Azapirones
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Overview
Azapirones are a class of anxiolytic medications that act as partial agonists at serotonin 5-HT1A receptors. Buspirone is the only azapirone approved for clinical use. Unlike benzodiazepines, azapirones have no sedative, muscle relaxant, or anticonvulsant properties and carry no risk of physical dependence or withdrawal.
How do azapirones work?
Buspirone acts as a partial agonist at presynaptic and postsynaptic serotonin 5-HT1A receptors. At presynaptic autoreceptors, it initially inhibits serotonin firing (which may explain the 2-4 week delay in therapeutic effect), but with chronic administration, these autoreceptors desensitize, leading to enhanced serotonergic transmission. It also has weak dopamine D2 receptor activity. Unlike benzodiazepines, it does not interact with the GABA-benzodiazepine receptor complex.
Drugs in this class
- Buspirone (BuSpar)