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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 [[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> | |||
'''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> | |||
==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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==Subjective effects== | ==Subjective effects== | ||
{{Preamble/SubjectiveEffects}} | {{Preamble/SubjectiveEffects}} | ||
{{effects/base | |||
|{{effects/physical| | |||
*'''[[Effect::Sedation]]''' | *'''[[Effect::Sedation]]''' | ||
*'''[[Effect::Appetite enhancement]]''' | |||
*'''[[Effect::Dizziness]]''' | *'''[[Effect::Dizziness]]''' | ||
*'''[[Effect::Dehydration]]''' | *'''[[Effect::Dehydration]]''' | ||
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*'''[[Effect::Orgasm suppression]]''' | *'''[[Effect::Orgasm suppression]]''' | ||
}} | |||
|{{effects/cognitive| | |||
The general head space of prochlorperazine is often described as one of sleepiness, emptiness, apathy, stupor and catatonia. The specific cognitive effects can be broken down into several components which progressively intensify proportional to dosage. These are described below and generally include: | The general head space of prochlorperazine is often described as one of sleepiness, emptiness, apathy, stupor and catatonia. The specific cognitive effects can be broken down into several components which progressively intensify proportional to dosage. These are described below and generally include: | ||
*'''[[Effect::Thought deceleration]]''' | *'''[[Effect::Thought deceleration]]''' | ||
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*'''[[Effect::Dream potentiation]]''' | *'''[[Effect::Dream potentiation]]''' | ||
*'''[[Effect::Analysis suppression]]''' | *'''[[Effect::Analysis suppression]]''' | ||
*'''[[Effect::Language suppression]]''' | *'''[[Effect::Language suppression]]''' | ||
*'''[[Effect::Amnesia]]''' | *'''[[Effect::Amnesia]]''' | ||
*'''[[Effect::Anxiety suppression]]''' | *'''[[Effect::Anxiety suppression]]''' | ||
*'''[[Effect::Focus suppression]]''' | *'''[[Effect::Focus suppression]]''' | ||
*'''[[Effect::Motivation suppression]]''' | |||
}} | |||
}} | |||
==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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*[[Quetiapine]] | *[[Quetiapine]] | ||
*[[Depressant]] | *[[Depressant]] | ||
==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== | ||
<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:Antipsychotic]] | |||