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单次口服给药后硝苯地平在肝硬化患者中的药代动力学

[Nifedipine pharmacokinetics in liver cirrhosis patients after the administration of a single oral dose].

作者信息

Leucuţa S E, Grigorescu M, Dumitraşcu D

机构信息

Facultatea de Farmacie, Institutul de Medicină şi Farmacie, Cluj-Napoca.

出版信息

Rev Med Interna Neurol Psihiatr Neurochir Dermatovenerol Med Interna. 1990 Mar-Apr;42(2):185-90.

PMID:1982192
Abstract

The niphedipine pharmacokinetics was investigated in the patients with hepatic cirrhosis, in comparison with a group of healthy subjects, after administering unique doses of 10 mg per os. The niphedipine concentrations in serum were determined by a gas chromatography method. The niphedipine pharmacokinetics may be described in correspondence with the open pharmacokinetic model. The values of pharmacokinetic parameters of niphedipine in the patients with hepatic cirrhosis are significantly modified in comparison with those noticed in the healthy subjects. An increase in the level of the maximum concentrations (158 ng/ml versus 68 ng/ml), of the biological half time (11.9 hours versus 2.5 hours) and of the area under the curve of the drug concentrations in time (450 ng.ml-1.hour versus 205 ng.ml-1.hour) were found. The relative bioavailability [correction of biodisponibility] of niphedipine was double in the patients with hepatic cirrhosis versus the healthy subjects. The modified pharmacokinetics of niphedipine in the patients with hepatic cirrhosis and the great individual variations found, require a decrease of the dose in this category of patients and a surveillance of the clinical effect.

摘要

在口服单剂量10 mg硝苯地平后,对肝硬化患者的硝苯地平药代动力学进行了研究,并与一组健康受试者进行了比较。采用气相色谱法测定血清中硝苯地平浓度。硝苯地平药代动力学可用开放药代动力学模型描述。与健康受试者相比,肝硬化患者硝苯地平的药代动力学参数值有显著改变。发现最大浓度(158 ng/ml对68 ng/ml)、生物半衰期(11.9小时对2.5小时)和药物浓度-时间曲线下面积(450 ng·ml⁻¹·小时对205 ng·ml⁻¹·小时)水平升高。肝硬化患者硝苯地平的相对生物利用度[生物处置的校正]是健康受试者的两倍。肝硬化患者硝苯地平药代动力学的改变以及发现的个体差异较大,需要降低此类患者的剂量并监测临床效果。

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