Weber M A, Drayer J I, Kaufman C A
J Clin Pharmacol. 1984 Feb-Mar;24(2-3):103-12. doi: 10.1002/j.1552-4604.1984.tb02772.x.
Labetalol, an agent with both alpha- and beta-adrenoreceptor blocking properties, and the beta blocker propranolol were each given for one month to groups of 15 patients with essential hypertension. With either treatment, 11 of the 15 patients experienced decreased supine diastolic blood pressure to less than 90 mm Hg without evidence of fluid retention. Propranolol significantly increased plasma concentrations of uric acid and potassium, whereas labetalol significantly increased plasma concentration of high-density lipoproteins (HDL) and decreased the total cholesterol:HDL ratio; neither drug significantly changed renal function. During three additional months of labetalol treatment, there was a slight tendency to orthostatic decreases in systolic blood pressure as compared with the values after the initial month. Labetalol had variable effects on plasma renin activity and aldosterone excretion, but within individual patients the values were constant; there were close correlations between changes measured after one month and after four months for both renin (r = 0.86) and aldosterone (r = 0.94). The manifestations of labetalol's alpha-blocking component appeared to be a small postural effect on systolic blood pressure and an increase in plasma HDL.
拉贝洛尔是一种兼具α和β肾上腺素能受体阻断特性的药物,β受体阻滞剂普萘洛尔分别给予15例原发性高血压患者,为期1个月。两种治疗方法中,15例患者中有11例仰卧位舒张压降至90 mmHg以下,且无液体潴留迹象。普萘洛尔显著升高尿酸和钾的血浆浓度,而拉贝洛尔显著升高高密度脂蛋白(HDL)的血浆浓度并降低总胆固醇与HDL的比值;两种药物均未显著改变肾功能。在拉贝洛尔治疗的另外三个月中,与初始月份后的数值相比,收缩压有轻微的体位性下降趋势。拉贝洛尔对血浆肾素活性和醛固酮排泄有不同影响,但在个体患者中数值是恒定的;肾素(r = 0.86)和醛固酮(r = 0.94)在1个月和4个月后测量的变化之间存在密切相关性。拉贝洛尔的α阻断成分的表现似乎是对收缩压有较小的体位性影响以及血浆HDL升高。