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Cholinesterase inhibitor

January 01, 1970

Not to be confused with Acetylcholinesterase inhibitor, Anticholinergic, or Cholinergic.

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]

Cholinesterase inhibitor
Drug class
Class identifiers
UseAlzheimer's disease
ATC codeN06#N06DA Anticholinesterases
Mechanism of actionEnzyme inhibitor
Biological targetCholinesterase
Clinical data
Drugs.comDrug Classes
WebMDMedicineNet 
External links
MeSHD002800
Legal status
In Wikidata
Acetylcholine
Sarin molecule, C4H10FO2P
Tetraethyl pyrophosphate molecule, C8H20O7P2

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]

Medical use edit

Further information: Donepezil § Medical uses

While 4 ChEIs are approved in the US for the treatment of Alzheimer's Disease, only three of these are available commercially.[6] The three available are rivastigmine, donepezil, and galantamine, while tacrine is not.[6] They are generally used to treat Alzheimer's disease and dementia.[6] If a benefit occurs, it is generally during the second or third month after starting.[6]

It is difficult to determine which ChEI has greater efficacy, due to design flaws in head-to-head comparison studies.[11]

Pyridostigmine is used in the treatment of myasthenia gravis.[12]

Neostigmine is used in combination with a muscarinic antagonist to reverse the effects of non-depolarizing muscle relaxants e.g. rocuronium bromide

Cholinesterase inhibitor toxicity edit

Further information: Organophosphate poisoning and cholinergic crisis

Common side effects of one ChEI include insomnia, nausea and vomiting, accidental injury, headache, dizziness, bradycardia, hypotension, ecchymosis, and sleep disturbance.[13]

Binding affinity edit

Acetylcholinesterase inhibitors edit

Donepezil, phenserine, huperzine A, and BW284c51 are selective AChE inhibitors.[14][11]

Butyrylcholinesterase inhibitor edit

Tetra (monoisopropyl) pyrophosphoramide (Iso-OMPA) and ethopropazine are selective BChE inhibitors.[14]

AChE and BChE inhibitor edit

Paraoxon and rivastigmine are both acetylcholinesterase inhibitors and butyrylcholinesterase inhibitors.[14][11][7]

In 2015, the United States Food and Drug Administration's Adverse Event Reporting System database compared rivastigmine to the other ChEI drugs donepezil and galantamine found that rivastigmine was associated with a higher frequency of reports of death as an adverse event.[15]

Acetylcholinesterase inhibitors and nicotinic receptor modulator edit

See also: Allosteric modulator and nicotinic receptor

Galantamine might be less well tolerated than donepezil and rivastigmine.[11]

Chemical weapons edit

Further information: Chemical weapon

Assassination Attempt edit

Cholinesterase inhibitors came to a public attention in 2020 when Russian opposition and dissent figure Alexei Navalny was treated in Berlin Charité hospital for poisoning by a Russian-made nerve agent which is known since 2019 as belonging to the Novichok agents subgroup of ChEI.[16]

See also edit

Further reading edit

  • Institute, National; (UK), Care Excellence (2019-12-27). Cholinesterase inhibitors and memantine for dementia. Retrieved 2019-12-27. {{cite book}}: |website= ignored (help)
  • Parsons, Chris G.; Danysz, Wojciech; Dekundy, Andrzej; Pulte, Irena (2013-05-09). "Memantine and Cholinesterase Inhibitors: Complementary Mechanisms in the Treatment of Alzheimer's Disease". Neurotoxicity Research. 24 (3). Springer Science and Business Media LLC: 358–369. doi:10.1007/s12640-013-9398-z. ISSN 1029-8428. PMC 3753463. PMID 23657927.
  • Meng, Yan‑Hong; Wang, Pan‑Pan; Song, Ya‑Xue; Wang, Jian‑Hua (2019-03-01). "Cholinesterase inhibitors and memantine for Parkinson's disease dementia and Lewy body dementia: A meta‑analysis". Experimental and Therapeutic Medicine. 17 (3): 1611–1624. doi:10.3892/etm.2018.7129. ISSN 1792-0981. PMC 6364145. PMID 30783428. Retrieved 2019-12-27.

References edit

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.
  4. ^ "Cholinesterase Inhibitors (Medical Use & WMD)". PharmWiki. Tulane University School of Medicine. Retrieved 24 August 2020.
  5. ^ 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.
  6. ^ a b c d e 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.
  7. ^ a b 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.
  8. ^ 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.
  9. ^ Castelvecchi, Davide (2019). "Novichok nerve agents banned by chemical-weapons treaty". Nature. doi:10.1038/d41586-019-03686-y. PMID 33244185.
  10. ^ Chai, Peter R.; Hayes, Bryan D.; Erickson, Timothy B.; Boyer, Edward W. (2018). "Novichok agents: A historical, current, and toxicological perspective". Toxicology Communications. 2 (1): 45–48. doi:10.1080/24734306.2018.1475151. PMC 6039123. PMID 30003185.
  11. ^ a b c d Hersen, Michel (2006). Comprehensive handbook of personality and psychopathology (Tertiary source). Hoboken, New Jersey: John Wiley. p. 514. ISBN 978-0-471-75725-2. OCLC 63041762.
  12. ^ World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. p. 429. hdl:10665/44053. ISBN 9789241547659.
  13. ^ "Prescribing information : Aricept" (PDF). FDA access data. Eisai Inc. and Pfizer Inc. 2012. (PDF) from the original on 2016-02-21. Retrieved 6 May 2021.
  14. ^ a b c Waiskopf, Nir; Soreq, Hermona (2015). "Cholinesterase Inhibitors". Handbook of Toxicology of Chemical Warfare Agents. Elsevier. pp. 761–778. doi:10.1016/b978-0-12-800159-2.00052-x. ISBN 978-0-12-800159-2.
  15. ^ Ali TB, Schleret TR, Reilly BM, Chen WY, Abagyan R (2015). "Adverse Effects of Cholinesterase Inhibitors in Dementia, According to the Pharmacovigilance Databases of the United-States and Canada". PLOS ONE. 10 (12): e0144337. Bibcode:2015PLoSO..1044337A. doi:10.1371/journal.pone.0144337. PMC 4671709. PMID 26642212.
  16. ^ "Alexei Navalny was poisoned 'using Novichok' nerve agent, say German government". Telegraph Media Group Limited. 2 September 2020.

January 01, 1970
cholinesterase, inhibitor, confused, with, acetylcholinesterase, inhibitor, anticholinergic, cholinergic, cheis, also, known, anti, cholinesterase, chemicals, that, prevent, breakdown, neurotransmitter, acetylcholine, butyrylcholine, this, increases, amount, a. Not to be confused with Acetylcholinesterase inhibitor Anticholinergic or Cholinergic 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 Cholinesterase inhibitorDrug classClass identifiersUseAlzheimer s diseaseATC codeN06 N06DA AnticholinesterasesMechanism of actionEnzyme inhibitorBiological targetCholinesteraseClinical dataDrugs comDrug ClassesWebMDMedicineNet External linksMeSHD002800Legal statusIn Wikidata Acetylcholine Sarin molecule C4H10FO2P Tetraethyl pyrophosphate molecule C8H20O7P2 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 Contents 1 Medical use 2 Cholinesterase inhibitor toxicity 3 Binding affinity 3 1 Acetylcholinesterase inhibitors 3 2 Butyrylcholinesterase inhibitor 3 3 AChE and BChE inhibitor 3 4 Acetylcholinesterase inhibitors and nicotinic receptor modulator 4 Chemical weapons 4 1 Assassination Attempt 5 See also 6 Further reading 7 ReferencesMedical use editFurther information Donepezil Medical uses While 4 ChEIs are approved in the US for the treatment of Alzheimer s Disease only three of these are available commercially 6 The three available are rivastigmine donepezil and galantamine while tacrine is not 6 They are generally used to treat Alzheimer s disease and dementia 6 If a benefit occurs it is generally during the second or third month after starting 6 It is difficult to determine which ChEI has greater efficacy due to design flaws in head to head comparison studies 11 Pyridostigmine is used in the treatment of myasthenia gravis 12 Neostigmine is used in combination with a muscarinic antagonist to reverse the effects of non depolarizing muscle relaxants e g rocuronium bromideCholinesterase inhibitor toxicity editFurther information Organophosphate poisoning and cholinergic crisis Common side effects of one ChEI include insomnia nausea and vomiting accidental injury headache dizziness bradycardia hypotension ecchymosis and sleep disturbance 13 Binding affinity editAcetylcholinesterase inhibitors edit Donepezil phenserine huperzine A and BW284c51 are selective AChE inhibitors 14 11 Butyrylcholinesterase inhibitor edit Tetra monoisopropyl pyrophosphoramide Iso OMPA and ethopropazine are selective BChE inhibitors 14 AChE and BChE inhibitor edit Paraoxon and rivastigmine are both acetylcholinesterase inhibitors and butyrylcholinesterase inhibitors 14 11 7 In 2015 the United States Food and Drug Administration s Adverse Event Reporting System database compared rivastigmine to the other ChEI drugs donepezil and galantamine found that rivastigmine was associated with a higher frequency of reports of death as an adverse event 15 Acetylcholinesterase inhibitors and nicotinic receptor modulator edit See also Allosteric modulator and nicotinic receptor Galantamine might be less well tolerated than donepezil and rivastigmine 11 Chemical weapons editFurther information Chemical weapon Assassination Attempt edit Cholinesterase inhibitors came to a public attention in 2020 when Russian opposition and dissent figure Alexei Navalny was treated in Berlin Charite hospital for poisoning by a Russian made nerve agent which is known since 2019 as belonging to the Novichok agents subgroup of ChEI 16 See also editOrganophosphate and carbamateFurther reading editInstitute National UK Care Excellence 2019 12 27 Cholinesterase inhibitors and memantine for dementia Retrieved 2019 12 27 a href Template Cite book html title Template Cite book cite book a website ignored help Parsons Chris G Danysz Wojciech Dekundy Andrzej Pulte Irena 2013 05 09 Memantine and Cholinesterase Inhibitors Complementary Mechanisms in the Treatment of Alzheimer s Disease Neurotoxicity Research 24 3 Springer Science and Business Media LLC 358 369 doi 10 1007 s12640 013 9398 z ISSN 1029 8428 PMC 3753463 PMID 23657927 Meng Yan Hong Wang Pan Pan Song Ya Xue Wang Jian Hua 2019 03 01 Cholinesterase inhibitors and memantine for Parkinson s disease dementia and Lewy body dementia A meta analysis Experimental and Therapeutic Medicine 17 3 1611 1624 doi 10 3892 etm 2018 7129 ISSN 1792 0981 PMC 6364145 PMID 30783428 Retrieved 2019 12 27 References edit 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 amp 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 a b c d e 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 a b 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 Castelvecchi Davide 2019 Novichok nerve agents banned by chemical weapons treaty Nature doi 10 1038 d41586 019 03686 y PMID 33244185 Chai Peter R Hayes Bryan D Erickson Timothy B Boyer Edward W 2018 Novichok agents A historical current and toxicological perspective Toxicology Communications 2 1 45 48 doi 10 1080 24734306 2018 1475151 PMC 6039123 PMID 30003185 a b c d Hersen Michel 2006 Comprehensive handbook of personality and psychopathology Tertiary source Hoboken New Jersey John Wiley p 514 ISBN 978 0 471 75725 2 OCLC 63041762 World Health Organization 2009 Stuart MC Kouimtzi M Hill SR eds WHO Model Formulary 2008 World Health Organization p 429 hdl 10665 44053 ISBN 9789241547659 Prescribing information Aricept PDF FDA access data Eisai Inc and Pfizer Inc 2012 Archived PDF from the original on 2016 02 21 Retrieved 6 May 2021 a b c Waiskopf Nir Soreq Hermona 2015 Cholinesterase Inhibitors Handbook of Toxicology of Chemical Warfare Agents Elsevier pp 761 778 doi 10 1016 b978 0 12 800159 2 00052 x ISBN 978 0 12 800159 2 Ali TB Schleret TR Reilly BM Chen WY Abagyan R 2015 Adverse Effects of Cholinesterase Inhibitors in Dementia According to the Pharmacovigilance Databases of the United States and Canada PLOS ONE 10 12 e0144337 Bibcode 2015PLoSO 1044337A doi 10 1371 journal pone 0144337 PMC 4671709 PMID 26642212 Alexei Navalny was poisoned using Novichok nerve agent say German government Telegraph Media Group Limited 2 September 2020 Retrieved from https en wikipedia org w index php title Cholinesterase inhibitor amp oldid 1211280944, wikipedia, wiki, book, books, library,

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