Baldwin Claudine M, Keam Susan J
Wolters Kluwer Health Adis, Auckland, New Zealand.
Am J Cardiovasc Drugs. 2009;9(4):253-60. doi: 10.2165/1120274-000000000-00000.
Nebivolol is a beta-adrenergic receptor antagonist with a dual mechanism of action. It shows high selectivity for beta(1)-adrenergic receptors and appears to have nitric oxide-mediated vasodilatory activity. Once-daily nebivolol effectively lowered BP in patients with mild to moderate hypertension in four randomized, double-blind, placebo-controlled, 12-week trials. Trough sitting DBP and SBP were reduced to a significantly greater extent in nebivolol than in placebo recipients in trials in demographically heterogenous hypertensive patient groups, as well as in trials involving only Black patients and in patients continuing previous stable antihypertensive drug therapies. Treatment response (defined as a mean sitting DBP <90 mmHg or a >or=10 mmHg reduction from baseline) rates were significantly higher in nebivolol versus placebo recipients in trials enrolling patient groups considered representative of the US hypertensive population (46-65% vs 25%), in Black patients (57-64% vs 27%), and in patients concurrently treated with other antihypertensive drugs (53-65% vs 41%). Nebivolol was generally well tolerated in the treatment of hypertension, with the majority of adverse events described as being mild or moderate in severity. The incidences of fatigue, bradycardia, dyspnea, depression, and erectile dysfunction (events commonly associated with beta-adrenergic receptor antagonist use) did not significantly differ between nebivolol and placebo recipients in the 12-week trials.
奈必洛尔是一种具有双重作用机制的β-肾上腺素能受体拮抗剂。它对β1-肾上腺素能受体表现出高度选择性,并且似乎具有一氧化氮介导的血管舒张活性。在四项随机、双盲、安慰剂对照的12周试验中,每日一次的奈必洛尔有效地降低了轻至中度高血压患者的血压。在人口统计学特征各异的高血压患者组试验中,以及在仅涉及黑人患者和继续接受先前稳定抗高血压药物治疗的患者的试验中,奈必洛尔组的低谷坐位舒张压和收缩压降低幅度均显著大于安慰剂组。在纳入被认为代表美国高血压人群的患者组(46 - 65%对25%)、黑人患者(57 - 64%对27%)以及同时接受其他抗高血压药物治疗的患者(53 - 65%对41%)的试验中,奈必洛尔组的治疗反应率(定义为平均坐位舒张压<90 mmHg或较基线降低≥10 mmHg)显著高于安慰剂组。奈必洛尔在高血压治疗中总体耐受性良好,大多数不良事件的严重程度被描述为轻度或中度。在12周试验中,奈必洛尔组和安慰剂组之间疲劳、心动过缓、呼吸困难、抑郁和勃起功能障碍(通常与使用β-肾上腺素能受体拮抗剂相关的事件)的发生率没有显著差异。