Cholinesterase inhibitor

Uncommon card · No. 176362

Cholinesterase inhibitors (ChEIs) inhibit the enzyme cholinesterase from breaking down the neurotransmitter acetylcholine into choline and acetate. This increases both the level and duration of action of acetylcholine in the central nervous system, autonomic ganglia and neuromuscular junctions, the synaptic clefts of which are rich in acetylcholine receptors. ChEIs are indirect-acting parasympathomimetic drugs. Both the acetyl­cholin­esterase (AChE) and the butyryl­cholin­esterase (BChE) play a role in the breakdown of acetylcholine at neuromuscular junctions and ChEIs generally target both. Only a handful are selective enough to be properly called an AChE inhibitor or a BChE inhibitor. (The butyryl­cholin­esterase is named for its ability to hydrolyze a wider range of choline esters, including butyrylcholine (BCh) in vitro. BCh is not naturally made by the human body.) As with all enzyme inhibitors, ChEIs are classified as reversible or irreversible, according to how hard they are to dislodge...

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