Health Dictionary
Reliable, easy-to-read patient information on common medical conditions — written in plain language, free of jargon, and grounded in current evidence. Browse the most frequent diagnoses, understand what they mean for everyday life, and learn which steps and questions help you have a focused conversation with your doctor.
Cholinesterase inhibitors
Introduction
Overview
Overview
An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine.
Uses
Uses
Acetylcholinesterase inhibitors:
- occur naturally as venoms and poisons
- are used as weapons in the form of nerve agents
- are used medicinally:
- to treat myasthenia gravis. In myasthenia gravis, they are used to increase neuromuscular transmission.
- to treat Alzheimer’s disease
- as an antidote to anticholinergic poisoning
Examples
Examples
Reversible inhibitor
Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:
- Organophosphates
- Carbamates
- Phenanthrine derivatives
- Piperidines
- donepezil, also known as E2020
- Tacrine, also known as tetrahydroaminoacridine (THA’)
- Edrophonium
- Phenothiazines
Quasi-irreversible inhibitor
Compounds which function as quasi-irreversible inhibitors of cholinesterase are those most likely to have use as chemical weapons or pesticides. These include:
Natural Compounds (Supplements)
Effects
Effects
Some major effects of anticholinesterases:
- Actions on the autonomic nervous system, that is parasympathetic nervous system will cause bradycardia, hypotension, hypersecretion, bronchoconstriction, GIT hypermotility, and decrease intraocular pressure.
- SLUD syndrome.
- Actions on the neuromuscular junction will result in prolonged muscle contraction.
Related Chapters
Related Chapters
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]