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Biological: Behavioural genetics · Evolutionary psychology · Neuroanatomy · Neurochemistry · Neuroendocrinology · Neuroscience · Psychoneuroimmunology · Physiological Psychology · Psychopharmacology (Index, Outline)
- See also: Anticholinergic
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[]
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[]
reversible inhibitor[]
Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:
- Carbamates
- physostigmine
- neostigmine
- pyridostigmine
- ambenonium
- demarcarium
- rivastigmine
- Phenanthrine derivatives
- Piperidines
- donepezil, also known as E2020
- Organophosphates
- metrifonate
- Tacrine, also known as tetrahydroaminoacridine (THA')
- Edrophonium
- Phenothiazines
These need classifying[]
Comparison table[]
Inhibitor | Duration[1] | Main site of action[1] | Clinical use[1] | Adverse effects[1] |
---|---|---|---|---|
edrophonium | short | neuromuscular junction | diagnosis of myasthenia gravis | |
neostigmine | medium | neuromuscular junction |
|
visceral |
physiostigmine | medium | postganglionic parasympathetic | treat glaucoma (eye drops) | |
pyridostigmine | medium | neuromuscular junction |
|
|
dyflos | long | postganglionic parasympathetic | historically to treat glaucoma (eye drops) | toxic |
ecothiopate | long | postganglionic parasympathetic | treat glaucoma (eye drops) | systemic effects |
parathion | long | none | toxic |
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:
- Organophosphates
- Carbamates
- aldicarb
- bendiocarb
- bufencarb
- carbaryl
- carbendazim
- carbetamide
- carbofuran
- chlorbufam
- chloropropham
- ethiofencarb
- formetanate
- methiocarb
- methomyl
- oxamyl
- phenmedipham
- pinmicarb
- pirimicarb
- propamocarb
- propham
- propoxur
Natural Compounds (Supplements)[]
Effects[]
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.
See also[]
- Antiemetic drugs
- Antispasmodic drugs
- Cholinergic nerves
- Cholinomimetic drugs
- Deliriants
- Hallucinogenic drugs
- Pesticide poisoning
- Phenothiazine derivatives
References[]
External links[]
Pharmacology: enzyme inhibition | |
---|---|
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) |
Anticholinesterases (N06DA, N07AA) | |
---|---|
Carbamates |
Ambenonium - Demecarium - Stigmine (Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine) |
Other |
Galantamine - Metrifonate - Donepezil - Tacrine - Edrophonium |
Psychoanaleptics: anti-dementia drugs (N06D) | |
---|---|
Anticholinesterases |
Tacrine - Donepezil - Rivastigmine - Galantamine |
Other |
NMDA receptor antagonist (Memantine) - Ginkgo biloba |
Parasympathomimetics (N07A) | |
---|---|
Anticholinesterases |
Stigmine (Neostigmine, Pyridostigmine, Distigmine) - Ambenonium |
Choline esters | |
Other parasympathomimetics |
Pilocarpine - Choline alfoscerate |
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