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Single dose pharmacokinetics of trimethoprim

Insights

Pediatric pharmacokinetics of trimethoprim showed rapid absorption and distribution in children. Faster clearance and shorter half-life in children suggest increased metabolism compared to adults, with sustained therapeutic urine concentrations.

Area of Science:

  • Pharmacology
  • Pediatric Medicine
  • Drug Metabolism

Background:

  • Trimethoprim is an antibiotic commonly used to treat bacterial infections.
  • Understanding trimethoprim pharmacokinetics in children is crucial for appropriate dosing and efficacy.
  • Limited data exists on trimethoprim's pharmacokinetic profile in diverse pediatric age groups.

Purpose of the Study:

  • To determine the pharmacokinetic parameters of a single oral dose of trimethoprim in children.
  • To compare trimethoprim's absorption, distribution, metabolism, and excretion in children versus adults.
  • To assess the achievement and duration of therapeutic urine concentrations in pediatric patients.

Main Methods:

  • A single oral dose pharmacokinetic study was conducted.
  • Eighteen children aged 3 months to 13 years were enrolled.
  • Trimethoprim concentrations in plasma and urine were measured over time.

Main Results:

  • Trimethoprim was rapidly absorbed and widely distributed in pediatric subjects.
  • Mean clearance was significantly faster, and elimination half-life was shorter in children compared to adults.
  • Urinary recovery of trimethoprim was lower in children, suggesting greater metabolism; however, concentrations exceeded MICs for pathogens for at least 16 hours.

Conclusions:

  • Children exhibit distinct trimethoprim pharmacokinetics compared to adults, characterized by faster elimination.
  • The observed metabolic profile in children necessitates careful consideration for optimal therapeutic outcomes.
  • Achieved and sustained high urinary trimethoprim concentrations indicate potential for effective treatment of pediatric urinary tract infections.

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