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头孢甲肟在健康志愿者、肾功能不全患者及血液透析患者中的药代动力学。

Cefmenoxime pharmacokinetics in healthy volunteers and subjects with renal insufficiency and on hemodialysis.

作者信息

Gambertoglio J G, Alexander D P, Barriere S L

出版信息

Antimicrob Agents Chemother. 1984 Dec;26(6):845-9. doi: 10.1128/AAC.26.6.845.

Abstract

The pharmacokinetics of cefmenoxime were characterized in five healthy volunteers and in 15 subjects with various degrees of renal insufficiency after a single 10-mg/kg, 5-min intravenous infusion. Five of these subjects were studied both on hemodialysis and during an interdialytic period. Plasma, urine and dialysate were assayed for cefmenoxime by a specific high-pressure liquid chromatographic assay. Peak plasma concentrations of cefmenoxime were ca. 94 micrograms/ml after completion of the infusion. The mean plasma and renal clearances in the healthy volunteers were 281 +/- 66 and 228 +/- 52 ml/min, respectively. Plasma clearance declined in patients with renal insufficiency and correlated significantly with creatine clearance. The mean apparent volume of distribution at steady state in the healthy volunteers was 0.23 liters/kg and was not found to be significantly different in subjects with renal insufficiency. The mean cumulative 24-h urinary recovery of cefmenoxime in healthy volunteers was 81% of the administered dose and decreased with reduced renal function. Cefmenoxine dosage should be reduced in proportion to the decline in creatinine clearance. A simple nomogram for dose selection is provided.

摘要

在5名健康志愿者和15名不同程度肾功能不全的受试者中,静脉注射10mg/kg头孢甲肟5分钟后,对其药代动力学进行了研究。其中5名受试者在血液透析期间和透析间期均进行了研究。采用特定的高压液相色谱法测定血浆、尿液和透析液中的头孢甲肟。输注结束后,头孢甲肟的血浆峰浓度约为94μg/ml。健康志愿者的平均血浆清除率和肾脏清除率分别为281±66和228±52ml/min。肾功能不全患者的血浆清除率下降,且与肌酐清除率显著相关。健康志愿者稳态时的平均表观分布容积为0.23升/千克,肾功能不全受试者的这一数值无显著差异。健康志愿者中头孢甲肟24小时的平均累积尿回收率为给药剂量的81%,且随肾功能减退而降低。头孢甲肟的剂量应与肌酐清除率的下降成比例减少。提供了一个简单的剂量选择列线图。

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