Ruf G, Trenk D, Jähnchen E, Roskamm H
Abteilung für Klinische Pharmakologie, Benedikt Kreutz Rehabilitationszentrum, Bad Krozingen, Germany.
Int J Cardiol. 1994 Mar 1;43(3):279-85. doi: 10.1016/0167-5273(94)90208-9.
The anti-ischemic effect of 5 mg nebivolol o.i.d., a newly developed beta 1-selective adrenoceptor blocking drug with vasodilating properties, was compared with that of atenolol (100 mg o.i.d.) following a treatment period of 6 days. The study was performed in 24 patients with documented coronary artery disease and stable angina pectoris according to a double-blind randomized study, designed using conventional symptom-limited exercise testing. Exercise testing 3 h after the first dose showed a more marked ST-segment reduction by atenolol than by nebivolol (59% vs. 18%). ST-segment depression measured 24 h after administration of the penultimate dose was statistically significantly reduced by nebivolol (from 0.19 +/- 0.07 to 0.13 +/- 0.07 mV; P = 0.0059) but not by atenolol (from 0.17 +/- 0.06 to 0.14 +/- 0.10 mV; P = 0.0703). Approximately 3 h after the last dose, the reduction was comparable (45% and 38% by nebivolol and atenolol, respectively). Exercise duration, exercise time necessary to produce ST-segment depression by 0.1 mV and exercise time to the onset of angina were also prolonged following administration of both drugs. Thus, at steady-state single daily doses of 100 mg atenolol and 5 mg nebivolol were about equieffective when measured at time of maximal effect (i.e. 3 h after drug administration). However, duration of action with respect to the ST-segment depression seems to be slightly longer for nebivolol.
将新开发的具有血管舒张特性的β1选择性肾上腺素能受体阻断药奈必洛尔(每日口服5毫克)的抗缺血作用,与阿替洛尔(每日口服100毫克)在6天治疗期后的抗缺血作用进行了比较。该研究根据双盲随机研究,在24例有冠状动脉疾病记录且患有稳定型心绞痛的患者中进行,采用传统的症状限制运动试验设计。首剂给药3小时后的运动试验显示,阿替洛尔使ST段压低比奈必洛尔更明显(59%对18%)。倒数第二剂给药24小时后测量的ST段压低,奈必洛尔使其有统计学显著降低(从0.19±0.07毫伏降至0.13±0.07毫伏;P = 0.0059),而阿替洛尔则未使其降低(从0.17±0.06毫伏降至0.14±0.10毫伏;P = 0.0703)。末次给药约3小时后,降低程度相当(奈必洛尔和阿替洛尔分别为45%和38%)。两种药物给药后,运动持续时间、使ST段压低0.1毫伏所需的运动时间以及心绞痛发作的运动时间也都延长了。因此,在稳态下,每日单剂量100毫克阿替洛尔和5毫克奈必洛尔在最大效应时(即给药后3小时)测量时约等效。然而,就ST段压低而言,奈必洛尔的作用持续时间似乎略长。