Buspirone

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

Not to be confused with Bupropion.

Buspirone
Clinical data
Pronunciation/ˈbjuːspɪroʊn/ (BEW-spi-rohn)
Trade namesBuspar, Namanspin
Other namesMJ 9022-1
AHFS/Drugs.comMonograph
MedlinePlusa688005
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class C1 (Other controlled substances)
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability3.9%
Protein binding86–95%
MetabolismLiver (via CYP3A4)
Metabolites5-OH-Buspirone; 6-OH-Buspirone; 8-OH-Buspirone; 1-PPTooltip 1-(2-pyrimidinyl)piperazine
Elimination half-life2.5 hours
ExcretionUrine: 29–63%
Feces: 18–38%
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
Chemical and physical data
FormulaC21H31N5O2
Molar mass385.512 g·mol−1
3D model (JSmol)
SMILES
  • 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 Y
  • Key:QWCRAEMEVRGPNT-UHFFFAOYSA-N Y
  (verify)

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

Buspirone was developed in 1968 and approved for medical use in the United States in 1986. It is available as a generic medication. In 2021, it was the 53rd most-commonly prescribed medication in the United States, with more than 12 million prescriptions.

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