Cholinesterase inhibitors (ChEIs), also known as anti-cholinesterase, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or butyrylcholine. This increases the amount of the acetylcholine or butyrylcholine in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others. This group of inhibitors is divided into two subgroups, acetylcholinesterase inhibitors (AChEIs) and butyrylcholinesterase inhibitors (BChEIs).[1][2][3]
ChEIs may be used as drugs for Alzheimer's and myasthenia gravis, and also as chemical weapons and insecticides.[4][5] Side effects when used as drugs may include loss of appetite, nausea, vomiting, loose stools, vivid dreams at night, dehydration, rash, bradycardia, peptic ulcer disease, seizures, weight loss, rhinorrhea, salivation, muscle cramps, and fasciculations.[6][7]
ChEIs are indirect-acting parasympathomimetic drugs.[8]
ChEls are widely used as chemical weapons. Since November 2019 the group of ACheIs known as Novichoks have been banned as agents of warfare under the Chemical Weapons Convention.[9] Novichok agents are neurotoxic organophosphorus compounds and are considered more potent than VX gas, also a neurotoxic organophosphorus compound.[10]
^English, Brett A.; Webster, Andrew A. (2012). "Acetylcholinesterase and its Inhibitors". Primer on the Autonomic Nervous System. Elsevier. pp. 631–633. doi:10.1016/b978-0-12-386525-0.00132-3. ISBN 978-0-12-386525-0.
^Deutch, Ariel Y.; Roth, Robert H. (2014). "Pharmacology and Biochemistry of Synaptic Transmission". From Molecules to Networks. Elsevier. pp. 207–237. doi:10.1016/b978-0-12-397179-1.00007-5. ISBN 978-0-12-397179-1.
^Colovic, Mirjana B.; Krstic, Danijela Z.; Lazarevic-Pasti, Tamara D.; Bondzic, Aleksandra M.; Vasic, Vesna M. (2013-04-01). "Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current Neuropharmacology. 11 (3). Bentham Science Publishers Ltd.: 315–335. doi:10.2174/1570159x11311030006. ISSN 1570-159X. PMC 3648782. PMID 24179466.
^"Cholinesterase Inhibitors (Medical Use & WMD)". PharmWiki. Tulane University School of Medicine. Retrieved 24 August 2020.
^Mandour, Raafat (2013). "Environmental Risks of Insecticides Cholinesterase Inhibitors". Toxicology International. 20 (1). United States National Library of Medicine: 30–34. doi:10.4103/0971-6580.111556. PMC 3702124. PMID 23833435.
^Budson, Andrew E.; Solomon, Paul R. (2016). "Cholinesterase Inhibitors". Memory Loss, Alzheimer's Disease, and Dementia. Elsevier. pp. 160–173. doi:10.1016/b978-0-323-28661-9.00016-0. ISBN 978-0-323-28661-9.
^Khoury, Rita; Rajamanickam, Jayashree; Grossberg, George T. (2018-01-08). "An update on the safety of current therapies for Alzheimer's disease: focus on rivastigmine". Therapeutic Advances in Drug Safety. 9 (3). SAGE Publications: 171–178. doi:10.1177/2042098617750555. ISSN 2042-0986. PMC 5810854. PMID 29492246.
^Forrester, John V.; Dick, Andrew D.; McMenamin, Paul G.; Roberts, Fiona; Pearlman, Eric (2016). "General and ocular pharmacology". The Eye. Elsevier. pp. 338–369.e1. doi:10.1016/b978-0-7020-5554-6.00006-x. ISBN 978-0-7020-5554-6. Parasympathomimetics are a group of drugs that act either by directly stimulating the muscarinic receptor, for example pilocarpine, or by inhibiting the enzyme acetylcholinesterase, which hydrolyses the acetylcholine in the synapse.
Cholinesteraseinhibitors (ChEIs), also known as anti-cholinesterase, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or...
with acetylcholin esterase inhibitors and electrical stimulation, the muscle develops trigger points. A cholinesteraseinhibitor (or "anticholinesterase")...
Acetylcholinesterase inhibitors (AChEIs) also often called cholinesteraseinhibitors, inhibit the enzyme acetylcholinesterase from breaking down the neurotransmitter...
toxins and venoms produced by plants and animals also contain cholinesteraseinhibitors. In clinical use, they are administered in low doses[why?] to...
Rivastigmine (sold under the trade name Exelon among others) is a cholinesteraseinhibitor used for the treatment of mild to moderate Alzheimer's disease...
crisis may be masked by the concomitant use of atropine along with cholinesteraseinhibitor medication in order to prevent side effects. Flaccid paralysis...
organophosphates, dimethoate is an acetylcholinesterase inhibitor which disables cholinesterase, an enzyme essential for central nervous system function...
acetylcholinesterase inhibitor and indirect cholinergic agonist (parasympathomimetic). It was the first centrally acting cholinesteraseinhibitor approved for...
Mytelase) is a cholinesteraseinhibitor used in the management of myasthenia gravis. It is classified as a reversible cholinesteraseinhibitor. Ambenonium...
discharged from the hospital on 22 September 2020. The OPCW said that a cholinesteraseinhibitor from the Novichok group was found in Navalny's blood, urine, skin...
muscarinic receptors (thus mimicking acetylcholine), or indirectly by inhibitingcholinesterase, promoting acetylcholine release, or other mechanisms. Common...
amphetamines, which enhance dopamine release directly by binding to and inhibiting VMAT2. The following are examples of dopaminergic substances: Dopamine...
causative agents have been excreted. Reversible acetylcholinesterase inhibitor agents such as physostigmine can be used as an antidote in life-threatening...
doi:10.1002/ps.4502. PMID 27976502. Gage, J. C. (1 June 1953). "A cholinesteraseinhibitor derived from OO -diethyl O - p -nitrophenyl thiophosphate in vivo"...
to suppress sebum production. H1-antihistamines refer to compounds that inhibit the activity of the H1 receptor. Since the H1 receptor exhibits constitutive...
announcement, confirming that Navalny had been poisoned with a cholinesteraseinhibitor. Ivan Zhdanov, chief of Navalny's Anti-Corruption Foundation, said...
acetylhydrolase), also known as AChE, AChase or acetylhydrolase, is the primary cholinesterase in the body. It is an enzyme that catalyzes the breakdown of acetylcholine...
Paraoxon is a parasympathomimetic which acts as an cholinesteraseinhibitor. It is an organophosphate oxon, and the active metabolite of the insecticide...
Dimethylcarbamoyl fluoride is highly toxic because it's a potent cholinesteraseinhibitor and is lethal even at low doses. Dimethylcarbamoyl chloride Cuomo...
chemist. He was known for the synthesis of the first organophosphate cholinesteraseinhibitor (tetraethyl pyrophosphate, TEPP). He worked in Adolphe Wurtz's...
pseudocholinesterase, or plasma (cholin)esterase, is a nonspecific cholinesterase enzyme that hydrolyses many different choline-based esters. In humans...
has been used for control of soil-borne nematodes. Aldicarb is a cholinesteraseinhibitor, which prevents the breakdown of acetylcholine in the synapse....
inhibition the substrate and inhibitor cannot bind to the enzyme at the same time.: 134 This usually results from the inhibitor having an affinity for the...
ACE inhibitor therapy.[citation needed] More recently, they have been used for the treatment of heart failure in patients intolerant of ACE inhibitor therapy...
chocolate-brown color. Calabar bean contains physostigmine, a reversible cholinesteraseinhibitor alkaloid. The alkaloid physostigmine acts in effect like nerve...
obsolete organophosphate insecticide. Schradan itself is a weak cholinesteraseinhibitor and requires metabolic activation to become active. Dimefox Mipafox...
decrease in slope and a reduced maximum are obtained. Enzyme inhibitor Growth factor receptor inhibitor Selective receptor modulator "Pharmacology Guide: In vitro...
nature. Naturally occurring aminals Physostigmine,a highly toxic cholinesteraseinhibitor found in the Calabar bean. Hodgkinsine, an alkaloid with antiviral...
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