Predel H G, Mainka W, Schillings W, Knigge H, Montiel J, Fallois J, Agrawal R, Schramm T, Graf C, Giannetti B M, Bjarnason-Wehrens B, Prinz U, Rost R E
Institute of Cardiology and Sports Medicine, German Sports University, Cologne, Germany.
J Hum Hypertens. 2001 Oct;15(10):715-21. doi: 10.1038/sj.jhh.1001257.
The present study was designed to investigate the integrated effects of the beta-1-selective blocker with vasodilator properties, nebivolol, on systemic haemodynamics, neurohormones and energy metabolism as well as oxygen uptake and exercise performance in physically active patients with moderate essential hypertension (EH).
Eighteen physically active patients with moderate EH were included: age: 46.9 +/- 2.38 years, weight: 83.9 +/- 2.81 kg, blood pressure (BP): 155.8 +/- 3.90/102.5 +/- 1.86 mm Hg, heart rate: 73.6 +/- 2.98 min(-1). After a 14-day wash-out period a bicycle spiroergometry until exhaustion (WHO) was performed followed by a 45-min submaximal exercise test on the 2.5 mmol/l lactate-level 48 h later. Before, during and directly after exercise testing blood samples were taken. An identical protocol was repeated after a 6-week treatment period with 5 mg nebivolol/day.
Nebivolol treatment resulted in a significant (P < 0.01) decrease in systolic and diastolic BP and heart rate at rest and during maximal and submaximal exercise. Maximal physical work performance, blood lactate and rel. oxygen uptake (rel. VO(2)) before and after nebivolol treatment at rest and during maximal and submaximal exercise remained unaltered. Free fatty acid, free glycerol, plasma catecholamines, beta-endorphines and atrial natriuretic peptide (ANP) increased before and after treatment during maximal and submaximal exercise but remained unaltered by nebivolol treatment. In contrast, plasma ANP levels at rest were significantly higher in the presence of nebivolol, endothelin-1 levels were unchanged.
Nebivolol was effective in the control of BP at rest and during exercise in patients with EH. Furthermore, nebivolol did not negatively affect lipid and carbohydrate metabolism and substrate flow. The explanation for the effects on ANP at rest remain elusive. This pharmacodynamic profile of nebivolol is potentially suitable in physically active patients with EH.
本研究旨在探讨具有血管舒张特性的β1选择性阻滞剂奈必洛尔对中度原发性高血压（EH）且身体活动的患者的全身血流动力学、神经激素和能量代谢以及摄氧量和运动表现的综合影响。
纳入18例中度EH且身体活动的患者：年龄：46.9±2.38岁，体重：83.9±2.81 kg，血压（BP）：155.8±3.90/102.5±1.86 mmHg，心率：73.6±2.98次/分钟（-1）。经过14天的洗脱期后，进行力竭性自行车运动心肺功能测试（WHO），48小时后在2.5 mmol/l乳酸水平下进行45分钟的次最大运动测试。在运动测试前、期间和刚结束后采集血样。在接受5 mg奈必洛尔/天治疗6周后重复相同方案。
奈必洛尔治疗导致静息、最大和次最大运动时收缩压和舒张压以及心率显著降低（P<0.01）。奈必洛尔治疗前后静息、最大和次最大运动时的最大体力工作表现、血乳酸和相对摄氧量（rel.VO₂）保持不变。最大和次最大运动期间治疗前后游离脂肪酸、游离甘油、血浆儿茶酚胺、β-内啡肽和心钠素（ANP）升高，但奈必洛尔治疗使其保持不变。相比之下，服用奈必洛尔时静息血浆ANP水平显著更高，内皮素-1水平未改变。
奈必洛尔对EH患者静息和运动时的血压控制有效。此外，奈必洛尔对脂质和碳水化合物代谢以及底物流动无负面影响。静息时对ANP影响的解释仍不清楚。奈必洛尔的这种药效学特征可能适用于中度EH且身体活动的患者。
