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血液透析对持续静脉输注硝苯地平的药代动力学及血流动力学效应的影响。

Influence of haemodialysis on the pharmacokinetics and haemodynamic effects of nifedipine during continuous intravenous infusion.

作者信息

Kleinbloesem C H, van Brummelen P, Woittiez A J, Faber H, Breimer D D

出版信息

Clin Pharmacokinet. 1986 Jul-Aug;11(4):316-22. doi: 10.2165/00003088-198611040-00004.

DOI:10.2165/00003088-198611040-00004
PMID:3757391
Abstract

The pharmacokinetics and haemodynamic effects of nifedipine were studied in 5 patients on long term haemodialysis. In addition, clearance of the drug on 2 different types of artificial kidneys were measured in vitro. Nifedipine was administered intravenously (1.3 mg/h) from 6 hours before starting haemodialysis to the end of haemodialysis, performed according to the standard protocol of each patient. Before and during haemodialysis, blood samples were taken for determination of free and total plasma nifedipine concentrations. Recovery was determined by measuring nifedipine concentrations in the dialysate. Heart rate and systolic and diastolic blood pressures were determined serially. The haemodynamic changes during nifedipine were compared with those of 3 previous dialysis sessions. Haemodialysis was accompanied by a slight decrease in steady-state nifedipine concentrations. The recovery in dialysate varied between 0.6 and 0.9% of the amount infused during the period of dialysis. Artificial kidney clearance of nifedipine varied between 2.8 and 8.3 ml/min, which was in agreement with in vitro data. Changes in steady-state nifedipine concentrations were most likely due to changes in systemic clearance caused by haemodialysis itself. Systolic and diastolic blood pressure dropped by approximately 15% and 25%, respectively, in comparison with dialysis without nifedipine, but changes in heart rate were not different. It is concluded that nifedipine is poorly dialysable. During haemodialysis, blood pressure is markedly reduced but dose schedules need not to be changed.

摘要

在5例长期接受血液透析的患者中研究了硝苯地平的药代动力学和血流动力学效应。此外,还在体外测量了该药物在两种不同类型人工肾中的清除率。在开始血液透析前6小时至血液透析结束期间,按照每位患者的标准方案静脉输注硝苯地平(1.3mg/h)。在血液透析前和透析期间,采集血样以测定游离和总血浆硝苯地平浓度。通过测量透析液中的硝苯地平浓度来确定回收率。连续测定心率以及收缩压和舒张压。将硝苯地平治疗期间的血流动力学变化与之前3次透析治疗的变化进行比较。血液透析伴随着稳态硝苯地平浓度的轻微下降。透析液中的回收率在透析期间输注量的0.6%至0.9%之间变化。硝苯地平的人工肾清除率在2.8至8.3ml/min之间变化,这与体外数据一致。稳态硝苯地平浓度的变化很可能是由于血液透析本身导致的全身清除率变化所致。与未使用硝苯地平的透析相比,收缩压和舒张压分别下降约15%和25%,但心率变化无差异。结论是硝苯地平的透析性较差。在血液透析期间,血压会显著降低,但给药方案无需改变。

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本文引用的文献

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Effects of calcium-entry antagonists in hypertension.钙通道阻滞剂在高血压治疗中的作用。
Clin Exp Hypertens A. 1982;4(1-2):271-84. doi: 10.3109/10641968209061590.
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Hypotensive effect of nifedipine in hypertensive patients with chronic renal failure.硝苯地平对慢性肾衰竭高血压患者的降压作用。
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Kinetics of pharmacologic response.药理反应动力学
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Acute and chronic hypotensive effects of nifedipine and niludipine in hypertensive patients with chronic renal failure.硝苯地平与尼鲁地平对慢性肾衰竭高血压患者的急性和慢性降压作用
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Treatment of hypertension in hemodialysis patients with nifedipine.用硝苯地平治疗血液透析患者的高血压
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[Clinical study on the pharmacokinetics of radioactively labelled 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester].[放射性标记的4-(2'-硝基苯基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸二甲酯的药代动力学临床研究]
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[The binding of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (nifedipine) as well as other coronary active substances to serum albumins].[4-(2'-硝基苯基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸二甲酯(硝苯地平)以及其他冠状动脉活性物质与血清白蛋白的结合]
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