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Table 2 Comparison of Features of Acetylcholinesterase Inhibitors (AChEIs)

From: Current pharmacologic options for patients with Alzheimer's disease

AChEI (Binding)

Mechanism of Action

Dosing Schedule

Recommended Daily Dosage Range

Half-life

Comments

Tacrine (Non-competitive, reversible)

Inhibition of AChE Inhibition of BuChE

4 times daily

120–160 mg/day (Initial dose 40 mg/day)

3–5 hours

Used in the United States as a last-line agent due to its short half-life and high incidence of hepatotoxicity

Donepezil (Non-competitive reversible)

Inhibition of AChE

Once daily

5–10 mg/day (Initial dose 5 mg/day)

70 hours

Well tolerated, with positive effects on cognition, global function, and ADL

Rivastigmine (Non-competitive, reversible)

Inhibition of AChE Inhibition of BuChE

Twice daily

6–12 mg/day (Initial dose 3 mg/day)

1.5 hours

Well tolerated, with positive effects on cognition, global function, and ADL

Galantamine (Competitive, reversible)

Inhibition of AChE Allosteric modulation of nicotinic acetylcholine receptors

Twice daily

16–24 mg/day (Initial dose 8 mg/day)

7 hours

Well tolerated, with positive effects on cognition, global function, ADL, behavior, and caregiver time

  1. AChE, acetylcholinesterase; BuChE, butyrylcholinesterase; ADL, activities of daily living.