Cefotaxime: microbiology, pharmacology, and clinical use

The microbiological activity, pharmacology, and clinical efficacy of the third-generation cephalosporin cefotaxime are reviewed. Cefotaxime has greater activity than other available first- and second-generation cephalosporins against Enterobacteriaceae. It is more active than older cephalosporins against Pseudomonas aeruginosa and Acinetobacter spp., but most strains are still considered resistant. Cefotaxime is also active against some gram-negative bacilli that are resistant to aminoglycosides, including amikacin. Cefotaxime has activity comparable with other cephalosporins against gram-positive cocci, except staphylococci and enterococci, which are resistant. Cefotaxime in combination with penicillins or aminoglycosides may be synergistic against selected gram-negative bacilli. Cefotaxime is metabolized in vivo to the desacetyl derivative, which is also microbiologically active. Cefotaxime appears to penetrate most body tissues and fluids, including cerebrospinal fluid. Clinical use of cefotaxime has resulted in response rates between 70 and 95% in most infections. The ultimate role of cefotaxime and other third-generation cephalosporins is not established since controlled clinical comparisons with standard antimicrobial regimens are lacking. Possibilities include the empiric and specific therapy of serious gram-negative bacillary infection probably in combination with a penicillin or an aminoglycoside. Cefotaxime appears to be potentially useful in the management of gram-negative bacillary meningitis.