Nebivolol:: Comparison of the effects of dl-nebivolol, d-nebivolol, 1-nebivolol, atenolol, and placebo on exercise-induced increases in heart rate and systolic blood pressure

被引:41
作者
Van Neuten, L
De Crée, J
机构
[1] Janssen Res Fdn, Int Clin R&D, B-2340 Beerse, Belgium
[2] Jan Palfijn Hosp, Clin Res Unit, Merksem, Belgium
关键词
dl-nebivolol; d-nebivolol; l-nebivolol; atenolol; beta-blockade; nitric oxide; endothelium;
D O I
10.1023/A:1007760515117
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
The effects of racemic nebivolol, 2.5, 5.0, and 10.0 mg; d-nebivolol, 2.5 mg; 1-nebivolol, 2.5 mg; atenolol, 50 mg; and placebo, each given once daily for 7 days, on exercise-induced increases in heart rate and systolic blood pressure mere compared in a seven-way double-blind randomized crossover trial in 14 healthy male volunteers. Observations on these variables were made 3 and 24 hours after dosing on the first and last days of therapy. Similar effects on both exercise-induced tachycardia and increases in systolic blood pressure were seen with nebivolol 5.0 mg and with d-nebivolol 2.5 mg; 1-nebivolol 2.5 mg mas no different from placebo. These data show that the beta-blocking effects of nebivolol reside in the d-isomer. A dose-related response mas evident with racemic nebivolol in inhibiting exercise-induced tachycardia over the range of doses studied. Whereas the effects of atenolol on both exercise-induced tachycardia and increases in systolic blood pressure were fully evident on the first day of treatment, those of nebivolol, especially with regard to heart rate, and, to a lesser degree, systolic pressure, mere greater on the final than on the first day. Nebivolol had a clearly superior trough-to-peak efficacy ratio than atenolol.
引用
收藏
页码:339 / 344
页数:6
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