Floras J S, Hassan M O, Jones J V, Sleight P
J Am Coll Cardiol. 1985 Jul;6(1):186-95. doi: 10.1016/s0735-1097(85)80273-4.
The ability of cardioselective and nonselective beta-adrenoceptor blocking drugs, with and without partial agonist activity, to control increases in blood pressure associated with mental and physical activity was compared in 35 subjects with hypertension. Direct measurements of blood pressure and radioenzymatic determinations of plasma norepinephrine were obtained before, during and after four activities, and were repeated after random allocation to treatment with atenolol, metoprolol, pindolol or propranolol. Cardioselective and nonselective drugs modestly reduced the pressor response to reaction time testing, but not to mental arithmetic or isometric exercise. The increase in systolic blood pressure during bicycling was attenuated significantly by the cardioselective drugs atenolol (by 23 mm Hg, or 38%) and metoprolol (21 mm Hg, or 41%), but not by the nonselective agents pindolol (with partial agonist activity) (13 mm Hg, or 20%) and propranolol (10 mm Hg, or 17%) (p less than 0.02 cardioselective versus nonselective; p = NS pindolol versus propranolol). Only bicycle exercise increased plasma norepinephrine concentrations (by 80%). These results suggest that beta-adrenoceptor blocking drugs will not attenuate increases in blood pressure during mental or physical activities unless intense sympathoadrenal activation also occurs. Marked elevations in circulating epinephrine, with or without norepinephrine, and peripheral beta 2-blockade appear necessary for alpha-mediated vasoconstriction to predominate and for the contrasting effects of cardioselective and nonselective drugs to be appreciated.
在35名高血压患者中,比较了具有和不具有部分激动剂活性的心脏选择性和非选择性β-肾上腺素能受体阻断药物控制与精神和体力活动相关的血压升高的能力。在四项活动之前、期间和之后,直接测量血压并通过放射酶法测定血浆去甲肾上腺素,并在随机分配接受阿替洛尔、美托洛尔、吲哚洛尔或普萘洛尔治疗后重复测量。心脏选择性和非选择性药物适度降低了对反应时间测试的升压反应,但对心算或等长运动没有作用。在骑自行车过程中,心脏选择性药物阿替洛尔(收缩压降低23 mmHg,即38%)和美托洛尔(收缩压降低21 mmHg,即41%)显著减弱了收缩压的升高,但有部分激动剂活性的非选择性药物吲哚洛尔(收缩压降低13 mmHg,即20%)和普萘洛尔(收缩压降低10 mmHg,即17%)则没有(心脏选择性药物与非选择性药物相比,P<0.02;吲哚洛尔与普萘洛尔相比,P=无显著性差异)。只有骑自行车运动增加了血浆去甲肾上腺素浓度(增加80%)。这些结果表明,除非同时发生强烈的交感肾上腺激活,β-肾上腺素能受体阻断药物不会减弱精神或体力活动期间的血压升高。循环肾上腺素显著升高,无论有无去甲肾上腺素,以及外周β2受体阻断似乎是α介导的血管收缩占主导以及认识到心脏选择性和非选择性药物的对比作用所必需的。