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] |