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对具有内在拟交感活性的β受体阻滞剂的降压和激素反应:吲哚洛尔与依泮洛尔的比较。

Antihypertensive and hormonal responses to beta-blockade with intrinsic sympathomimetic activity: pindolol versus epanolol.

作者信息

Simon G, Wittig V J

机构信息

Veterans Administration Medical Center, Minneapolis, Minnesota 55417.

出版信息

J Cardiovasc Pharmacol. 1987 Nov;10(5):543-7. doi: 10.1097/00005344-198711000-00008.

Abstract

After a 2-week placebo period, 30 men, aged 60 years (mean), with mild or moderate hypertension were randomly assigned to one of three treatment groups: pindolol, 10 mg b.i.d.; epanolol, 200 mg b.i.d.; and epanolol, 400 mg q.d. At the end of the placebo period and of 4 weeks of active treatment, heart rate, blood pressure, plasma renin activity (PRA), and nonepinephrine (NE) concentration of subgroups of subjects, were measured during isoproterenol infusion (30 ng/kg.min-1 for 15 min) and submaximal ergometric exercise (89 W, mean). Sitting heart rates were reduced with 200 mg b.i.d. epanolol (p less than 0.01) but unchanged with pindolol and 400 mg q.d. epanolol. Reductions of systolic and diastolic blood pressures occurred in all treatment groups but were most pronounced with pindolol. Isoproterenol-induced cardioacceleration and rise in PRA and plasma NE concentration were abolished by pindolol but only attenuated by epanolol. Pindolol also abolished the isoproterenol-induced reduction in diastolic blood pressure; epanolol had no effect on it. The hemodynamic and hormonal responses to exercise were attenuated by pindolol and epanolol in proportion to their beta-blocking activities. In the doses used, epanolol had moderate beta 1-selective blocking action. The intrinsic sympathomimetic activity of epanolol is dose dependent.

摘要

在为期2周的安慰剂期后,30名平均年龄为60岁的轻度或中度高血压男性被随机分配到三个治疗组之一:吲哚洛尔,每日2次,每次10毫克;依泮洛尔,每日2次,每次200毫克;依泮洛尔,每日1次,每次400毫克。在安慰剂期结束时以及4周的积极治疗结束时,在异丙肾上腺素输注(30纳克/千克·分钟 -1,持续15分钟)和次极量测力计运动(平均89瓦)期间,测量了各亚组受试者的心率、血压、血浆肾素活性(PRA)和去甲肾上腺素(NE)浓度。每日2次服用200毫克依泮洛尔可降低静息心率(p小于0.01),但吲哚洛尔和每日1次服用400毫克依泮洛尔时静息心率无变化。所有治疗组的收缩压和舒张压均有所降低,但吲哚洛尔组最为明显。吲哚洛尔可消除异丙肾上腺素诱导的心动加速以及PRA和血浆NE浓度升高,但依泮洛尔仅使其减弱。吲哚洛尔还消除了异丙肾上腺素诱导的舒张压降低;依泮洛尔对此无影响。吲哚洛尔和依泮洛尔对运动的血流动力学和激素反应的减弱程度与其β受体阻断活性成比例。在所使用的剂量下,依泮洛尔具有中度β1选择性阻断作用。依泮洛尔的内在拟交感活性呈剂量依赖性。

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