Levetiracetam is clinically used to treat a wide variety of seizure disorders, including partial, myoclonic, and tonic-clonic seizures as well as mood and psychiatric disorders such as anxiety, autism, and Tourette’s syndrome. Levetiracetam displays anticonvulsant/antiepileptic, neuromodulatory, anxiolytic, and cognition enhancing activities. Levetiracetam binds to synaptic vesicle glycoprotein SV2A, a membrane glycoprotein common to all synaptic and endocrine vesicles. SV2A plays a role in Ca2+-induced vesicle fusion, action potential proliferation, normal CNS function, and survival. Altering SV2A function inhibits presynaptic Ca2+ release, reduces excitatory postsynaptic potentials, and inhibits synaptic transmission. This compound is also under examination as a potential treatment for Alzheimer’s disease, as it reduces memory and learning deficits, synaptic dysfunction, and hippocampal remodeling in a transgenic murine model of the disease.