Magnani B, Ambrosioni E, Costa F V, Malini P L, Magelli C
Int J Clin Pharmacol Ther Toxicol. 1981 Oct;19(10):440-4.
In a double-blind, cross-over trial, 37 hypertensive patients were treated in random order, after a 4-week run-in period, with 100 mg atenolol in a single daily dose, or 250 mg methyldopa three times daily (or 500 mg three times daily in case of poor response). Both therapeutic regimens significantly reduced blood pressure (13/13 mmHg for atenolol and 17/10 mmHg for methyldopa) in an erect position. The higher dose of methyldopa gave a further significant reduction only for the systolic standing blood pressure. No statistical difference was found between the antihypertensive activity of the two drugs, but atenolol reduced heart rate more than did methyldopa. Side effects occurred more frequently during methyldopa administration and most often during the first days of treatment. During exercise (treadmill test) the two drugs induced the same antihypertensive response, but atenolol provoked a greater reduction of exercise tachycardia. Whereas total oxygen consumption was not affected by the two drugs, atenolol induced a much greater reduction of the myocardial oxygen consumption evaluated by the product of the systolic blood pressure X heart rate. These findings show that atenolol at the 100-mg daily dose is as effective as the full dosage of methyldopa and in addition shows better tolerance, a simpler therapeutic scheme, and less incidence of side effects.
在一项双盲交叉试验中,37名高血压患者在经过4周的导入期后,被随机安排接受治疗,分别为每日单次服用100毫克阿替洛尔,或每日三次服用250毫克甲基多巴(若反应不佳则每日三次服用500毫克)。两种治疗方案均能显著降低直立位血压(阿替洛尔降低13/13毫米汞柱,甲基多巴降低17/10毫米汞柱)。较高剂量的甲基多巴仅使收缩期站立血压进一步显著降低。两种药物的降压活性无统计学差异,但阿替洛尔降低心率的作用比甲基多巴更强。甲基多巴给药期间副作用出现得更频繁,且大多在治疗的头几天出现。在运动(跑步机测试)期间,两种药物产生相同的降压反应,但阿替洛尔能更显著地降低运动性心动过速。两种药物均未影响总耗氧量,但阿替洛尔通过收缩压×心率的乘积评估,能更显著地降低心肌耗氧量。这些研究结果表明,每日100毫克剂量的阿替洛尔与全剂量甲基多巴效果相当,此外还具有更好的耐受性、更简单的治疗方案和更低的副作用发生率。