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Effect of Quercetin on the Pharmacokinetics of Rosiglitazone, a CYP2C8 Substrate, in Healthy Subjects
Author(s) -
Kim KyoungAh,
Park PilWhan,
Kim HyungKee,
Ha JongMyung,
Park JiYoung
Publication year - 2005
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270005278407
Subject(s) - rosiglitazone , quercetin , pharmacokinetics , pharmacology , placebo , cmax , medicine , crossover study , cyp2c8 , chemistry , biochemistry , metabolism , cyp3a4 , receptor , antioxidant , alternative medicine , pathology , cytochrome p450
Previous in vitro studies have demonstrated that quercetin inhibits CYP2C8, but there are no available data to indicate that quercetin inhibits CYP2C8 in vivo. The effect of long‐term use of quercetin on the pharmacokinetics of rosiglitazone was evaluated. After administration of quercetin or matched placebo for 3 weeks in a crossover manner, rosiglitazone 4 mg was administered, and the pharmacokinetics of rosiglitazone and N‐desmethylrosiglitazone were determined. For AUC ∞ , AUC last , and C max , the geometric mean ratios (90% confidence interval) for (quercetin + rosiglitazone/placebo + rosiglitazone) were 0.98 (0.92, 1.05), 0.99 (0.92, 1.05), and 1.01 (0.88, 1.14), respectively. Metabolic conversion based on the AUC ratio of N‐desmethylrosiglitazone/rosiglitazone in the quercetin phase (0.49 ± 0.17) was similar to that of the placebo phase (0.47 ± 0.14) (P = .574). Even though the acute interaction that would occur during the first few days of concurrent administration of quercetin cannot be excluded, these results indicate that long‐term use of quercetin does not inhibit CYP2C8 activity, and the usage has little possibility of interacting with drugs that are metabolized by CYP2C8, including rosiglitazone.