Fagerberg B, Berglund A, Holme E, Wilhelmsen L, Elmfeldt D
Department of Medicine, Gottenburg University, Sahlgrenska Hospital, Göteborg, Sweden.
J Intern Med. 1990 Jan;227(1):37-43. doi: 10.1111/j.1365-2796.1990.tb00116.x.
In a double-blind, randomized, cross-over study with a single-blind placebo run-in period a new controlled-release (CR) formulation of metoprolol 200 mg once daily was compared with atenolol tablets 100 mg once daily in 22 patients (age 60.9 +/- 0.93 (SE) years) with primary hypertension and impaired or diabetic glucose tolerance. Each period lasted for three weeks. The two agents produced similar blood pressure 3 h as well as 24 h after drug intake. Three hours after drug intake, heart rate was lower on atenolol than metoprolol CR treatment, indicating a higher degree of beta-receptor blockade for atenolol at this point in time, when the plasma concentration of atenolol was most likely to be close to its peak. Concentrations of blood glucose, serum insulin, and serum C-peptide in the fasting state or after an oral glucose load did not differ between the active agents. HbA1c was marginally, but significantly, lower on atenolol than metoprolol CR treatment. No differences were found in serum levels of total, low density lipoprotein (LDL), and high density lipoprotein (HDL) cholesterol or apoA-I, and apoB lipoproteins or triglycerides. In comparison to the placebo run-in period, both agents showed an unexpected improvement in glucose tolerance, a decrease in HDL cholesterol and for metoprolol CR a small, but significant decrease in LDL cholesterol. Thus, treatment with metoprolol CR tablets producing even plasma levels without high peak concentrations and conventional atenolol treatment had similar effects on metabolic control in hypertensive men and abnormal glucose tolerance.
在一项双盲、随机、交叉研究中，有一个单盲安慰剂导入期，将每日一次服用200毫克美托洛尔的新型控释（CR）制剂与每日一次服用100毫克阿替洛尔片，在22例（年龄60.9±0.93（标准误）岁）原发性高血压且糖耐量受损或患有糖尿病的患者中进行比较。每个阶段持续三周。两种药物在服药后3小时以及24小时产生相似的血压。服药后3小时，阿替洛尔治疗组的心率低于美托洛尔CR治疗组，表明此时阿替洛尔对β受体的阻滞程度更高，而此时阿替洛尔的血浆浓度很可能接近其峰值。在空腹状态或口服葡萄糖负荷后，活性药物之间的血糖、血清胰岛素和血清C肽浓度没有差异。阿替洛尔治疗组的糖化血红蛋白（HbA1c）略低于但显著低于美托洛尔CR治疗组。在总胆固醇、低密度脂蛋白（LDL）、高密度脂蛋白（HDL）胆固醇或载脂蛋白A-I、载脂蛋白B脂蛋白或甘油三酯的血清水平上未发现差异。与安慰剂导入期相比，两种药物均显示出糖耐量意外改善、HDL胆固醇降低，美托洛尔CR治疗组的LDL胆固醇有小幅但显著的降低。因此，服用能产生均匀血浆水平且无高浓度峰值的美托洛尔CR片治疗与传统阿替洛尔治疗对高血压男性的代谢控制和异常糖耐量有相似的效果。
