Ebixa


memantine

Ebixa (CA) (UK), Namenda

Pharmacologic class: N-methyl-D-aspartate receptor antagonist (NMDA)

Therapeutic class: Anti-Alzheimer's agent

Pregnancy risk category B

Action

Unclear. Thought to act as a low- to moderate-affinity NMDA receptor antagonist, binding to NMDA receptor-operated channels. (Activation of these channels is thought to contribute to Alzheimer's symptoms.)

Availability

Oral solution: 2 mg/ml

Tablets: 5 mg, 10 mg

Tablets (titration pack): 28 tablets of 5 mg and 21 tablets of 10 mg

Indications and dosages

Moderate to severe Alzheimer's-type dementia

Adults: Initially, 5 mg P.O. daily. Then titrate at intervals of at least 1 week in 5-mg increments, to a maximum of 10 mg P.O. b.i.d.

Dosage adjustment

• Moderate renal impairment

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• neurologic conditions, moderate to severe renal impairment, genitourinary conditions that increase pH

• pregnant or breastfeeding patients.

Administration

• Give with or without food.

Adverse reactions

CNS: dizziness, headache, syncope, aggressive reaction, confusion, somnolence, hallucinations, agitation, insomnia, vertigo, ataxia, abnormal gait, hypokinesia, anxiety, transient ischemic attack, cerebrovascular accident (CVA)

CV: hypertension, cardiac failure

EENT: cataract, conjunctivitis

GI: nausea, vomiting, diarrhea, constipation, anorexia

GU: frequent voiding, urinary incontinence, urinary tract infection

Hematologic: anemia

Musculoskeletal: back pain, arthralgia

Respiratory: cough, dyspnea, bronchitis, pneumonia

Skin: rash

Other: weight loss, fatigue, pain, falls, flulike symptoms, peripheral edema

Interactions

Drug-drug. Cimetidine, hydrochlorothiazide, nicotine, quinidine, ranitidine, triamterene: altered blood levels of both drugs

Urine-alkalizing drugs (carbonic anhydrase inhibitors, sodium bicarbonate): decreased memantine elimination

Drug-diagnostic tests. Alkaline phosphatase: increased level

Patient monitoring

See Check for heart failure and signs and symptoms of CVA.

• Monitor kidney function tests.

Patient teaching

• Tell patient to take with or without food.

• Instruct patient or caregiver not to mix solution with other liquids and to take or give oral solution only with included dosing device.

• Make sure patient or caregiver understands dose escalation.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

memantine

(me-man-teen) memantine,

Ebixa

(trade name),

Namenda

(trade name),

Namenda XR

(trade name)

Classification

Therapeutic: anti alzheimers agents
Pharmacologic: n methyl d aspartate antagonist
Pregnancy Category: B

Indications

Moderate to severe dementia/neurocognitive disorder associated with Alzheimer's disease.

Action

Binds to CNS N-methyl-D-aspartate (NMDA) receptor sites, preventing binding of glutamate, an excitatory neurotransmitter.

Therapeutic effects

Decreased symptoms of dementia/cognitive decline. Does not slow progression.Cognitive enhancement.Does not cure disease.

Pharmacokinetics

Absorption: Well absorbed after oral administration.Distribution: Unknown.Metabolism and Excretion: 57–82% excreted unchanged in urine by active tubular secretion moderated by pH dependent tubular reabsorption. Remainder metabolized; metabolites are not pharmacologically active.Half-life: 60–80 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POunknown3–7 hr12 hr
PO-ERunknown9–12 hr24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity.Use Cautiously in: Severe renal impairment (↓ dose);Concurrent use of other NMDA antagonists (amantadine, rimantadine, ketamine, dextromethorphan);Concurrent use of drugs or diets that cause alkaline urine;Conditions that ↑ urine pH including severe urinary tract infections or renal tubular acidosis (lead to ↓ excretion and ↑ levels); Obstetric / Lactation / Pediatric: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness
  • fatigue
  • headache
  • sedation

Cardiovascular

  • hypertension

Dermatologic

  • rash

Gastrointestinal

  • diarrhea
  • weight gain

Genitourinary

  • urinary frequency

Hematologic

  • anemia

Interactions

Drug-Drug interaction

Medications that ↑ urine pH (e.g. carbonic anhydrase inhibitors, sodium bicarbonate ) may↓ excretion and ↑ blood levels.

Route/Dosage

Oral (Adults) Immediate-release—5 mg once daily initially, ↑ at weekly intervals to 10 mg/day (5 mg twice daily), then 15 mg/day (5 mg once daily, 10 mg once daily as separate doses), then to target dose of 20 mg/day (10 mg twice daily); Extended-release—7 mg once daily, ↑ at weekly intervals by 7 mg/day to target dose of 28 mg once daily.

Renal Impairment

(Adults) CCr 5–29 mL/min—Immediate-release: Target dose is 10 mg/day (5 mg twice daily); Extended-release: Target dose is 14 mg once daily.

Availability

Immediate-release tablets: 5 mg, 10 mg, titration package containing twenty-eight 5 mg tablets and twenty-one 10 mg tablets Cost: 5 mg $887.69 / 180Extended-release capsules: 7 mg, 14 mg, 21 mg, 28 mg Cost: 7 mg $302.62 / 30, 14 mg $907.85 / 90, 21 mg $302.62 / 30, 28 mg $907.85 / 90Oral solution, sugar-free, alcohol-freepeppermint: 2 mg/mL Cost: $668.50 / 360 mL

Nursing implications

Nursing assessment

  • Assess cognitive function (memory, attention, reasoning, language, ability to perform simple tasks) periodically during therapy.
  • Lab Test Considerations: May cause anemia.

Potential Nursing Diagnoses

Disturbed thought process (Indications)
Risk for injury (Side Effects)
Impaired environmental interpretation syndrome

Implementation

  • Dose increases should occur no more frequently than weekly.
  • To switch from Namenda to Namenda XR, patients taking 10 mg twice daily of Namenda tablets may be switched to Namenda XR 28 mg once daily capsules the day following the last dose of a 10 mg Namenda tablet. Patients with renal impairment may use the same procedure to switch from Namenda 5 mg twice daily to Namenda XR 14 mg once daily.
  • Oral: May be administered without regard to food.
    • Administer oral solution using syringe provided. Do not dilute or mix with other fluids.
    • Swallow extended release capsules whole; do not crush, chew, or divide. Capsules may be opened, sprinkled on applesauce, and swallowed. Entire contents of each capsule should be consumed; do not divide dose.

Patient/Family Teaching

  • Instruct patient and caregiver on how and when to administer memantine and how to titrate dose. Take missed doses as soon as remembered but not just before next dose; do not double doses. Advise patient and caregiver to read Patient Instructions sheet.
  • Caution patient and caregiver that memantine may cause dizziness.
  • Advise patient and caregiver to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Teach patient and caregivers that improvement in cognitive functioning may take months; degenerative process is not reversed.

Evaluation/Desired Outcomes

  • Improvement in neurocognitive decline (memory, attention, reasoning, language, ability to perform simple tasks) in patients with Alzheimer's disease.

memantine

An NMDA (N-methyl D-aspartate) receptor antagonist that counters the toxic effects of glutamate excess to manage the symptoms of moderate to severe Alzheimer’s disease.
Adverse effects
Hallucinations, confusion, dizziness, headache, hypertonia, nausea, vomiting, constipation, hypertonia, cystitis, increased libido.
 
Proposed mechanism
Interferes with homocysteine binding at the NMDA receptor; homocysteine also mediates excitotoxicity, and disturbs glutamatergic neurotransmission.

Ebixa

A brand name for MEMANTINE.