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memantine (Namenda XR, Namenda)

 

Classes: NMDA Antagonists

Dosing and uses of Namenda XR (memantine)

 

Adult dosage forms and strengths

tablet

  • 5mg
  • 10mg

capsule, extended-release

  • 7mg
  • 14mg
  • 21mg
  • 28mg

oral solution

  • 2mg/mL

 

Alzheimer-Type Dementia

Treatment of moderate-to-severe dementia

Tablet: 5 mg PO once daily initially; increased by increments of 5 mg/day each week; maintenance target dosage (>5 weeks): 20 mg/day PO divided q12hr

Extended-release capsule: 7 mg PO qDay initially; may be increased by increments of 7 mg/day each week; maintenance target dose is 28 mg PO qDay

 

Dosage modifications

Renal impairment

  • Mild or moderate: No dosage adjustment required
  • Severe: (CrCl 5-29 mL/min): Not to exceed 14 mg/day (extended-release) or 5 mg BID (prompt-release)

Hepatic impairment

  • Mild or moderate (Child Pugh A/B): No dosage adjustment required
  • Severe (Child Pugh C): Caution

 

Administration

May take with or without food

Consume entire capsule contents, do not divide the dose

Swallow capsule whole or open and sprinkle on spoonful of applesauce; do not chew or crush

Do not mix oral solution with any other liquid

Missed dose: Do not double next dose, the next dose should be taken as scheduled; if missed for several days, dosing may need to be resumed at lower doses and retitrated as described above

 

Mild-to-Moderate Vascular Dementia (Off-label)

5 mg (immediate-release) PO qDay; titrate by 5 mg q7days to target dose 10 mg twice daily

 

Pediatric dosage forms and strengths

Not indicated

 

Namenda XR (memantine) adverse (side) effects

1-10%

Dizziness (7%)

Confusion (6%)

Headache (6%)

Constipation (5%)

Cough (4%)

Hypertension (4%)

Backache (3%)

Pain (3%)

Somnolence (3%)

Syncope (3%)

Vomiting (3%)

Dyspnea (2%)

Fatigue (2%)

 

<1%

Acute renal failure

Cerebral infarction

Cerebrovascular accident

Deep venous thrombosis

Hepatitis, liver failure

Intracranial hemorrhage

Neuroleptic malignant syndrome

Seizure (including grand mal)

Stevens-Johnson syndrome

Transient ischemic attack

 

Postmarketing Reports

Blood and lymphatic system disorders: Agranulocytosis, leukopenia (including neutropenia), pancytopenia, thrombocytopenia, thrombotic thrombocytopenic purpura

Cardiac disorders: Cardiac failure congestive

Gastrointestinal disorders: Pancreatitis

Hepatobiliary disorders: Hepatitis

Psychiatric disorders: Suicidal ideation

Renal and urinary disorders: Acute renal failure (including increased creatinine and renal insufficiency)

Skin disorders: Stevens Johnson syndrome

 

Warnings

Contraindications

Hypersensitivity to memantine or components of the formulation

 

Cautions

Not evaluated in patients with seizure disorder; seizures occurred in 0.2% of patients

Conditions that raise urine pH may decrease urinary elimination and increase plasma levels of memantine

Use caution in cardiovascular disease, seizure disorder, ophthalmic disease, hepatic and/or renal impairment

 

Pregnancy and lactation

Pregnancy category: B

Lactation: Unknown whether drug is excreted into breast milk; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Namenda XR (memantine)

Mechanism of action

Low- to moderate-affinity uncompetitive N-methyl-D-aspartate (NMDA) receptor (NMDAR) antagonist that binds preferentially to NMDAR-operated cation channels, blocking receptor only under conditions of excessive stimulation, with no effect on normal neurotransmission

 

Absorption

Peak plasma time: 3-7 hr (immediate release); 9-12 hr (extended release)

 

Distribution

Protein bound: 45%

Vd: 9-11 L/kg

 

Metabolism

Metabolites: 3 polar metabolites (minimally active)

 

Elimination

Half-life: 60-80 hr

Excretion: Urine (74%)