Tacrine, the first drug specifically approved for Alzheimer's disease,
produces symptomatic improvement. The theoretical rationale behind tr
eating Alzheimer's disease with tacrine is based on central cholinergi
c depletion. Tacrine is centrally acting, uncompetitive reversible inh
ibitor of acetylcholinesterase and butyrylcholinesterase. Multiple cli
nical trials support the effectiveness of tacrine in Alzheimer's disea
se. High dosages of tacrine are required for efficacy, with the potent
ial for hepatic and mild gastrointestinal adverse effects. However, th
e benefits of tacrine currently outweigh its risks, and a trial of the
drug should be offered to patients. As clinical experience with tacri
ne increases, the long term risk-benefit equation may be refined.