Prochlorperazine

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Prochlorperazine
Prochlorperazine.svg
Clinical data
AHFS/Drugs.com Monograph
MedlinePlus a682116
Pregnancy
category
Routes of
administration
Oral, buccal, rectal, IM, IV
ATC code
Legal status
Legal status
  • AU: S3 (Pharmacist only)
  • UK: POM (Prescription only) but packs of 8 buccal tablets for nausea/vomiting associated with migraine are sold as pharmacy medicines
  • US: ℞-only
Pharmacokinetic data
Bioavailability Unknown, but presumed substantial
Protein binding 91–99%
Metabolism Mainly hepatic (CYP2D6 and/or CYP3A4)
Biological half-life 4–8 hours, differs with the method of administration
Excretion Biliary, (colored) inactive metabolites in urine
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.000.345
Chemical and physical data
Formula C20H24ClN3S
Molar mass 373.943 g/mol
3D model (JSmol)
  (verify)

Prochlorperazine 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. It is also a highly potent typical antipsychotic, 10–20 times more potent than chlorpromazine. It is also used to treat migraine headaches. Intravenous administration can be used to treat status migrainosus.

Medical uses[edit]

Prochlorperazine is used to prevent vomiting caused by chemotherapy, radiation therapy and in the pre- and postoperative setting.[1] A 2015 Cochrane review found no differences in efficacy among drugs commonly used for this purpose in emergency rooms.[2]

IV prochlorperazine is also used to treat migraine in acute outpatient settings,[3] and in emergency rooms, and is recommended for ER use by The American Headache Society.[4]

In the UK, prochlorperazine is available for the treatment of nausea caused by migraine as a tablet dissolved in the mouth; it is sold as a "pharmacy medicine", meaning it does not require a prescription but is only available after talking with a pharmacist.[5][6]

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[7]

Side effects[edit]

Sedation is very common, and extrapyramidal side effects are common and include restlessness, dystonic reactions, pseudoparkinsonism, and akathisia; the extrapyramidal symptoms can affect 2% of people at low doses, whereas higher doses may affect as many as 40% of people.[8][9]

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, abnormal heart rhythms (arrhythmias). VA and FDA research show injection site reactions.

Adverse effects are similar in children.[1]

Pharmacology[edit]

Prochlorperazine is thought to exert its antipsychotic effects by blocking dopamine receptors.[10]

Prochlorperazine is analogous to chlorpromazine, both of these agents antagonize dopaminergic D2 receptors 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 antagonists 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.

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).

Society and culture[edit]

Prochlorperazine is available as tablets, suppositories, and in an injectable form.[11]

As of September 2017 it was marketed under the trade names Ametil, Antinaus, Antinaus, Buccastem, Bukatel, Chlormeprazine, Chloropernazine, Compro, Daolin, Dhaperazine, Emedrotec, Emetiral, Eminorm, Lotamin, Mitil, Mormal, Nautisol, Novamin, Novomit, Proazine, Procalm, Prochlorperazin, Prochlorperazine, Prochlorpérazine, Prochlorperazinum, Prochlozine, Proclorperazina, Promat, Promin, Promtil, Roumin, Scripto-metic, Seratil, Stemetil, Steremal, Vergon, Vestil, and Volimin.[11]

It was also marketed at that time as a combination drug for humans with paracetamol as Vestil-A, as a combination drug for veterinary use, with isopropamide as Darbazine.[11]

Research[edit]

Alexza Pharmaceuticals studied an inhaled form of prochlorperazine for the treatment of migraine through Phase II trials under the development name AT-001; development was discontinued in 2011.[12]

References[edit]

  1. ^ a b Lau Moon Lin, M; Robinson, PD; Flank, J; Sung, L; Dupuis, LL (June 2016). "The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis". Drug safety. 39 (6): 509–16. doi:10.1007/s40264-016-0398-9. PMID 26884326. 
  2. ^ Furyk, JS; Meek, RA; Egerton-Warburton, D (28 September 2015). "Drugs for the treatment of nausea and vomiting in adults in the emergency department setting". The Cochrane database of systematic reviews (9): CD010106. doi:10.1002/14651858.CD010106.pub2. PMID 26411330. 
  3. ^ Patniyot, IR; Gelfand, AA (January 2016). "Acute Treatment Therapies for Pediatric Migraine: A Qualitative Systematic Review". Headache. 56 (1): 49–70. doi:10.1111/head.12746. PMID 26790849. 
  4. ^ Orr, SL; Friedman, BW; Christie, S; Minen, MT; Bamford, C; Kelley, NE; Tepper, D (June 2016). "Management of Adults With Acute Migraine in the Emergency Department: The American Headache Society Evidence Assessment of Parenteral Pharmacotherapies". Headache. 56 (6): 911–40. doi:10.1111/head.12835. PMID 27300483. 
  5. ^ "Buccastem M - Summary of Product Characteristics (SPC) - (eMC)". UK Electronic Medicines Compendium. 16 February 2016. Retrieved 19 September 2017. 
  6. ^ "Medicines information". NHS Choices. Retrieved 19 September 2017. 
  7. ^ Coatesworth AP (November 2000). "Assessment and treatment of dizziness". Journal of Neurology, Neurosurgery, and Psychiatry. 69 (5): 706. doi:10.1136/jnnp.69.5.706. PMC 1763384Freely accessible. PMID 11184241. 
  8. ^ Brown, Thomas Markham; Stoudemire, Alan (1998). "Antipsychotics". Psychiatric Side Effects of Prescription and Over-The-Counter Medications. American Psychiatric Publishing. p. 1946. ISBN 9780880488686. 
  9. ^ Drugs.com
  10. ^ Manuchair S. Ebadi, Desk reference of clinical pharmacology. 2007
  11. ^ a b c "Prochlorperazine international brands". Drugs.com. Retrieved 19 September 2017. 
  12. ^ Chua, AL; Silberstein, S (September 2016). "Inhaled drug therapy development for the treatment of migraine". Expert opinion on pharmacotherapy. 17 (13): 1733–43. doi:10.1080/14656566.2016.1203901. PMID 27416108. 

External links[edit]