Tacrine is a centrally acting acetylcholinesterase inhibitor and indirect cholinergic agonist. It was the first centrally acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex. Tacrine (9-amino-1,2,3,4-tetrahydroacridine) is a low-molecular-weight, lipophilic heterocycle that crosses the blood brain barrier to increase synaptic acetylcholine through reversible inhibition of acetylcholinesterase. It is absorbed orally, undergoes extensive hepatic metabolism primarily via cytochrome P450 1A2 to hydroxylated metabolites that are subsequently conjugated, and is eliminated mainly as metabolites in urine. Clinically important properties include a relatively short plasma half-life requiring multiple daily dosing historically, a narrow therapeutic index with dose-related hepatotoxicity observed in a subset of patients, and potential for drug interactions with other CYP1A2 substrates or inhibitors.
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