Walstad R A, Berg K J, Wessel-Aas T, Nilsen O G
Acta Med Scand Suppl. 1982;665:135-41. doi: 10.1111/j.0954-6820.1982.tb00423.x.
Labetalol (Trandate) is a new antihypertensive agent with both alpha- and beta-adrenoceptor blocking properties. In a double-blind cross-over study the antihypertensive action and side-effects of labetalol and propranolol were compared in 18 previously untreated outpatients with hypertension, WHO stage I--III. Mean daily dose of labetalol was 667 mg and of propranolol 129 mg. Labetalol reduced systolic and diastolic blood pressure in the seated and upright position significantly more than propranolol. The pulse rate reduction was greater with propranolol. Side-effects were more pronounced with propranolol. The antihypertensive effect, effect on pulse rate and pharmacokinetics of a single oral dose of 400 mg labetalol were studied in 6 patients with normal and 6 patients with impaired renal function (creatinine clearance less than 20 ml/min), all belonging to WHO stage I--II. A significant fall in pulse rate and systolic and diastolic blood pressure was observed in both groups, the duration being more than 25 h. No difference was found between the two groups. From the serum concentration-time curves the elimination rate constant, elimination half-life and area under the curve were calculated. The mean values of the two groups did not differ significantly. A pronounced interindividual variation was found in both groups.
拉贝洛尔（柳胺苄心定）是一种新型抗高血压药物，具有α和β肾上腺素能受体阻滞特性。在一项双盲交叉研究中，对18例未经治疗的WHO I - III期高血压门诊患者比较了拉贝洛尔和普萘洛尔的降压作用及副作用。拉贝洛尔的平均日剂量为667mg，普萘洛尔为129mg。拉贝洛尔在坐位和立位时降低收缩压和舒张压的幅度明显大于普萘洛尔。普萘洛尔降低脉搏率的幅度更大。普萘洛尔的副作用更明显。对6例肾功能正常和6例肾功能受损（肌酐清除率低于20ml/min）的WHO I - II期患者研究了单次口服400mg拉贝洛尔的降压作用、对脉搏率的影响及药代动力学。两组患者的脉搏率、收缩压和舒张压均显著下降，持续时间超过25小时。两组之间未发现差异。根据血清浓度 - 时间曲线计算了消除速率常数、消除半衰期和曲线下面积。两组的平均值无显著差异。两组均发现明显的个体间差异。
