Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats
Joint Authors
Liu, Yan
Liu, Rui
Liu, Gaofeng
Zhang, Zhiren
Dong, Feng
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2010-11-28
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Abstract EN
Flos carthami is a traditional Chinese herbal medicine.
Clinically, the Flos carthami Injection has been used concomitantly with other Western drugs and may be used concomitantly with β-blockers, such as metoprolol, to treat cerebrovascular and coronary heart diseases, in China.
Metoprolol is a CYP2D6 substrate and is predominantly metabolized by this isozyme.
However, we do not know whether there is an effect of Flos carthami on CYP2D6 and the consequences of such an effect.
Concern is raised regarding the possible herb-drug interaction.
In this report, the effects of Flos carthami on the activity of CYP2D6 in vivo and in vitro and on the pharmacokinetics of metoprolol, in rats, are investigated.
To assess the inhibitory potency of Flos carthami, the concentration associated with 50% inhibition (IC50) of dextromethorphan metabolism was determined based on the concentration-inhibition curves.
The inhibitory effect of Flos carthami on CYP2D6 was also compared with cimetidine in vitro.
Flos carthami could significantly inhibit CYP2D6 in rats both in vitro and in vivo (P<.05) and could slow down the metabolic rate of metoprolol as suggested by prolonged t1/2 (67.45%), by increased Cmax (74.51%) and AUC0−∞ (76.89%).
These results suggest that CYP2D6 is a risk factor when Flos carthami is administered concomitantly with metoprolol or other CYP2D6 substrates.
American Psychological Association (APA)
Liu, Gaofeng& Liu, Yan& Liu, Rui& Dong, Feng& Zhang, Zhiren. 2010. Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats. Evidence-Based Complementary and Alternative Medicine،Vol. 2011, no. 2011, pp.1-7.
https://search.emarefa.net/detail/BIM-454515
Modern Language Association (MLA)
Liu, Gaofeng…[et al.]. Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats. Evidence-Based Complementary and Alternative Medicine No. 2011 (2011), pp.1-7.
https://search.emarefa.net/detail/BIM-454515
American Medical Association (AMA)
Liu, Gaofeng& Liu, Yan& Liu, Rui& Dong, Feng& Zhang, Zhiren. Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats. Evidence-Based Complementary and Alternative Medicine. 2010. Vol. 2011, no. 2011, pp.1-7.
https://search.emarefa.net/detail/BIM-454515
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-454515