Rivastigmine

Brand Names: Exelon

Drug Class: Cholinesterase inhibitor

Overview

Rivastigmine is a cholinesterase inhibitor used for the treatment of mild to moderate dementia of the Alzheimer's type and mild to moderate dementia associated with Parkinson's disease. It works by increasing acetylcholine levels in the brain to improve cognitive function.

Mechanism of Action

Rivastigmine is a reversible cholinesterase inhibitor that increases acetylcholine concentration in the cerebral cortex by slowing the degradation of acetylcholine released by intact cholinergic neurons. It inhibits both acetylcholinesterase and butyrylcholinesterase in the brain.

Indications

  • Treatment of mild to moderate dementia of the Alzheimer's type
  • Treatment of mild to moderate dementia associated with Parkinson's disease

Common Doses

  • 1.5 mg
  • 3 mg
  • 4.5 mg
  • 6 mg

Dosage

Initial dose: 1.5 mg twice daily with food. May increase to 3 mg twice daily after at least 2 weeks, then to 4.5 mg and 6 mg twice daily at minimum 2-week intervals. Maximum recommended dose: 6 mg twice daily.

Contraindications

  • Known hypersensitivity to rivastigmine, other carbamate derivatives, or other components of the formulation
  • Previous history of application site reaction with rivastigmine transdermal patch suggestive of allergic contact dermatitis without negative allergy testing

Side Effects

  • Nausea
  • Vomiting
  • Diarrhea
  • Anorexia
  • Weight loss
  • Dizziness
  • Headache
  • Abdominal pain
  • Fatigue
  • Insomnia
  • Tremor
  • Confusion
  • Hallucinations
  • Bradycardia
  • Syncope

Interactions

  • Anticholinergic medications may reduce efficacy
  • Cholinergic agonists may have additive effects
  • Beta-blockers may increase risk of bradycardia
  • Succinylcholine-type muscle relaxants may have prolonged effects

Counseling Points

  • Take with food to minimize gastrointestinal side effects
  • Do not stop abruptly without consulting healthcare provider
  • Report severe nausea, vomiting, or weight loss
  • Transdermal patch should be applied to clean, dry, hairless skin and rotated daily
  • Avoid alcohol consumption
  • Monitor for signs of gastrointestinal bleeding