Pharmacokinetics of gabapentin in paediatric patients with uncontrolled seizures

J Clin Pharm Ther. 2004 Dec;29(6):511-5. doi: 10.1111/j.1365-2710.2004.00596.x.

Abstract

Purpose: The pharmacokinetics of gabapentin in paediatric patients with uncontrolled seizures was studied.

Methods: Thirteen paediatric patients (mean age: 9.4 years) with uncontrolled partial seizures were included. Patients received gabapentin orally until doses were individualized to 9.6-39.8 mg/kg/day. Blood samples were obtained just prior to the dose and over 8 h after gabapentin was administered in the fasting state. The plasma concentration of gabapentin was measured by a high-performance liquid chromatography assay. Pharmacokinetic parameters for gabapentin were determined by non-compartment methods using multivariate regression analysis.

Results: Data from nine patients were suitable for pharmacokinetic analysis. The C(max) from 0.9 to 5.8 microg/mL (mean: 2.6 +/- 1.7 microg/mL) and T(max) from 0.5 to 2.0 h (mean: 1.6 +/- 1.0 h). The apparent clearance (Cl/F) ranged from 0.12 to 1.12 L/h/kg (mean: 0.50 +/- 0.29 L/h/kg), and the elimination half-life from 3.2 to 12.2 h (mean: 5.5 +/- 0.8 h). Five patients experienced moderate (n = 4) to severe (n = 1) aggressive behaviour and another gained weight on gabapentin.

Conclusions: Our data suggests that gabapentin pharmacokinetics can vary substantially among paediatric patients. Gabapentin was well tolerated in patients with uncontrolled partial seizures up to 6 months of therapy.

Publication types

  • Clinical Trial
  • Comparative Study

MeSH terms

  • Adolescent
  • Amines / administration & dosage
  • Amines / pharmacokinetics*
  • Amines / therapeutic use
  • Anticonvulsants / administration & dosage
  • Anticonvulsants / pharmacokinetics*
  • Anticonvulsants / therapeutic use
  • Child
  • Child, Preschool
  • Cyclohexanecarboxylic Acids / administration & dosage
  • Cyclohexanecarboxylic Acids / pharmacokinetics*
  • Cyclohexanecarboxylic Acids / therapeutic use
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Epilepsy, Partial, Sensory / drug therapy*
  • Female
  • Gabapentin
  • Humans
  • Male
  • Multivariate Analysis
  • Time Factors
  • gamma-Aminobutyric Acid / administration & dosage
  • gamma-Aminobutyric Acid / pharmacokinetics*
  • gamma-Aminobutyric Acid / therapeutic use

Substances

  • Amines
  • Anticonvulsants
  • Cyclohexanecarboxylic Acids
  • gamma-Aminobutyric Acid
  • Gabapentin