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Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses
11:17

Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses

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Single dose pharmacokinetics of linezolid in infants and children

G L Kearns1, S M Abdel-Rahman, J L Blumer

  • 1Department of Pediatrics, University of Missouri-Kansas City, USA. gkearns@cmh.edu

The Pediatric Infectious Disease Journal
|January 6, 2001
PubMed

Insights

Linezolid, an antibiotic effective against resistant bacteria, showed age-dependent pharmacokinetics in children. A dose of 10 mg/kg twice daily is suggested for pediatric trials.

Area of Science:

  • Pharmacology
  • Pediatric Infectious Diseases
  • Drug Metabolism

Background:

  • Linezolid is an oxazolidinone antibiotic with potent in vitro activity against Gram-positive bacteria, including resistant strains.
  • Understanding the safety and pharmacokinetics of intravenous linezolid in pediatric populations is crucial for effective treatment.
  • This study investigated age-dependent disposition characteristics of linezolid in children and adolescents.

Purpose of the Study:

  • To evaluate the safety and pharmacokinetics of intravenous linezolid in pediatric patients.
  • To determine if linezolid disposition is dependent on age in children and adolescents.
  • To inform appropriate dosing strategies for linezolid in pediatric populations.

Main Methods:

  • Fifty-eight children aged 3 months to 16 years received single intravenous doses of linezolid (1.5 or 10 mg/kg).
  • Plasma samples were collected over 24 hours and analyzed for linezolid concentrations using high-performance liquid chromatography with mass spectrometry detection.
  • Model-independent pharmacokinetic analysis was employed to evaluate plasma concentration-time data.

Main Results:

  • Linezolid was well-tolerated across all age groups studied.
  • Linezolid disposition was found to be age-dependent, with a weak correlation between age and total body clearance.
  • Clearance and volume of distribution were significantly higher in children compared to adults, potentially leading to lower peak concentrations and sub-therapeutic levels at 12 hours post-dose with the 10 mg/kg regimen.

Conclusions:

  • A twice or thrice daily intravenous dose of 10 mg/kg linezolid is proposed as appropriate for pediatric clinical trials.
  • The findings highlight the need for weight-based dosing adjustments in pediatric patients due to age-dependent pharmacokinetics.
  • Further research is warranted to optimize linezolid dosing in children to ensure therapeutic efficacy.
Abstract

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