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Prochlorperazine: Difference between revisions
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{{SubstanceBox/Prochlorperazine}} | {{SubstanceBox/Prochlorperazine}} | ||
'''Prochlorperazine''' ('''Compazine''', '''Stemzine''', '''Buccastem M''', '''Stemetil''', '''Phenotil''') is a [[dopamine|dopaminergic]] D2 [[receptor]] [[antagonist]] that belongs to the [[phenothiazine]] class of [[antipsychotic]] agents that are used for the treatment of nausea and vertigo. It is also a highly potent typical antipsychotic and is 10–20× more potent than chlorpromazine. It is also used to treat migraine headaches.<ref>Husseini, A; Gianakos, D (February 2006). "The 15-Minute Visit". Patient Care 40: 9–10.</ref> | '''Prochlorperazine''' ('''Compazine''', '''Stemzine''', '''Buccastem M''', '''Stemetil''', '''Phenotil''') is a [[dopamine|dopaminergic]] D2 [[receptor]] [[antagonist]] that belongs to the [[chemical class::phenothiazine]] class of [[psychoactive class::antipsychotic]] agents that are used for the treatment of nausea and vertigo. It is also a highly potent typical antipsychotic and is 10–20× more potent than chlorpromazine. It is also used to treat migraine headaches.<ref>Husseini, A; Gianakos, D (February 2006). "The 15-Minute Visit". Patient Care 40: 9–10.</ref> | ||
==Chemistry== | ==Chemistry== | ||
Prochlorperazine is a piperazine derivative of the phenothiazine class of organic compounds. Prochlorperazine contains a thiazine ring, a six-member ring which includes one nitrogen and one sulfur atom. The thiazine ring is fused to two benzene rings, creating a tricyclic phenothiazine. Prochlorperazine contains a chlorine atom bound to R<sub>2</sub> of the phenothiazine group. | Prochlorperazine is a piperazine derivative of the phenothiazine class of organic compounds. Prochlorperazine contains a thiazine ring, a six-member ring which includes one nitrogen and one sulfur atom. The thiazine ring is fused to two benzene rings, creating a tricyclic phenothiazine. Prochlorperazine contains a chlorine atom bound to R<sub>2</sub> of the phenothiazine group. | ||
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==Pharmacology== | ==Pharmacology== | ||
[[File:Prochlorperazine 5mg.jpg|thumbnail|200px|5mg oral tablet of Prochlorperazine]] | [[File:Prochlorperazine 5mg.jpg|thumbnail|200px|5mg oral tablet of Prochlorperazine]] | ||
Prochlorperazine is thought to exert its [[antipsychotic]] effects by blocking [[dopamine]] receptors.<ref> | Prochlorperazine is thought to exert its [[antipsychotic]] effects by blocking [[dopamine]] receptors.<ref>{{cite book | vauthors=((Ebadi, M.)) | date=31 October 2007 | title=Desk Reference of Clinical Pharmacology | publisher=CRC Press | isbn=9781420047448}}</ref> | ||
Prochlorperazine is analogous to [[chlorpromazine]]; both of these agents [[antagonist|antagonize]] [[dopamine|dopaminergic]] D2 receptors in various pathways of the central nervous system. This D2 blockade results in antipsychotic, antiemetic and other effects. | Prochlorperazine is analogous to [[chlorpromazine]]; both of these agents [[antagonist|antagonize]] [[dopamine|dopaminergic]] D2 receptors in various pathways of the central nervous system. This D2 blockade results in antipsychotic, antiemetic and other effects. | ||
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==Toxicity and harm potential== | ==Toxicity and harm potential== | ||
Nervous system side effects have been associated with the use of prochlorperazine. [http://en.wikipedia.org/wiki/Extrapyramidal_symptoms Extrapyramidal side effects] such as acute [http://en.wikipedia.org/wiki/Dystonia dystonic] reactions, [http://en.wikipedia.org/wiki/Parkinsonism pseudoparkinsonism] (not to be confused with Parkinson's disease), or akathisia can affect 2% of patients at low doses, whereas higher doses may affect as many as 40% of patients.<ref>Psychiatric Side Effects of Prescription and Over-the-counter Medications | | Nervous system side effects have been associated with the use of prochlorperazine. [http://en.wikipedia.org/wiki/Extrapyramidal_symptoms Extrapyramidal side effects] such as acute [http://en.wikipedia.org/wiki/Dystonia dystonic] reactions, [http://en.wikipedia.org/wiki/Parkinsonism pseudoparkinsonism] (not to be confused with Parkinson's disease), or akathisia can affect 2% of patients at low doses, whereas higher doses may affect as many as 40% of patients.<ref>{{cite book | vauthors=((Brown, T. M.)), ((Stoudemire, A.)) | date= 1998 | title=Psychiatric Side Effects of Prescription and Over-the-counter Medications: Recognition and Management | publisher=American Psychiatric Pub | isbn=9780880488686}}</ref><ref>http://www.drugs.com/sfx/procot-side-effects.html</ref> | ||
Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome (NMS). Some symptoms of NMS include a high fever, stiff muscles, confusion, irregular pulse or blood pressure, a fast heart rate (tachycardia), sweating, or irregular heart rhythms (arrhythmias). | Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome (NMS). Some symptoms of NMS include a high fever, stiff muscles, confusion, irregular pulse or blood pressure, a fast heart rate (tachycardia), sweating, or irregular heart rhythms (arrhythmias). | ||
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As with other antipsychotics, dependence can be present with long-term use and is both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage. | As with other antipsychotics, dependence can be present with long-term use and is both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage. | ||
==Legal | ==Legal status== | ||
[[File:Buccastem M (Prochlorperazine maleate 3 mg) Buccal tablets.jpg|250px|thumbnail|right|An 8-pack of Buccastem M, the brand name for OTC prochlorperazine maleate in the UK.]] | [[File:Buccastem M (Prochlorperazine maleate 3 mg) Buccal tablets.jpg|250px|thumbnail|right|An 8-pack of Buccastem M, the brand name for OTC prochlorperazine maleate in the UK.]] | ||
*'''Australia | *'''Australia''': The substance is Schedule 3, meaning it is available with the advice of a pharmacist without a prescription.{{citation needed}} | ||
*''' | *'''United Kingdom''': The drug is available over the counter as a pharmacy medicine and as a prescription medication. The OTC brand is Buccastem M, a [[Routes of Administration#Buccal|buccal]] delivery system of prochlorperazine for motion sickness or nausea.<ref>Package leaflet: Information for the user. Buccastem® M Buccal Tablets (PROCHLORPERAZINE MALEATE 3 MG, EQUIVALENT TO 1.85 MG PROCHLORPERAZINE BASE) Alliance Pharmaceuticals, LTD. (2016) {{#l:Buccastem M use guide, last revised in January 2016..pdf}}</ref> | ||
*''' | *'''United States''': Prochlorperazine is available only through prescription.{{citation needed}} | ||
==See also== | ==See also== | ||
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==External links== | ==External links== | ||
*[https://en.wikipedia.org/wiki/Prochlorperazine Prochlorperazine (Wikipedia)] | *[https://en.wikipedia.org/wiki/Prochlorperazine Prochlorperazine (Wikipedia)] | ||
*[https://isomerdesign.com/PiHKAL/explore.php?id=11392 Prochlorperazine (Isomer Design)] | |||
==References== | ==References== | ||
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[[Category:Psychoactive substance]] | [[Category:Psychoactive substance]] | ||
[[Category:Substance]] | [[Category:Substance]] | ||
[[Category:Piperazine]] | |||
[[Category:Phenothiazine]] | |||
[[Category:Antihistamine]] | |||
[[Category:Depressant]] | [[Category:Depressant]] | ||
[[Category: | [[Category:Antipsychotic]] | ||