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, 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
- Alzheimer dementia (2000)
- Parkinson dementia (2006)
FDA label
Read the full label on DailyMed ↗
| 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
NO BOXED WARNINGS
Principal riskBradycardia; GI intolerance limits titration
Classes and tags
Clinical profile
Legacy pregnancy categoryB
Defining liabilityBradycardia, syncope or GI effects for symptomatic drugs; anti-amyloid agents add edema/hemorrhage risk.
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