Piper C, Cawello W, Bonn R, Weber E
Arzneimittelforschung. 1983;33(7):988-96.
Pharmacodynamics and Pharmacokinetics of Bemetizide Compared with Hydrochlorothiazide/Controlled clinical study of acute effects Bemetizide in doses of 1, 5, 10, 20, 50 mg versus 25 mg of hydrochlorothiazide were examined in a placebo-controlled randomized single-dose study under standardized conditions in normal male volunteers. The diuretic effects of bemetizide and hydrochlorothiazide were qualitatively equal, though after higher doses bemetizide showed greater maximal, statistically significant effects on the excretion of sodium, chloride and urine volume (relative efficacy). A trend to increased elimination of potassium was detectable. Diuresis of calcium and magnesium and pH of urine were unchanged. The effects of the reference dosis of hydrochlorothiazide were constantly lower than those of higher doses of bemetizide conferring to the 24-h aliquot and the fractioned samples. The action of both substances began within 1 to 2 h after oral application exceeding 24 h. Kinetics of effects and pharmacokinetics were closely correlated. The evidence of dose-dependent kinetics for bemetizide supports the assumption, that it is absorbed incompletely in higher doses. Because of the lack of a parenteral preparation it is not possible to provide reliable information on the maximal potency of bemetizide.
苄氟噻嗪与氢氯噻嗪的药效学和药代动力学/苄氟噻嗪急性效应的对照临床研究 在正常男性志愿者的标准化条件下，进行了一项安慰剂对照的随机单剂量研究，比较了1、5、10、20、50mg苄氟噻嗪与25mg氢氯噻嗪的疗效。苄氟噻嗪和氢氯噻嗪的利尿作用在性质上是相同的，尽管在较高剂量下，苄氟噻嗪对钠、氯排泄和尿量显示出更大的最大、具有统计学意义的作用（相对疗效）。可检测到钾排泄增加的趋势。钙、镁的利尿作用和尿液pH值未改变。氢氯噻嗪参比剂量的作用始终低于苄氟噻嗪较高剂量对24小时等分试样和分次采集样本的作用。两种药物的作用在口服后1至2小时内开始，持续超过24小时。效应动力学和药代动力学密切相关。苄氟噻嗪剂量依赖性动力学的证据支持了这样的假设，即其在较高剂量下吸收不完全。由于缺乏胃肠外制剂，无法提供关于苄氟噻嗪最大效能的可靠信息。
