title: Efficacy of cefoperazone in combination with sulbactam in experimental Staphylococcus aureus endocarditis in rabbits.
abstract: The activity of cefoperazone with and without sulbactam was studied in vitro and in vivo against strains of methicillin-resistant and methicillin-susceptible Staphylococcus aureus. Cefoperazone with or without sulbactam was inactive in vitro against the methicillin-resistant strain and was bound by penicillin-binding protein 2a with an IC50 of 190 mg/L (the concentration that reduced radio-labelling with 3H-penicillin by 50%). Cefoperazone was hydrolysed by beta-lactamase in vitro but sulbactam improved cefoperazone activity in a rabbit model of aortic valve endocarditis caused by a beta-lactamase producing methicillin-susceptible strain.
authors.affiliation: Department of Medicine, San Francisco General Hospital, CA 94110.
authors.forename: H F
authors.initials: HF
authors.lastname: Chambers
authors.forename: M A
authors.initials: MA
authors.lastname: Fournier
mesh_terms: D000818:Animals; D001426:Bacterial Proteins; D002352:Carrier Proteins / Q000378:metabolism; D002438:Cefoperazone / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D004359:Drug Therapy, Combination / Q000494:pharmacology* / Q000627:therapeutic use; D004697:Endocarditis, Bacterial / Q000188:drug therapy* / Q000382:microbiology; D006602:Hexosyltransferases; D016106:Methicillin Resistance; D002267:Muramoylpentapeptide Carboxypeptidase / Q000378:metabolism; D046915:Penicillin-Binding Proteins; D010458:Peptidyl Transferases; D011817:Rabbits; D013203:Staphylococcal Infections / Q000188:drug therapy* / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D013407:Sulbactam / Q000494:pharmacology / Q000627:therapeutic use; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D001426:Bacterial Proteins; D002352:Carrier Proteins; D046915:Penicillin-Binding Proteins; D065093:beta-Lactamase Inhibitors; D002438:Cefoperazone; D010458:Peptidyl Transferases; D006602:Hexosyltransferases; D002267:Muramoylpentapeptide Carboxypeptidase; D001618:beta-Lactamases; D013407:Sulbactam