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消旋维拉帕米在肾功能受损患者中的药代动力学。

The pharmacokinetics of racemic verapamil in patients with impaired renal function.

作者信息

Zachariah P K, Moyer T P, Theobald H M, Frantz R P, Kurtz S B, McCarthy J T, Smith R L

机构信息

Division of Hypertension and Internal Medicine, Mayo Clinic, Rochester, MN 55905.

出版信息

J Clin Pharmacol. 1991 Jan;31(1):45-53. doi: 10.1002/j.1552-4604.1991.tb01885.x.

Abstract

The pharmacokinetics of verapamil were studied in patients with renal failure who were undergoing maintenance hemodialysis and in normal subjects after an IV infusion of 10 mg and a single oral dose of 120 mg. Plasma levels of verapamil and its active metabolite, norverapamil, were analyzed by a sensitive and specific HPLC procedure. Severe renal failure requiring hemodialysis did not change the time course of verapamil and norverapamil plasma concentrations after either the IV or oral dose. The terminal elimination rate constant, clearance, volume of distribution, and bioavailability of verapamil were not significantly different between the two groups of subjects. In addition, the apparent maximal plasma concentration, terminal elimination rate constant, and area under the curve for norverapamil were similar in patients with renal failure and normal subjects. The study showed that the plasma disposition of verapamil and norverapamil was not affected in patients with impaired renal function. Furthermore, this study does not indicate that any change in dosage is necessary when single doses of verapamil are administered to patients with renal failure.

摘要

在接受维持性血液透析的肾衰竭患者以及正常受试者中,静脉输注10mg维拉帕米并单次口服120mg后,对其药代动力学进行了研究。采用灵敏且特异的高效液相色谱法分析维拉帕米及其活性代谢产物去甲维拉帕米的血浆水平。需要血液透析的严重肾衰竭患者在静脉或口服给药后,维拉帕米和去甲维拉帕米的血浆浓度随时间的变化过程未发生改变。两组受试者之间,维拉帕米的终末消除速率常数、清除率、分布容积和生物利用度无显著差异。此外,肾衰竭患者和正常受试者中,去甲维拉帕米的表观最大血浆浓度、终末消除速率常数和曲线下面积相似。该研究表明,肾功能受损患者中维拉帕米和去甲维拉帕米的血浆处置不受影响。此外,该研究未表明对肾衰竭患者单次给予维拉帕米时需要进行任何剂量调整。

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