Davies R, Payne N N, Slater J D
Am J Cardiol. 1976 Mar 31;37(4):637-41. doi: 10.1016/0002-9149(76)90408-2.
Beta adrenergic receptor antagonists (beta blockers) differ greatly in their cardioselectivity and intrinsic sympathomimetic activity, and these differences may have important therapeutic consequences. We have therefore studied the effect on blood pressure, heart rate and plasma renin activity of the beta blocking drug oxprenolol (Trasicor) which has considerable intrinsic sympathomimetic activity, both alone and in combination with the benzothiadiazine cyclopenthiazide. Eleven patients with mild to moderate benign essential hypertension were randomly allocated to one of two treatment groups. Oxprenolol was given as the first drug to Group 1, and cyclopenthiazide as the first drug to Group 2. The patients were assessed before the start of treatment, after 2 to 3 weeks of treatment with one drug and after a further 2 to 3 weeks of treatment with both drugs. Heart rate, blood pressure and plasma renin activity were measured with the patients recumbent and after a standardized tilt to 85 degrees to provide a reflection of day to day cardiovascular stress. Oxprenolol reduced arterial blood pressure without inducing significant bradycardia. The addition of cyclopenthiazide had little further effect. Oxprenolol alone suppressed plasma renin activity both at rest and during tilt and also abolished the increase in plasma renin activity after administration of cyclopenthiazide. The combination of (1) moderate reduction of blood pressure. (2) inhibition of the otherwise inevitable increase in plasma renin activity with the use of a diuretic drug, and (3) only moderate inhibition of overall sympathetic activity indicates that it is possible to achieve physiologic balance with the appropriate beta blocking drug.
β肾上腺素能受体拮抗剂(β受体阻滞剂)在心脏选择性和内在拟交感活性方面差异很大,这些差异可能具有重要的治疗意义。因此,我们研究了具有相当内在拟交感活性的β受体阻滞剂氧烯洛尔(心得平)单独使用以及与苯并噻二嗪类环戊噻嗪联合使用时对血压、心率和血浆肾素活性的影响。11例轻度至中度良性原发性高血压患者被随机分为两个治疗组。氧烯洛尔作为第一种药物给予第1组,环戊噻嗪作为第一种药物给予第2组。在治疗开始前、使用一种药物治疗2至3周后以及两种药物进一步治疗2至3周后对患者进行评估。在患者卧位时以及在标准化倾斜至85度后测量心率、血压和血浆肾素活性,以反映日常心血管应激情况。氧烯洛尔降低动脉血压而不引起明显心动过缓。加用环戊噻嗪几乎没有进一步影响。单独使用氧烯洛尔在静息和倾斜时均抑制血浆肾素活性,并且也消除了给予环戊噻嗪后血浆肾素活性的升高。(1)适度降低血压、(2)抑制使用利尿剂时血浆肾素活性不可避免的升高以及(3)仅适度抑制总体交感神经活性的联合作用表明,使用合适的β受体阻滞剂有可能实现生理平衡。