Buspirone
- Atc Codes:N05BE01
- CAS Codes:33386-08-2#36505-84-7
- PHARMGKB ID:33386-08-2#36505-84-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Buspar; Cyprus: Anxiron, Busiral, Kallmiren; Czech Republic: Buspiron; Denmark: Buspiron; Finland: Anksilon, Buspar, Buspiron; France: Buspar, Buspirone; Germany: Anxut, Busp, Buspar; Greece: Abivax, Anchocalm, Antipsichos, Bergamol, Bespar, Boronex, Buspirone, Epsilast, Hiremon, Hobatstress, Komasin, Lanamont, Lebilon, Ledion, Lostress, Loxapin, Nadrifor, Nervostal, Nevrorestol, Norbal, Pendium, Stressigal, Svitalark, Tendan, Tensipes, Trafuril, Umolit, Vulbefer; Hungary: Anxiron, Spitomin; Ireland: Buspar; Luxembourg: Buspar; Netherlands: Buspiron; Poland: Buspirone, Buxal, Mabuson, Spamilan; Portugal: Ansiten, Busansil, Buscalma, Buspar, Itagil; Romania: Spitomin, Stressigal; Slovakia: Anxiron, Spitomin; Spain: Buspar, Buspirona; Sweden: Buspar, Buspiron; UK: Buspar, Buspirone.
North America
Canada: Buspar, Buspirex, Buspirone, Bustab; USA: Buscar, Buspirone.
Latin America
Argentina: Ansial, Aristopirón; Brazil: Ansitec, Buspar; Mexico: Buspar.
Drug combinations
Chemistry
Buspirone Hydrochloride: C~21~H~31~N~5~O~2~ HCl. Mw: 421.96. (1) 8-Azaspiro[4,5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, monohydrochloride; (2) N-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-1,1-cyclopentanediacetamide monohydrochloride. CAS-33386-08-2; CAS-36505-84-7 (buspirone)(1973).
Pharmacologic Category
Anxiolytics, Sedatives, and Hypnotics; Miscellaneous. (ATC-Code: N05BE01).
Mechanism of action
Decreases the spontaneous firing of serotonin-containing neurons in the CNS by selectively binding to and acting as agonist at presynaptic CNS serotonin 5-HT~1A~ receptors. Possesses partial agonist activity (mixed agonist/antagonist) at postsynaptic 5-HT~2A~ receptors. Does not bind to benzodiazepine-GABA receptors. Binds to dopamine D~2~ receptors. May have other effects on other neurotransmitter systems.
Therapeutic use
Management of generalized anxiety disorder and for short-term relief of symptoms of anxiety.
Pregnancy and lactiation implications
There are no adequate studies in pregnant women. Use not recommended during lactation.
Unlabeled use
Management of aggression in mental retardation and secondary mental disorders. Major depression. Potential augmenting agent for antidepressants. Premenstrual syndrome.
Contraindications
Hypersensitivity to buspirone or any component of the formulation. Severe hepatic/renal impairment.
Warnings and precautions
Low potential for cognitive or motor impairment. Restlessness syndrome reported (may be attributable to buspirone’s antagonism of central dopamine receptors). Use with MAO inhibitors may result in hypertensive reactions (should not be used concurrently or within 10 days). Tolerance of buspirone’s adverse effects (e.g. dizziness) may be slightly less in geriatric patients than in younger adults. Buspirone is relatively nonsedating compared with other currently available anxiolytics (e.g. benzodiazepines). Dream disturbances may occur (although a causal relationship to the drug has not been established). The potential of buspirone for causing acute and chronic changes in dopamine-mediated neurologic function (e.g. dystonia, parkinsonian-like manifestations, akathisia, tardive dyskinesia) has not been fully elucidated. Myoclonus, which may have been serotonergically mediated, also reported. Use in severe hepatic/renal imparirment is not recommended.