Acetylcholinesterase inhibitor

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Overview

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:

• 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

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, GIT hypermotility, and decrease intraocular pressure.
• SLUD syndrome.
• Actions on the neuromuscular junction will result in prolonged muscle contraction.

See also

• Pesticide poisoning

External links

• MeSH Acetylcholinesterase+inhibitors

v • d • e 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)

v • d • e Anticholinesterases (N06DA, N07AA)
Carbamates	Ambenonium - Demecarium - Stigmine (Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine)
Other	Galantamine - Metrifonate - Donepezil - Tacrine - Edrophonium

v • d • e Psychoanaleptics: anti-dementia drugs (N06D)
Anticholinesterases	Tacrine - Donepezil - Rivastigmine - Galantamine
Other	NMDA receptor antagonist (Memantine) - Ginkgo biloba

v • d • e Parasympathomimetics (N07A)
Anticholinesterases	Stigmine (Neostigmine, Pyridostigmine, Distigmine) - Ambenonium
Choline esters	Carbachol - Bethanechol
Other parasympathomimetics	Pilocarpine - Choline alfoscerate

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .