The postantibiotic effect and post-β-lactamase-inhibitor effect of ceftazidime, ceftaroline and aztreonam in combination with avibactam against target Gram-negative bacteria

Lett Appl Microbiol. 2016 Aug;63(2):96-102. doi: 10.1111/lam.12592.

Abstract

The magnitudes of the postantibiotic effect (PAE) and post-β-lactamase-inhibitory effect (PLIE) of ceftazidime-avibactam, ceftaroline-avibactam, and aztreonam-avibactam were determined against isolates of Enterobacteriaceae and Pseudomonas aeruginosa that either harboured genes encoding serine and/or metallo-β-lactamases, or did not harbour bla genes. The bla genes included ones that encoded extended spectrum β-lactamases, AmpC and KPC β-lactamases, and one metallo-β-lactamase, NDM-1. No substantial PAE was observed for any combination against any isolate. One substantial PLIE was found: a value of 1·9 h for ceftazidime-avibactam against Klebsiella pneumoniae (blaKPC-2 ). From comparison with results in the literature, we propose that the existence of a substantial PLIE depends on the bacterial isolate and on the specific β-lactamase inhibitor and β-lactam combination.

Significance and impact of the study: A wave of new β-lactamase inhibitors is entering either therapeutic use or clinical trials. The present work characterizes the postantibiotic effect (PAE) and post-β-lactamase-inhibitory effect (PLIE) of the clinically most advanced of these compounds, avibactam. We show that the existence of a measurable PLIE is strain- (and possibly compound-) dependent, and cannot be relied upon as a standard component of the primary pharmacology of a new β-lactamase inhibitor. This variability was not reported in earlier studies of clavulanic acid or sulbactam.

Keywords: antibacterial agents; post-β-lactamase-inhibitor effect; postantibiotic effect; primary pharmacodynamics; β-lactamase inhibitors; β-lactams.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Azabicyclo Compounds / pharmacology*
  • Aztreonam / pharmacology*
  • Bacterial Proteins / genetics*
  • Ceftaroline
  • Ceftazidime / pharmacology*
  • Cephalosporins
  • Drug Combinations
  • Humans
  • Klebsiella pneumoniae / drug effects*
  • Klebsiella pneumoniae / genetics
  • Microbial Sensitivity Tests
  • Pseudomonas aeruginosa / drug effects*
  • Pseudomonas aeruginosa / genetics
  • Sulbactam / pharmacology
  • beta-Lactamase Inhibitors / pharmacology*
  • beta-Lactamases / genetics*

Substances

  • Anti-Bacterial Agents
  • Azabicyclo Compounds
  • Bacterial Proteins
  • Cephalosporins
  • Drug Combinations
  • avibactam, ceftazidime drug combination
  • beta-Lactamase Inhibitors
  • Ceftazidime
  • beta-lactamase KPC-1
  • AmpC beta-lactamases
  • beta-Lactamases
  • beta-lactamase NDM-1
  • Aztreonam
  • Sulbactam