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Memantine

Class
Indications
  • Moderate to severe Alzheimer's disease
Administration/Absorption
  • Well absorbed orally with a bioavailability of approximately 100%
  • Peak plasma concentrations are reached in 3-7 hours
Dosage

Distribution

Mechanism
  • Low-affinity voltage-dependent uncompetitive antagonist at glutamatergic NMDA receptors
  • Binds to the NMDA receptor with a higher affinity than Mg2+ ions
    • Therefore able to inhibit the prolonged influx of Ca2+ ions, which forms the basis of neuronal excitotoxicity
  • The low affinity and rapid off-rate kinetics of memantine at the level of the NMDA receptor-channel, however, preserves the physiological function of the receptor
  • Secondary effects of unknown clinical significance:
Excretion
  • Excreted largely unchanged
    • About 20% is metabolized to 1-amino-3-hydroxymethyl-5-methyl-adamantane and 3-amino-1-hydroxy-5,7-dimethyl-adamantane.
  • Half-life 60-100 hrs
Side effects
  • Confusion, dizziness, drowsiness, headache, insomnia, agitation, and/or hallucinations
Interactions

Contraindications

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