Kierdorf H, Müller A, Blanke P M, Gellert J, Heintz B, Rämsch K D, Wargenau M, Kindler J
Department of Internal Medicine II, Technical University, Aachen, Germany.
Eur J Clin Pharmacol. 1993;45(2):129-34. doi: 10.1007/BF00315493.
Nitrendipine solution 5 mg.ml-1 in the dose of 5 mg was given orally to 20 patients with chronic renal failure and elevated diastolic blood pressure (> or = 110 mmHg), of whom 10 were on maintenance haemodialysis (endogenous creatinine clearance < 5 ml.min-1) and 10 were at the predialysis stage (endogenous creatinine clearance 5-20 ml.min-1). The aim of the study was to investigate the influence of kidney function and/or dialysis treatment on the pharmacokinetic and pharmacodynamic profile of a solution of nitrendipine and to assess its antihypertensive efficacy. After 10 min there was a significant reduction in blood pressure from 188/113 to 173/100 (patients not dependent on dialysis) and from 197/112 to 161/94 mmHg (patients dependent on dialysis). The maximum fall in blood pressure (approximately 30%) was attained after 90 min in the dialysis patients and after 120 min in the non-dialysis group. Blood pressure increased again about 3 h after the administration of nitrendipine but it was still below baseline after 12 h. The terminal elimination half-life (4.1 h in the dialysis patients and 3.6 h in non-dialysis patients) was similar to that observed in patients with normal renal function. The pharmacokinetics of nitrendipine did not differ between the dialysis and non-dialysis groups. There was a correlation between plasma concentration and the blood pressure reduction. The maximum plasma concentration of nitrendipine was reached after 0.5 h (median) and did not differ between the two groups.(ABSTRACT TRUNCATED AT 250 WORDS)
给20例慢性肾衰竭且舒张压升高(≥110 mmHg)的患者口服5 mg剂量的5 mg·ml⁻¹尼群地平溶液,其中10例患者接受维持性血液透析(内生肌酐清除率<5 ml·min⁻¹),10例处于透析前阶段(内生肌酐清除率5 - 20 ml·min⁻¹)。本研究的目的是调查肾功能和/或透析治疗对尼群地平溶液药代动力学和药效学特征的影响,并评估其降压疗效。10分钟后,未依赖透析的患者血压从188/113显著降至173/100,依赖透析的患者血压从197/112降至161/94 mmHg。透析患者在90分钟后血压降幅最大(约30%),非透析组在120分钟后达到最大降幅。服用尼群地平约3小时后血压再次升高,但12小时后仍低于基线。终末消除半衰期(透析患者为4.1小时,非透析患者为3.6小时)与肾功能正常患者观察到的相似。尼群地平的药代动力学在透析组和非透析组之间没有差异。血浆浓度与血压降低之间存在相关性。尼群地平的最大血浆浓度在0.5小时(中位数)后达到,两组之间无差异。(摘要截短至250字)