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.

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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:

• Organophosphates
  • metrifonate
• Carbamates
  • physostigmine
  • neostigmine
  • pyridostigmine
  • ambenonium
  • demarcarium
  • rivastigmine
• Phenanthrine derivatives
  • galantamine
• Piperidines
  • donepezil, also known as E2020
• Tacrine, also known as tetrahydroaminoacridine (THA')
• Edrophonium
• Phenothiazines

Comparison table

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
  • echothiophate
  • diisopropyl fluorophosphate
  • cyclosarin
  • sarin
  • soman
  • tabun
  • VX
  • VE
  • VG
  • VM
  • diazinon
  • malathion
  • parathion
• Carbamates
  • aldicarb
  • bendiocarb
  • bufencarb
  • carbaryl
  • carbendazim
  • carbetamide
  • carbofuran
  • chlorbufam
  • chloropropham
  • ethiofencarb
  • formetanate
  • methiocarb
  • methomyl
  • oxamyl
  • phenmedipham
  • pinmicarb
  • pirimicarb
  • propamocarb
  • propham
  • propoxur

Natural Compounds (Supplements)

• Huperzine A

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