Acetylcholinesterase Inhibitors and Dementia-Related Medications

Primer

Acetylcholinesterase Inhibitors and Related Medications are commonly used in the treatment of neurodegenerative disorders.

Acetylcholinesterase Inhibitors

Acetylcholinesterase Inhibitors (AChEIs) include donepezil, rivastigmine, and galantamine. Many of these inhibitors also interact with the second known cholinesterase, butyrylcholinesterase (BChE).[1]

Comparison

Acetylcholinesterase Inhibitors

Drug Half-life Metabolism Dosing Notes
Donepezil 70 hours CYP2D6
CYP3A4 		2.5–5 mg daily, can increase by 2.5–5mg q 4 weeks up to maximum of 10 mg Most commonly prescribed; longest half-life
Galantamine 7 hours CYP2D6
CYP3A4 		8 mg daily, ↑ by 8 mg q 4 weeks up to maximum of 24mg Lower risk for muscle cramps than donepezil
Rivastigmine oral 1.5 hours AChE, BChE-mediated hydrolysis 1.5 mg BID, ↑ by 1.5 mg BID q2–4 weekly up to maximum of 6mg BID GI symptoms with oral may limit ability to get to max dose; patch has lower risk for GI symptoms
Rivastigmine patch 3 hours Patch: 4.6 mg for 4 weeks, then increase to 9.5 mg for 4 weeks, then up to maximum of 13.3 mg Use if unable to tolerate PO

References

1) Pohanka M. (2014). Inhibitors of acetylcholinesterase and butyrylcholinesterase meet immunity. International journal of molecular sciences, 15(6), 9809–9825.