Memantine
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Anti-dementia medicine, NMDA receptor antagonist (uncompetitive, low-affinity), Adamantane derivative
Memantine
Namenda (IR), Namenda XR (extended-release), Namzaric (with donepezil)
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Summary
Classes
Common uses
Alzheimer disease dementia, moderate to severe (FDA, often with donepezil)0, Vascular dementia (off-label)0, Lewy body dementia (off-label)0, Parkinson disease dementia (off-label)0
Pharmacy
Starting dose
5 mg PO once daily; titrate by 5 mg weekly to target 10 mg PO BID. XR formulation: 7 mg/day, titrate to 28 mg/day
Preparations
IR tablets 5, 10 mg; oral solution 2 mg/mL; XR capsules 7, 14, 21, 28 mg
US FDA Max
20 mg/day (IR); 28 mg/day (XR)
Pharmacology
Routes
Oral
Onset
Cognitive effect emerges gradually over weeks to months; symptomatic effect only
Duration
BID dosing for IR; once-daily for XR
Half-life
60-100 hours (long)[1]
Bioavailability
~100% (oral)[1]
Pregnancy
Limited human data; rarely indicated in pregnancy given the patient population.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Uncompetitive, voltage-dependent NMDA receptor antagonist with low-to-moderate affinity. Binds within the open channel pore, preferentially blocking the pathological tonic NMDA activity that drives glutamate excitotoxicity in Alzheimer disease, while permitting the physiological transient NMDA activity required for long-term potentiation and memory formation. The "Goldilocks affinity" (strong enough to block excess but weak enough to detach during normal synaptic events) distinguishes memantine from high-affinity NMDA antagonists like ketamine, dextromethorphan, and phencyclidine that produce dissociative anesthesia.0 Symptomatic-only effect; does not alter the underlying neurodegenerative trajectory. Generally well tolerated; principal adverse effects are dizziness, headache, and confusion. Renally eliminated, with dose adjustment required in severe renal impairment[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Namenda (memantine hydrochloride), Allergan/AbbVie, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s019,021627s019lbl.pdf