Haloperidol

Haloperidol
Clinical data
Pronunciation/ˌhæloʊˈpɛrɪdɒl/
Trade namesHaldol, others
AHFS/Drugs.comMonograph
MedlinePlusa682180
License data
Pregnancy
category
Routes of
administration		By mouth, intramuscular, intravenous, depot (as decanoate ester)
Drug classTypical antipsychotic
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class C1 (Other controlled substances)[2]
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability60–70% (by mouth)[3]
Protein binding~90%[3]
MetabolismLiver-mediated[3]
Metabolites• HPP+[4][5][6]
Elimination half-life14–26 hours (IV), 20.7 hours (IM), 14–37 hours (oral)[3]
ExcretionBiliary (hence in feces) and in urine[3][7]
Identifiers
IUPAC name
  • 4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.000.142
Chemical and physical data
FormulaC21H23ClFNO2
Molar mass375.87 g·mol−1
3D model (JSmol)
SMILES
  • c1cc(ccc1C(=O)CCCN2CCC(CC2)(c3ccc(cc3)Cl)O)F
InChI
  • InChI=1S/C21H23ClFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2 Y
  • Key:LNEPOXFFQSENCJ-UHFFFAOYSA-N Y
  (verify)

Haloperidol, sold under the brand name Haldol among others, is a typical antipsychotic medication.[8] Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.[8][9][10] It may be used by mouth or injection into a muscle or a vein.[8] Haloperidol typically works within 30 to 60 minutes.[8] A long-acting formulation may be used as an injection every four weeks for people with schizophrenia or related illnesses, who either forget or refuse to take the medication by mouth.[8]

Haloperidol may result in movement disorders such as tardive dyskinesia, and akathisia, both of which may be permanent.[8] Neuroleptic malignant syndrome and QT interval prolongation may occur, the latter particularly with IV administration.[8] In older people with psychosis due to dementia it results in an increased risk of death.[8] When taken during pregnancy it may result in problems in the infant.[8][11] It should not be used by people with Parkinson's disease.[8]

Haloperidol was discovered in 1958 by the team of Paul Janssen,[12] prepared as part of a structure-activity relationship investigation into analogs of pethidine (meperidine).[13] It is on the World Health Organization's List of Essential Medicines.[14] It is the most commonly used typical antipsychotic.[15] In 2020, it was the 303rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[16]

  1. ^ "Haloperidol Use During Pregnancy". Drugs.com. 10 February 2020. Retrieved 13 September 2020.
  2. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  3. ^ a b c d e Cite error: The named reference PK1999 was invoked but never defined (see the help page).
  4. ^ Cite error: The named reference Kostrzewa2022 was invoked but never defined (see the help page).
  5. ^ Cite error: The named reference Igarashi1998 was invoked but never defined (see the help page).
  6. ^ Cite error: The named reference GórskaMarszałłSloderbach2015 was invoked but never defined (see the help page).
  7. ^ "Product Information Serenace" (PDF). TGA eBusiness Services. Aspen Pharma Pty Ltd. 29 September 2011. Archived from the original on 14 March 2017. Retrieved 29 May 2014.
  8. ^ a b c d e f g h i j "Haloperidol". The American Society of Health-System Pharmacists. Archived from the original on 2 January 2015. Retrieved 2 January 2015.
  9. ^ Schuckit MA (November 2014). "Recognition and management of withdrawal delirium (delirium tremens)". The New England Journal of Medicine. 371 (22): 2109–2113. doi:10.1056/NEJMra1407298. PMID 25427113. S2CID 205116954.
  10. ^ Plosker GL (July 2012). "Quetiapine: a pharmacoeconomic review of its use in bipolar disorder". PharmacoEconomics. 30 (7): 611–631. doi:10.2165/11208500-000000000-00000. PMID 22559293.
  11. ^ "Prescribing medicines in pregnancy database". Australian Government. 3 March 2014. Archived from the original on 8 April 2014. Retrieved 2 January 2015.
  12. ^ Sneader W (2005). Drug discovery: a history (Rev. and updated ed.). Chichester: Wiley. p. 124. ISBN 978-0-471-89979-2. Archived from the original on 8 December 2015.
  13. ^ Ravina E (2011). The evolution of drug discovery: from traditional medicines to modern drugs (1. Aufl. ed.). Weinheim: Wiley-VCH. p. 62. ISBN 978-3-527-32669-3. Archived from the original on 8 December 2015.
  14. ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  15. ^ Stevens A (2004). Health care needs assessment: the epidemiologically based needs assessment reviews (2nd ed.). Abingdon: Radcliffe Medical. p. 202. ISBN 978-1-85775-892-4. Archived from the original on 8 December 2015.
  16. ^ "Haloperidol - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
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