The mechanism by which gabapentin exerts its anticonvulsant action is unknown, but in animal test systems designed to detect anticonvulsant activity, gabapentin prevents seizures as do other marketed anticonvulsants. The relevance of these models to human epilepsy is not known. Several test systems ordinarily used to assess activity at the NMDA receptor have been examined.
Results are contradictory.
Accordingly, no general statement about the effects, if any, of gabapentin at the NMDA receptor can be made. In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of rat brain including neocortex and hippocampus. The identity and function of this binding site remain to be elucidated. Food has no effect on the rate and extent of absorption of gabapentin. Gabapentin is eliminated from the systemic circulation by renal excretion as unchanged drug.