Esai and Pfizer; patent expires 2010.
Mild to moderate Alzheimer’s dementia.
Moderate to severe Alzheimer's dementia.
Off-label use for mild cognitive impairment.
Acetylcholinesterase inhibitor. Enhances brain cholinergic function.
5 mg white and 10 mg yellow tablets
Orally disintegrating tablets: 5 mg white and 10 mg yellow.
Start at 5 mg QD, increase to 10 mg QD after four weeks. Morning dosing may minimize insomnia and vivid dreams.
No dose adjustment needed in renal impairment; only a minimal dose decrease required in hepatic impairment.
Most common: nausea, diarrhea, insomnia, fatigue.
Occasionally: agitation, vivid dreams.
May aggravate stomach ulcers (potential class effect of all cholinesterase inhibitors)
Pregnancy risk category C.
Partly metabolized by P450 3A4, so theoretically levels could be increased by 3A4 inhibitors such as Luvox, and levels could be decreased by inducers such as Tegretol.
Metabolized mostly by liver; about 20% is excreted unchanged in the urine.
Half-life 3 days.
Aricept has the best evidence for effectiveness in mild cognitive impairment of all cholinesterase inhibitors.