Notable Drug-Drug Interaction Between Etizolam and Itraconazole in Poor Metabolizers of Cytochrome P450 2C19

2017 ◽  
Vol 57 (11) ◽  
pp. 1491-1499 ◽  
Author(s):  
Takehito Yamamoto ◽  
Kenichi Furihata ◽  
Akihiro Hisaka ◽  
Takashi Moritoyo ◽  
Kazuaki Ogoe ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Poor Metabolizers ◽  
Cytochrome P450 2C19 ◽  
Drug Drug Interaction

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.

Use of Multiple Probes to Assess Transporter- and Cytochrome P450-Mediated Drug–Drug Interaction Potential of the Pangenotypic HCV NS5A Inhibitor Velpatasvir

2015 ◽  
Vol 55 (5) ◽  
pp. 605-613 ◽  
Author(s):  
Erik Mogalian ◽  
Polina German ◽  
Brian P. Kearney ◽  
Cheng Yong Yang ◽  
Diana Brainard ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Interaction Potential ◽  
Ns5a Inhibitor ◽  
Drug Drug Interaction
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