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肾功能损害患者口服磷酸丙吡胺的药代动力学。

Pharmacokinetics of oral disopyramide phosphate in patients with renal impairment.

作者信息

Johnston A, Henry J A, Warrington S J, Hamer N A

出版信息

Br J Clin Pharmacol. 1980 Sep;10(3):245-8. doi: 10.1111/j.1365-2125.1980.tb01751.x.

Abstract

1 The pharmacokinetics of disopyramide were studied after the oral administration of a 300 mg dose to 11 patients with stable chronic renal impairment (creatinine clearance 2-53 ml min-1). 2 Absorption half-life and volume of distribution were similar to those seen in normal subjects. 3 Mean plasma elimination half-life in these patients was 12.7 h, which is substantially greater than that reported for normal subjects. Elimination half-life tended to increase as creatinine clearance fell, and renal clearance of disopyramide correlated significantly (r=0.814; P < 0.001) with creatinine clearance. 4 From these results, we have calculated that patients with renal impairment should be started on a dose of disopyramide 1.5 mg kg-1 thrice daily and the regimen subsequently altered according to plasma concentrations of the drug. However, further studies are needed to define the handling of the metabolites of disopyramide.

摘要
  1. 对11例稳定的慢性肾功能损害患者(肌酐清除率为2 - 53 ml·min⁻¹)口服300 mg剂量的丙吡胺后,研究了其药代动力学。2. 吸收半衰期和分布容积与正常受试者相似。3. 这些患者的平均血浆消除半衰期为12.7小时,显著长于正常受试者的报告值。消除半衰期倾向于随着肌酐清除率的下降而增加,丙吡胺的肾清除率与肌酐清除率显著相关(r = 0.814;P < 0.001)。4. 根据这些结果,我们计算出肾功能损害患者应以1.5 mg·kg⁻¹的丙吡胺剂量每日三次开始给药,随后根据药物的血浆浓度调整用药方案。然而,需要进一步研究来确定丙吡胺代谢产物的处理方式。

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