Gabapentin (Neurontin) was first introduced in 1994 to treat partial epilepsy.72 It is structurally similar to GABA, possibly exerting GABA-ergic activity by binding to receptors in neocortex and hippocampus. However, it does not bind conventional GABA(A), GABA(B), glycine, glutamate, benzodiazepine, or N-methyl-D-aspartate (NMDA) receptors.73,74
It is well absorbed, reaching peak plasma concentrations in 2 to 3 hours, is not protein-bound, does not undergo metabolism, and is excreted unchanged in the urine.
Gabapentin is well tolerated in doses of 1,800 to 3,600 mg per day in divided doses.75
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Reviewed and revised May 2004 by Steven C. Schachter, MD, epilepsy.com Editorial Board.
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