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头孢匹罗在肾功能损害患者中的单剂量药代动力学。

Single-dose pharmacokinetics of cefpirome in patients with renal impairment.

作者信息

Lameire N, Malerczyk V, Drees B, Lehr K, Rosenkranz B

机构信息

Department of Medicine, University of Ghent, Belgium.

出版信息

Clin Pharmacol Ther. 1992 Jul;52(1):24-30. doi: 10.1038/clpt.1992.98.

Abstract

The pharmacokinetic parameters of cefpirome (HR 810) were examined in 22 patients with different degrees of renal impairment. HPLC was used to analyze samples of blood and urine for cefpirome; and enzymatic assay of creatinine in serum and urine was used to assess kidney function. Creatinine clearance correlated linearly with both total and renal clearance of cefpirome. The loss of kidney function resulted in a decreased renal clearance, whereas the volume of distribution remained the same. This result led to an increase in the terminal half-life of the drug, from 2 hours in healthy subjects to 14 1/2 hours in patients with uremia. This increase also resulted in a prolonged high serum concentration well above the minimum inhibitory concentration. The following dosages are thus recommended: (1) creatinine clearance greater than 50 ml/min: normal daily dose, (2) creatinine clearance from 20 to 50 ml/min: 50% of normal daily dose, and (3) creatinine clearance less than 20 ml/min: 25% of normal daily dose. An initial loading dose of 1 gm, independent of renal function, is advised. Cefpirome was safe and well tolerated.

摘要

在22例不同程度肾功能损害的患者中研究了头孢匹罗(HR 810)的药代动力学参数。采用高效液相色谱法分析血液和尿液中的头孢匹罗样本;采用酶法测定血清和尿液中的肌酐以评估肾功能。肌酐清除率与头孢匹罗的总清除率和肾清除率均呈线性相关。肾功能丧失导致肾清除率降低,而分布容积保持不变。这一结果导致药物的终末半衰期延长,从健康受试者的2小时延长至尿毒症患者的14.5小时。这种延长还导致血清高浓度持续时间延长,远高于最低抑菌浓度。因此推荐以下剂量:(1)肌酐清除率大于50 ml/min:正常日剂量;(2)肌酐清除率20至50 ml/min:正常日剂量的50%;(3)肌酐清除率小于20 ml/min:正常日剂量的25%。建议初始负荷剂量为1克,与肾功能无关。头孢匹罗安全且耐受性良好。

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