Inhibition of Desipramine Hydroxylation (Cytochrome P450-2D6) in Vitro by Quinidine and by Viral Protease Inhibitors: Relation to Drug Interactions in Vivo

1998 ◽  
Vol 87 (10) ◽  
pp. 1184-1189 ◽  
Author(s):  
Lisa L. von Moltke ◽  
David J. Greenblatt ◽  
Su Xiang Duan ◽  
Johanna P. Daily ◽  
Jerold S. Harmatz ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Protease Inhibitors ◽  
Cytochrome P450 2D6 ◽  
Viral Protease ◽  
P450 2D6

scholarly journals Influence du cytochrome P450 2D6 sur le métabolisme de la TFMPP (1-(3-trifluoro-méthylphenyl) pipérazine) : étude à l'aide de modèles in vitro et in vivo

2003 ◽  
Vol 15 (4) ◽  
pp. 243-249
Author(s):  
Roland F. Staack ◽  
Lilane D. Paul ◽  
Dietmar Springer ◽  
Thomas Kraemer ◽  
Hans H. Maurer
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 2D6 ◽  
P450 2D6

In vitro inhibitory effects of glucosamine, chondroitin and diacerein on human hepatic CYP2D6

2021 ◽  
Vol 36 (4) ◽  
pp. 259-270
Author(s):  
Boon Hooi Tan ◽  
Nafees Ahemad ◽  
Yan Pan ◽  
Uma Devi Palanisamy ◽  
Iekhsan Othman ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
High Performance ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Time Curve ◽  
Clinical Drugs ◽  
Inhibition Potencies ◽  
P450 2D6

Abstract Objectives Glucosamine, chondroitin and diacerein are natural compounds commonly used in treating osteoarthritis. Their concomitant intake may trigger drug–natural product interactions. Cytochrome P450 (CYP) has been implicated in such interactions. Cytochrome P450 2D6 (CYP2D6) is a major hepatic CYP involved in metabolism of 25% of the clinical drugs. This study aimed to investigate the inhibitory effect of these antiarthritic compounds on CYP2D6. Methods CYP2D6 was heterologously expressed in Escherichia coli. CYP2D6–antiarthritic compound interactions were studied using in vitro enzyme kinetics assay and molecular docking. Results The high-performance liquid chromatography (HPLC)-based dextromethorphan O-demethylase assay was established as CYP2D6 marker. All glucosamines and chondroitins weakly inhibited CYP2D6 (IC50 values >300 µM). Diacerein exhibited moderate inhibition with IC50 and K i values of 34.99 and 38.27 µM, respectively. Its major metabolite, rhein displayed stronger inhibition potencies (IC50=26.22 μM and K i =32.27 μM). Both compounds exhibited mixed-mode of inhibition. In silico molecular dockings further supported data from the in vitro study. From in vitro–in vivo extrapolation, rhein presented an area under the plasma concentration-time curve (AUC) ratio of 1.5, indicating low potential to cause in vivo inhibition. Conclusions Glucosamine, chondroitin and diacerein unlikely cause clinical interaction with the drug substrates of CYP2D6. Rhein, exhibits only low potential to cause in vivo inhibition.

scholarly journals Cytochrome P450-Based Drug-Drug Interactions of Vonoprazan In Vitro and In Vivo

2020 ◽  
Vol 11 ◽  
Author(s):  
Yiran Wang ◽  
Changxiong Wang ◽  
Shuanghu Wang ◽  
Quan Zhou ◽  
Dapeng Dai ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions

Effect of 24 Cytochrome P450 2D6 Variants Found in the Chinese Population on Atomoxetine Metabolism in vitro

Pharmacology ◽  
2015 ◽  
Vol 97 (1-2) ◽  
pp. 78-83 ◽  
Author(s):  
Bingqing Liang ◽  
Yunyun Zhan ◽  
Ying Wang ◽  
Ermin Gu ◽  
Dapeng Dai ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Chinese Population ◽  
Cytochrome P450 2D6 ◽  
P450 2D6

scholarly journals An investigation of morphine‐to‐codeine metabolic ratios in postmortem blood, drug interactions, and cytochrome P450 2D6 (CYP2D6) genotype

2013 ◽  
Vol 27 (S1) ◽  
Author(s):  
Jessica Lam ◽  
Karen Woodall ◽  
Patricia Solbeck ◽  
Colin JD Ross ◽  
Bruce Carleton ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Cyp2d6 Genotype ◽  
Cytochrome P450 2D6 ◽  
Postmortem Blood ◽  
P450 2D6
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