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Buspirone information


Buspirone
Clinical data
Pronunciation/ˈbjuːspɪrn/ (BEW-spi-rohn)
Trade namesBuspar, Namanspin
Other namesMJ 9022-1[1]
AHFS/Drugs.comMonograph
MedlinePlusa688005
License data
  • US DailyMed: Buspirone
Pregnancy
category
  • AU: B1
Routes of
administration
By mouth
ATC code
  • N05BE01 (WHO)
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
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
IUPAC name
  • 8-{4-[4-(Pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
CAS Number
  • 36505-84-7 checkY
  • as HCl: 33386-08-2
PubChem CID
  • 2477
IUPHAR/BPS
  • 36
DrugBank
  • DB00490 checkY
ChemSpider
  • 2383 checkY
UNII
  • TK65WKS8HL
KEGG
  • D07593 checkY
ChEBI
  • CHEBI:3223 checkY
ChEMBL
  • ChEMBL49 checkY
CompTox Dashboard (EPA)
  • DTXSID2022707 Edit this at Wikidata
ECHA InfoCard100.048.232 Edit this at Wikidata
Chemical and physical data
FormulaC21H31N5O2
Molar mass385.512 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2ncccn2)CC1
InChI
  • 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.[10][11] It is a serotonin 5-HT1A receptor 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 2021, it was the 53rd 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 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  15. ^ "Buspirone - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.

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Buspirone

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Buspirone, sold under the brand name Buspar, among others, is an anxiolytic, a medication primarily used to treat anxiety disorders, particularly generalized...

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List of side effects of buspirone

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Side effects of buspirone by incidence include: Very common (>10% incidence) Dizziness/lightheadedness Headache Somnolence (sleepiness) Common (1–10%...

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Anxiolytic

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anxiety disorders due to their fast onset but carry the risk of dependence. Buspirone is indicated for GAD, which has much slower onset but with the advantage...

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Pyrimidinylpiperazine

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A number of pyrimidinylpiperazine derivatives are drugs, including: Buspirone – anxiolytic Dasatinib – anticancer agent Eptapirone – anxiolytic Gepirone –...

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Azapirone

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(S-20,499) Binospirone (MDL-73,005) BMY-7,378 (CAS number: 21102-95-4 ) Buspirone (Buspar) Enilospirone (CERM-3,726) Eptapirone (F-11,440) Gepirone (Exxua)...

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Cerebellar ataxia

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to moderate cerebellar ataxia may be treatable with buspirone. It is thought that the buspirone increases the serotonin levels in the cerebellum and...

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Gepirone

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the D2 receptor (30- to 50-fold lower in comparison to buspirone). However, similarly to buspirone, gepirone metabolizes into 1-(2-pyrimidinyl)piperazine...

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Agonist

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specific type of receptor. E.g. buspirone is a selective agonist for serotonin 5-HT1A. Partial agonists (such as buspirone, aripiprazole, buprenorphine,...

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Tandospirone

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azapirone class of drugs and is closely related to other azapirones like buspirone and gepirone. Tandospirone was introduced for medical use in Japan in...

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Raphe nuclei

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the brain and decrease the release of serotonin. The anxiolytic drug Buspirone acts as partial agonist against these receptors. Selective serotonin reuptake...

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Partial agonist

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have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine. Examples of...

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Attention deficit hyperactivity disorder

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agonists Clonidine Guanfacine Antidepressants Amitriptyline Bupropion Buspirone Desipramine Duloxetine Imipramine Milnacipran Moclobemide Nortriptyline...

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Gabapentin

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v t e Anxiolytics (N05B) 5-HT1ARTooltip 5-HT1A receptor agonists Buspirone Gepirone Tandospirone GABAARTooltip GABAA receptor PAMsTooltip positive allosteric...

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Serotonin syndrome

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(TCAs), amphetamines, pethidine (meperidine), tramadol, dextromethorphan, buspirone, L-tryptophan, 5-hydroxytryptophan, St. John's wort, triptans, MDMA, metoclopramide...

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Hydroxyzine

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Insufficient data were available to compare the drug with benzodiazepines and buspirone. Hydroxyzine can also be used for the treatment of allergic conditions...

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MDMA

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cariprazine, clozapine, lurasidone, quetiapine, ziprasidone) Azapirones (e.g., buspirone, eptapirone, gepirone, perospirone, tandospirone) Bay R 1531 Befiradol...

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Mirtazapine

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(aripiprazole, brexpiprazole, lurasidone, olanzapine, quetiapine, risperidone) Buspirone Lithium (lithium carbonate, lithium citrate) Thyroid hormones (triiodothyronine...

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Brazilian Controlled Drugs and Substances Act

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Benzoctamine Benzquinamide Biperiden Brexpiprazole Brivaracetam Bupropion Buspirone Butaperazine Butriptyline Cannabidiol - Synthetic form with no other cannabinoid...

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Methamphetamine

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agonists Clonidine Guanfacine Antidepressants Amitriptyline Bupropion Buspirone Desipramine Duloxetine Imipramine Milnacipran Moclobemide Nortriptyline...

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List of psychotropic medications

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- a long-acting CNS stimulant used to treat ADHD Buspar (buspirone) – an anxiolytic used to treat generalized anxiety disorder Belbuca, Buprenex...

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Ketamine

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Trimipramine Others: 3-PPP Alpiropride Azapride Bromerguride Bromocriptine Buspirone Desmethoxyfallypride EEDQ F-15063 Fallypride Fananserin Fenfluramine Iodobenzamide...

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Selective serotonin reuptake inhibitor

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cause jaw pain/jaw spasm reversible syndrome (although it is not common). Buspirone appears to be successful in treating bruxism on SSRI/SNRI induced jaw...

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Nitrous oxide

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cariprazine, clozapine, lurasidone, quetiapine, ziprasidone) Azapirones (e.g., buspirone, eptapirone, gepirone, perospirone, tandospirone) Bay R 1531 Befiradol...

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Adrenaline

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Agonists 6-FNE Amidephrine Buspirone Cirazoline Corbadrine Deoxyepinephrine (epinine, N-methyldopamine) Desglymidodrine Dexisometheptene Dipivefrine Dopamine...

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