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]
Tetra (monoisopropyl) pyrophosphoramide (Iso-OMPA) and ethopropazine are selective BChE inhibitors.[14]
AChE and BChE inhibitor
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
Galantamine might be less well tolerated than donepezil and rivastigmine.[11]
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.
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^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.
^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 eBudson, 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 bKhoury, 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.
^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 dHersen, 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 cWaiskopf, 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.