The burden and management of cytochrome P450 2D6 (CYP2D6)-mediated drug-drug interaction (DDI): co-medication of metoprolol and paroxetine or fluoxetine in the elderly

2017 ◽  
Vol 26 (7) ◽  
pp. 752-765 ◽  
Author(s):  
Muh. Akbar Bahar ◽  
Eelko Hak ◽  
Jens H.J. Bos ◽  
Sander D. Borgsteede ◽  
Bob Wilffert
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
The Elderly ◽  
Cytochrome P450 2D6 ◽  
Drug Drug Interaction ◽  
P450 2D6

Modeling Human Cytochrome P450 2D6 Metabolism and Drug-Drug Interaction by a Novel Panel of Knockout and Humanized Mouse Lines

2011 ◽  
Vol 81 (1) ◽  
pp. 63-72 ◽  
Author(s):  
Nico Scheer ◽  
Yury Kapelyukh ◽  
Jillian McEwan ◽  
Vincent Beuger ◽  
Lesley A. Stanley ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Cytochrome P450 2D6 ◽  
Humanized Mouse ◽  
Human Cytochrome ◽  
Drug Drug Interaction ◽  
P450 2D6 ◽  
Mouse Lines

scholarly journals In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Qun Zhang ◽  
Zengqiang Qu ◽  
Yanqing Zhou ◽  
Jin Zhou ◽  
Junwei Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Liver Microsomes ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Drug Drug Interaction ◽  
Dose Dependent

Abstract Background Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Methods Cornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated. Results Cornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the KI/Kinact value of 6.40/0.055 min− 1·μM− 1. Conclusions The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.

Probing Small-Molecule Binding to Cytochrome P450 2D6 and 2C9: An In Silico Protocol for Generating Toxicity Alerts

ChemMedChem ◽  
2010 ◽  
Vol 5 (12) ◽  
pp. 2088-2101 ◽  
Author(s):  
Gianluca Rossato ◽  
Beat Ernst ◽  
Martin Smiesko ◽  
Morena Spreafico ◽  
Angelo Vedani
Keyword(s):  
Cytochrome P450 ◽  
Small Molecule ◽  
In Silico ◽  
Cytochrome P450 2D6 ◽  
P450 2D6

From Genotype to Phenotype: Cytochrome P450 2D6-Mediated Drug Clearance in Humans

2017 ◽  
Vol 14 (3) ◽  
pp. 649-657 ◽  
Author(s):  
Jie Gao ◽  
Xin Tian ◽  
Jun Zhou ◽  
Ming-Zhu Cui ◽  
Hai-Feng Zhang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Clearance ◽  
Cytochrome P450 2D6 ◽  
P450 2D6

Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity

2005 ◽  
Vol 15 (10) ◽  
pp. 2647-2652 ◽  
Author(s):  
Bertrand Le Bourdonnec ◽  
Christopher W. Ajello ◽  
Pamela R. Seida ◽  
Roberta G. Susnow ◽  
Joel A. Cassel ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Opioid Receptor ◽  
Inhibitory Activity ◽  
Cytochrome P450 2D6 ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists ◽  
P450 2D6
Sign in / Sign up

Export Citation Format

Share Document