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Cholinesterase inhibitors

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Acetylcholine-skeletal

Acetylcholine

Acetylcholinesterase-1EA5

Acetylcholinesterase

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:

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 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:

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

References

  1. 1.0 1.1 1.2 1.3 Unless else specified n boxes, then ref is:Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 156

External links





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