Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia

Crit Care Med. 2005 Jul;33(7):1529-33. doi: 10.1097/01.ccm.0000168206.59873.80.

Abstract

Objective: To determine the steady-state plasma pharmacokinetic variables and epithelial lining fluid concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.

Design: Prospective, open-label study.

Setting: An intensive care unit and research ward in a university hospital.

Patients: Sixteen critically ill adult patients with ventilator-associated pneumonia.

Interventions: All subjects received 1-hr intravenous infusions of linezolid 600 mg twice daily. After 2 days of therapy, the steady-state plasma pharmacokinetic variables and epithelial lining fluid concentrations of linezolid were determined by high-performance liquid chromatography.

Measurements and main results: The mean +/- sd linezolid peak and trough concentrations were 17.7 +/- 4.0 mg/L and 2.4 +/- 1.2 mg/L in plasma and 14.4 +/- 5.6 mg/L and 2.6 +/- 1.7 mg/L in epithelial lining fluid, respectively, showing a mean linezolid percentage penetration in epithelial lining fluid of approximately 100%. The mean +/- sd area under concentration-time curve during the observational period (AUC0-12) was 77.3 +/- 23.7 mg x hr/L, corresponding to a mean AUC0-24 of 154.6 mg x hr/L.

Conclusions: Our study shows satisfactory results, with linezolid concentrations exceeding the susceptibility breakpoint for Gram-positive bacteria in both plasma and epithelial lining fluid. This suggests that a dosage of 600 mg administered intravenously twice daily to critically ill patients with Gram-positive ventilator-associated pneumonia would achieve success against organisms with minimum inhibitory concentrations as high as 2-4 mg/L in both plasma and epithelial lining fluid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / blood
  • Acetamides / pharmacokinetics*
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics*
  • Area Under Curve
  • Bronchoalveolar Lavage Fluid / chemistry
  • Cross Infection / drug therapy*
  • Cross Infection / etiology
  • Female
  • Hospitals, University
  • Humans
  • Intensive Care Units
  • Linezolid
  • Lung / metabolism*
  • Male
  • Middle Aged
  • Oxazolidinones / blood
  • Oxazolidinones / pharmacokinetics*
  • Pneumonia, Bacterial / drug therapy*
  • Pneumonia, Bacterial / etiology
  • Prospective Studies
  • Respiration, Artificial / adverse effects*
  • Respiratory Mucosa / metabolism

Substances

  • Acetamides
  • Anti-Bacterial Agents
  • Oxazolidinones
  • Linezolid