Rivastigmine (Exelon)

Class

Acetylcholinesterase and butyrylcholinesterase inhibitor

Mechanism

Reversibly inhibits acetylcholinesterase and butyrylcholinesterase, increasing acetylcholine levels and enhancing cholinergic neurotransmission in the brain

FDA-Approved Use

Mild to moderate Alzheimer’s disease (AD), Parkinson’s disease dementia (PDD)

Off-Label Use

Vascular dementia, post-stroke apathy, apathy in Parkinson’s disease (PD)

Formulation

Oral capsules, oral solution, transdermal patch

Titration

Oral: start 1.5 mg p.o. twice daily, titrated gradually as tolerated. Patch: start 4.6 mg/24 hours daily, increase to 9.5 mg/24 hours after 4 weeks; maximum 13.3 mg/24 hours

Dose Range

Oral: 1.5–12 mg/day; Patch: 4.6–13.3 mg/24 hours

Kinetics

Half-life approximately 1.5 hours (oral), with longer duration via patch; metabolized by cholinesterases rather than CYP enzymes

Common AEs

Nausea, vomiting, diarrhea, dizziness, fatigue

Serious/Rare AEs

Rare cases of bradycardia, syncope, and gastrointestinal bleeding

Monitoring

Monitor for gastrointestinal symptoms, weight loss, and cardiac effects especially in elderly or frail patients

Black Box Warning

None

Considerations

May benefit cognitive and behavioral symptoms in vascular dementia and post-stroke cognitive impairment. Preferred in Parkinson’s disease dementia due to dual FDA approval and relatively better tolerability in patients with motor disorders.