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Cholinesterase inhibitor

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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]

Uses

Acetylcholinesterase inhibitors:[2]

Effects

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]

Examples

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

References

External links

  • Medical Subject Headings (MeSH)
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