Rivastigmine
EXELON
Pronunciation: ri-va-STIG-meen
“Excel on River Stigmine”
baby blue theme → muscarinic
What it isAcetylcholinesterase and butyrylcholinesterase inhibitor; Alzheimer and Parkinson disease dementia.
Why this oneThe only cholinesterase inhibitor approved for Parkinson disease dementia. The patch causes less nausea than capsules (7 % at 9.5 mg/24 h vs 23 % at 6 mg twice daily), but significant GI effects and dehydration still occur.
What limits itNausea and vomiting limit oral titration. Bradycardia; the patch must be rotated and the old one removed.
Pearls
- Patch 9.5 mg/24 h matches oral 12 mg/day, less nausea.
- Oral: take with meals; titrate every 2 weeks (4 in PDD).
- Also helps behavior in Lewy body dementia.
- Symptomatic only; does not halt decline, not for MCI.
Rivastigmine prescription history
Animated chart of estimated U.S. prescriptions per year, Dementia meds (1993–2026). Rivastigmine enters in 2000 (estimated).
FDA-approved for
- Alzheimer dementia (2000)
- Parkinson dementia (2006)
Principal riskBradycardia; GI intolerance limits titration
Classes and tags
Clinical profile
Legacy pregnancy categoryB
Defining liabilityDose-related nausea, vomiting, diarrhea, anorexia and weight loss (dehydration); bradycardia and syncope; patch: allergic contact dermatitis, and overdose from wearing more than one patch.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Alzheimer's disease dementia | Adults | 1.5 mg BID | 3-6 mg BID (titrate through 3, 4.5, 6 mg BID) | 6 mg BID |
| Parkinson's disease dementia | Adults | 1.5 mg BID | 3-6 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
- Take with meals in divided doses (morning and evening)
- If dosing is interrupted for more than 3 days, restart at 1.5 mg BID and re-titrate
- Low body weight (<50 kg): titrate and monitor carefully; consider dose reduction
Available strengths
- cap 1.5, 3, 4.5, 6 mg
- patch 4.6, 9.5, 13.3 mg/24 hr
Contraindications
- History of application-site reaction with rivastigmine transdermal patch suggestive of allergic contact dermatitis, absent negative allergy testing
Cautions
- GI adverse reactions (nausea, vomiting, diarrhea, anorexia, weight loss); dehydration can be serious
- Disseminated allergic dermatitis - discontinue if it occurs
- May exacerbate/induce extrapyramidal symptoms; worsening Parkinson tremor
- Seizures
- Peptic ulcers/GI bleeding (increased gastric acid secretion)
- Exaggerates succinylcholine-type muscle relaxation during anesthesia
- Vagotonic effects on heart rate (bradycardia); caution in sick sinus syndrome/conduction conditions
- Urinary obstruction; caution in asthma/obstructive pulmonary disease
Adverse reactions
- Nausea
- Vomiting
- Anorexia
- Dyspepsia
- Asthenia
- Diarrhea
- Dizziness
- Tremor
- Weight loss
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).
Cost
Generic entry2007
Open Rivastigmine in the interactive console ↗
Memory aids: interaction avatars
Open Rivastigmine in the interactive console ↗
Self-check
- Rivastigmine: Which delivery form reduces oral GI effects?
The patch. - Rivastigmine: What must be removed before a new patch?
The old patch.