Changes: Acetylcholinesterase inhibitors

Revision as of 10:16, 10 April 2007

Biological: Behavioural genetics · Evolutionary psychology · Neuroanatomy · Neurochemistry · Neuroendocrinology · Neuroscience · Psychoneuroimmunology · Physiological Psychology · Psychopharmacology (Index, Outline)

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

Anticholinesterases occur naturally as venoms and poisons, are used as weapons in the form of nerve agents, and are used medicinally to treat diseases such as myasthenia gravis and Alzheimer's disease, and as an antidote to anticholinergic poisoning. In myasthenia gravis, they are used to increase neuromuscular transmission.

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

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

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.

External links

MeSH Acetylcholinesterase+inhibitors

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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)