A study of topiramate pharmacokinetics and tolerability in children with epilepsy

Pediatr Neurol. 1999 May;20(5):339-44. doi: 10.1016/s0887-8994(99)00011-9.

Abstract

The pharmacokinetic and safety profile of topiramate as adjunctive therapy was assessed in pediatric patients with epilepsy in an open-label, 4-week, single-center study. Six children from each of the following age groups were enrolled: 4-7 years, 8-11 years, and 12-17 years. Patients received topiramate 1 mg/kg/day for 1 week, with subsequent progressive weekly increases in dosage to 3, 6, and then 9 mg/kg/day or 800 mg/day, whichever was less. Topiramate oral plasma clearance (CI/F) was independent of dose, and steady-state plasma concentrations increased in proportion to dose. Weight-normalized topiramate CL/F was higher (P = 0.003) in pediatric patients receiving enzyme-inducing concomitant antiepileptic drugs (AEDs) (mean = 70.1 ml/minute/70 kg) than in those not receiving enzyme-inducing AEDs (mean = 33.1 mL/ minute/kg). Topiramate CL/F in children was approximately 50% greater than that observed in adults regardless of the type of concomitant AED therapy. Thus steady-state plasma topiramate concentrations for the same mg/kg dose will be approximately 33% lower in pediatric patients than in adult patients. The most frequently reported treatment-emergent adverse events considered related to topiramate therapy included anorexia, fatigue, and nervousness, and no patient discontinued therapy. This study indicates that, in children 4-17 years of age, topiramate has linear pharmacokinetics, 50% higher clearance than in adults, and is generally well tolerated.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Age Factors
  • Anticonvulsants / adverse effects*
  • Anticonvulsants / classification
  • Anticonvulsants / pharmacokinetics*
  • Area Under Curve
  • Child
  • Child, Preschool
  • Drug Interactions
  • Drug Therapy, Combination
  • Enzyme Induction
  • Epilepsy / drug therapy*
  • Epilepsy / metabolism*
  • Female
  • Fructose / adverse effects
  • Fructose / analogs & derivatives*
  • Fructose / pharmacokinetics
  • Humans
  • Male
  • Prospective Studies
  • Topiramate
  • Treatment Outcome

Substances

  • Anticonvulsants
  • Topiramate
  • Fructose