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16-September-2008 16:15:14 - Acetylcholinesterase inhibitor Acetylcholine Acetylcholine Acetylcholinesterase 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. Contents 1 Uses 2 Examples 2.1 Reversible inhibitor 2.1.1 Comparison table 2.2 Quasi-irreversible inhibitor 2.3 Natural Compounds Supplements 3 Effects 4 See also 5 References 6 External links 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 To treat Lewy Body Dementia 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 irreversible Carbamates Physostigmine Neostigmine Pyridostigmine Ambenonium Demarcarium Rivastigmine Phenanthrene derivatives Galantamine Piperidines Donepezil, also known as E2020 Tacrine, also known as tetrahydroaminoacridine THA' Edrophonium Comparison table Comparison of reversible acetylcholinesterase inhibitors Inhibitor Duration1 Main site of action1 Clinical use1 Adverse effects1 Edrophonium short 10 min. neuromuscular junction diagnosis of myasthenia gravis Neostigmine medium 1-2 hrs. neuromuscular junction Reverse neuromuscular block intravenously Treat myasthenia gravis orally visceral Physiostigmine medium 0.5-5 hrs. postganglionic parasympathetic treat glaucoma eye drops Pyridostigmine medium 2-3 hrs. 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 irreversible 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: Organophosphates Echothiophate Diisopropyl fluorophosphate Cyclosarin Dimethoate 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 Galantamine Effects Some major effects of anticholinesterase inhibitors: 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 References ^ a b c d Unless else specified n boxes, then ref is:Rang, H. P. 2003. Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 156 External links ATSDR Case Studies in Environmental Medicine: Cholinesterase Inhibitors, Including Pesticides and Chemical Warfare Nerve Agents U.S. Department of Health and Human Services MeSH Acetylcholinesterase+inhibitors v d e Pharmacology: enzyme inhibition Class Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition Substrate Oxidoreductase EC 1: Aromatase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors Transferase EC 2: Integrase inhibitor - Protein kinase inhibitors - Reverse transcriptase inhibitors - COMT inhibitors Hydrolase EC 3: Acetylcholinesterase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors ACE inhibitor, Trypsin inhibitor - Histone deacetylase inhibitor Lyase EC 4: Carbonic anhydrase inhibitors v d e Psychoanaleptics: anti-dementia drugs N06D Anticholinesterases Tacrine - Donepezil - Rivastigmine - Galantamine Other NMDA receptor antagonist Memantine - Ginkgo biloba v d e Parasympathomimetics / cholinergic agonists / acetylcholinesterase inhibitors N06DA, N07AA Direct at receptor muscarinic: Muscarine - Oxotremorine - M1 Xanomeline - M3 Bethanechol, Pilocarpine, Arecoline, Cevimeline, Aceclidine nicotinic: Nicotine - Lobeline - Varenicline - Epibatidine M N: Acetylcholine/Choline alfoscerate - Methacholine - Carbachol Indirect/AIs in synapse Reversible carbamates: Ambenonium - Stigmine Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine, Distigmine Edrophonium anti-dementia Galantamine, Donepezil, Tacrine Irreversible/ organophosphate ophthalmological Echothiophate, Isoflurophate antiparasitic Malathion, Metrifonate chemical warfare see Nerve agent v d e Receptor agonists, antagonists, and reuptake inhibitors BA/M 5-HT serotonin receptor Serotonin receptor agonist 5-HT4 Serotonin antagonist 5-HT3 Serotonin uptake inhibitor SSRI Dopamine receptor Dopamine agonist Dopamine antagonist Dopamine reuptake inhibitor Adrenergic receptor Adrenergic agonist Alpha, Beta 1/2 Adrenergic antagonist Alpha 1/2, Beta Adrenergic uptake inhibitor Histamine receptor Histamine agonist Histamine antagonist H1, H2, H3 AA GABA receptor GABA agonist GABA antagonist Glutamate receptor NMDA receptor NMDA receptor antagonist AMPA receptor Ampakine Excitatory amino acid agonist Excitatory amino acid antagonist ANS Acetylcholine receptor Cholinergic Muscarinic, Nicotinic Anticholinergic Muscarinic, Nicotinic/Ganglionic blocker/Neuromuscular-blocking drugs Acetylcholinesterase inhibitor Adrenergic receptor SANS only -- see above for details PANS Parasympathomimetic Cholinergic, Acetylcholinesterase inhibitor - Parasympatholytic Anticholinergic, Ganglionic blocker SANS Sympathomimetic Adrenergic agonist, Monoamine oxidase inhibitor - Sympatholytic Adrenergic antagonist, Alpha blocker, Ganglionic blocker Retrieved from http://en..org/wiki/Acetylcholinesterase_inhibitor Categories: Anticholinesterases Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Català Español Italiano This page was last modified on 4 August 2008, at 23:11
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