=Silberstein|first2=S|title=Inhaled drug therapy development for the treatment of migraine.|journal=Expert opinion on pharmacotherapy|date=September 2016|volume=17|issue=13|pages=1733–43|doi=10.1080/14656566.2016.1203901|pmid=27416108}}</ref> == References == {{Reflist|2}} == External links == * [http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682116.html Prochlorperazine]. MedlinePlus. [[United States National Library of Medicine|U.S. National Library of Medicine]]. [[National Institutes of Health]]. * [http://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+58-38-8 Prochlorperazine]. [[Hazardous Substances Data Bank]] (HSDB). [[United States National Library of Medicine|U.S. National Library of Medicine]]. [[National Institutes of Health]]. * {{Cite episode |title=Suspicious Behavior |url=http://snapjudgment.org/Suspicious-Behavior |accessdate=May 19, 2014 |series=Snap Judgment |serieslink=Snap Judgment (radio show) |network=[[Public Radio Exchange]] and [[NPR]] |date= |number=405}} The segment "Hands Up" relates an anecdote about the side effects of prochlorperazine. {{Antipsychotics}} {{Navboxes | title = [[Pharmacodynamics]] | titlestyle = background:#ccccff | list1 = {{Adrenergic receptor modulators}} {{Dopamine receptor modulators}} {{GHB receptor modulators}} {{Histamine receptor modulators}} {{Serotonin receptor modulators}} }} {{Tricyclics}} [[Category:Antiemetics]] [[Category:Antimigraine drugs]] [[Category:Typical antipsychotics]] [[Category:Chloroarenes]] [[Category:GHB receptor ligands]] [[Category:Hepatotoxins]] [[Category:Phenothiazines]] [[Category:Piperazines]]'