Pharm

Rivastigmine

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Rivastigmine, Exelon

  • Mechanism
  1. See Acetylcholinesterase Inhibitor
  2. Carbamate-based noncompetitive Cholinesterase Inhibitor
  3. Inhibits butyrylcholinesterase and Acetylcholinesterase
  4. Increases Cholinergic transmission
  • Dosing
  1. Oral Route
    1. Initial: 1.5 mg orally twice daily with food for at least 2 weeks (4 weeks for Lewy Body Dementia)
    2. Next: 3 mg orally twice daily with food for at least 2 weeks (4 weeks for Lewy Body Dementia)
    3. Next: 4.5 mg orally twice daily with food for at least 2 weeks (4 weeks for Lewy Body Dementia)
    4. Next: 6 mg orally twice daily with food
  2. Transdermal Patch
    1. Initial: 4.6 mg patch every 24 hours for at least 4 weeks
    2. Next: 9.5 mg patch every 24 hours for at least 4 weeks
    3. Next: 13.3 mg patch every 24 hours
    4. Change patch application locations to prevent skin irritation
  • Adverse Effects
  1. See Acetylcholinesterase Inhibitor
  2. Specific adverse effects reported for Rivastigmine, not seen with other Acetylcholinesterase Inhibitors
    1. Abdominal Pain
    2. Atrial Fibrillation
    3. Myocardial Infarction
    4. Contact Dermatitis (allergic or irritant)
  3. Cardiovascular
    1. Syncope
    2. Atrioventricular Block
    3. Bradycardia
  4. Gastrointestinal
    1. Diarrhea
    2. Nausea or Vomiting
    3. Decreased appetite and Weight loss
  5. Neuropsychiatric
    1. Headache
    2. Myalgias
    3. Tremors
    4. Insomnia
    5. Dizziness and Fall Risk
    6. Vivid dreams
  • Pharmacokinetics
  • Oral Route
  1. Peak: 1 hour
  2. Duration: 10 hours
  • Drug Interactions
  1. No significant Drug Interactions
  • Efficacy
  1. Modestly improves scores on Neuropsychological Tests
  2. Benefits decrease after 40 weeks of treatment