Jounela A J, Pentikäinen P J, Neuvonen P J
Int J Clin Pharmacol Biopharm. 1978 Apr;16(4):183-8.
Trimepranol (TMP) is a new propranolol-like, non-selective beta-adrenoreceptor blocking drug. Its antihypertensive effect versus placebo was evaluated in a double-blind corss-over study in 25 ambulatory patients, whose supine diastolic blood pressure (BP) was at least 95 mm Hg. After four weeks treatment with placebo, the dose of TMP was titrated weekly until the supine diastolic BP was below 95 mm Hg or intolerable side effects occurred. The trimepranol dose thus determined was 10 mg bid for three patients, 20 mg bid for twelve patients and 40 mg bid for ten patients. The subsequent double-blind cross-over study consisted of two six weeks treatment periods, either with trimepranol followed by placebo (Group I) or in reverse order (Group II). BP and heart rate at the end of these periods were compared. Supine BP fell from 156 +/- 3/105 +/- 2 mm Hg at the end of placebo periods to 140 +/- 2/93 +/- 1 mm Hg (p less than 0.001) for systolic and diastolic BP at the end of trimepranol periods, when the data of Groups I and II are pooled. In 19 out of 25 patients, supine diastolic BP declined below 95 mmHg during the trimepranol period. A statistically significant correlation was found between the antihypertensive and bradycardic effects of trimepranol. Mild side effects occurred in the heart volumes of the patients. We conclude that bid trimepranol is an effective antihypertensive agent.
曲美托洛尔(TMP)是一种新型的类似普萘洛尔的非选择性β-肾上腺素能受体阻滞剂。在一项双盲交叉研究中,对25名门诊患者评估了其与安慰剂相比的降压效果,这些患者的仰卧位舒张压(BP)至少为95毫米汞柱。在接受四周安慰剂治疗后,每周滴定TMP剂量,直至仰卧位舒张压低于95毫米汞柱或出现无法耐受的副作用。最终确定的曲美托洛尔剂量为:3名患者每日两次,每次10毫克;12名患者每日两次,每次20毫克;10名患者每日两次,每次40毫克。随后的双盲交叉研究包括两个六周的治疗期,要么先使用曲美托洛尔,然后使用安慰剂(第一组),要么顺序相反(第二组)。比较了这些治疗期结束时的血压和心率。当合并第一组和第二组的数据时,仰卧位血压从安慰剂期结束时的156±3/105±2毫米汞柱降至曲美托洛尔期结束时的收缩压和舒张压的140±2/93±1毫米汞柱(p<0.001)。在25名患者中的19名患者中,曲美托洛尔治疗期间仰卧位舒张压降至95毫米汞柱以下。发现曲美托洛尔的降压作用和心动过缓作用之间存在统计学上的显著相关性。患者心脏容积出现轻度副作用。我们得出结论,每日两次服用曲美托洛尔是一种有效的降压药物。