Buspirone Hydrochloride: A Unique New Anxiolytic Agent; Pharmacokinetics, Clinical Pharmacology, Abuse Potential and Clinical Efficacy

Abstract

Buspirone is the first of a new class of anxioselective agents, the azaspirodecanediones. It achieves peak serum concentrations within one hour and has a serum half-life of 2 to 5 hours. Animal studies have suggested antianxiety activity and the absence of abuse potential. Buspirone is both a dopamine agonist and antagonist, and appears to interact with numerous neurochemical systems in the brain, but not with gamma-aminobutyric acid or at benzodiazepine receptors. Buspirone increases prolactin and growth hormone levels under experimental conditions. In healthy subjects, it has much less effect on psychomotor performance and electroencephalographic results than diazepam. Buspirone offsets some of the impairment due to alcohol when the agents are combined. The drug has anxiolytic properties comparable to those of diazepam, with less sedating effects. It had no abuse potential in tests with casual drug users.