Frick M H, Halttunen P, Himanen P, Huttunen M, Pörsti P, Pitkäjärvi T, Pöyhönen L, Pyykönen M L, Reinikainen P, Salmela P
Br J Clin Pharmacol. 1986;21 Suppl 1(Suppl 1):55S-62S. doi: 10.1111/j.1365-2125.1986.tb02854.x.
The efficacy and safety of doxazosin and atenolol were compared following once-daily administration for up to 1 year, with a minimum of 20 weeks' active treatment. According to response, patients received doxazosin 1-16 mg day-1 or atenolol 50-100 mg day-1. Mean daily doses at the final efficacy assessment (between 20 weeks and 1 year) were doxazosin 11.8 mg and atenolol 94.2 mg. Atenolol produced somewhat greater falls in blood pressure than doxazosin. The differences were statistically significant in the supine but not in the standing position. A small mean reduction in heart rate was produced by doxazosin whereas atenolol produced a marked bradycardia. Analysis of the same patient group at 20 weeks revealed similar overall profiles of activity except that atenolol produced greater falls in blood pressure than in the longer term analysis. Serum concentrations of HDL/total cholesterol ratio were raised in the doxazosin treatment group and lowered in the atenolol group. Triglyceride concentrations fell in the doxazosin group and rose in the atenolol group. Significant differences (P less than 0.001) were observed between treatment groups for these parameters, all differences being in favour of doxazosin. Pharmacokinetics of doxazosin, measured at steady state in 36 patients, showed dose-related plasma concentrations, a mean half-life of about 12 h and relatively low intersubject variation. The incidence of side-effects was slightly greater for patients in the doxazosin group. Drug-related side-effects were mostly mild to moderate in severity with no serious drug-related occurrences in either treatment group. No serious drug-related abnormalities in laboratory biochemistry and haematology tests were observed in either treatment group.
在每日一次给药长达1年、至少20周的积极治疗后,比较了多沙唑嗪和阿替洛尔的疗效与安全性。根据反应情况,患者接受多沙唑嗪每日1 - 16毫克或阿替洛尔每日50 - 100毫克。最终疗效评估(20周和1年之间)时的平均日剂量为多沙唑嗪11.8毫克和阿替洛尔94.2毫克。阿替洛尔降低血压的幅度比多沙唑嗪稍大。这些差异在仰卧位有统计学意义,但站立位无统计学意义。多沙唑嗪使心率有小幅度的平均降低,而阿替洛尔则导致明显的心动过缓。对同一患者组在20周时的分析显示,除了阿替洛尔在血压降低方面比长期分析时更大外,总体活性特征相似。多沙唑嗪治疗组的血清高密度脂蛋白/总胆固醇比值升高,阿替洛尔组降低。多沙唑嗪组甘油三酯浓度下降,阿替洛尔组上升。治疗组之间在这些参数上观察到显著差异(P小于0.001),所有差异均有利于多沙唑嗪。在36名患者中稳态时测量的多沙唑嗪药代动力学显示,血浆浓度与剂量相关,平均半衰期约为12小时,个体间差异相对较低。多沙唑嗪组患者的副作用发生率略高。与药物相关的副作用大多为轻度至中度,两个治疗组均未出现严重的与药物相关的情况。两个治疗组在实验室生化和血液学检查中均未观察到严重的与药物相关的异常。