Emerging perspectives on the mechanism of action of gabapentin

Significant advances have been made in understanding the molecular and cellular mechanisms underlying seizure disorders and the actions of antiepileptic drugs. Agents with new mechanisms of action or enhanced activity via known mechanisms might provide improved seizure control or more selective therapy for specific epilepsies. Gabapentin is a new antiepileptic drug that is structurally similar to the neurotransmitter GABA and the endogenous amino acid L-leucine. The mechanism of action of gabapentin is not fully understood, but its distinct profile of anticonvulsant activity in animal seizure models and its lack of activity at many drug binding sites associated with other antiepileptic drugs indicate that its mechanism of action is novel.