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~86% Use in Specific Populations Special Populations: Renal Function ImpairmentĪUC increased 4-fold. Serum: 40 to 90 minutes Half-Life EliminationĢ to 3 hours increased with renal or hepatic impairment Protein Binding Urine: 29% to 63% (primarily as metabolites) feces: 18% to 38% Time to Peak Hepatic oxidation, primarily via CYP3A4 to several metabolites including an active metabolite, 1-pyrimidinylpiperazine (1-PP exhibits about 25% of the activity of buspirone) extensive first-pass effect Excretion

Rapid and complete bioavailability is limited by extensive first-pass effect only ~1% of the oral dose reaches the systemic circulation unchanged Distribution Pharmacokinetics/Pharmacodynamics Absorption Buspirone has moderate affinity for dopamine D 2 receptors.

Buspirone has a high affinity for serotonin 5-HT 1A and 5-HT 2 receptors, without affecting benzodiazepine-GABA receptors. The mechanism of action of buspirone is unknown.