Van Bortel L M, van Baak M A
Department of Pharmacology, University of Limburg, Maastricht, The Netherlands.
Cardiovasc Drugs Ther. 1992 Jun;6(3):239-47. doi: 10.1007/BF00051145.
Patients treated with beta-blocking agents often complain of fatigue during exercise. Exercise capacity is decreased under this condition. Nebivolol is a new beta 1-adrenoceptor antagonist with a particular hemodynamic profile, which might be due to an ancillary property. Five milligrams once daily seems the optimal dose for antihypertensive treatment. In a double-blind, placebo-controlled crossover study, the effects of nebivolol on maximal and endurance exercise capacity are compared with those of atenolol in healthy volunteers. The hemodynamic and metabolic effects during exercise are also studied. Nebivolol 5 mg once daily and atenolol 100 mg once daily decrease blood pressure at rest similarly. At these dosages nebivolol shows a smaller decrease in heart rate than atenolol. During exercise, the rise in systolic blood pressure and heart rate is less depressed with nebivolol than with atenolol. In contrast to atenolol, nebivolol does not decrease maximal and endurance exercise capacity, and does not increase perceived exertion significantly. Changes in hemodynamics influence maximal exercise capacity. Since nebivolol has less effect on exercise hemodynamics than atenolol, this might explain why maximal work capacity is not changed during nebivolol. During endurance exercise metabolic effects are thought to be more important. Under nebivolol glycerol and NEFA production is less depressed during exercise and might explain the preserved endurance capacity. These data suggest less beta blockade during nebivolol than during atenolol at the dosages used in this study. In conclusion, at a dose known to be antihypertensive, nebivolol does not alter exercise capacity significantly in healthy volunteers.
接受β受体阻滞剂治疗的患者在运动时常常抱怨疲劳。在此情况下运动能力会下降。奈必洛尔是一种新型β1肾上腺素能受体拮抗剂,具有独特的血流动力学特征,这可能归因于其辅助特性。每日一次5毫克似乎是抗高血压治疗的最佳剂量。在一项双盲、安慰剂对照的交叉研究中,将奈必洛尔对最大运动能力和耐力运动能力的影响与阿替洛尔在健康志愿者中的影响进行了比较。还研究了运动期间的血流动力学和代谢效应。奈必洛尔每日一次5毫克和阿替洛尔每日一次100毫克在静息时降低血压的效果相似。在这些剂量下,奈必洛尔导致的心率下降幅度小于阿替洛尔。在运动期间,与阿替洛尔相比,奈必洛尔对收缩压和心率升高的抑制作用较小。与阿替洛尔不同,奈必洛尔不会降低最大运动能力和耐力运动能力,也不会显著增加主观用力感觉。血流动力学变化会影响最大运动能力。由于奈必洛尔对运动血流动力学的影响小于阿替洛尔,这可能解释了在使用奈必洛尔期间最大工作能力为何没有改变。在耐力运动期间,代谢效应被认为更为重要。在奈必洛尔治疗下,运动期间甘油和游离脂肪酸的产生受到的抑制较小,这可能解释了耐力能力得以保留的原因。这些数据表明,在本研究使用的剂量下,奈必洛尔的β受体阻滞作用比阿替洛尔小。总之,在已知具有抗高血压作用的剂量下,奈必洛尔不会显著改变健康志愿者的运动能力。