World Library  
Flag as Inappropriate
Email this Article

Cholinesterase inhibitor

Article Id: WHEBN0023275770
Reproduction Date:

Title: Cholinesterase inhibitor  
Author: World Heritage Encyclopedia
Language: English
Subject: Tacrine, Azinphos-methyl, Dichlorvos
Publisher: World Heritage Encyclopedia

Cholinesterase inhibitor

Not to be confused with ACE inhibitor.

An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical that inhibits the acetylcholinesterase enzyme from breaking down acetylcholine, thereby increasing both the level and duration of action of the neurotransmitter acetylcholine. Reversible, quasi-irreversible (or pseudirreversible in some sources) and irreversible inhibitors exist.[1]


Acetylcholinesterase inhibitors:[2]


Potential side effects of acetylcholinesterase inhibitors[10][11]
mild – usually goes away potentially serious

Some major effects of cholinesterase inhibitors:

Administration of reversible cholinoesterase inhibitors is contraindicated with those that have urinary retention due to obstruction.

Titration phase

When used in the central nervous system to alleviate neurological symptoms, such as rivastigmine in Alzheimer's disease, all cholinesterase inhibitors require doses to be increased gradually over several weeks, and this is usually referred to as the titration phase. Many other types drug treatments may require a titration or stepping up phase. This strategy is used to build tolerance to adverse events or to reach a desired clinical effect. [12]


Reversible inhibitor

Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:

Comparison table

Comparison of reversible acetylcholinesterase inhibitors
Inhibitor Duration Main site of action Clinical use Adverse effects
Edrophonium short (10 min.)[18] neuromuscular junction[18] diagnosis of myasthenia gravis[18]
Neostigmine medium (1–2 hrs.)[18] neuromuscular junction[18] visceral[18]
Physostigmine medium (0.5-5 hrs.)[18] postganglionic parasympathetic[18] treat glaucoma (eye drops)[18]
Pyridostigmine medium (2–3 hrs.)[18] neuromuscular junction[18]
Dyflos long[18] postganglionic parasympathetic[18] historically to treat glaucoma (eye drops)[18] toxic[18]
Ecothiopate (irreversible) long[18] postganglionic parasympathetic[18] treat glaucoma (eye drops)[18] systemic effects[18]
Parathion (irreversible) long[18] none[18] toxic[18]

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:

Natural Compounds

See also


External links

  • Medical Subject Headings (MeSH)
This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.

Copyright © World Library Foundation. All rights reserved. eBooks from World eBook Library are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.