头孢噻肟（HR756）去乙酰代谢物与头孢噻肟及其他头孢菌素的活性比较。
Activity of the cefotaxime (HR756) desacetyl metabolite compared with those of cefotaxime and other cephalosporins.
作者信息
Wise R, Wills P J, Andrews J M, Bedford K A
出版信息
Antimicrob Agents Chemother. 1980 Jan;17(1):84-6. doi: 10.1128/AAC.17.1.84.
Abstract
The desacetyl metabolite (DES) of cefotaxime (HR756) is formed in vivo to a significant extent. The in vitro activities of DES, the parent compound, and cefazolin, cefoxitin, and cefuroxime were compared against 70 bacterial isolates. DES was found to possess approximately 1/10th the activity of the parent compound against the common Enterobacteriaceae, but was somewhat more active than the other three compounds tested. DES had no useful activity against Pseudomonas aeruginosa and was less active than cefotaxime or cefoxitin against Staphylococcus aureus or Bacteroides fragilis. Because DES may accumulate in renal failure or be concentrated in the biliary tract, its antimicrobial activity may have considerable clinical significance.
摘要
头孢噻肟（HR756）的去乙酰代谢物（DES）在体内有相当程度的生成。将DES、母体化合物以及头孢唑林、头孢西丁和头孢呋辛的体外活性针对70株细菌分离株进行了比较。结果发现，DES对常见肠杆菌科细菌的活性约为母体化合物的1/10，但比所测试的其他三种化合物略具活性。DES对铜绿假单胞菌无有效活性，且对金黄色葡萄球菌或脆弱拟杆菌的活性低于头孢噻肟或头孢西丁。由于DES可能在肾衰竭时蓄积或在胆道中浓缩，其抗菌活性可能具有相当大的临床意义。
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