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口服尼群地平溶液在晚期肾衰竭高血压患者中的药效学和药代动力学

Pharmacodynamics and pharmacokinetics of oral nitrendipine solution in hypertensive patients with advanced renal failure.

作者信息

Kierdorf H, Müller A, Blanke P M, Gellert J, Heintz B, Rämsch K D, Wargenau M, Kindler J

机构信息

Department of Internal Medicine II, Technical University, Aachen, Germany.

出版信息

Eur J Clin Pharmacol. 1993;45(2):129-34. doi: 10.1007/BF00315493.

Abstract

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)

摘要

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)

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