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Rivastigmine

EXELON

What it isAcetylcholinesterase and butyrylcholinesterase inhibitor; Alzheimer and Parkinson disease dementia.

Why this oneThe only cholinesterase inhibitor approved for Parkinson disease dementia, and the patch avoids the GI effects that limit the oral form.

What limits itNausea and vomiting limit oral titration. Bradycardia; the patch must be rotated and the old one removed.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Alzheimer's disease dementiaAdults1.5 mg BID3-6 mg BID (titrate through 3, 4.5, 6 mg BID)6 mg BID
Parkinson's disease dementiaAdults1.5 mg BID3-6 mg BID (titrate through 3, 4.5, 6 mg BID)6 mg BID

Titration Alzheimer's: increase at intervals of at least 2 weeks; Parkinson's disease dementia: increase at intervals of at least 4 weeks

Renal Moderate to severe impairment: may tolerate only lower doses

Hepatic Mild or moderate impairment: may tolerate only lower doses; no data in severe impairment

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No adequate human data; no adverse embryo-fetal effects in animals at 2-4x MRHD.

Lactation No human data; excreted in rat milk (~2x maternal plasma).

NO BOXED WARNINGS

Principal riskBradycardia; GI intolerance limits titration

Cost, est. cash$10–$500/month

Generic entry2007

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades2 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryB

Defining liabilityBradycardia, syncope or GI effects for symptomatic drugs; anti-amyloid agents add edema/hemorrhage risk.

Mechanism of action: Rivastigmine ballicule

Rivastigmine ballicule: receptor binding, kinetics and half-life diagram

Open Rivastigmine in the interactive console ↗

Memory aids: mascots and interaction avatars

Rivastigmine EXELON mascot mnemonic cartoon
“Excel on River Stigmine”
baby blue theme → muscarinic
Rivastigmine butyrylcholinesterase inhibitor avatar
butyrylcholinesterase inhibitor

Open Rivastigmine in the interactive console ↗