Prochlorperazine

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Prochlorperazine
Prochlorperazine.svg
Clinical data
Trade namesCompro, others
AHFS/Drugs.comMonograph
MedlinePlusa682116
Pregnancy
category
Routes of
administration
By mouth, 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
BioavailabilityUnknown, but presumed substantial
Protein binding91–99%
MetabolismMainly hepatic (CYP2D6 and/or CYP3A4)
Elimination half-life4–8 hours, differs with the method of administration
ExcretionBiliary, (colored) inactive metabolites in urine
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.000.345 Edit this at Wikidata
Chemical and physical data
FormulaC20H24ClN3S
Molar mass373.943 g/mol g·mol−1
3D model (JSmol)
  (verify)

Prochlorperazine, sold under the brand name Compro among others, is a medication used to treat nausea, schizophrenia, migraines, and anxiety.[1][2][3] It is a less preferred medication for anxiety.[1] It maybe taken by mouth, rectally, injection into a vein, or injection into a muscle.[1]

Common side effects include sleepiness, blurry vision, low blood pressure, and dizziness.[1] Serious side effects may include movement disorders including tardive dyskinesia and neuroleptic malignant syndrome.[1] Use in pregnancy and breastfeeding is generally not recommended.[4] It is a typical antipsychotic which is believed to work by affecting levels of dopamine in the brain.[1]

Prochlorperazine was approved for medical use in the United States in 1956.[1] It is avaliable as a generic medication.[2] A dose in the United Kingdom costs the NHS about 0.04 £ as of 2019.[2] In the United States the wholesale cost of this amount is about 0.24 USD.[5] In 2016 it was the 288th most prescribed medication in the United States with more than a million prescriptions.[6]

Medical uses[edit]

Prochlorperazine is used to prevent vomiting caused by chemotherapy, radiation therapy and in the pre- and postoperative setting.[7] A 2015 Cochrane review found no differences in efficacy among drugs commonly used for this purpose in emergency rooms.[8]

IV prochlorperazine is also used to treat migraine in acute outpatient settings,[9] and in emergency rooms, and is recommended by The American Headache Society.[3]

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.[10][11]

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[12]

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.[13][14]

Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome (NMS). Some symptoms of NMS include high fever, stiff muscles, neck muscle spasm, 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.[7]

Pharmacology[edit]

Prochlorperazine is thought to exert its antipsychotic effects by blocking dopamine receptors.[15]

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).

Marketing[edit]

Prochlorperazine is available as tablets, suppositories, and in an injectable form.[16]

As of September 2017 it was marketed under the trade names Ametil, Antinaus, Buccastem, Bukatel, Chlormeprazine, Chloropernazine, Compazine, 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.[16][17]

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.[16]

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.[18]

References[edit]

  1. ^ a b c d e f g "Prochlorperazine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  2. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 385–386. ISBN 9780857113382.
  3. ^ a b 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.
  4. ^ "Prochlorperazine Use During Pregnancy". Drugs.com. Retrieved 3 March 2019.
  5. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
  6. ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
  7. ^ 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.
  8. ^ 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.
  9. ^ 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.
  10. ^ "Buccastem M - Summary of Product Characteristics (SPC) - (eMC)". UK Electronic Medicines Compendium. 16 February 2016. Retrieved 19 September 2017.
  11. ^ "Medicines information". NHS Choices. Retrieved 19 September 2017.
  12. ^ Coatesworth AP (November 2000). "Assessment and treatment of dizziness". Journal of Neurology, Neurosurgery, and Psychiatry. 69 (5): 706–707. doi:10.1136/jnnp.69.5.706. PMC 1763384. PMID 11184241.
  13. ^ Brown, Thomas Markham; Stoudemire, Alan (1998). "Antipsychotics". Psychiatric Side Effects of Prescription and Over-The-Counter Medications. American Psychiatric Publishing. p. 1946. ISBN 9780880488686.
  14. ^ "Procot Side Effects in Detail". Drugs.com.
  15. ^ Manuchair S. Ebadi, Desk reference of clinical pharmacology. 2007
  16. ^ a b c "Prochlorperazine international brands". Drugs.com. Retrieved 19 September 2017.
  17. ^ "Compazine (Prochlorperazine) Patient Information: Side Effects and Drug Images at RxList". RxList.
  18. ^ 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]