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'{{Drugbox | verifiedrevid = 464214968 | IUPAC_name = 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-<BR>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 = [[Prescription drug|POM]], 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 = not exactly known, but substantial | protein_bound = 91–99% | metabolism = Mainly [[Liver|hepatic]] ([[CYP2D6]] and/or [[CYP3A4]]) | elimination_half-life = 4–8 hoursS, 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 }} '''Prochlorperazine''' ('''Compazine''', '''Stemzine''', '''Buccastem''', '''Stemetil''', '''Phenotil''') 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]].<ref>{{cite journal | vauthors = Husseini A, Gianakos D | date = February 2006 | title = The 15-Minute Visit | journal = Patient Care | volume = 40 | pages = 9–10}}</ref> Intravenous administration can be used to treat [[status migrainosus]]. == Indications == Prochlorperazine is a phenothiazine drug. Most drugs in this category are used as anti-psychotics (neuroleptics).<ref>{{cite journal | vauthors = Casey JF, Lasky JJ, Klett CJ, Hollister LE | title = Treatment of schizophrenic reactions with phenothiazine derivatives. A comparative study of chlorpromazine, triflupromazine, mepazine, prochlorperazine, perphenazine, and phenobarbital | journal = [[American Journal of Psychiatry]] | volume = 117 | issue = | pages = 97–105 | date = August 1960 | pmid = 13808146 | doi = 10.1176/appi.ajp.117.2.97 | doi_brokendate = 2015-01-09 }}</ref> Neuroleptic means "nerve seizing", and describes the semi-paralyzing effect these drugs have on the brain and nervous system. Stemetil is no longer being manufactured for sale in Canada as an anti-psychotic, but it is still available for treatment of nausea. It is now relatively seldom used for the treatment of [[psychosis]] and the [[mania|manic]] phase of [[bipolar disorder]]. It has a prominent [[antiemetic]]/[[antivertiginoic]] activity and is most often used for the (short-time) treatment of nausea and vomiting and [[vertigo]] as follows: # To alleviate the symptoms of [[vertigo]]<ref>{{cite journal | vauthors = Benson AJ | title = Effect of diphenidol and prochlorperazine on semicircular canal function in man | journal = Aerospace Medicine | volume = 40 | issue = 6 | pages = 589–95 | date = June 1969 | pmid = 4891872 }}</ref> # As an [[antiemetic]], particularly for nausea and vomiting caused by [[chemotherapy]], [[radiation therapy]] and [[Postoperative nausea and vomiting|in the pre- and postoperative setting]]<ref>{{cite journal | vauthors = Gralla RJ, Osoba D, Kris MG, Kirkbride P, Hesketh PJ, Chinnery LW, Clark-Snow R, Gill DP, Groshen S, Grunberg S, Koeller JM, Morrow GR, Perez EA, Silber JH, Pfister DG | title = Recommendations for the use of antiemetics: evidence-based, clinical practice guidelines | journal = Journal of Clinical Oncology | volume = 17 | issue = 9 | pages = 2971–94 | date = September 1999 | pmid = 10561376 | url = http://jco.ascopubs.org/cgi/content/full/17/9/2971 }}</ref> # In the UK, prochlorperazine maleate is available as Buccastem M in [[Cheek|buccal]] form as an over-the-counter treatment for migraine.<ref>{{cite journal | vauthors = Siow HC, Young WB, Silberstein SD | title = Neuroleptics in headache | journal = Headache | volume = 45 | issue = 4 | pages = 358–71 | date = April 2005 | pmid = 15836574 | doi = 10.1111/j.1526-4610.2005.05074.x }}</ref> 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 [[adverse drug reaction|side effect]]s 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<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> == 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. == Formulations and pharmacokinetics == [[File:Prochlorperazine 5mg.jpg|thumbnail|left|5mg oral tablet of Prochlorperazine]] Prochlorperazine is available as an oral liquid, tablets, cream for trans dermal (compounding pharmacy), and suppositories, as well as in an injectable form. 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). It is available in Egypt under the brand name '''Emedrotec''' buccal adhesive tablets by Eva pharma. There is an inhaled form of prochlorperazine under development by Alexza Pharmaceuticals, currently (November 2009 at the time of writing) in Phase II clinical trials.<ref> {{cite press release | title = Alexza Announces Agreement to Acquire Symphony Allegro, Including All Rights to AZ-004, AZ-104 and AZ-002 | publisher = Alexza Pharmaceuticals | date = 2009-06-15 | url = http://www.prnewswire.com/news-releases/alexza-announces-agreement-to-acquire-symphony-allegro-including-all-rights-to-az-004-az-104-and-az-002-62125847.html | accessdate = 2009-11-29 }}</ref> == Side effects == Nervous system side effects have been associated with the use of prochlorperazine. [[Extrapyramidal symptoms|Extrapyramidal side effects]] such as acute [[dystonicsuck my dick]] reactions, [[pseudoparkinsonism]], or [[akathisia]] can affect 2% of patients at low doses, whereas higher doses may affect as many as 40% of patients.<ref>{{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 = http://books.google.com/?id=K7kevbILCuQC | accessdate = 2013-01-18| 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, irregular heart rhythms (arrhythmias). VA and FDA research shows injection site reaction.suck my == 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://web.archive.org/web/20070928175950/http://www.leaddiscovery.co.uk/pr/Alexza_Initiates_AZ-001_Phase_IIb_Clinical_Trial_in_Patients_With_Migraine_Headaches.html AZ-001 (Staccato prochlorperazine)] ([http://www.leaddiscovery.co.uk/pr/Alexza_Initiates_AZ-001_Phase_IIb_Clinical_Trial_in_Patients_With_Migraine_Headaches.html original article]) Press release pertaining to phase IIb clinical trial of inhaled prochlorperazine for migraine headache * [http://www.drugs.com/pro/prochlorperazine.html Prochlorperazine edisylate Injection prescribing information] Drugs.com * [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}} {{Cholinergics}} {{Dopaminergics}} {{Histaminergics}} {{Piperazines}} {{Tricyclics}} [[Category:Antiemetics]] [[Category:Antimigraine drugs]] [[Category:Typical antipsychotics]] [[Category:Chloroarenes]] [[Category:GHB receptor ligands]] [[Category:Phenothiazines]] [[Category:Piperazines]]'