Memantine. A Review of its Use in Alzheimer’s Disease
Memantine is an orally active, low-to-moderate affinity, uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist with voltage-dependent binding characteristics approved in the US, Canada and Europe for the treatment of patients with moderate-to-severe Alzheimer’s disease. Memantine blocks the excessive influx of calcium, induced by chronic overstimulation of the NMDA receptor, that promotes neuronal necrosis and apoptosis. In well designed clinical trials in patients with mild-to-moderate or moderate-to-severe Alzheimer’s disease, oral memantine, as monotherapy or in conjunction with the anticholinesterase donepezil, slowed the progressive decline in global and individual measures of cognitive performance, function and behaviour with respect to placebo or placebo plus donepezil. Memantine was generally well tolerated during clinical trials with most adverse events being of mild or moderate severity. Thus, memantine is a useful option for the treatment of Alzheimer’s disease and is the only pharmacotherapeutic agent shown to have beneficial effects in moderate-to-severe disease.
