Influence of protein binding under controlled conditions on the bactericidal activity of daptomycin in an in vitro pharmacodynamic model

J Antimicrob Chemother. 2004 Jul;54(1):259-62. doi: 10.1093/jac/dkh259. Epub 2004 May 18.

Abstract

Objective: Daptomycin exhibits bactericidal activity against clinically significant Gram-positive bacteria despite being highly bound to human proteins. Evaluations characterizing the effect of protein on daptomycin pharmacodynamics are warranted.

Methods: We utilized an in vitro pharmacodynamic model to simulate daptomycin regimens of 6 mg/kg/day under controlled conditions of pH, calcium and/or protein. Free concentrations were simulated in broth, whereas total concentrations were simulated in broth supplemented with human albumin. Bacterial density was profiled over 48 h for two methicillin-resistant Staphylococcus aureus (MRSA) and two vancomycin-resistant Enterococcus faecium (VREF) clinical isolates.

Results: Daptomycin exhibited bactericidal activity against both MRSA isolates, with time to 99.9% killing occurring at 0.5 h and 8 h in broth and in albumin-supplemented broth, respectively. Initial kill was observed against both VREF isolates followed by regrowth. There was no statistical difference (P>0.05) in extent of bacterial kill at 24 or 48 h between the different media.

Conclusions: Although delayed, the extent of kill for daptomycin was unaltered against all isolates in albumin-supplemented broth. Further antimicrobial studies that incorporate protein are warranted to assess the influence of protein in the pharmacodynamic evaluation of antimicrobials.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology*
  • Culture Media
  • Daptomycin / pharmacokinetics
  • Daptomycin / pharmacology*
  • Drug Resistance, Bacterial
  • Enterococcus faecium / drug effects
  • Gram-Positive Bacterial Infections / microbiology
  • Humans
  • Methicillin Resistance
  • Microbial Sensitivity Tests
  • Protein Binding
  • Serum Albumin / metabolism
  • Serum Bactericidal Test
  • Staphylococcus aureus / drug effects
  • Vancomycin Resistance

Substances

  • Anti-Bacterial Agents
  • Culture Media
  • Serum Albumin
  • Daptomycin