THERAPEUTICS

Class

  • Neuroscience-based Nomenclature: glutamate receptor antagonist (Glu-RAn)
  • NMDA receptor antagonist; NMDA subtype of glutamate receptor antagonist; cognitive enhancer

MEMANTINE commonly prescribed for

(Bold for FDA approved)

• Alzheimer disease (moderate to severe)
• Alzheimer disease (mild to moderate)
• Memory disorders in other conditions
• Mild cognitive impairment
• Chronic pain

How MEMANTINE works

• Is a low to moderate affinity noncompetitive (open-channel) NMDA receptor antagonist, which binds preferentially to the NMDA receptor-operated cation channels

• Presumably interferes with the postulated persistent activation of NMDA receptors by excessive glutamate release in Alzheimer disease

How long until MEMANTINE works

• Memory improvement is not expected and it may take months before any stabilization in degenerative course is evident

SIDE EFFECTS

Notable Side Effects

• Dizziness, headache

• Constipation

Life Threatening Side Effects

• Seizures (rare)

weight gain

unusual

unusual

sedation

unusual

unusual

What to do about MEMANTINE side effects

• Wait

• Wait

• Wait

• Consider lowering dose or switching to a different agent

DOSING AND USE

usual dosage range

• 10 mg twice daily

• 28 mg once daily (extended-release)

• Namzaric extended-release (combination memantine/donepezil) 7 mg/10 mg, 14 mg/10 mg, 21 mg/10 mg, 28 mg/10 mg

Dosage Forms

• Tablet 5 mg, 10 mg

• Oral solution 2 mg/mL

• Extended-release capsule 7 mg, 14 mg, 21 mg, 28 mg

long term use

• Drug may lose effectiveness in slowing degenerative course of Alzheimer disease after 6 months

habit forming

• No

SPECIAL POPULATIONS

Renal Impairment

• No dose adjustment in mild or moderate impairment

• Reduce dose in severe impairment

• Severe renal impairment: the recommended maintenance dose for Namzaric is 14 mg/10 mg once daily in the evening

Hepatic Impairment

• Not likely to require dosage adjustment

Cardiac Impairment

• Not likely to require dosage adjustment

Elderly

• Pharmacokinetics similar to younger adults

Children and Adolescents

• Memantine use has not been studied in children or adolescents

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• Animal studies do not show adverse effects

• Not recommended for use in pregnant women or women of childbearing potential

Breast Feeding

• Unknown if memantine is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed

• Memantine is not recommended for use in nursing women