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Acetylcholinesterase inhibitor



    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.

Additional recommended knowledge

Contents

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:

Comparison table

Comparison of reversible acetylcholinesterase inhibitors
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
  • reverse neuromuscular block (intravenously)
  • treat myasthenia gravis (orally)
visceral
physiostigmine medium postganglionic parasympathetic treat glaucoma (eye drops)
pyridostigmine medium neuromuscular junction
  • treat myasthenia gravis (orally)
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:

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

  • Pesticide poisoning
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Acetylcholinesterase_inhibitor". A list of authors is available in Wikipedia.
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