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 language | English |
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Pages (from-to) | 941-946 |
Number of pages | 6 |
Journal | Journal of Clinical Pharmacology |
Volume | 45 |
Issue number | 8 |
DOIs | |
Publication status | Published - 2005 Aug |
Externally published | Yes |
Keywords
- Cytochrome P450 2C8 (CYP2C8)
- Drug interaction
- Quercetin
- Rosiglitazone
ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)