1. Donepezil (Aricept) is the drug of choice for improving cognitive functioning in Alzheimer's dementia. It works by central reversible inhibition of acetylcholinesterase thereby increasing CNS levels of acetylcholine. It may slow progress of the disease.
a. Beginning dose is 5 mg qhs which, after 4-6 weeks, may be increased to 10 mg qhs if necessary.
b. Donepezil has no reported hepatic toxicity or significant drug interactions. Side effects include GI upset or diarrhea.
2. Rivastigmine (Exelon) is an acetylcholinesterase inhibitor with a similar mechanism of action as donepezil.
a. Dosing is begun at 1.5 mg bid, and increased to 4.5 mg bid and then 6.0 mg bid at two-week intervals. Efficacy is greatest at the higher dose.
b. The most common side effects are nausea, diarrhea and syncope. GI side effects are reduced by coadministration with food. There is no hepatic toxicity.
3. Tacrine (Cognex) is a less specific esterase inhibitor that requires monitoring of AST and SLT levels weekly for 18 weeks, every month for 4 months, and then every 3 months thereafter. Initial dose is10 mg qid, increased every 6 weeks to 40 mg qid. Tacrine is hepatotoxic and not used.
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