Document Detail

The effects of flavonoids on the ABC transporters: consequences for the pharmacokinetics of substrate drugs.
MedLine Citation:
PMID:  23289831     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: The flavonoids are a large group of dietary plant compounds with suggested health benefits. There is accumulating evidence that many of these flavonoids can interact with the major drug transporters (and metabolizing enzymes) in the body, leading to alterations in the pharmacokinetics of substrate drugs, and thus their efficacy and toxicity.
AREAS COVERED: This review summarizes and updates the reported in vitro and in vivo interactions between common dietary flavonoids and the major drug-effluxing ABC transporters; these include P-glycoprotein, breast cancer resistance protein and multidrug resistance proteins 1 and 2. In contrast to previous reviews, the ADME of flavonoids are considered, along with their glycosides and Phase II conjugates. The authors also consider their possible interactions with the ABC transporters in the oral absorption, distribution into pharmacological sanctuaries and excretion of substrate drugs. Electronic databases, including PubMed, Scopus and Google Scholar were searched to identify appropriate in vitro and in vivo ABC transporter-flavonoid interactions, particularly within the last 10 years.
EXPERT OPINION: Caution is advised when taking flavonoid-containing supplements or herbal remedies concurrently with drugs. Further clinical studies are warranted to explore the impact of flavonoids and their metabolites on the pharmacokinetics, efficacy and toxicity of drugs.
Yan Li; James W Paxton
Publication Detail:
Type:  Journal Article; Review     Date:  2013-01-06
Journal Detail:
Title:  Expert opinion on drug metabolism & toxicology     Volume:  9     ISSN:  1744-7607     ISO Abbreviation:  Expert Opin Drug Metab Toxicol     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-19     Completed Date:  2013-08-15     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  101228422     Medline TA:  Expert Opin Drug Metab Toxicol     Country:  England    
Other Details:
Languages:  eng     Pagination:  267-85     Citation Subset:  IM    
Auckland University of Technology, Faculty of Health and Environmental Sciences, Department of Interdisciplinary Studies, Auckland, New Zealand.
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MeSH Terms
ATP-Binding Cassette Transporters / drug effects*,  genetics,  metabolism
Adenosine Triphosphate / genetics,  metabolism
Administration, Oral
Carrier Proteins
Dietary Supplements
Drug Interactions
Drug Resistance / drug effects
Flavonoids / pharmacokinetics*
Multidrug Resistance-Associated Proteins / genetics,  metabolism
P-Glycoprotein / genetics,  metabolism
Xenobiotics / metabolism
Reg. No./Substance:
0/Carrier Proteins; 0/Flavonoids; 0/Multidrug Resistance-Associated Proteins; 0/P-Glycoprotein; 0/Xenobiotics; 0/multidrug resistance-associated protein 1; 0/multidrug resistance-associated protein 2; 56-65-5/Adenosine Triphosphate

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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