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肾衰竭时呋塞米的动力学

Furosemide kinetics in renal failure.

作者信息

Tilstone W J, Fine A

出版信息

Clin Pharmacol Ther. 1978 Jun;23(6):644-50. doi: 10.1002/cpt1978236644.

Abstract

Furosemide kinetics were studied in normal volunteers and patients with renal failure. Comparison of results from intravenous bolus and intravenous infusion in normal subjects showed no significant model dependency of estimations of furosemide clearance, although the average clearance by fitting to a one-compartment model was 16% higher than that obtained by fitting to a two-compartment model. Normal subjects had a total body clearance of furosemide of 1.53 +/- 0.11 (SE) ml/min/kg, a volume of the central compartment of 2.61 +/- 0.37 L, a volume of the peripheral compartment of 2.48 +/- 0.24 L, and a half-life of 0.8 +/- 0.06 hr and they absorbed 68.9% +/- 7.1% of a solution of furosemide given by mouth. The corresponding values in patients with renal failure were 0.27 +/- 0.03 ml/min/kg, 8.02 +/- 0.96 L, 14.1 +/- 3.57 L, 14.2 +/- 2.30 hr, and 43.4% +/- 8.0%, all differing significantly different from the normal. The bioavailability of 500-mg tablets of furosemide in the renal failure patients was 43.4% +/- 7.4%, equivalent to the absorption of the dose given to the same patients in the form of a solution.

摘要

在正常志愿者和肾衰竭患者中研究了呋塞米的动力学。对正常受试者静脉推注和静脉输注的结果进行比较,结果表明,尽管通过拟合单室模型得到的平均清除率比拟合双室模型得到的平均清除率高16%,但呋塞米清除率的估计值没有显著的模型依赖性。正常受试者的呋塞米总体清除率为1.53±0.11(标准误)ml/(min·kg),中央室容积为2.61±0.37L,外周室容积为2.48±0.24L,半衰期为0.8±0.06小时,口服呋塞米溶液的吸收率为68.9%±7.1%。肾衰竭患者的相应值分别为0.27±0.03ml/(min·kg)、8.02±0.96L、14.1±3.57L、14.2±2.30小时和43.4%±8.0%,所有这些值与正常情况均有显著差异。肾衰竭患者中500mg呋塞米片剂的生物利用度为43.4%±7.4%,与以溶液形式给予同一患者的剂量的吸收率相当。

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