1986
DOI: 10.1128/aac.29.5.845
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Affinity of cephalosporins for beta-lactamases as a factor in antibacterial efficacy

Abstract: Strains of Escherichia coli, Enterobacter aerogenes, and Enterobacter cloacae that were resistant to ceftazidime (MIC > 16 ,ug/ml) but susceptible to BMY 28142 (MIC < 4 ,ug/ml) were found to contain higher levels of j-lactamase activity (50-to 3,340-fold) than control strains of the corresponding species. Ceftazidime was at least as resistant as BMY 28142 to hydrolysis by these enzymes. However, the apparent K, of BMY 28142 for each enzyme was larger (8-to >20-fold) than that of ceftazidime; i.e., the affinity… Show more

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Cited by 75 publications
(52 citation statements)
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“…In addition, cefepime appears to have a low affinity for chromosomally derived P-lactamases (23). Clinical experience indicates that cefepime is safe and well tolerated when single or multiple (every 8 or 12 h) doses of 250 to 2,000 mg are given by the intravenous (4, 5) or intramuscular (9) routes of administration.…”
mentioning
confidence: 99%
“…In addition, cefepime appears to have a low affinity for chromosomally derived P-lactamases (23). Clinical experience indicates that cefepime is safe and well tolerated when single or multiple (every 8 or 12 h) doses of 250 to 2,000 mg are given by the intravenous (4, 5) or intramuscular (9) routes of administration.…”
mentioning
confidence: 99%
“…In agreement with the notion that low hydrolysis rates at low sub;trate concentrations represent the most important factor in producing truly P-lactamase-stable compounds, they share low affinities or high Km values for type I enzymes and are therefore expected to be hydrolyzed much more slowly in pharmacologically relevant situations. These compounds include cefepime (BMY-28142) (14), cefpirome (HR-810) (7), and E-1040 (23). They are characterized by containing, at the 3 position, substituents with quaternary nitrogen atoms (Fig.…”
mentioning
confidence: 99%
“…A considerable number of ceftazidime/cefotaxime-resistant Gram-negative bacteria were found to be inhibited by BMY-28142. This may be explained, in part, by the finding of PHELPS et al 15) that BMY-28142 has low binding affinity for (3-lactamases combined with high resistance to hydrolysis. The anti-pseudomonal bactericidal activity of BMY-28142 was similar to that of ceftazidime.…”
Section: Discussionmentioning
confidence: 96%