Evaluation of pharmacokinetic target attainment and hematological toxicity of linezolid in pediatric patients

Eur J Clin Pharmacol. 2024 Nov;80(11):1807-1817. doi: 10.1007/s00228-024-03740-3. Epub 2024 Aug 25.

Abstract

Background: Linezolid is commonly used to treat severe and/or resistant Gram-positive infections. Few studies have assessed its pharmacokinetic (PK) target attainment in pediatrics.

Objective: To evaluate the percentage of pediatrics achieving the PK targets of linezolid with standard dosing regimens and to assess the incidence and risk factors associated with its hematologic toxicity.

Methods: This prospective observational study included pediatric patients aged 0-14 who received linezolid for suspected or proven Gram-positive infections. Linezolid trough concentrations and the 24-h area under the curve (AUC24) were estimated, and hematologic toxicity was assessed.

Results: Seventeen pediatric patients (5 neonates and 12 older pediatrics) were included. A wide variability was observed in linezolid's trough and AUC24 (ranging from 0.5 to 14.4 mg/L and from 86 to 700 mg.h/L, respectively). The median AUC24 was significantly higher in neonates than older pediatrics (436 [350-574] vs. 200 [134-272] mg,h/L, P = 0.01). Out of all patients, only 41% achieved adequate drug exposure (AUC24 160-300 mg.h/L and trough 2-7 mg/L), with 24% having subtherapeutic, and 35% having higher-than-optimal exposures. Hematological toxicity was observed in 53% of cases. Identified risk factors include treatment duration over 7 days, baseline platelet counts below 150 × 109/L, sepsis/septic shock, and concomitant use of meropenem.

Conclusions: Linezolid's standard dosing failed to achieve its PK targets in approximately half of our pediatric cohort. Our findings highlight the complex interplay between the risk factors of linezolid-associated hematological toxicity and underscore the importance of its vigilant use and monitoring, particularly in pediatrics with concomitant multiple risk factors.

Keywords: Drug exposure; Hematologic toxicity; Linezolid; Pediatrics; Pharmacokinetics.

Publication types

  • Observational Study

MeSH terms

  • Adolescent
  • Anti-Bacterial Agents* / administration & dosage
  • Anti-Bacterial Agents* / adverse effects
  • Anti-Bacterial Agents* / pharmacokinetics
  • Area Under Curve
  • Child
  • Child, Preschool
  • Female
  • Gram-Positive Bacterial Infections / drug therapy
  • Humans
  • Infant
  • Infant, Newborn
  • Linezolid* / administration & dosage
  • Linezolid* / adverse effects
  • Linezolid* / blood
  • Linezolid* / pharmacokinetics
  • Male
  • Prospective Studies
  • Risk Factors

Substances

  • Linezolid
  • Anti-Bacterial Agents