Objective: The mechanism of action of levetiracetam (LEV), an antiepileptic drug, is related to a novel binding site, SV2, but LEV acts on GABA-A receptors. The objective of the study described here was to determine if LEV modulates brain GABA in vivo.
Methods: Concentrations of cerebral GABA and serum LEV were obtained in seven healthy individuals using 1H magnetic resonance spectroscopy at baseline and 3 and 6 hours following oral administration of 1 g of LEV.
Results: Brain cerebral GABA acutely concentrations did not change from baseline.
Conclusion: The results indicate that LEV does not increase human cerebral GABA concentrations acutely in healthy individuals.