Population pharmacokinetics of micafungin in ICU patients with sepsis and mechanical ventilation

J Antimicrob Chemother. 2017 Jan;72(1):181-189. doi: 10.1093/jac/dkw352. Epub 2016 Sep 8.

Abstract

Objectives: To identify the factors associated with the interindividual pharmacokinetic (PK) variability of micafungin and to evaluate the probability of reaching the previously determined PK/pharmacodynamic efficacy thresholds (AUC/MIC >5000 for non-parapsilosis Candida sp. and ≥285 for Candida parapsilosis) with the recommended 100 mg daily dose in ICU patients with sepsis and mechanical ventilation.

Methods: One hundred patients were included and 436 concentrations were available for PK analysis performed with NONMEM software. PTA was determined by Monte Carlo simulations.

Results: Micafungin obeyed a two-compartment model with first-order elimination from the central compartment. Mean parameter estimates (percentage interindividual variability) were 1.34 L/h (34%) for clearance (CL), 11.80 L (38%) and 7.68 L (39%) for central (Vc) and peripheral (Vp) distribution volumes, respectively, and 4.67 L/h (37%) for distribution clearance. CL, Vc and Vp increased by 14% when the albumin level was ≤25 g/L and CL decreased by 25% when SOFA score was ≥10. Body weight was related to CL, Vc and Vp by allometric models. PTA was ≥90% in Candida albicans and Candida glabrata infections, except when the MIC was ≥0.015 mg/L, and ranged between 0% and 40% for C. parapsilosis infections with MIC ≥0.5 mg/L.

Conclusions: A possible increase in the dose should be evaluated for infections due to C. parapsilosis and for infections due to C. albicans and C. glabrata with MICs ≥0.015 mg/L.

Publication types

  • Clinical Trial

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antifungal Agents / administration & dosage
  • Antifungal Agents / pharmacokinetics*
  • Antifungal Agents / pharmacology*
  • Candida / drug effects
  • Candidemia / drug therapy*
  • Echinocandins / administration & dosage
  • Echinocandins / pharmacokinetics*
  • Echinocandins / pharmacology*
  • Female
  • Humans
  • Intensive Care Units
  • Lipopeptides / administration & dosage
  • Lipopeptides / pharmacokinetics*
  • Lipopeptides / pharmacology*
  • Male
  • Micafungin
  • Microbial Sensitivity Tests
  • Middle Aged
  • Monte Carlo Method
  • Respiration, Artificial*

Substances

  • Antifungal Agents
  • Echinocandins
  • Lipopeptides
  • Micafungin