Wise R, Wright N, Wills P J
Antimicrob Agents Chemother. 1981 Apr;19(4):526-31. doi: 10.1128/AAC.19.4.526.
The pharmacology of cefotaxime and the metabolite desacetyl cefotaxime was studied in 40 patients with various degrees of renal and hepatic failure who received 0.5 or 1 g of cefotaxime intravenously. Patients with severe renal impairment (creatinine clearance, 3 to 10 ml/min) had a cefotaxime serum half-life of 2.6 h and desacetyl cefotaxime serum half-life of 10.0 h. The equivalent figures were 1.0 and 1.5 h, respectively, in subjects with normal renal function. The presence of an acute coexisting illness together with severe renal impairment was associated with a further prolongation of the serum half-lives. Hepatic dysfunction was accompanied by a reduction in desacetyl metabolite formation. A reduction of cefotaxime dosing to 0.5 g twice a day would appear prudent when the creatinine clearance is 5 ml/min or less to avoid accumulation of the parent compound and the metabolite.
对40例不同程度肾衰和肝衰患者静脉注射0.5或1克头孢噻肟，研究了头孢噻肟及其代谢产物去乙酰头孢噻肟的药理学。严重肾功能损害（肌酐清除率3至10毫升/分钟）患者的头孢噻肟血清半衰期为2.6小时，去乙酰头孢噻肟血清半衰期为10.0小时。肾功能正常受试者的相应数值分别为1.0小时和1.5小时。急性并存疾病与严重肾功能损害同时存在会使血清半衰期进一步延长。肝功能障碍伴随着去乙酰代谢产物形成减少。当肌酐清除率为5毫升/分钟或更低时，将头孢噻肟剂量减至每日两次0.5克似乎是谨慎的，以避免母体化合物及其代谢产物的蓄积。
