Country: South Africa
Language: English
Source: South African Health Products Regulatory Authority (SAHPRA)
Bm_squib
BUSPAR 10 mg TABLETS SCHEDULING STATUS S5 PROPRIETARY NAME (and dosage form) BUSPAR 10 mg TABLETS COMPOSITION Tablets containing 10 mg buspirone hydrochloride. PHARMACOLOGICAL CLASSIFICATION A 2.6.5 Tranquillizers, miscellaneous structures. PHARMACOLOGICAL ACTION BUSPAR, buspirone hydrochloride (an azapirone) is an anxiolytic agent. It is not chemically or pharmacologically related to the benzodiazepines and in animal studies it does not appear to interact directly with either the benzodiazepine or GABA receptors. In vitro pre-clinical studies have shown that buspirone has a high affinity for sertonin (5-HT 1A ) receptors. However, in man, details of its mechanism of anxiolytic action remain to be elucidated. In humans, BUSPAR is rapidly absorbed, reaching peak plasma levels 60 to 90 minutes after dosing. The mean plasma concentration of buspirone hydrochloride appears to be linearly related to the administered dose. Administration of BUSPAR with food results in higher blood levels of unchanged buspirone, but the clinical significance of this finding is unknown. BUSPAR is approximately 95% bound by human plasma proteins. In pharmacokinetic studies mean plasma half-lives have varied from 2 to 11 hours. BUSPAR is excreted primarily as metabolites of buspirone hydrochloride in the urine. Buspar is metabolised primarily by oxidation, which in vitro has been shown to be mediated by cytochrome P450 3A4 (CYP3A4). Several hydroxylated derivatives of BUSPAR are produced along with 1-pyrimidinyl piperazine, which is pharmacologically active. The latter is approximately 20% as active as BUSPAR in animal models, predictive of anxiolytic activity in humans. Buspirone clearance is reduced in patients with hepatic impairment as well as in patients with impaired renal function. INDICATIONS BUSP Read the complete document