Dahlöf B, Danielson M, Andersson O, Thulin T, Ohman P, Mörlin C, Boberg J, Karlberg B E, Jern S, Hansson L
Br J Clin Pharmacol. 1984 Dec;18(6):831-6. doi: 10.1111/j.1365-2125.1984.tb02552.x.
The objective of this placebo controlled double-blind multicentre (six centres) trial was to investigate the safety and efficacy of ICI 141,292 (Visacor), a new selective beta 1-adrenoceptor antagonist with modest intrinsic sympathomimetic activity (ISA), in hypertensive patients. Fifty-nine patients with mild essential hypertension were randomized to two of five treatment alternatives (placebo, 50 mg, 100 mg 200 mg or 300 mg of ICI 141,292) each given once daily for 2 weeks with a 4 week placebo period before (run in) and in between (wash out) active periods. Thus, each of the five treatments was evaluated in 20-24 patients. After 2 weeks (24 h after last dose) the reduction in recumbent blood pressure for all doses except 50 mg of ICI 141,292 was statistically significant and in the order of 6/4 mm Hg. Standing systolic blood pressure was reduced in a dose-dependent way but only significant for 200 mg of ICI 141,292 (8 mm Hg). Heart rate changes (delta) less than 4 beats/min) were not statistically significant for any dose. It is concluded that ICI 141,292 was well tolerated and had a significant but weak antihypertensive effect which might be explained by too much beta 1-adrenoceptor ISA.
这项安慰剂对照双盲多中心（六个中心）试验的目的是研究ICI 141,292（Visacor），一种具有适度内在拟交感活性（ISA）的新型选择性β1肾上腺素能受体拮抗剂，在高血压患者中的安全性和疗效。59例轻度原发性高血压患者被随机分为五种治疗方案中的两种（安慰剂、50毫克、100毫克、200毫克或300毫克的ICI 141,292），每种方案每日给药一次，持续2周，在治疗期之前（导入期）和期间（洗脱期）有4周的安慰剂期。因此，五种治疗方案中的每种方案都在20 - 24例患者中进行了评估。2周后（最后一剂后24小时），除50毫克ICI 141,292外，所有剂量的卧位血压降低均具有统计学意义，降低幅度约为6/4毫米汞柱。立位收缩压以剂量依赖性方式降低，但仅200毫克ICI 141,292的降低具有统计学意义（8毫米汞柱）。任何剂量的心率变化（差值小于4次/分钟）均无统计学意义。结论是ICI 141,292耐受性良好，具有显著但较弱的降压作用，这可能是由于过多的β1肾上腺素能受体ISA所致。
