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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Bacterial Proteins*
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Carrier Proteins / metabolism
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Cefoperazone / metabolism
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Cefoperazone / pharmacology
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Cefoperazone / therapeutic use
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Drug Therapy, Combination / pharmacology*
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Drug Therapy, Combination / therapeutic use
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Endocarditis, Bacterial / drug therapy*
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Endocarditis, Bacterial / microbiology
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Hexosyltransferases*
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Methicillin Resistance
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Muramoylpentapeptide Carboxypeptidase / metabolism
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Penicillin-Binding Proteins
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Peptidyl Transferases*
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Rabbits
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Staphylococcal Infections / drug therapy*
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Staphylococcal Infections / microbiology
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / enzymology
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Staphylococcus aureus / metabolism
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Sulbactam / pharmacology
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Sulbactam / therapeutic use
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beta-Lactamase Inhibitors
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beta-Lactamases / metabolism
Substances
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Bacterial Proteins
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Carrier Proteins
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Penicillin-Binding Proteins
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beta-Lactamase Inhibitors
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Cefoperazone
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Peptidyl Transferases
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Hexosyltransferases
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Muramoylpentapeptide Carboxypeptidase
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beta-Lactamases
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Sulbactam