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头孢甲肟在肾功能受损患者及接受血液透析患者中的药代动力学。

Pharmacokinetics of cefmenoxime in patients with impaired renal function and in those undergoing hemodialysis.

作者信息

Konishi K

出版信息

Antimicrob Agents Chemother. 1986 Dec;30(6):901-5. doi: 10.1128/AAC.30.6.901.

Abstract

The pharmacokinetics of cefmenoxime were studied after a single intravenous 1.0-g dose to 24 subjects grouped according to their renal functions. Creatinine clearance was above 85, 50 to 85, 10 to 50, and below 10 ml/min per 1.73 m2 in groups 1, 2, 3, and 4, respectively. Cefmenoxime obeyed two-compartment-model kinetics in all four groups. The volume of distribution based on the area under the serum concentration-time curve was renal function independent, the average value being 0.270 +/- 0.075 liters/kg. The elimination-phase half-life (t1/2 beta) was 0.82 +/- 0.30 h in group 1, 1.38 +/- 0.36 h in group 2, 3.32 +/- 1.82 h in group 3, and 7.60 +/- 1.28 h in group 4. Cumulative 24-h urinary excretion accounted for 65.5 +/- 7.6% of the dose in group 1 and for 7.50 +/- 3.72% in group 4. Recommendations for dosage adjustment in patients with renal insufficiency are proposed based on the data obtained in this study. The effect of hemodialysis on cefmenoxime pharmacokinetics was studied in six patients in group 4; hemodialysis shortened the average t1/2 beta from 7.60 +/- 1.28 to 4.19 +/- 1.66 h. It was estimated that in a hypothetical anephric subject with a body weight of 60 kg, 5-h hemodialysis would remove 28.2% of the drug present in the body at the start of hemodialysis.

摘要

对24名受试者单次静脉注射1.0克头孢甲肟后,根据其肾功能分组研究了头孢甲肟的药代动力学。第1、2、3和4组的肌酐清除率分别高于85、50至85、10至50以及低于10 ml/(min·1.73 m²)。头孢甲肟在所有四组中均符合二室模型动力学。基于血清浓度 - 时间曲线下面积的分布容积与肾功能无关,平均值为0.270±0.075升/千克。消除相半衰期(t1/2β)在第1组为0.82±0.30小时,第2组为1.38±0.36小时,第3组为3.32±1.82小时,第4组为7.60±1.28小时。24小时累积尿排泄量在第1组占剂量的65.5±7.6%,在第4组占7.50±3.72%。根据本研究获得的数据,提出了肾功能不全患者剂量调整的建议。对第4组的6名患者研究了血液透析对头孢甲肟药代动力学的影响;血液透析使平均t1/2β从7.60±1.28小时缩短至4.19±1.66小时。据估计,在一名体重60千克的假设无肾受试者中,5小时血液透析将清除血液透析开始时体内28.2%的药物。

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