Azaspirodecanedione

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Azaspirodecanediones are a class of drugs with anxiolytic effects used in the treatment of anxiety. Azaspirodecanediones have fewer side effects than some other common antianxiety drugs such as benzodiazepines. Unlike benzodiazepines, azaspirodecanediones are not addictive and do not induce tolerance. They are thought to agonize serotonin (specifically the 5-HT1A receptor), primarily in the hippocampus.

Examples

The common azaspirodecanediones used include buspirone (Buspar), gepirone, and ipsapirone.

Pharmacokinetics

Buspirone is well absorbed from the gastrointestinal tract, and peak blood levels are achieved in 1 to 1.5 hours; the drug is more than 95% bound to plasma proteins. Buspirone is extensively metabolized, with less than 1% of the parent drug excreted into the urine unchanged. At least one of the metabolic products of buspirone is biologically active. The parent drug has an elimination half-life of 4 to 6 hours.

Uses

Useful as an augmentation to SSRI for Parkinson's disease, social phobia, MD and sexual dysfunction.



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