Drug-drug interactions by azole antifungals: Beyond a dogma of CYP3A4 enzyme activity inhibition

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F11%3A33119053" target="_blank" >RIV/61989592:15310/11:33119053 - isvavai.cz</a>

Result on the web

<a href="http://dx.doi.org/10.1016/j.toxlet.2011.01.027" target="_blank" >http://dx.doi.org/10.1016/j.toxlet.2011.01.027</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.toxlet.2011.01.027" target="_blank" >10.1016/j.toxlet.2011.01.027</a>

Result language

angličtina

Original language name

Drug-drug interactions by azole antifungals: Beyond a dogma of CYP3A4 enzyme activity inhibition

Original language description

Azoles antifungals are widespread used drugs for various medicinal indications. These drugs are well known for their numerous drug-drug interactions, which are believed to occur via inhibition of CYP3A4 enzymatic activity and consequently altering pharmacokinetic of co-administered drugs. In the current communication a complex view on the molecular interactions between azoles antimycotics and CYP3A4 is presented. Beside inhibition of CYP3A4 catalytic activity, azoles influence transcriptional activity of pregnane X receptor (PXR) and consequently expression of drug-metabolizing enzymes, including CYP3A4. Interactions between azoles and PXR occur by multiple mechanisms, including modulation of ligand-dependent activation of PXR (agonism, antagonism) oraffecting recruitment of PXR co-activators SRC-1 (steroid receptorco-activator 1)and HNF4 alpha (hepatocyte nuclear factor 4 alpha). Miconazole and ketoconazole are antagonists of glucocorticoid receptor (GR), therefore these drugs inhibi

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2011

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Toxicology Letters

ISSN

0378-4274

e-ISSN

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Volume of the periodical

202

Issue of the periodical within the volume

2

Country of publishing house

IE - IRELAND

Number of pages

4

Pages from-to

129-132

UT code for WoS article

000289708000007

EID of the result in the Scopus database

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