Prochlorperazine (oral): Difference between revisions

Prochlorperazine (oral)
	File:Prochlorperazine.svg
Clinical data
Pregnancy; category	C (Au, U.S.);
Routes of; administration	Oral, buccal, rectal, IM
ATC code	N05AB04 (WHO) ;
Legal status
Legal status	OTC/POM (UK);
Pharmacokinetic data
Bioavailability	not exactly known, but substantial
Protein binding	91–99%
Metabolism	Mainly hepatic (CYP2D6 and/or CYP3A4)
Elimination half-life	4-8 hours, differs with the mode of application
Excretion	Biliary, (colored) inactive metabolites in urine
Identifiers
	IUPAC name 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-; 10H-phenothiazine;
CAS Number	58-38-8;
PubChem CID	4917;
DrugBank	APRD00624;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C20H24ClN3S
Molar mass	373.943 g/mol

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VisualWikitext

Revision as of 20:40, 12 February 2014

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [2]

For patient information about Prochlorperazine, click here.

Synonyms / Brand Names: ^®,

Overview

Prochlorperazine (marketed under the names Compazine, Buccastem, Stemetil, Phenotil) is a drug that belongs to the phenothiazine class of antipsychotic agent that is used for the treatment of nausea and vertigo. It is also a typical antipsychotic drug and a highly potent neuroleptic, 10 to 20 times more potent than chlorpromazine. In Pakistan, it is marketed under the name Phenotil by Unexo Labs.

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 as follows:

To alleviate the symptoms of vertigo
As an antiemetic, particularly for nausea and vomiting caused by cancer treatment, radiation and 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 side effects 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

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 nauses/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.

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.

FDA Package Insert

PHENADOZ (promethazine hydrochloride) suppository Normal 0 false false false EN-US X-NONE X-NONE

PHENERGAN (promethazine hydrochloride) injection Normal 0 false false false EN-US X-NONE X-NONE

PROMETHAZINE HYDROCHLORIDE solution Normal 0 false false false EN-US X-NONE X-NONE

PROMETHAZINE HYDROCHLORIDE tablet Normal 0 false false false EN-US X-NONE X-NONE

Mechanism of Action

^[1]   Normal  0          false  false  false    EN-US  X-NONE  X-NONE

^[2] Normal 0 false false false EN-US X-NONE X-NONE

^[3]   Normal  0          false  false  false    EN-US  X-NONE  X-NONE

References

Template:Antimigraine preparations

External links

Prochlorperazine medlineplus.org article
AZ-001 (Staccato(TM) prochlorperazine) Press release pertaining to phase IIb clinical trial of inhaled prochlorperazine for migraine headache

sv:Proklorperazin sex

[dailymed.nlm.nih.gov-1] "PHENADOZ (PROMETHAZINE HYDROCHLORIDE) SUPPOSITORY [PADDOCK LABORATORIES, INC.]".

[2] "PHENERGAN (PROMETHAZINE HYDROCHLORIDE) INJECTION [WEST-WARD PHARMACEUTICAL CORP.]".

[3] "PROMETHAZINE HYDROCHLORIDE SOLUTION [HI-TECH PHARMACAL CO., INC.]".

[1]

[2]

[3]

@@ Line 1: / Line 1: @@
+__NOTOC__
+{{Prochlorperazine}}
+{{CMG}}; {{AE}} {{PB}}
+'''''For patient information about Prochlorperazine, click [[Prochlorperazine (patient information)|here]].'''''
+{{SB}} <sup>®</sup>,
+==Overview==
 {{drugbox |
 | IUPAC_name = 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-<BR>10''H''-phenothiazine
@@ Line 41: / Line 50: @@
 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]].
+==Category==
+==FDA Package Insert==
+==PHENADOZ (promethazine hydrochloride) suppository   Normal  0          false  false  false    EN-US  X-NONE  X-NONE                                                                                                                                                                                                                                                                                                                                                            ==
+'''  [[PHENADOZ (promethazine hydrochloride) suppository indications and usage|Indications and Usage]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository dosage and administration|Dosage and Administration]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository dosage forms and strengths|Dosage Forms and Strengths]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository contraindications|Contraindications]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository warnings and precautions|Warnings and Precautions]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository adverse reactions|Adverse Reactions]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository drug interactions|Drug Interactions]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository use in specific populations|Use in Specific Populations]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository overdosage|Overdosage]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository description|Description]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository clinical pharmacology|Clinical Pharmacology]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository nonclinical toxicology|Nonclinical Toxicology]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository clinical studies|Clinical Studies]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository how supplied storage and handling|How Supplied/Storage and Handling]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository patient counseling information|Patient Counseling Information]]'''
+'''| [[PHENADOZ (promethazine hydrochloride) suppository labels and packages|Labels and Packages]]'''
+==PHENERGAN (promethazine hydrochloride) injection   Normal  0          false  false  false    EN-US  X-NONE  X-NONE                                                                                                                                                                                                                                                                                                                                                            ==
+'''  [[PHENERGAN (promethazine hydrochloride) injection indications and usage|Indications and Usage]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection dosage and administration|Dosage and Administration]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection dosage forms and strengths|Dosage Forms and Strengths]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection contraindications|Contraindications]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection warnings and precautions|Warnings and Precautions]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection adverse reactions|Adverse Reactions]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection drug interactions|Drug Interactions]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection use in specific populations|Use in Specific Populations]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection overdosage|Overdosage]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection description|Description]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection clinical pharmacology|Clinical Pharmacology]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection nonclinical toxicology|Nonclinical Toxicology]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection clinical studies|Clinical Studies]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection how supplied storage and handling|How Supplied/Storage and Handling]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection patient counseling information|Patient Counseling Information]]'''
+'''| [[PHENERGAN (promethazine hydrochloride) injection labels and packages|Labels and Packages]]'''
+==PROMETHAZINE HYDROCHLORIDE solution   Normal  0          false  false  false    EN-US  X-NONE  X-NONE                                                                                                                                                                                                                                                                                                                                                            ==
+'''  [[PROMETHAZINE HYDROCHLORIDE solution indications and usage|Indications and Usage]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution dosage and administration|Dosage and Administration]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution dosage forms and strengths|Dosage Forms and Strengths]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution contraindications|Contraindications]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution warnings and precautions|Warnings and Precautions]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution adverse reactions|Adverse Reactions]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution drug interactions|Drug Interactions]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution use in specific populations|Use in Specific Populations]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution overdosage|Overdosage]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution description|Description]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution clinical pharmacology|Clinical Pharmacology]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution nonclinical toxicology|Nonclinical Toxicology]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution clinical studies|Clinical Studies]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution how supplied storage and handling|How Supplied/Storage and Handling]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution patient counseling information|Patient Counseling Information]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE solution labels and packages|Labels and Packages]]'''
+==PROMETHAZINE HYDROCHLORIDE tablet   Normal  0          false  false  false    EN-US  X-NONE  X-NONE                                                                                                                                                                                                                                                                                                                                                            ==
+'''  [[PROMETHAZINE HYDROCHLORIDE tablet indications and usage|Indications and Usage]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet dosage and administration|Dosage and Administration]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet dosage forms and strengths|Dosage Forms and Strengths]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet contraindications|Contraindications]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet warnings and precautions|Warnings and Precautions]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet adverse reactions|Adverse Reactions]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet drug interactions|Drug Interactions]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet use in specific populations|Use in Specific Populations]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet overdosage|Overdosage]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet description|Description]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet clinical pharmacology|Clinical Pharmacology]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet nonclinical toxicology|Nonclinical Toxicology]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet clinical studies|Clinical Studies]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet how supplied storage and handling|How Supplied/Storage and Handling]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet patient counseling information|Patient Counseling Information]]'''
+'''| [[PROMETHAZINE HYDROCHLORIDE tablet labels and packages|Labels and Packages]]'''
+==Mechanism of Action==
+ <ref name="dailymed.nlm.nih.gov">{{Cite web  | last =  | first =  | title = PHENADOZ (PROMETHAZINE HYDROCHLORIDE) SUPPOSITORY [PADDOCK LABORATORIES, INC.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=9aa7b3f2-4429-4a61-ad8e-876afb14cc45 | publisher =  | date =  | accessdate = }}</ref>   Normal  0          false  false  false    EN-US  X-NONE  X-NONE
+<ref>{{Cite web  | last =  | first =  | title = PHENERGAN (PROMETHAZINE HYDROCHLORIDE) INJECTION [WEST-WARD PHARMACEUTICAL CORP.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=481866da-a712-48a5-853f-8e84aacaab6d | publisher =  | date =  | accessdate = }}</ref>   Normal  0          false  false  false    EN-US  X-NONE  X-NONE
+ <ref>{{Cite web  | last =  | first =  | title = PROMETHAZINE HYDROCHLORIDE SOLUTION [HI-TECH PHARMACAL CO., INC.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=bd8d1f9a-242c-440b-a5eb-a50f64a1c1d9 | publisher =  | date =  | accessdate = }}</ref>   Normal  0          false  false  false    EN-US  X-NONE  X-NONE
+==References==
+{{Reflist|2}}
+{{Antimigraine preparations}}
+[[Category:Drugs]]
 ==External links==

v t e Antipsychotics (neuroleptics) (N05A)
Typical	Benzamides: Levosulpiride • Nemonapride • Sulpiride • Sultopride • Tiapride • Veralipride; Butyrophenones: Azaperone • Benperidol • Bromperidol • Droperidol • Fluanisone • Haloperidol • Lenperone • Moperone • Pipamperone • Spiperone • Timiperone • Trifluperidol; Diphenylbutylpiperidines: Clopimozide • Fluspirilene • Penfluridol • Pimozide; Phenothiazines: Acepromazine • Acetophenazine • Butaperazine • Carphenazine • Chloracizine • Chlorproethazine • Chlorpromazine • Cyamemazine • Dixyrazine • Fluacizine • Fluphenazine • Levomepromazine/Methotrimeprazine • Mesoridazine • Perazine • Periciazine • Perphenazine • Piperacetazine • Pipotiazine • Prochlorperazine • Promazine • Promethazine • Propiomazine • Sulforidazine • Thiethylperazine • Thiopropazate • Thioproperazine • Thioridazine • Trifluoperazine • Triflupromazine; Thioxanthenes: Chlorprothixene • Clopenthixol • Flupentixol • Thiothixene • Zuclopenthixol; Tricyclics: Amoxapine • Butaclamol • Fluotracen • Loxapine • Metitepine/Methiothepin • Octoclothiepin • Trimipramine; Others: Prothipendyl
Atypical	Benzamides: Amisulpride • Remoxipride; Butyrophenones: Cinuperone • Setoperone; Benzo(iso)oxazole piperidines: Iloperidone • Ocaperidone • Paliperidone • Risperidone; Benzo(iso)thiazole piperazines: Lurasidone • Perospirone • Revospirone • Tiospirone • Ziprasidone; Diphenylbutylpiperazines: Amperozide; Phenylpiperazines: Aripiprazole • Bifeprunox • Elopiprazole • Umespirone; Tricyclics: Asenapine • Carpipramine • Clocapramine • Clotiapine • Clozapine • Fluperlapine • Gevotroline • Metitepine/Methiothepin • Mosapramine • NDMC • Olanzapine • Piquindone • Quetiapine • Tenilapine • Zotepine; Others: Blonanserin • Cariprazine • Molindone • Pimavanserin • Roxindole • Sarizotan • Sertindole • Spiramide
Others	Azacyclonol • Cannabidiol • D-Cycloserine • Lithium • Mifepristone • Oxypertine • Reserpine • Rimcazole • Secretin • Talnetant • Tetrabenazine • Vabicaserin
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III Template:Psychology navs

Clinical data
File:Prochlorperazine.svg
Pregnancy category	C (Au, U.S.)
Routes of administration	Oral, buccal, rectal, IM
ATC code	N05AB04 (WHO)
Legal status
Legal status	OTC/POM (UK)
Pharmacokinetic data
Bioavailability	not exactly known, but substantial
Protein binding	91–99%
Metabolism	Mainly hepatic (CYP2D6 and/or CYP3A4)
Elimination half-life	4-8 hours, differs with the mode of application
Excretion	Biliary, (colored) inactive metabolites in urine
Identifiers
IUPAC name 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]- 10H-phenothiazine
CAS Number	58-38-8
PubChem CID	4917
DrugBank	APRD00624
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C₂₀H₂₄ClN₃S
Molar mass	373.943 g/mol