Država: Sjedinjene Američke Države
Jezik: engleski
Izvor: NLM (National Library of Medicine)
BUSPIRONE HYDROCHLORIDE (UNII: 207LT9J9OC) (BUSPIRONE - UNII:TK65WKS8HL)
Major Pharmaceuticals
BUSPIRONE HYDROCHLORIDE
BUSPIRONE HYDROCHLORIDE 15 mg
PRESCRIPTION DRUG
Abbreviated New Drug Application
BUSPIRONE HYDROCHLORIDE- BUSPIRONE HYDROCHLORIDE TABLET MAJOR PHARMACEUTICALS ---------- BUSPIRONE HYDROCHLORIDE TABLETS, USP 5200 RX ONLY DESCRIPTION Buspirone hydrochloride is an antianxiety agent that is not chemically or pharmacologically related to the benzodiazepines, barbiturates, or other sedative/anxiolytic drugs. Buspirone hydrochloride is a white crystalline, water soluble compound. Chemically, buspirone hydrochloride is _N_-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,1-cyclopentanediacetamide monohydrochloride, which can be represented by the following structural formula: C H N O •HCl MW 421.96 Each tablet, for oral administration, contains 15 mg of buspirone hydrochloride, USP (equivalent to 13.7 mg of buspirone free base). The 15 mg tablets are scored such that they may be bisected. Thus, a single 15 mg tablet can provide the following doses: 15 mg (entire tablet), 10 mg (two-thirds of a tablet), 5 mg (one-third of a tablet). Buspirone hydrochloride tablets, USP contain the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. CLINICAL PHARMACOLOGY The mechanism of action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. _In vitro_ preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT ) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding _in vitro_ or _in vivo_ when tested in preclinical models. Buspirone has moderate affinity for brain D -dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. Buspirone is rapidly absorbed in man and undergoes extensive first-pass metabolism. In a radiolabeled study, unchanged buspirone in the plasma accounted for on Pročitajte cijeli dokument