Altered Expression/Activity of Cytochrome P450 (CYP) 3A4 Enzyme: Implications in Drug Safety and Efficacy
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چکیده
منابع مشابه
Fentanyl metabolism by human hepatic and intestinal cytochrome P450 3A4: implications for interindividual variability in disposition, efficacy, and drug interactions.
The synthetic opioid fentanyl undergoes extensive metabolism in humans. Systemic elimination occurs primarily by hepatic metabolism. When administered as a lozenge for oral transmucosal absorption, swallowed fentanyl is subject to first pass metabolism in the liver and possibly small intestine. Little is known, however, about the identity and formation of human fentanyl metabolites. This invest...
متن کاملEffect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme.
CONTEXT St John's wort is a popular herbal product used to treat depression but it has been implicated in drug interactions. OBJECTIVE To assess the potential of St John's wort administration to alter the activity of the cytochrome P450 (CYP) enzymes extensively involved in drug metabolism. DESIGN, SETTING, AND PARTICIPANTS Open-label crossover study with fixed treatment order conducted Mar...
متن کاملKinetics of electron transfer between NADPH-cytochrome P450 reductase and cytochrome P450 3A4.
We have incorporated CYP3A4 (cytochrome P450 3A4) and CPR (NADPH-cytochrome P450 reductase) into liposomes with a high lipid/protein ratio by an improved method. In the purified proteoliposomes, CYP3A4 binds testosterone with Kd (app)=36±6 μM and Hill coefficient=1.5±0.3, and 75±4% of the CYP3A4 can be reduced by NADPH in the presence of testosterone. Transfer of the first electron from CPR to ...
متن کاملModeling of interactions between xenobiotics and cytochrome P450 (CYP) enzymes
The adverse effects to humans and environment of only few chemicals are well known. Absorption, distribution, metabolism, and excretion (ADME) are the steps of pharmaco/toxicokinetics that determine the internal dose of chemicals to which the organism is exposed. Of all the xenobiotic-metabolizing enzymes, the cytochrome P450 (CYP) enzymes are the most important due to their abundance and versa...
متن کاملCytochrome P450 3A4-mediated interaction of diclofenac and quinidine.
The metabolism of diclofenac to its 5-hydroxylated derivative in humans is catalyzed by cytochrome P450 (CYP)3A4. We report herein that in vitro this biotransformation pathway is stimulated by quinidine. When diclofenac was incubated with human liver microsomes in the presence of quinidine, the formation of 5-hydroxydiclofenac increased approximately 6-fold relative to controls. Similar phenome...
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ژورنال
عنوان ژورنال: Journal of Clinical Trials
سال: 2016
ISSN: 2167-0870
DOI: 10.4172/2167-0870.1000e123