The Sound of Evolution
Memantine
Mechanism of action:
Memantine is an NMDA receptor antagonist. Memantine binds within the ion channel of the NMDA receptor, but it does not compete for the same binding site as glutamate or glycine. In Alzheimer's disease, chronic, low-level but persistent glutamate exposure causes abnormal activation of NMDA receptors, resulting in sustained calcium influx into neurons. This leads to mitochondrial dysfunction, increased oxidative stress, neuronal injury, and cell death. Memantine selectively blocks this pathological calcium influx.
Reference(s):
1. Cacabelos R et al. (1999). The glutamatergic system and neurodegeneration in dementia: preventive strategies in Alzheimer's disease. Int J Geriatr Psychiatry.
2. Rogawski MA et al. (2003). The neuropharmacological basis for the use of memantine in the treatment of Alzheimer's disease. CNS Drug Rev.
3. Robinson DM et al. (2006). Memantine: a review of its use in Alzheimer's disease. Drugs.