Pharm

Galantamine

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Galantamine, Reminyl, Razadyne, Benzgalantamine, Zunveyl

  • Indications
  • Contraindications
  1. Severe hepatic dysfunction (Child-Pugh >9)
  2. GFR <9 ml/min
  • Mechanism
  1. Competitive and Reversible Acetylcholinesterase Inhibitor
  2. Acts also at Nicotinic Receptors
  3. Derived from Daffodil bulbs
  • Pharmacokinetics
  1. Half-Life: 7 hours in elderly patients
  2. Metabolized by liver enzymes: CYP2D6 and CYP3A4
  • Medications
  1. Galantamine
    1. Tabs: 4, 8, 12 mg
    2. XR caps: 8, 16, 24 mg
    3. Oral Solution: 4 mg/ml
  2. Benzgalantamine (Zunveyl)
    1. Delayed Release Tablets: 5 mg, 10 mg, 15 mg
    2. New Galantamine prodrug due for release in 2025
    3. Twice daily delayed release agent with fewer gastrointestinal adverse effects, but at $800/month
      1. Contrast with extended release Galantamine ($30/month)
    4. Most of efficacy and safety data is extrapolated from Galantamine data
    5. (2025) Presc Lett 32(7): 41
  • Dosing
  • Galantamine
  1. May require concurrent Antiemetic use
  2. Immediate Release
    1. Start: 4 mg orally twice daily with breakfast and dinner for 4 weeks
    2. Maintenance: 8 mg orally twice daily for at least 4 weeks
    3. Consider increase to 12 mg orally twice daily if indicated
  3. Extended Release
    1. Start: 8 mg orally daily for 4 weeks
    2. Maintenance: 16 mg orally daily for at least 4 weeks
    3. Consider increase to 24 mg orally daily if indicated
  4. Renal Dosing
    1. GFR 9 to 59 ml/min: Maximum dose 16 mg/day
    2. GFR <9 ml/min: Avoid Galantamine
  • Dosing
  • Benzgalantamine (Zunveyl)
  1. Start: 5 mg orally twice daily swallowed whole without crushing, chewing or splitting
  2. May be taken with or without food
  3. Increase as needed to 10 mg orally twice daily after 4 weeks
  4. Maximum dose
    1. Normal renal and hepatic function: 15 mg orally twice daily
    2. Moderate liver disease (Child-Pugh 7-9) or GFR 10-60 ml/min: 10 mg orally twice daily
    3. GFR <9 ml/min: Avoid Benzgalantamine
  • Adverse Effects
  1. See Acetylcholinesterase Inhibitor
  2. Cardiovascular
    1. Syncope
    2. Atrioventricular Block
    3. Bradycardia
  3. Gastrointestinal
    1. Diarrhea
    2. Nausea (21%) or Vomiting (11%)
    3. Decreased appetite and Weight loss
    4. Increased gastric acid secretion (may increase risk of Peptic Ulcer Disease)
  4. Genitourinary
    1. Urinary Outflow Obstruction
  5. Neuropsychiatric
    1. Headache (7%)
    2. Myalgias
    3. Dizziness (8%) and Fall Risk
    4. Vivid dreams
  6. Serious skin reactions (<1% of patients)
    1. Stevens Johnson Syndrome
    2. Acute Generalized Exanthematous Pustulosis
  • Safety
  1. Monitor renal and hepatic function at baseline and with clinical change
  • Efficacy
  1. Moderately preserved cognitive function for >6 months
  2. References
    1. Raskind (2000) Neurology 54:2261 [PubMed]
    2. Tariot (2000) Neurology 54:2269 [PubMed]