Cefotaxime and desacetylcefotaxime: an example of advantageous antimicrobial metabolism.
Although the antibacterial activity of desacetylcefotaxime (des-CTX), the principal metabolite of cefotaxime (CTX), is eightfold lower than cefotaxime, the metabolite inhibits many B-lactamase-producing Enterobacteriaceae and unusual Pseudomonas species resistant to agents such as cefamandole, cefoxitin, and cefoperazone. des-CTX is more stable than CTX to attack by beta-lactamases of some species such as Bacteroides fragilis, Proteus vulgaris, and the k-1 enzyme of Enterobacter-Klebsiella. des-CTX acts synergistically with CTX against many Enterobacteriaceae and Streptococcus faecalis. The antibacterial activity of the combination of CTX/des-CTX indicates that the drug can be administered every 8-12 hr and provides excellent, broad-spectrum antimicrobial activity.
D001419:Bacteria / Q000187:drug effects*; D001439:Bacteroides / Q000187:drug effects; D002439:Cefotaxime / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000494:pharmacology; D004357:Drug Synergism; D004755:Enterobacteriaceae / Q000187:drug effects; D013293:Enterococcus faecalis / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D011549:Pseudomonas / Q000187:drug effects; D001618:beta-Lactamases / Q000378:metabolism
C029281:desacetylcefotaxime; D001618:beta-Lactamases; D002439:Cefotaxime