Pregabalin, the most recently approved antiepileptic drug, is a structural analog of GABA with a favorable pharmacokinetic profile. Pregabalin binds to the alpha2-delta subunit of a neuronal voltage-gated calcium channel and is believed to exert its anticonvulsant effect by modulating the release of specific neurotransmitters from hyperexcited presynaptic neurons. Animal models of epilepsy have suggested that this drug will be efficacious against partial-onset and generalized tonic-clonic seizures. Four pivotal, add-on clinical trials conducted in patients with partial-onset seizures demonstrated that pregabalin at daily doses of 150-600 mg is efficacious and associated with dose-dependent adverse events. Meta-analyses of efficacy and tolerability indicated that pregabalin is an efficacious and relatively well-tolerated antiepileptic drug.