Novartis; patent expires 2012.
Mild to moderate Alzheimer’s dementia.
Mild to moderate dementia associated with Parkinson’s disease.
Off-label use for severe dementia and mild cognitive impairment.
Acetylcholinesterase inhibitor. Enhances brain cholinergic function.
1.5 mg yellow, 3 mg orange, 4.5 mg red, and 6 mg orange and red capsules.
Oral solution available in 2 mg/mL strength.
Start at 1.5 mg BID, wait at least two weeks before increasing to 3 mg BID. The maximum recommended dose is 6 mg BID.
You may need to decrease the dose in both hepatic and renal impairment.
Most common: nausea (47% of patients in clinical trials), vomiting (31%), dizziness (21%), diarrhea (19%), insomnia, fatigue.
Occasionally: agitation, nightmares.
May aggravate stomach ulcers (potential class effect of all cholinesterase inhibitors).
Pregnancy risk category B.
Metabolized by the liver, but the P450 system is not involved.
Half-life 1.5 hours.
High rate of nausea and vomiting; dose cautiously to avoid this.
Exelon patch likely to be approved soon.