Section 05 · Monograph

Rivastigmine

Reviewed Nov 2026FDA label

Exelon patch / capsAChE/BuChE inhibitor

Indications

Mild, moderate, and severe dementia of the Alzheimer's type (oral capsule/solution and transdermal patch)FDA-labeled
Mild-to-moderate dementia associated with Parkinson's disease (oral capsule/solution and transdermal patch)FDA-labeled

Carbamate-class 'pseudo-irreversible' inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)
Forms a covalent carbamylated complex with the enzyme that dissociates slowly, producing inhibition that outlasts plasma drug levels
Relatively selective for the G1 (monomeric) form of AChE enriched in Alzheimer's-affected brain regions
Dual AChE/BuChE inhibition postulated to provide additional benefit as BuChE activity increases with disease progression

Oral capsules/solution: initiate 1.5 mg twice daily with food
Titrate oral dose upward by 1.5 mg BID increments at intervals of ≥2 weeks, to a target maintenance range of 3-6 mg BID (max 6 mg BID)
Transdermal patch: initiate 4.6 mg/24h once daily to intact skin on upper back, chest, or upper arm, rotating sites
After ≥4 weeks on 4.6 mg/24h, increase to usual effective dose of 9.5 mg/24h if tolerated
For Alzheimer's disease only, after ≥4 additional weeks at 9.5 mg/24h, may increase to 13.3 mg/24h
Only one patch should be worn at a time
If therapy is interrupted for more than several days, restart at the lowest dose and re-titrate

Known hypersensitivity to rivastigmine, other carbamate derivatives, or formulation excipients
Prior allergic contact dermatitis from the rivastigmine transdermal patch

Other cholinesterase inhibitors or cholinergic agonists: additive cholinergic toxicity
Anticholinergic drugs may antagonize therapeutic effect
Succinylcholine and similar agents: risk of exaggerated muscle relaxation during anesthesia
Metoclopramide: concurrent use not recommended due to additive extrapyramidal effects
Beta-blockers and other bradycardia-inducing drugs: additive risk of bradycardia and syncope
NSAIDs: increased risk of GI bleeding

Nausea, vomiting, and diarrhea (more frequent with oral formulation than patch)
Application-site skin reactions with the patch: erythema, pruritus, contact dermatitis
Anorexia and weight loss
Dizziness and headache
Asthenia/fatigue
Bradycardia and syncope
Agitation and confusion

Weight and nutritional/hydration status, especially during oral titration
GI tolerability with each dose increase
Application site for irritation; rotate patch sites
Heart rate and symptoms of syncope, particularly with sick sinus syndrome or conduction defects
Adherence to correct patch strength and single-patch use to avoid overdose
Hepatic and renal function status when initiating in impaired patients

No adequate, well-controlled studies in pregnant women
Animal reproduction studies did not demonstrate teratogenicity but showed maternal/fetal toxicity at high, maternally toxic doses
Use during pregnancy only if potential benefit justifies potential fetal risk
Unknown whether excreted in human milk; not recommended during breastfeeding given lack of safety data