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尿毒症患者扑米酮消除的药代动力学。

Pharmacokinetics of primidone elimination by uremic patients.

作者信息

Lee C S, Marbury T C, Perchalski R T, Wilder B J

出版信息

J Clin Pharmacol. 1982 Jul;22(7):301-8. doi: 10.1002/j.1552-4604.1982.tb02679.x.

Abstract

The hemodialyzability of primidone was investigated in four patients on long-term hemodialysis. Primidone, 500 or 250 mg, was given orally 2 hours before hemodialysis. Blood and dialyzate samples were collected periodically during the 4-hour dialysis and measured by gas-liquid chromatography and high-performance liquid chromatography for primidone. Dialysis clearance calculated by the instantaneous dialyzate method averaged 97.7 ml/min, which is considerably greater than the metabolic clearance of 30 ml/min for the drug. The extraction efficiency of the hollow-fiber dialyzers averaged 40.2 pr cent for plasma samples. A mean of 31.7 per cent of the administered dose of primidone was removed during hemodialysis. The half-life was 5.1 hours in our patients during hemodialysis, a nearly two-thirds reduction of the 13.9-hour half-life calculated in uremic patients. Because of the reduction in elimination half-life, greater dialysis clearance than metabolic clearance, high extraction efficiency, and significant drug removal during dialysis, we conclude that primidone is dialyzable.

摘要

在4例长期血液透析患者中研究了扑米酮的血液透析性。在血液透析前2小时口服500或250毫克扑米酮。在4小时的透析过程中定期采集血液和透析液样本,并用气相色谱法和高效液相色谱法测定扑米酮。用瞬时透析液法计算的透析清除率平均为97.7毫升/分钟,这大大高于该药物30毫升/分钟的代谢清除率。中空纤维透析器对血浆样本的提取效率平均为40.2%。在血液透析过程中,平均31.7%的给药剂量的扑米酮被清除。在我们的患者进行血液透析期间,半衰期为5.1小时,比在尿毒症患者中计算出的13.9小时半衰期缩短了近三分之二。由于消除半衰期缩短、透析清除率高于代谢清除率、提取效率高以及透析过程中药物清除显著,我们得出结论,扑米酮是可透析的。

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