Rivastigmine
A carbamate cholinesterase inhibitor, given as capsules or a skin patch, for Alzheimer's and Parkinson's disease dementia.
Drug card
- How it works
- Blocking acetylcholinesterase so more acetylcholine stays in the brain
- Used for
- Mild to moderate Alzheimer's dementia
- Mild to moderate dementia in Parkinson's disease
- Known for
- Nausea and vomiting
- Slow heart rate and heart block
- Its name
- -stigmine means a cholinesterase inhibitor
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does rivastigmine work?
A carbamate that inhibits both acetylcholinesterase and butyrylcholinesterase: it binds them covalently and inactivates them for hours, so acetylcholine released by surviving neurons lasts longer. The cholinesterases themselves break it down, so CYP enzymes play little part in its clearance.
Like other cholinesterase inhibitors for dementia: These drugs enter the brain and inhibit acetylcholinesterase, the enzyme that breaks down acetylcholine, so more acetylcholine stays at the synapses of the cholinergic neurons that still work in Alzheimer's or Parkinson's dementia. Memory and thinking improve for a time, but the disease is not slowed and the benefit fades as neurons are lost. Extra acetylcholine in the gut and heart causes the main side effects.
Uses
What is rivastigmine used for?
- Mild to moderate Alzheimer's dementia
- Mild to moderate dementia in Parkinson's disease
Side effects
Side effects of rivastigmine
- Nausea and vomitingKnown for
- Slow heart rate and heart blockKnown forSerious
- Diarrhea
- Loss of appetite and weight loss
- Severe vomiting with dehydrationSerious
- Dizziness and headache
- Worse tremor and parkinsonism
- QT prolongationSerious
- Stomach ulcers and bleedingSerious
- SeizuresSerious
- Allergic skin reactions, mostly from the patch
- Falls in Parkinson's disease dementia
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- After a break of more than 3 days it is restarted at the lowest dose, as full doses can cause severe vomiting.
- With beta blockers the added slowing of the heart can cause fainting, so the pair is not recommended.
- Metoclopramide adds to its extrapyramidal effects and is not recommended with it.
- Allergic contact dermatitis from the patch can rule out every form of rivastigmine later.
Good to know: Unlike donepezil it also blocks butyrylcholinesterase, is broken down by cholinesterases rather than the liver's CYP enzymes, and comes as a skin patch.
Remember it
A way to remember it
More acetylcholine: a slower heart and a busier gut.
Outside the brain the extra acetylcholine slows the heart (bradycardia, heart block, fainting) and stirs the gut (nausea, vomiting, diarrhea), the two side effects these drugs are known for.
Written for biofideX
Its name
-stigmine means cholinesterase inhibitor
Neostigmine reverses non-depolarizing muscle relaxants and rivastigmine treats dementia. Donepezil, a cholinesterase inhibitor used for dementia, doesn't carry the stem.
- Every drug name stem
Its class
Cholinesterase inhibitors for dementia
Other cholinesterase inhibitors for dementia with a card:
Easily mixed up with anticholinesterases, NMDA receptor antagonists and antimuscarinics.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Rivastigmine tartrate capsules: label (DailyMed)
- Rivastigmine: product information (EMA)
- Rivastigmine tartrate (NCI Thesaurus)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Parkinson's, dementia and migraine
Rivastigmine is one of 9 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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