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Acetylcholinesterase inhibitor: Wikis


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An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, increasing both the level and duration of action of the neurotransmitter acetylcholine.



Acetylcholinesterase inhibitors:



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[1] Main site of action[1] Clinical use[1] Adverse effects[1]
Edrophonium short (10 min.) neuromuscular junction diagnosis of myasthenia gravis
Neostigmine medium (1-2 hrs.) neuromuscular junction visceral
Physostigmine medium (0.5-5 hrs.) postganglionic parasympathetic treat glaucoma (eye drops)
Pyridostigmine medium (2-3 hrs.) neuromuscular junction
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:

Natural Compounds


Some major effects of cholinesterase 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.
  • SLUDGE syndrome.
  • Actions on the neuromuscular junction will result in prolonged muscle contraction.

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.[2]

See also


  1. ^ 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
  2. ^ Inglis F. “The tolerability and safety of cholinesterase inhibitors in the treatment of dementia.” Int J Clin Pract. 2002;(127):45-63. PMID 12139367

External links


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