Azaspirodecanediones

Brand Name(s) BuSpar, BuSpar Dividose Chemical Class Azaspirodecanedione... 

Beta-adrenoceptor antagonists, particularly propranolol, have been shown to be effective for anxiety symptoms particularly in situational anxiety and GAD. Buspirone, an azaspirodecanedione, is an agonist at 5-HTlA receptors and seems to have anxiolytic effects, though it is less potent than the BDZs and the effects take up to three weeks to become evident. There is high first pass metabolism and a considerable proportion of the effect is due to a metabolite (1-PP). The principal adverse effects of buspirone are nausea, gastrointestinal upset and headache. Antidepressant drugs, both the older tricyclic antidepressants and the newer drugs, have been demonstrated to have anxiolytic effects in mixed anxiety-depressive patients, GAD and panic disorder. 

The anxiolytic agents consist of benzodiazepine derivatives and azaspirodecanedione derivatives. 

The azaspirodecanedione derivatives include buspirone, gepirone, and ipsapirone. 

Figure 9.13. Chemical structure of some azaspirodecanedione anxiolytics.

The anxiolytic agents consist of benzodiazepine derivatives and azaspirodecanedione derivatives. For a long period of... 

Azaspirodecanediones have gained prominence as antipsychotic agents recently. In mid-eighties a member of this family, namely, buspirone was introdueed in the United States and is discussed here. 

Data, expressed as pKj values, are from [56,57,59]. S15535 is from [58], parafluorobenzamide ASD=azaspirodecanedione. 

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