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Acetylcholinesterase inhibitor
From Wikipedia, the free encyclopedia
(Redirected from Anticholinesterase)
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.
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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
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
Compounds which function as quasi-irreversible inhibitors of cholinesterase are those most likely to have use as chemical weapons or pesticides. These include:
Some major effects of anticholinesterases:
- Actions on the autonomic nervous system, that is parasympathetic nervous system will cause bradycardia, hypotension, hypersecretion, bronchoconstriction, GI tract hypermotility, and decrease intraocular pressure.
- SLUD syndrome.
- Actions on the neuromuscular junction will result in prolonged muscle contraction.
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| Class | Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition |
| Substrate | Acetylcholinesterase inhibitors - Aromatase inhibitors - Carbonic anhydrase inhibitors - Integrase inhibitor - Kinase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors - Reverse transcriptase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors (ACE inhibitor, Trypsin inhibitor) |
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| Carbamates | Ambenonium - Demecarium - Stigmine (Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine) |
| Other | Galantamine - Metrifonate - Donepezil - Tacrine - Edrophonium |
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| Anticholinesterases | Tacrine - Donepezil - Rivastigmine - Galantamine |
| Other | NMDA receptor antagonist (Memantine) - Ginkgo biloba |
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| Anticholinesterases | Stigmine (Neostigmine, Pyridostigmine, Distigmine) - Ambenonium |
| Choline esters | Carbachol - Bethanechol |
| Other parasympathomimetics | Pilocarpine - Choline alfoscerate |