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与硝苯地平相比,双醋洛尔(R,R-拉贝洛尔)对高血压患者静息及运动时心率、血压和肌肉血流的影响。

Effects of dilevalol (R,R-labetalol) compared with nifedipine on heart rate, blood pressure and muscle blood flow at rest and on exercise in hypertensive patients.

作者信息

Walley T, Tsao Y, Scott A, Mackay E, Vandenburg M, Breckenridge A

机构信息

Department of Pharmacology and Therapeutics, University of Liverpool.

出版信息

Br J Clin Pharmacol. 1993 Jun;35(6):623-8. doi: 10.1111/j.1365-2125.1993.tb04192.x.

Abstract
  1. Dilevalol (R,R-labetalol) is a non-selective beta-adrenoceptor antagonist with beta 2-adrenoceptor agonist activity. Its effects after 1 month's administration on heart rate, blood pressure and muscle blood flow were studied in a double-blind crossover comparison with nifedipine in 16 hypertensive patients. 2. Dilevalol and nifedipine were similarly effective in lowering systolic and diastolic blood pressure at rest, but dilevalol limited the rise in systolic blood pressure induced by exercise more than nifedipine (rise of 27 vs 53 mm Hg respectively, P < 0.01). 3. Dilevalol decreased resting heart rate compared with nifedipine (73 vs 92 beats min-1 respectively, P < 0.01). Dilevalol limited the exercise induced rise in heart rate more than nifedipine (36 vs 48 beats min-1 respectively, P < 0.01). 4. Muscle blood flow (measured by strain gauge plethysmography) was not affected by either dilevalol or nifedipine at rest. After exercise, dilevalol caused an increase in excess blood flow compared with placebo (10.8 vs 5.1 ml min-1 dl-1 respectively, P < 0.01). The difference between dilevalol and nifedipine did not reach statistical significance (10.8 vs 6.5 ml min-1 dl-1 respectively, P > 0.05). 5. On blood pressure and heart rate, dilevalol demonstrated beta-adrenoceptor blocker activity at rest and on exercise. On muscle blood flow, dilevalol appeared to have no effect at rest, but may have acted as a beta-adrenoceptor blocker rather than as a beta 2-adrenoceptor agonist during exercise.
摘要
  1. 二醋洛尔(R,R-拉贝洛尔)是一种具有β2肾上腺素能受体激动活性的非选择性β肾上腺素能受体拮抗剂。在16例高血压患者中,采用双盲交叉对照试验,比较了二醋洛尔与硝苯地平用药1个月后对心率、血压及肌肉血流的影响。2. 二醋洛尔和硝苯地平在降低静息收缩压和舒张压方面同样有效,但二醋洛尔比硝苯地平更能限制运动诱发的收缩压升高(分别升高27 mmHg和53 mmHg,P<0.01)。3. 与硝苯地平相比,二醋洛尔降低了静息心率(分别为73次/分钟和92次/分钟,P<0.01)。二醋洛尔比硝苯地平更能限制运动诱发的心率升高(分别为36次/分钟和48次/分钟,P<0.01)。4. 静息时,二醋洛尔和硝苯地平均不影响肌肉血流(通过应变片体积描记法测量)。运动后,与安慰剂相比,二醋洛尔使额外血流增加(分别为10.8 ml·min-1·dl-1和5.1 ml·min-1·dl-1,P<0.01)。二醋洛尔与硝苯地平之间的差异未达到统计学显著性(分别为10.8 ml·min-1·dl-1和6.5 ml·min-1·dl-1,P>0.05)。5. 在血压和心率方面,二醋洛尔在静息和运动时均表现出β肾上腺素能受体阻断活性。在肌肉血流方面,二醋洛尔在静息时似乎无作用,但在运动期间可能作为β肾上腺素能受体阻断剂而非β2肾上腺素能受体激动剂发挥作用。

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