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Buspirone
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{{Short description|Medication used to treat anxiety disorders}} {{Distinguish|Bupropion|Buprenorphine}} {{Use dmy dates|date=January 2024}} {{cs1 config|name-list-style=vanc|display-authors=6}} {{Infobox drug | Watchedfields = changed | verifiedrevid = 459522704 | image = Buspirone 200.svg | image_class = skin-invert-image | width = 250 | alt = | image2 = Buspirone 3D structure.png | alt2 = <!-- Clinical data --> | pronounce = {{IPAc-en|ˈ|b|juː|s|p|ᵻ|r|oʊ|n}} ({{respell|BEW|spi-rohn}}) | tradename = Buspar, others | Drugs.com = {{drugs.com|monograph|buspirone-hydrochloride}} | MedlinePlus = a688005 | DailyMedID = Buspirone | pregnancy_AU = B1 | pregnancy_AU_comment = <ref>{{cite web | url=http://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent=&id=CP-2025-PI-01080-1 | title=TGA eBS - Product and Consumer Medicine Information Licence }}</ref> | pregnancy_category = | routes_of_administration = [[Oral administration|By mouth]] | class = | ATC_prefix = N05 | ATC_suffix = BE01 | ATC_supplemental = <!-- Legal status --> | legal_AU = S4 | legal_AU_comment = <ref>{{cite web | title=Anksilon (Orion Pharma (AUS) Pty Limited) | website=Therapeutic Goods Administration (TGA) | date=19 February 2025 | url=https://www.tga.gov.au/resources/prescription-medicines-registrations/anksilon-orion-pharma-aus-pty-limited | access-date=7 March 2025}}</ref><ref>{{cite web | title=Anksilon buspirone hydrochloride 5 mg tablet blister pack (422891) | website=Therapeutic Goods Administration (TGA) | date=17 January 2025 | url=https://www.tga.gov.au/resources/artg/422891 | access-date=7 March 2025}}</ref> | legal_BR = C1 | legal_BR_comment = <ref>{{cite web |author=Anvisa |author-link=Brazilian Health Regulatory Agency |date=31 March 2023 |title=RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial |trans-title=Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control |url=https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |url-status=live |archive-url=https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |archive-date=3 August 2023 |access-date=16 August 2023 |publisher=[[Diário Oficial da União]] |language=pt-BR |publication-date=4 April 2023}}</ref> | legal_CA = Rx-only | legal_CA_comment = | legal_DE = <!-- Anlage I, II, III or Unscheduled --> | legal_DE_comment = | legal_NZ = <!-- Class A, B, C --> | legal_NZ_comment = | legal_UK = POM | legal_UK_comment = | legal_US = Rx-only | legal_US_comment = | legal_EU = | legal_EU_comment = | legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> | legal_UN_comment = | legal_status = <!-- For countries not listed above --> <!-- Pharmacokinetic data --> | bioavailability = 3.9%<ref name="pmid22608068">{{cite journal | vauthors=Loane C, Politis M | title=Buspirone: what is it all about? | journal=Brain Research | volume=1461 | pages=111–118 | date=June 2012 | pmid=22608068 | doi=10.1016/j.brainres.2012.04.032 | s2cid=11734819 }}</ref> | protein_bound = 86–95%<ref name=MSR>{{cite web|title=buspirone (Rx) - BuSpar, Buspirex, more..|work=Medscape Reference|publisher=WebMD|url=http://reference.medscape.com/drug/buspar-buspirone-342913|access-date=14 November 2013}}</ref> | metabolism = [[Liver]] (via [[CYP3A4]])<ref name="pmid10320950" /><ref name="pmid15640381">{{cite journal | vauthors=Zhu M, Zhao W, Jimenez H, Zhang D, Yeola S, Dai R, Vachharajani N, Mitroka J | title=Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes | journal=Drug Metabolism and Disposition | volume=33 | issue=4 | pages=500–507 | date=April 2005 | pmid=15640381 | doi=10.1124/dmd.104.000836 | s2cid=10142905 }}</ref> | metabolites = 5-OH-Buspirone; <br>6-OH-Buspirone; <br>8-OH-Buspirone; <br>{{abbrlink|1-PP|1-(2-pyrimidinyl)piperazine}}<ref name="pmid3515929" /><ref name="SchatzbergNemeroff2009" /><ref name="pmid17494642" /> | onset = | elimination_half-life = 2.5 hours<ref name="pmid10320950">{{cite journal | vauthors=Mahmood I, Sahajwalla C | title=Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug | journal=Clinical Pharmacokinetics | volume=36 | issue=4 | pages=277–287 | date=April 1999 | pmid=10320950 | doi=10.2165/00003088-199936040-00003 | s2cid=1102318 | url=https://zenodo.org/record/1236411 }}</ref> | duration_of_action = | excretion = [[Urine]]: 29–63%<ref name=MSR/><br />[[Feces]]: 18–38%<ref name=MSR/> <!-- Identifiers --> | index2_label = as HCl | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 36505-84-7 | CAS_number2 = 33386-08-2 | CAS_supplemental = | PubChem = 2477 | IUPHAR_ligand = 36 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00490 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 2383 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = TK65WKS8HL | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D07593 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 3223 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 49 | NIAID_ChemDB = | PDB_ligand = | synonyms = MJ 9022-1<ref name="Elks2014" /> <!-- Chemical and physical data --> | IUPAC_name = 8-{4-[4-(Pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione | C = 21 | H = 31 | N = 5 | O = 2 | SMILES = O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2ncccn2)CC1 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChI_comment = | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = QWCRAEMEVRGPNT-UHFFFAOYSA-N | density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }} <!-- Definition and medical uses --> '''Buspirone''', sold under the brand name '''Buspar''' among others, is an [[anxiolytic]], a medication primarily used to treat [[anxiety disorder]]s, particularly [[generalized anxiety disorder]] (GAD).<ref name="AHFS2019">{{cite web |title=Buspirone Hydrochloride Monograph for Professionals | url=https://www.drugs.com/monograph/buspirone.html |website=[[Drugs.com]]}}</ref><ref name=Wil2018/> It is a [[serotonin]] [[5-HT1A receptor|5-HT<sub>1A</sub> receptor]] [[partial agonist]], increasing action at serotonin receptors in the brain.<ref name="pmid22608068" /> It is taken orally and takes two to six weeks to be fully effective.<ref name=AHFS2019/><ref name=Wil2018/> Common side effects of buspirone include [[nausea]], [[headache]]s, [[dizziness]], and difficulty concentrating.<ref name=AHFS2019/><ref name=BNF76>{{cite book |title=British national formulary: BNF 76 |date=2018 |publisher=Pharmaceutical Press |isbn=9780857113382 |pages=338 |edition=76}}</ref> Serious side effects may include [[movement disorder]]s, [[serotonin syndrome]], and [[seizures]].<ref name=BNF76/> Its use in [[pregnancy]] appears to be safe but has not been well studied, and use during [[breastfeeding]] has not been well studied either.<ref name=BNF76/><ref name=Preg2019>{{cite web |url=https://www.drugs.com/pregnancy/buspirone.html |title=Buspirone Pregnancy and Breastfeeding Warnings |website=[[Drugs.com]]}}</ref> Buspirone was developed in 1968 and approved for medical use in the United States in 1986.<ref name=AHFS2019/><ref name=Wil2018>{{cite journal | title=Buspirone | journal=StatPearls | date=January 2018 | pmid=30285372 | url=https://www.ncbi.nlm.nih.gov/books/NBK531477/ | vauthors=Wilson TK, Tripp J }}</ref> It is available as a [[generic medication]].<ref name=BNF76/> In 2022, it was the 54th most commonly prescribed medication in the United States, with more than 12{{nbsp}}million prescriptions.<ref>{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Buspirone Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Buspirone | access-date = 30 August 2024 }}</ref> {{TOC limit}}
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