Brodde O-E, Philipp T
Universitätsklinikum Essen, Klinik für Nieren- und Hochdruckkrankheiten, Institut für Pathophysiologie, Hufelandstrasse 55, 45147 Essen.
Dtsch Med Wochenschr. 2006 Nov 10;131(45):2545-50. doi: 10.1055/s-2006-955047.
Beta-blockers exert their effects through blockade of beta-adrenoceptors. First-generation beta-blockers non-selectively block beta1- and beta2-adrenoceptors, while second-generation beta-blockers predominantly block beta1-adrenoceptors. Third-generation beta-blockers possess additional vasodilator properties. Nebivolol is a highly selective b1-blocker with additional vasodilator effects which are mediated by the endothelial L-arginine/nitric oxide system. The hemodynamic action of nebivolol differs from those of first and second-generation beta-blockers: it acutely decreases peripheral resistance (while first and second-generation beta-blockers cause an initial transient increase in peripheral resistance) and decreases in heart rate that are less pronounced than those evoked by first and second-generation beta-blockers. Beta-blockers are frequently used in the treatment of hypertension, coronary artery disease and chronic heart failure. Nebivolol should thus be a suitable drug for treating these diseases, especially since nitric oxide has vasodilator and anti-atherogenic effects. One long-term trial (the SENIORS study) has shown that nebivolol, compared with a placebo, reduced death and hospital admission in elderly patients with chronic heart failure. Additional studies are needed to investigate the clinical relevance of nitric oxide-mediated vasodilatation and to show if nebivolol is as efficacious as the other beta-blockers--metoprolol, bisoprolol and carvedilol--in the treatment of chronic heart failure.
β受体阻滞剂通过阻断β肾上腺素能受体发挥作用。第一代β受体阻滞剂非选择性地阻断β1和β2肾上腺素能受体,而第二代β受体阻滞剂主要阻断β1肾上腺素能受体。第三代β受体阻滞剂具有额外的血管舒张特性。奈必洛尔是一种高度选择性的β1受体阻滞剂,具有额外的血管舒张作用,其由内皮型L-精氨酸/一氧化氮系统介导。奈必洛尔的血流动力学作用不同于第一代和第二代β受体阻滞剂:它能急性降低外周阻力(而第一代和第二代β受体阻滞剂会导致外周阻力最初短暂升高),且心率降低的程度不如第一代和第二代β受体阻滞剂引起的明显。β受体阻滞剂常用于治疗高血压、冠状动脉疾病和慢性心力衰竭。因此,奈必洛尔应该是治疗这些疾病的合适药物,特别是因为一氧化氮具有血管舒张和抗动脉粥样硬化作用。一项长期试验(SENIORS研究)表明,与安慰剂相比,奈必洛尔可降低老年慢性心力衰竭患者的死亡率和住院率。需要进一步研究来调查一氧化氮介导的血管舒张的临床相关性,并确定奈必洛尔在治疗慢性心力衰竭方面是否与其他β受体阻滞剂(美托洛尔、比索洛尔和卡维地洛)一样有效。