title: Cefoperazone: a review of its antimicrobial spectrum, beta-lactamase stability, enzyme inhibition, and other in vitro characteristics.
abstract: The in vitro qualities of cefoperazone were reviewed on the basis of international medical literature and some new observations. Cefoperazone is highly active against the Enterobacteriaceae. Its activity against Staphylococcus aureus is comparable to that of the other newer cephem antibiotics. Cefoperazone is also active against all beta-hemolytic streptococci and Streptococcus pneumoniae and is relatively inactive against methicillin-resistant S. aureus and enterococci. Against Pseudomonas aeruginosa cefoperazone is at least fourfold more active than cefotaxime or moxalactam and is approximately as active as azlocillin or piperacillin. Haemophilus and Neisseria species, regardless of beta-lactamase production, are highly susceptible to cefoperazone. Against the Bacteroides fragilis group, cefoperazone is either very active or quite inactive because of endemic variations. The drug is slightly less stable to some beta-lactamases than are cefotaxime-like or 7-methoxy cephem drugs. Cefoperazone is a bactericidal beta-lactam, and its minimal inhibitory concentrations are influenced only by high inoculum concentrations of beta-lactamase-producing strains. Its ability to permeate bacterial cell membranes appears similar to that of cefotaxime. Synergy studies with cefoperazone plus beta-lactamase inhibitors or aminoglycosides against Enterobacteriaceae and P. aeruginosa show enhanced killing. Cefoperazone is 70%-94% protein bound and has high affinities for bacterial penicillin-binding proteins 3, 1a, 2, and 1 bs.
mesh_terms: D000693:Anaerobiosis; D001419:Bacteria / Q000187:drug effects*; D001426:Bacterial Proteins; D002352:Carrier Proteins / Q000378:metabolism; D002438:Cefoperazone; D002463:Cell Membrane Permeability; D002511:Cephalosporins / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D004755:Enterobacteriaceae / Q000187:drug effects; D006602:Hexosyltransferases; D006801:Humans; D002267:Muramoylpentapeptide Carboxypeptidase; D046915:Penicillin-Binding Proteins; D010458:Peptidyl Transferases; D011485:Protein Binding; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism*
chemical_list: D001426:Bacterial Proteins; D002352:Carrier Proteins; D002511:Cephalosporins; D046915:Penicillin-Binding Proteins; D065093:beta-Lactamase Inhibitors; D002438:Cefoperazone; D010458:Peptidyl Transferases; D006602:Hexosyltransferases; D002267:Muramoylpentapeptide Carboxypeptidase; D001618:beta-Lactamases