Effect of quercetin on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in healthy subjects

Kyoung Ah Kim, Pil Whan Park, Hyung Kee Kim, Jong Myung Ha, Ji Young Park

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

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 watched 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, AUClast, and Cmax, 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.

Original languageEnglish
Pages (from-to)941-946
Number of pages6
JournalJournal of Clinical Pharmacology
Volume45
Issue number8
DOIs
Publication statusPublished - 2005 Aug

Keywords

  • Cytochrome P450 2C8 (CYP2C8)
  • Drug interaction
  • Quercetin
  • Rosiglitazone

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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