12 Facts About Buspirone

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

Buspirone was first made in 1968 and approved for medical use in the United States in 1986.

Buspirone is used for the short-term and long-term treatment of anxiety disorders or symptoms of anxiety.

Buspirone is relatively well tolerated, and is not associated with sedation, cognitive and psychomotor impairment, muscle relaxation, physical dependence, or anticonvulsant effects.

Buspirone appears to be relatively benign in cases of single-drug overdose, although no definitive data on this subject appear to be available.

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Buspirone has been shown in vitro to be metabolized by the enzyme CYP3A4.

Buspirone has lower affinities for the serotonin 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, and 5-HT7 receptors.

Buspirone has been found to bind with much higher affinity to the dopamine D3 and D4 receptors, where it is similarly an antagonist.

Buspirone has very weak and probably clinically unimportant affinity for the a1-adrenergic receptor.

Buspirone is metabolized primarily by CYP3A4, and prominent drug interactions with inhibitors and inducers of this enzyme have been observed.

Buspirone is a member of the azapirone chemical class, and consists of azaspirodecanedione and pyrimidinylpiperazine components linked together by a butyl chain.

Buspirone was first synthesized by a team at Mead Johnson in 1968 but was not patented until 1980.