ผู้วิจัย/Authors: Vicharn Vichaiya.

ชื่อเรื่อง/Title: Buspirone: Clinical Pharmarcology.

แหล่งที่มา/Source: Journal of The Psychiatric Association of Thailand, Vol. 33, No.3 July-September 1988, P 147-152

รายละเอียด / Details:

Buspirone is an azaspirodecanedione derivative. It is a lipophilic heterocyclic compound which posses anxiolytic activity comparable to those of benzodiazepines. Interestingly, buspirone lacks hypnotic, anticonvulsant and muscle relaxant properties. Thus, it has been term by some authorities and “anxioselective”. This agent was recently approved by Food and Drug Administration of United State of America for the management of anxiety disorders. The mechanism of action appears to involve complex interaction among central nervous system transmitters which differ from those of the benzodiazepines. To summarize, buspirone may enhance noradrenergic and dopaminergic cell firing and suppress serotonergic activity. This agent reaches its peak effect less quickly than diazepam but produces equal anxiolytic action in patients with or without depressive symptoms. To date, no withdrawal symptoms have occurred in patients who abruptly discontinued treatment after taking buspirone for up to 6 months. Most studies assessing the effects of oral buspirone on psychomotor function have been conducted in healthy volunteers and have demonstrated that minimal impairment of cognition and psychomotor function occurs after oral buspirone 20 mg or less. In contrast to benzodiazepines, buspirone does not produce an additive effect when combined with alcohol or other CNS depressants. Buspirone is rapidly and completely absorbed after oral administration; however, the absolute oral bioavailability ranges from 1-13~ because of the “first-pass” metabolism reduces the bioavailability of buspirone. Buspirone is about 95% bound to human plasma proteins in vitro and is bound to both albumin and alpha acid glycoprotein. The mean volume of distribution of buspirone is 5.31 L/kg. Humans metabolize buspirone in the liver by hydroxylation and oxidative dealkylation. The active metabolite is 1-(2-pyrimidinyl)-piperazine or l-PP The drug did not alter hepatic enzymatic activity in animal studies. In healthy subjects the elimination half-life of this agent range from 2 to 11 hours. Various open and double-blind, multiple doses, comparative clinical trials documented the buspirone achieves equivalent antianxiety effects as diazepam and clorazepate in elderly and young patients. The studies also reveal that buspirone may take up to 2 weeks to exert its maximal anxiolytic effects. Adverse effects are headache, dizziness, nervousness, gastrointestinal discomfort and insomnia but 67 to 88% of patients report no side effects. J Psychiatr Ass Thailand 1988; 33(3):

Keywords: buspirone, drug, minor tranquilizer, pharmacy, psychiatry, anxiety disorder, anxiolytic drugs

ปีที่เผยแพร่/Year: 1988

Address: Somdejchaopraya Hospital, Department of Mental Health, Ministry of Public Health.

Code: 100313303212

ISSN/ISBN: 0125-6985

Country of publication: Thailand.

Language: English.

Category: Abstract Journal.

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