Possible Role of Hydroxylated Metabolites of Tacrine in Drug Toxicity and Therapy of Alzheimers Disease

Title: Possible Role of Hydroxylated Metabolites of Tacrine in Drug Toxicity and Therapy of Alzheimers Disease

Volume: 9 Issue: 4

Author(s): Jiri Patocka, Daniel Jun and Kamil Kuca

Affiliation:

Keywords: Alzheimer's disease, tacrine, metabolite, drug toxicity, P450, hydroxyderivatives

Abstract: Tacrine belongs to the group of acetylcholinesterse (AChE) inhibitors used as drugs for treatment of Alzheimers disease (AD). The formation of hydroxyderivatives of tacrine is well-established step in the metabolization of this drug in liver by microsomal cytochrome P450 enzymes family. Genetic polymorphism of cytochrome P450 enzymes is probably responsible for balance between a number of stable and non-toxic metabolites and highly protein-reactive and toxic ones. By this manner may be explained why the hepatotoxicity of tacrine was observed only in the part of persons and why not every patient with AD responds to the treatment by this drug.

Cite this article as:

Patocka Jiri, Jun Daniel and Kuca Kamil, Possible Role of Hydroxylated Metabolites of Tacrine in Drug Toxicity and Therapy of Alzheimers Disease, Current Drug Metabolism 2008; 9 (4) . https://dx.doi.org/10.2174/138920008784220619