Comparative in vitro and in vivo efficacies of human simulated doses of ceftazidime and ceftazidime-avibactam against Pseudomonas aeruginosa

Antimicrob Agents Chemother. 2012 Dec;56(12):6137-46. doi: 10.1128/AAC.00851-12. Epub 2012 Sep 17.

Abstract

The combination of ceftazidime and avibactam possesses potent activity against resistant Gram-negative pathogens, including Pseudomonas aeruginosa. We compared the efficacies of human simulated doses of ceftazidime and ceftazidime-avibactam using a hollow-fiber system and neutropenic and immunocompetent murine thigh infection models. Twenty-seven clinical P. aeruginosa isolates with ceftazidime MICs of 8 to 128 mg/liter and ceftazidime-avibactam MICs of 4 to 32 mg/liter were utilized in neutropenic mouse studies; 15 of the isolates were also evaluated in immunocompetent mice. Six isolates were studied in both the hollow-fiber system and the neutropenic mouse. In both systems, the free drug concentration-time profile seen in humans given 2 g of ceftazidime every 8 h (2-h infusion), with or without avibactam at 500 mg every 8 h (2-h infusion), was evaluated. In vivo activity was pharmacodynamically predictable based on the MIC. Ceftazidime decreased bacterial densities by ≥0.5 log unit for 10/27 isolates, while ceftazidime-avibactam did so for 22/27 isolates. In immunocompetent animals, enhancements in activity were seen for both drugs, with ceftazidime achieving reductions of ≥0.3 log unit for 10/15 isolates, whereas ceftazidime-avibactam did so against all 15 isolates. In vitro, ceftazidime resulted in regrowth by 24 h against all isolates, while ceftazidime-avibactam achieved stasis or better against 4/7 isolates. Mutants with elevated ceftazidime-avibactam MICs appeared after 24 h from 3/7 isolates studied in vitro; however, no resistant mutants were detected in vivo. Against this highly ceftazidime-nonsusceptible population of P. aeruginosa, treatment with human simulated doses of ceftazidime-avibactam resulted in pharmacodynamically predictable activity, particularly in vivo, against isolates with MICs of ≤16 mg/liter, and this represents a potential new option to combat these difficult-to-treat pathogens.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / therapeutic use*
  • Azabicyclo Compounds / administration & dosage*
  • Azabicyclo Compounds / therapeutic use*
  • Ceftazidime / administration & dosage*
  • Ceftazidime / therapeutic use*
  • Drug Resistance, Bacterial
  • Female
  • Humans
  • Immunocompetence
  • Mice
  • Mice, Inbred ICR
  • Microbial Sensitivity Tests
  • Neutropenia / complications
  • Pseudomonas Infections / drug therapy*
  • Pseudomonas aeruginosa / drug effects
  • Thigh / pathology
  • beta-Lactamase Inhibitors

Substances

  • Anti-Bacterial Agents
  • Azabicyclo Compounds
  • beta-Lactamase Inhibitors
  • avibactam
  • Ceftazidime