Prochlorperazine
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2008-07-12T15:03:04Z
WikiDreamer Bot
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robot Adding: [[pl:Prochlorperazyna]]
{{Unreferenced|date=December 2007}}
{{drugbox |
| IUPAC_name = 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-<BR>10''H''-phenothiazine
| image = Prochlorperazine.svg
| CAS_number = 58-38-8
| ATC_prefix = N05
| ATC_suffix = AB04
| PubChem = 4917
| DrugBank = APRD00624
| C = 20 |H = 24 |Cl = 1 |N = 3 |S = 1
| molecular_weight = 373.943 [[Gram|g]]/[[Mole (unit)|mol]]
| bioavailability = not exactly known, but substantial
| protein_bound = 91–99%
| metabolism = Mainly [[Liver|hepatic]] ([[CYP2D6]] and/or [[CYP3A4]])
| elimination_half-life = 4-8 hours, differs with the mode of application
| excretion = Biliary, (colored) inactive metabolites in urine
| pregnancy_category = C <small>([[Australia|Au]], [[United States|U.S.]])</small>
| legal_status = OTC/[[Prescription drug|POM]] <small>([[United Kingdom|UK]])</small>
| routes_of_administration = Oral, [[buccal]], [[Suppository|rectal]], [[Intramuscular injection|IM]]
}}
'''Prochlorperazine''' (marketed under the names '''Compazine''', '''Buccastem''', '''Stemetil''' and '''Phenotil''') is a drug that belongs to the [[phenothiazine]] class of antipsychotic agents that are used for the treatment of [[nausea]] and [[vertigo (medical)|vertigo]]. It is also a [[typical antipsychotic]] drug and a highly potent [[neuroleptic]], 10 to 20 times more potent than [[chlorpromazine]].
==Indications==
It is now relatively seldom used for the treatment of [[psychosis]] and the [[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 (medical)|vertigo]] as follows:
# To alleviate the symptoms of vertigo
# As an [[antiemetic]], particularly for nausea and vomiting caused by [[cancer treatment]], [[radiation]] and [[Postoperative nausea and vomiting|in the pre- and postoperative setting]]
# Quite recently, in the UK prochlorperazine maleate has been made available as Buccastem M in [[buccal]] form as an over-the-counter treatment for migraine. In this indication it blocks the [[chemoreceptor trigger zone]] (CTZ) in the brain, which is responsible for causing severe nausea and vomiting. Its 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.
==Formulations and pharmacokinetics==
Prochlorperazine is available as an oral liquid, tablets, 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).
There is an inhaled form of prochlorperazine under development by Alexza Pharmaceuticals, currently in Phase II clinical trials.
==Side effects==
{{see|Typical antipsychotic}}
Due to the short duration of treatment it is usually well tolerated. It shares in general all side effects of [[chlorpromazine]], but these are seen less frequently so and are less disturbing to the patient, particularly as most patients with the aforementioned conditions are hospitalized. In the treatment of nausea/emesis it might be given together with an antiparkinsonian drug to prevent [[extrapyramidal side effects]] of prochlorperazine.
Some individuals are inherently allergic to this medicine. This medicine is known to produce [[seizures]] and seizure-like symptoms in individuals who might not have had prior seizures. In such cases, contact health-care facilities for immediate attention. Long-term delays might lead to long-term effects. In extreme cases, it has been known to produce permanent damage to the lower jaw and the jaw joint due to extended seizure symptoms. A common, over-the-counter remedy for side-effects is [[Diphenhydramine]].
If treating psychotic conditions on a long-term basis, the high incidence of early and late ([[tardive dyskinesia]]) extrapyramidal side effects should be considered carefully. Prochlorperazine has in the long-term treatment approximately the same incidence and severity of extrapyramidal side effects as [[haloperidol]].
==External links==
*[http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a682116.html Prochlorperazine] medlineplus.org article
*[http://www.leaddiscovery.co.uk/pr/Alexza_Initiates_AZ-001_Phase_IIb_Clinical_Trial_in_Patients_With_Migraine_Headaches.html AZ-001 (Staccato(TM) prochlorperazine)] Press release pertaining to phase IIb clinical trial of inhaled prochlorperazine for migraine headache
{{Antipsychotics}}
[[Category:Typical antipsychotics]]
[[Category:Antiemetics]]
[[Category:Phenothiazines]]
[[pl:Prochlorperazyna]]
[[ru:Прохлорперазин]]
[[sv:Proklorperazin]]