Grimm M, Weidmann P, Meier A, Schiffl H, Ziegler W H
Eur J Clin Pharmacol. 1981;20(2):79-84. doi: 10.1007/BF00607141.
The antihypertensive efficacy and endocrine profile of the new antihypertensive agent, Ro 12-4713, were evaluated in 23 patients (17 men and 6 women) with moderate to severe arterial hypertension. Following addition of Ro 12-4713 to pre-existing therapy with diuretics and beta-blockers or sympatholytics, blood pressure in most of the patients was normalized within one month by a daily dose of 60 to 120 mg. Heart rate was only slightly increased. Orthostatic hypotension was not observed. Weight gain or oedema formation occurred in 14 patients within the first four weeks, but could be controlled satisfactorily by intensified diuretic therapy. Increased hair growth occurred in most of the patients. After a mean duration of treatment of 2.8 months, plasma volume and plasma and urine sodium were unaltered, and plasma potassium was slightly decreased. Plasma renin activity was doubled, whereas plasma aldosterone concentrations were unaltered. Plasma norepinephrine levels were high before and increased only slightly during chronic Ro 12-4713 treatment, whereas urinary norepinephrine excretion was unchanged. Plasma and urinary epinephrine were unaltered by Ro 12-4713. Ro 12-4713 appears to be a potent vasodilator for the combination treatment of hypertension in men.
在23例(17例男性和6例女性)中重度动脉高血压患者中评估了新型抗高血压药物Ro 12 - 4713的降压疗效和内分泌特征。在已有的利尿剂、β受体阻滞剂或交感神经抑制剂治疗基础上加用Ro 12 - 4713后,大多数患者通过每日60至120毫克的剂量在1个月内血压恢复正常。心率仅略有增加。未观察到体位性低血压。14例患者在最初四周内出现体重增加或水肿形成,但通过强化利尿治疗可得到满意控制。大多数患者出现毛发增多。平均治疗2.8个月后,血浆容量、血浆和尿钠未改变,血浆钾略有下降。血浆肾素活性加倍,而血浆醛固酮浓度未改变。慢性Ro 12 - 4713治疗前血浆去甲肾上腺素水平较高,治疗期间仅略有升高,而尿去甲肾上腺素排泄未改变。Ro 12 - 4713对血浆和尿肾上腺素无影响。Ro 12 - 4713似乎是一种有效的血管扩张剂,可用于男性高血压的联合治疗。