Topiramate increases brain GABA, homocarnosine, and pyrrolidinone in patients with epilepsy

Neurology. 1999 Feb;52(3):473-8. doi: 10.1212/wnl.52.3.473.

Abstract

Objective: To measure the effects of topiramate on brain gamma-aminobutyric acid (GABA) in patients with epilepsy.

Background: Topiramate is a new antiepileptic medication with multiple putative mechanisms of action. In a recent meta-analysis of the newer antiepileptic drugs, topiramate was the most potent. Homocarnosine and pyrrolidinone are important metabolites of GABA with antiepileptic actions.

Methods: In vivo measurements of GABA, homocarnosine, and pyrrolidinone were made of a 14-cm3 volume in the occipital cortex using 1H spectroscopy with a 2.1-Tesla magnetic resonance spectrometer and an 8-cm surface coil. Twelve patients (eight women) with refractory complex partial seizures were studied while using topiramate. Nine epilepsy-free, drug-free volunteers served as control subjects.

Results: Topiramate increased mean brain GABA, homocarnosine, and pyrrolidinone concentrations in all patients. In paired measurements, brain GABA increased by 0.7 micromol/g (SD 0.3, n 7, 95% CI 0.4 to 1.0, p < 0.01). Homocarnosine increased by 0.5 micromol/g (SD 0.2, n 7, 95% CI 0.3 to 0.7, p < 0.001). Pyrrolidinone increased by 0.21 micromol/g (SD 0.06, n 7, 95% CI 0.16 to 0.27, p < 0.01). In two additional patients, GABA, homocarnosine, and pyrrolidinone increased after they were switched from vigabatrin to topiramate.

Conclusions: Topiramate increased brain GABA, homocarnosine, and pyrrolidinone to levels that could contribute to its potent antiepileptic action in patients with complex partial seizures.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adolescent
  • Adult
  • Anticonvulsants / metabolism*
  • Anticonvulsants / therapeutic use*
  • Brain / metabolism*
  • Carnosine / analogs & derivatives*
  • Carnosine / analysis
  • Epilepsy / drug therapy
  • Epilepsy / metabolism*
  • Female
  • Fructose / analogs & derivatives*
  • Fructose / metabolism
  • Fructose / therapeutic use
  • Humans
  • Magnetic Resonance Spectroscopy
  • Male
  • Middle Aged
  • Pyrrolidinones / analysis*
  • Topiramate
  • gamma-Aminobutyric Acid / analysis*

Substances

  • Anticonvulsants
  • Pyrrolidinones
  • Topiramate
  • Fructose
  • homocarnosine
  • gamma-Aminobutyric Acid
  • Carnosine