Buspirone

Not to be confused with Bupropion.

Buspirone
Clinical data
Pronunciation/ˈbjuːspɪroʊn/ (BEW-spi-rohn)
Trade namesBuspar
Other namesMJ 9022-1[1]
AHFS/Drugs.comMonograph
MedlinePlusa688005
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability3.9%[3]
Protein binding86–95%[4]
MetabolismLiver (via CYP3A4)[8][9]
Metabolites5-OH-Buspirone; 6-OH-Buspirone; 8-OH-Buspirone; 1-PPTooltip 1-(2-pyrimidinyl)piperazine[5][6][7]
Elimination half-life2.5 hours[8]
ExcretionUrine: 29–63%[4]
Feces: 18–38%[4]
Identifiers
  • 8-{4-[4-(Pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.048.232 Edit this at Wikidata
Chemical and physical data
FormulaC21H31N5O2
Molar mass385.512 g·mol−1
3D model (JSmol)
  • O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2ncccn2)CC1
  • InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2 checkY
  • Key:QWCRAEMEVRGPNT-UHFFFAOYSA-N checkY
  (verify)

Buspirone, sold under the brand name Buspar, among others, is an anxiolytic, a medication primarily used to treat anxiety disorders, particularly generalized anxiety disorder (GAD).[10][11] It is a serotonin 5-HT1A receptor partial agonist, increasing action at serotonin receptors in the brain.[3] It is taken orally, and takes two to six weeks to be fully effective.[10][11]

Common side effects of buspirone include nausea, headaches, dizziness, and difficulty concentrating.[10][12] Serious side effects may include movement disorders, serotonin syndrome, and seizures.[12] Its use in pregnancy appears to be safe but has not been well studied, and use during breastfeeding has not been well studied.[12][13]

Buspirone was developed in 1968 and approved for medical use in the United States in 1986.[10][11] It is available as a generic medication.[12] In 2022, it was the 54th most commonly prescribed medication in the United States, with more than 12 million prescriptions.[14][15]

  1. ^ Cite error: The named reference Elks2014 was invoked but never defined (see the help page).
  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 Loane C, Politis M (June 2012). "Buspirone: what is it all about?". Brain Research. 1461: 111–118. doi:10.1016/j.brainres.2012.04.032. PMID 22608068. S2CID 11734819.
  4. ^ a b c "buspirone (Rx) - BuSpar, Buspirex, more." Medscape Reference. WebMD. Retrieved 14 November 2013.
  5. ^ Cite error: The named reference pmid3515929 was invoked but never defined (see the help page).
  6. ^ Cite error: The named reference SchatzbergNemeroff2009 was invoked but never defined (see the help page).
  7. ^ Cite error: The named reference pmid17494642 was invoked but never defined (see the help page).
  8. ^ a b Mahmood I, Sahajwalla C (April 1999). "Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug". Clinical Pharmacokinetics. 36 (4): 277–287. doi:10.2165/00003088-199936040-00003. PMID 10320950. S2CID 1102318.
  9. ^ Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, et al. (April 2005). "Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes". Drug Metabolism and Disposition. 33 (4): 500–507. doi:10.1124/dmd.104.000836. PMID 15640381. S2CID 10142905.
  10. ^ a b c d "Buspirone Hydrochloride Monograph for Professionals". Drugs.com.
  11. ^ a b c Wilson TK, Tripp J (January 2018). "Buspirone". StatPearls. PMID 30285372.
  12. ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 338. ISBN 9780857113382.
  13. ^ "Buspirone Pregnancy and Breastfeeding Warnings". Drugs.com.
  14. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  15. ^ "Buspirone Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.