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. 2022 Mar 10;27(6):1816. doi: 10.3390/molecules27061816

Table 1.

Summary the AChEI drugs approved by FDA.

Classification Name Property Reported Correlation with AD Adverse Reaction References
First generation Tacrine Reversibility,
Lipid solubility
Inhibits AChE in plasma and tissues.
Promotes ACh release through M1 receptor.
Hepatotoxicity [106]
Second generation Donepezil Reversibility,
High selectivity
The only inhibitor that can act on both the peripheral and central catalytic sites of AChE.
Increases the concentration of AChE by reversibly inhibiting the ACh hydrolysis induced by AChE.
Increases the protein levels of PINK 1, NFASC, MYLK2 and NRAS in the hippocampus.
Nausea,
Vomiting
Diarrhea
Fatigue
[102]
Second generation Rivastigmine Reversibility Guides APP treatment away from BACE1 and toward A secretase.
Increases the concentration of AChE by reversibly inhibiting the ACh hydrolysis induced by AChE.
Dizziness
Vertigo
Upper respiratory tract infection
[21,105]
Second generation Galantamine Reversibility Allosteric activation effect on nicotinic ACh receptors.
Activates MARK, PI3K and other cell signal transduction pathways to play an anti-inflammatory effect.
Promotes the release of neurotransmitters associated with glutamate, norepinephrine and memory and mood.
Protects nerves against oxidative damage caused by hydrogen peroxide.
Salivation
Bradycardia
Dizziness
Abdominal pain
[107,108]