Cholinesterase inhibitors


Cholinesterase inhibitors (ChEIs), also known as anti-cholinesterase, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or butyrylcholine. 



They increases the amount of the acetylcholine or butyrylcholine in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others. 



ChEIs may be used as drugs for Alzheimer’s and myasthenia gravis, and also as chemical weapons and insecticides.



Side effects may include:  loss of appetite, nausea, vomiting, loose stools, vivid dreams, dehydration, rash, bradycardia, peptic ulcer disease, seizures, weight loss, rhinorrhea, salivation, muscle cramps, and fasciculations.



ChEIs are indirect-acting parasympathomimetic drugs.



While 4 ChEIs are approved in the US, only three are available commercially.



The three available are rivastigmine, donepezil, and galantamine.



Generally used to treat Alzheimer’s disease and dementia.



Side effects of ChEI include: insomnia, nausea and vomiting, accidental injury, headache, dizziness, bradycardia, hypotension, ecchymosis, and sleep disturbance.


Comparing  rivastigmine to the other ChEI drugs donepezil and galantamine:  was associated with a higher frequency of reports of death as an adverse event.



Galantamine might be less well tolerated than donepezil and rivastigmine.


In a study that included 6070 patients with Alzheimer’s disease, ChEI users had a significantly lower risk of cardiovascular events than nonusers.

Among ChEI users, patients with a high cumulative dose had a significantly lower risk of CVEs than those with a low cumulative dose.

The use of ChEIs was associated with a decreased risk of incident CVEs among patients with AD. 

The cardioprotective effect of ChEIs showed a dose-response relationship.


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