药品信息:
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CLINICAL PHARMACOLOGY General Nebivolol is a β-adrenergic receptor blocking agent. In extensive metabolizers (most of the population) and at doses less than or equal to 10 mg, nebivolol is preferentially β1 selective. In poor metabolizers and at higher doses, nebivolol inhibits both β1 - and β2 - adrenergic receptors. Nebivolol lacks intrinsic sympathomimetic and membrane stabilizing activity at therapeutically relevant concentrations. At clinically relevant doses, BYSTOLIC does not demonstrate α1-adrenergic receptor blockade activity. Various metabolites, including glucuronides, contribute to β-blocking activity. Pharmacodynamics The mechanism of action of the antihypertensive response of BYSTOLIC has not been definitively established. Possible factors that may be involved include: (1) decreased heart rate, (2) decreased myocardial contractility, (3) diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers, (4) suppression of renin activity and (5) vasodilation and decreased peripheral vascular resistance. Pharmacokinetics Nebivolol is metabolized by a number of routes, including glucuronidation and hydroxylation by CYP2D6. The active isomer (d-nebivolol) has an effective half-life of about 12 hours in CYP2D6 extensive metabolizers (most people), and 19 hours in poor metabolizers and exposure to d-nebivolol is substantially increased in poor metabolizers. This has less importance than usual, however, because the metabolites, including the hydroxyl metabolite and glucuronides (the predominant circulating metabolites), contribute to β-blocking activity. Plasma levels of d–nebivolol increase in proportion to dose in EMs and PMs for doses up to 20mg. Exposure to l-nebivolol is higher than to d-nebivolol but l-nebivolol contributes little to the drug’s activity as d-nebivolol’s beta receptor affinity is > 1000-fold higher than l-nebivolol. For the same dose, PMs attain a 5-fold higher Cmax and 10-fold higher AUC of d-nebivolol than do EMs. d-Nebivolol accumulates about 1.5-fold with repeated once-daily dosing in EMs. Absorption and Distribution Absorption of BYSTOLIC is similar to an oral solution. The absolute bioavailability has not been determined. Mean peak plasma nebivolol concentrations occur approximately 1.5 to 4 hours post-dosing in EMs and PMs. Food does not alter the pharmacokinetics of nebivolol. Under fed conditions, nebivolol glucuronides are slightly reduced. BYSTOLIC may be administered without regard to meals. The in vitro human plasma protein binding of nebivolol is approximately 98%, mostly to albumin, and is independent of nebivolol concentrations.
奈比洛尔为β-阻段剂系列高血压治疗药物的新成员。12月17日,FDA宣布批准抗高血压新药奈比洛尔(nebivolol,Bystolic)上市。奈比洛尔为β-阻段剂系列高血压治疗药物的新成员。 在美国,成年人高血压发病率约为1/3。高血压平时没有特别症状,但可导致中风、心衰、心脏病发作、肾衰竭甚至死亡的风险,因此常被称作隐行杀手。奈比洛尔为患者控制血压提供了新选择。
3项持续3个月以上的随机双盲多中心安慰剂对照的临床研究评价了奈比洛尔的疗效和安全性。 第4项安慰剂对照研究中,服用其它2种降压药物后降压效果不充分的患者,再接受本品治疗,达到了良好的效果。4项临床研究中总共超过2000例患者服用奈比洛尔,其药效与同类β-阻段剂药物的药效相当。 临床研究中,奈比洛尔最常见不良反应为头疼、疲劳、头晕和腹泻。
Bystolic由北卡罗莱纳州的Mylan Bertek制药公司开发,纽约Forest Laboratories公司负责奈比洛尔的销售。
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