Pharmacology · Cholinesterase inhibitors
Rivastigmine !
A cholinesterase inhibitor for Alzheimer dementia and the dementia of Parkinson disease, given as capsules or a skin patch.
Updated 2026-11-01
The figure shows Torpedo (electric ray) acetylcholinesterase after reaction with rivastigmine: its carbamoyl group stays bonded to the catalytic serine and its leaving phenol (NAP) remains in the gorge.
Mechanism of action
Rivastigmine is a carbamate that enters the brain and carbamylates both acetylcholinesterase and butyrylcholinesterase. The enzyme stays blocked for hours although the drug itself leaves the blood within about an hour (a «pseudo-irreversible» inhibitor). More acetylcholine at cortical synapses eases cognitive symptoms.
- Enters the brain
- Carbamylates acetylcholinesterase and butyrylcholinesterase
- Enzymes stay blocked for hours
- Acetylcholine lasts longer; cognition improves modestly
Pharmacokinetics
- Absorption
- Capsules by mouth or a daily transdermal patch, which gives steadier levels
- Metabolism
- Hydrolysed by cholinesterases themselves, hardly by CYP enzymes, so few drug interactions
- Elimination
- Metabolites in the urine
- Half-life
- About 1 hour in plasma after capsules, but enzyme inhibition lasts about 8 to 10 hours
Indications
- Mild to moderate dementia of the Alzheimer type Alzheimer disease →
- Mild to moderate dementia associated with Parkinson disease Parkinson disease →
Adverse effects
Common
- Nausea, vomiting, diarrhoea and loss of appetite, dose-related
- Weight loss
- Dizziness and headache
- Skin redness and itching at the patch site
Contraindications
- Hypersensitivity to rivastigmine or other carbamates
- Previous patch-site reaction suggesting allergic contact dermatitis, unless allergy tests are negative
Key interactions
- Metoclopramide
- Added extrapyramidal effects; combination not recommended
- Beta blockers, especially atenolol
- Additive bradycardia and fainting
- Anticholinergic drugs such as oxybutynin or tolterodine
- Opposite actions; each weakens the other
What is monitored
- Weight, appetite and hydration
- Heart rate and falls
- Skin at patch sites
- Tremor and movement in Parkinson disease
Administration and safety
- Doses are started low and raised slowly to limit vomiting; after more than three missed days the prescriber is contacted to restart at a low dose
- Only one patch at a time; the old one is removed before a new one is applied
- Patch site changed every day to reduce skin irritation
- Capsules are taken with meals
Nursing care
- Check for an old patch before applying a new one; double patches have caused overdoses
- Watch fluid intake and weight in frail older adults
- Inspect patch sites and report spreading rash
- Teach caregivers to report fainting, black stools or worsening tremor
Pregnancy and breastfeeding
No adequate data in pregnancy; it is used mainly in older adults.
Test yourself
Think of the answer, then tap the question to see it.
Which two enzymes does rivastigmine inhibit?
Acetylcholinesterase and butyrylcholinesterase.
Besides Alzheimer disease, which dementia is an approved use?
Mild to moderate dementia associated with Parkinson disease.
Why does rivastigmine have few CYP-based drug interactions?
It is broken down mainly by cholinesterase hydrolysis, not by liver CYP enzymes.
What is a key safety check before applying a rivastigmine patch?
Make sure the previous patch has been removed, to avoid a double dose.
Related drugs
Related conditions
← Back to the class: Cholinesterase inhibitors
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - RIVASTIGMINE TARTRATE capsule (DailyMed (U.S. National Library of Medicine), 2026); DailyMed - RIVASTIGMINE patch, extended release (DailyMed (U.S. National Library of Medicine), 2026); Rivastigmine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 21 (McGraw Hill, 2023).
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Representative model, for educational purposes only.