肾功能不全患者及血液透析期间头孢噻肟和去乙酰头孢噻肟的消除动力学

Elimination kinetics of cefotaxime and desacetyl cefotaxime in patients with renal insufficiency and during hemodialysis.

作者信息

Ohkawa M, Okasho A, Motoi I, Tokunaga S, Shoda R, Kawaguchi S, Sawaki M, Shimamura M, Hirano S, Kuroda K, Awazu S

出版信息

Chemotherapy. 1983;29(1):4-12. doi: 10.1159/000238166.

Abstract

The pharmacokinetics of cefotaxime, a new semi-synthetic cephalosporin for injection, was studied in 30 subjects with various degrees of renal function after a single 1-gram intramuscular injection. Serum and urinary concentrations of cefotaxime and desacetyl cefotaxime were determined by high pressure liquid chromatography. The pharmacokinetic parameters of cefotaxime were obtained using a one-compartment open model. The mean serum half-life of the parent compound (cefotaxime), 0.87 h in normal subjects, was prolonged to 2.35 h in hemodialysis patients. There was a significant linear correlation between the elimination rate constant of cefotaxime and creatinine clearance. The mean cumulative urinary recovery of the administered dose in the 24-hour urine was 51.7% as cefotaxime and 25.6% as desacetyl cefotaxime in normal subjects.

摘要

对一种新型注射用半合成头孢菌素头孢噻肟的药代动力学进行了研究，研究对象为30名肾功能程度各异的受试者，他们均接受了单次1克的肌肉注射。采用高压液相色谱法测定血清和尿液中头孢噻肟及去乙酰头孢噻肟的浓度。使用单室开放模型获得头孢噻肟的药代动力学参数。母体化合物（头孢噻肟）的平均血清半衰期在正常受试者中为0.87小时，在血液透析患者中延长至2.35小时。头孢噻肟的消除速率常数与肌酐清除率之间存在显著的线性相关性。在正常受试者中，给药剂量在24小时尿液中的平均累积回收率，以头孢噻肟计为51.7%，以去乙酰头孢噻肟计为25.6%。