Acetylcholinesterase inhibitor
- ↑ synaptic acetylcholine
- Cholinergic effects: nausea, diarrhea, bradycardia
- If BBB-crossing:
- Vivid dreams
- Modest cognitive benefit in dementia
- Reversible inhibition is therapeutic; irreversible inhibition causes cholinergic poisoning
Drugs with this mechanism (8)
- Donepezil — The most-prescribed cholinesterase inhibitor for Alzheimer dementia.
- Edrophonium — Ultra-short cholinesterase inhibitor once used to diagnose myasthenia.
- Galantamine — Cholinesterase inhibitor; also modulates nicotinic receptors.
- Neostigmine — Cholinesterase inhibitor to reverse neuromuscular blockade and treat myasthenia.
- Physostigmine — Tertiary cholinesterase inhibitor; the antidote for anticholinergic delirium.
- Pyridostigmine — Peripheral cholinesterase inhibitor; symptomatic mainstay for myasthenia gravis.
- Rivastigmine — Cholinesterase inhibitor available as a patch; also for Parkinson dementia.
- Sarin — A nerve-agent organophosphate; irreversibly inhibits cholinesterase.
Self-check
- What heart-rate adverse effect can acetylcholinesterase inhibition cause?
Bradycardia. - How do reversible and irreversible AChE inhibition differ clinically?
Reversible inhibition is therapeutic; irreversible inhibition causes cholinergic poisoning.
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