Wikipedia

User:Mr. Ibrahem/Buspirone

< User:Mr. Ibrahem
Mr. Ibrahem/Buspirone
Clinical data
Pronunciation/ˈbjuːspɪroʊn/ (BEW-spi-rohn)
Trade namesBuspar, Namanspin
Other namesMJ 9022-1[1]
AHFS/Drugs.comMonograph
MedlinePlusa688005
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth
Legal status
Legal status
Pharmacokinetic data
Bioavailability3.9%[2]
Protein binding86–95%[3]
MetabolismLiver (via CYP3A4)[7][8]
Metabolites5-OH-Buspirone; 6-OH-Buspirone; 8-OH-Buspirone; 1-PPTooltip 1-(2-pyrimidinyl)piperazine[4][5][6]
Elimination half-life2.5 hours[7]
ExcretionUrine: 29–63%[3]
Feces: 18–38%[3]
Identifiers
  • 8-{4-[4-(Pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
Chemical and physical data
FormulaC21H31N5O2
Molar mass385.512 g·mol−1
3D model (JSmol)
  • O=C1N(CCCCN2CCN(CC2)C3=NC=CC=N3)C(CC4(CCCC4)C1)=O
  • 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 a medication primarily used to treat anxiety disorders, particularly generalized anxiety disorder.[9][10] Benefits support its short term use.[11] It has not been found to be effective in treating psychosis.[9] It is taken by mouth, and it may take up to four weeks for an effect.[9][10]

Common side effects include nausea, headaches, dizziness, and trouble concentrating.[9][11] Serious side effects may include hallucinations, serotonin syndrome, and seizures.[11] Use in pregnancy appears to be safe but has not been well studied, while use during breastfeeding is not recommended.[11][13] How it works is not clear but it is unrelated to benzodiazepines.[9]

Buspirone was first made in 1968 and approved for medical use in the United States in 1986.[9][10] It is available as a generic medication.[11] A month supply in the United Kingdom costs the NHS about £10 as of 2019.[11] In the United States the wholesale cost of this amount is about US$3.[14] In 2017, it was the 80th most commonly prescribed medication in the United States, with more than ten million prescriptions.[15][16]

References edit

  1. ^ Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 192–. ISBN 978-1-4757-2085-3. Archived from the original on 12 March 2017. Retrieved 11 March 2017.
  2. ^ Loane C, Politis M (June 2012). "Buspirone: what is it all about?". Brain Research. 1461: 111–8. doi:10.1016/j.brainres.2012.04.032. PMID 22608068.
  3. ^ a b c "buspirone (Rx) - BuSpar, Buspirex, more." Medscape Reference. WebMD. Archived from the original on 13 July 2019. Retrieved 14 November 2013.
  4. ^ Gammans RE, Mayol RF, LaBudde JA (March 1986). "Metabolism and disposition of buspirone". The American Journal of Medicine. 80 (3B): 41–51. doi:10.1016/0002-9343(86)90331-1. PMID 3515929.
  5. ^ Schatzberg, Alan F.; Nemeroff, Charles B. (2009). The American Psychiatric Publishing Textbook of Psychopharmacology. American Psychiatric Pub. pp. 490–. ISBN 978-1-58562-309-9.
  6. ^ Wong H, Dockens RC, Pajor L, Yeola S, Grace JE, Stark AD, et al. (August 2007). "6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats". Drug Metabolism and Disposition. 35 (8): 1387–92. doi:10.1124/dmd.107.015768. PMID 17494642. S2CID 25558546.
  7. ^ a b Mahmood I, Sahajwalla C (April 1999). "Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug". Clinical Pharmacokinetics. 36 (4): 277–87. doi:10.2165/00003088-199936040-00003. PMID 10320950. Archived (PDF) from the original on 2021-08-28. Retrieved 2019-09-06.
  8. ^ 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): 500–7. doi:10.1124/dmd.104.000836. PMID 15640381. S2CID 10142905.
  9. ^ a b c d e f g h "Buspirone Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 6 March 2019. Retrieved 3 March 2019.
  10. ^ a b c d Wilson, TK; Tripp, J (January 2018). "Buspirone". StatPearls. PMID 30285372. Archived from the original on 2020-08-11. Retrieved 2019-03-05.
  11. ^ a b c d e f g British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 338. ISBN 9780857113382.
  12. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 7 November 2020. Retrieved 6 September 2020.
  13. ^ "Buspirone Pregnancy and Breastfeeding Warnings". Drugs.com. Archived from the original on 6 March 2019. Retrieved 3 March 2019.
  14. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Archived from the original on 2019-03-06. Retrieved 3 March 2019.
  15. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  16. ^ "Buspirone - Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.
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