Possible role of hydroxylated metabolites of tacrine in drug toxicity and therapy of Alzheimer's disease
Language English Country Netherlands Media print
Document type Journal Article, Research Support, Non-U.S. Gov't, Review
- MeSH
- Alzheimer Disease drug therapy MeSH
- Cholinesterase Inhibitors metabolism therapeutic use toxicity MeSH
- Hydroxylation MeSH
- Humans MeSH
- Nootropic Agents metabolism therapeutic use toxicity MeSH
- Cytochrome P-450 Enzyme System genetics metabolism MeSH
- Tacrine analogs & derivatives metabolism therapeutic use toxicity MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Review MeSH
- Names of Substances
- Cholinesterase Inhibitors MeSH
- Nootropic Agents MeSH
- Cytochrome P-450 Enzyme System MeSH
- Tacrine MeSH
Tacrine belongs to the group of acetylcholinesterse (AChE) inhibitors used as drugs for treatment of Alzheimer's 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.
References provided by Crossref.org
In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Development of 2-Methoxyhuprine as Novel Lead for Alzheimer's Disease Therapy
