MEMANTINE (me-man'teen)
Namenda Classifications: n-methyl-d-aspartate (nmda) receptor antagonist; antidementia agent; Therapeutic: antidementia agent; nmda receptor antagonist Pregnancy Category: B
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Availability
5 mg, 10 mg tablets; 2 mg/mL solution
Action
Glutamate activation at the (N-methyl-D-aspartate) NMDA receptor is needed for memory and learning processes in the brain. Excess glutamate may play a role in
Alzheimer's disease by over-stimulating NMDA receptors, thus causing increased Ca2+ movement into neurons leading to neuronal damage. Memantine is a low-affinity, uncompetitive antagonist at NMDA receptors
in the brain. Blockade of NMDA receptors may slow intracellular calcium accumulation, preventing nerve damage without interfering
with actions of glutamate that are required for memory and learning.
Therapeutic Effect
Improves cognitive functioning in moderate-to-severe Alzheimer's disease (AD) and in mild-to-moderate vascular dementia.
Uses
Treatment of symptoms of moderate to severe Alzheimer's disease.
Unlabeled Uses
Treatment of moderate to severe vascular dementia.
Contraindications
Renal failure. Safety and efficacy in children are unknown.
Cautious Use
Moderate to severe renal impairment; history of seizure disorder; older adults; concurrent use with carbonic anhydrase inhibitors,
or sodium bicarbonate, pregnancy (category B), lactation.
Route & Dosage
Alzheimer's Disease Adult: PO Initiate with 5 mg once daily, increase dose by 5 mg/wk over a 3-wk period to target dose of 10 mg b.i.d.
Severe Renal Impairment Decrease to 5 mg b.i.d.
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Administration
Oral
- Note: The recommended interval between dose increases is 1 wk.
- Dose reductions should be considered with moderate renal impairment.
- Store between 15°30° C (59°86° F).
Adverse Effects (≥1%)
Body as a Whole: Fatigue, pain, flu-like
symptoms, peripheral edema.
CNS: Dizziness, headache, confusion, somnolence, hallucinations, agitation,
insomnia, abnormal gait,
depression, anxiety, syncope,
TIA, vertigo, ataxia, hypokinesia, aggressive reaction.
CV: Hypertension, cardiac failure.
GI: Constipation, vomiting,
diarrhea, nausea, anorexia.
Hematologic: Anemia.
Metabolic: Weight loss, increased
alkaline phosphatase.
Musculoskeletal: Back pain,
arthralgia.
Respiratory: Coughing,
dyspnea,
bronchitis, upper respiratory infections,
pneumonia.
Skin: Rash.
Special Senses: Conjunctivitis.
Urogenital: Urinary incontinence, UTI, frequent micturition.
Interactions
Drug: Drugs that increase the pH of the urine (
CARBONIC ANHYDRASE INIBITORS,
sodium bicarbonate) may increase levels of memantine; may enhance the effects of
amantadine, dextromethorphan, ketamine, bromocriptine, pergolide, pramipexole, and
ropinirole; may enhance the adverse effects of
levodopa-containing drugs.
Pharmacokinetics
Absorption: 100% from GI tract.
Duration: 46 h.
Distribution: Easily crosses the bloodbrain barrier.
Metabolism: Minimal.
Elmination: Primarily excreted unchanged in urine. Increases in urinary pH can decrease elimination of drug.
Half-Life: 6080 h.
Nursing Implications
Assessment & Drug Effects
- Monitor respiratory and CV status, especially with preexisting heart disease.
- Assess for and report S&S of focal neurologic deficits (e.g., TIA, ataxia, vertigo).
- Lab tests: Periodic Hct & Hgb, serum sodium, alkaline phosphatase, and blood glucose.
- Monitor diabetics for loss of glycemic control.
Patient & Family Education
- Report any of the following to the physician: problems with vision, skin rash, shortness of breath, swelling in throat or
tongue, agitation or restlessness, confusion, dizziness, or incontinence.
- Do not drive or engage in other hazardous activities until reaction to drug is known.