On the kinetic interaction between ceftriaxone and some beta-lactamases

Drugs Exp Clin Res. 1988;14(1):25-30.

Abstract

The activity of beta-lactamases from Citrobacter diversus ULA-27 on ceftriaxone, a widely recognized third-generation cephalosporin, has been examined and compared to the activity of various other beta-lactamases from different sources. Ceftriaxone (Roche S.p.A. Milan) was found to be resistant to hydrolysis by beta-lactamases from Enterobacter cloacae and Bacillus cereus, but susceptible to beta-lactamases from Mycobacterium fortuitum strain Cow 18 and, mostly, to beta-lactamases from various strains of Citrobacter diversus. Derivatives with substituents in the 3-position of ceftriaxone, namely cefotaxime (Roussel Maestretti S.p.A., Milan) and ceftizoxime (Farmitalia Carlo Erba, Milan), were much less susceptible to hydrolysis by C. diversus ULA-27 enzymes (22 and 6% of ceftriaxone hydrolysis, respectively), the hydrolysis rate being paralleled by differences in MIC values. Ceftriaxone inhibited the activity of E. cloacae beta-lactamases toward cefazolin as substrate, but the inhibition was totally abolished by preincubation of ceftriaxone with the enzyme before addition of the substrate. Overall, the data point to a relevance of C. diversus ULA-27 beta-lactamases in the mechanism of resistance of this strain to the various third-generation cephalosporins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacillus / drug effects
  • Bacillus / enzymology*
  • Ceftriaxone / metabolism*
  • Ceftriaxone / pharmacology
  • Citrobacter / drug effects
  • Citrobacter / enzymology
  • Enterobacter / drug effects
  • Enterobacter / enzymology
  • Enterobacteriaceae / drug effects
  • Enterobacteriaceae / enzymology*
  • Kinetics
  • Mycobacterium / enzymology*
  • Nontuberculous Mycobacteria / drug effects
  • Nontuberculous Mycobacteria / enzymology*
  • Time Factors
  • beta-Lactamases / metabolism*
  • beta-Lactamases / pharmacology

Substances

  • Ceftriaxone
  • beta-Lactamases