Memantine
NMDA receptor antagonist, a prescription Alzheimer's drug that limits glutamate excitotoxicity.
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Pharmacology
Contents
WHAT IS MEMANTINE?
Detailed overview
Memantine is an uncompetitive, low-affinity, voltage-dependent antagonist of the NMDA subtype of glutamate receptor, approved by the FDA (2003) and the EMA for moderate-to-severe Alzheimer's disease under brand names such as Namenda, Ebixa and Axura. Its fast channel-leaving kinetics allow normal synaptic transmission during strong physiological glutamate signals while it dampens the chronic, low-level glutamate leakage thought to drive excitotoxic calcium overload and neuronal stress in disease. In randomized controlled trials it produces a modest slowing of cognitive and functional decline rather than reversal of the disease, and it is frequently combined with cholinesterase inhibitors such as donepezil. It has a long half-life of roughly 60 to 100 hours and is usually titrated gradually to a 20 mg daily target.
Mechanism
NMDA antagonist (uncompetitive, low-affinity)
Half-life
~60-100 hours
Legal status
Prescription drug (FDA/EMA approved)
Receptor profile
- NMDA receptorsStrong
- Excess glutamate / excitotoxic calcium influxStrong
- 5-HT3 and α7 nicotinic acetylcholine receptorsWeak
- Dopamine (indirect)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Dizziness
- Headache
- Confusion or cognitive slowing, especially at higher doses
- Constipation
- Somnolence, less often restlessness or agitation
- Occasional rise in blood pressure
Contraindications · 4
- Severe renal impairment: dose reduction required, risk of accumulation
- Pregnancy and breastfeeding: safety not established, use only if clearly needed
- History of seizures: use with caution
- Known hypersensitivity to memantine
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Memantine in moderate-to-severe Alzheimer's disease
Reisberg B, Doody R, Stöffler A, Schmitt F, Ferris S, Möbius HJ
Memantine treatment in patients with moderate to severe Alzheimer disease already receiving donepezil: a randomized controlled trial
Tariot PN, Farlow MR, Grossberg GT, Graham SM, McDonald S, Gergel I
Memantine treatment in mild to moderate Alzheimer disease: a 24-week randomized, controlled trial
Peskind ER, Potkin SG, Pomara N, Ott BR, Graham SM, Olin JT, McDonald S
The safety, tolerability, and efficacy of once-daily memantine (28 mg): a multinational, randomized, double-blind, placebo-controlled trial in patients with moderate-to-severe Alzheimer's disease taking cholinesterase inhibitors
Grossberg GT, Manes F, Allegri RF, et al.
Memantine for dementia
McShane R, Westby MJ, Roberts E, et al.
FAQ
FAQ
NMDA receptor antagonist, a prescription Alzheimer's drug that limits glutamate excitotoxicity.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.