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动物试验证明,乌拉地尔(urapidil,简称URA)具有α_1阻滞活性和中枢降压作用,后者可能与本品兴奋脑干中的5-HT_(1A)受体有关。动物试验还证明,URA有轻微的β_1阻滞活性及弱的触突前α_2阻滞作用和部分β_1激动作用。 URA口服吸收迅速且良好,口服URA缓释胶囊30mg后,生物利用度为72%,t_(max)为4～6小时,C_(max)为104～232μg/L,终末t_(1/2)为4.7小时,静注URA 25mg,血浆药物浓度呈双指数下降,分布相t_(1/2)为35分钟,清除相t_(1/2)为2.7小时,分布容积为0.58～1.16L/kg,蛋白结合率约为80%。URA在肝脏广
Animal experiments show that urapidil (Urapidil, URA) has α_1 blocking activity and central hypotensive effect, the latter may be related to excited 5-HT_ (1A) receptor in brain stem. Animal experiments also demonstrated that URA has a slight β 1 blocking activity and a weak pre-synaptic α 2 block and partial β 1 agonism. URA oral absorption quickly and well, oral administration of URA sustained-release capsules 30mg, bioavailability was 72%, t max 4 to 6 hours, C max 104 ~ 232μg / L, the terminal t_ (1/2 ) For 4.7 hours, intravenous URA 25mg, plasma drug concentration showed a double exponential decline, the distribution phase t_ (1/2) for 35 minutes, clear phase t_ (1/2) for 2.7 hours, the distribution volume of 0.58 ~ 1.16L / kg, protein binding rate of about 80%. URA is wide in the liver