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 |
|---|---|
| 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 1 |
| Externally published | Yes |
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Keywords
- Cytochrome P450 2C8 (CYP2C8)
- Drug interaction
- Quercetin
- Rosiglitazone
ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)
Cite this
Effect of quercetin on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in healthy subjects. / Kim, Kyoung Ah; Park, Pil Whan; Kim, Hyung Kee; Ha, Jong Myung; Park, Ji-Young.
In: Journal of Clinical Pharmacology, Vol. 45, No. 8, 01.08.2005, p. 941-946.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Effect of quercetin on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in healthy subjects
AU - Kim, Kyoung Ah
AU - Park, Pil Whan
AU - Kim, Hyung Kee
AU - Ha, Jong Myung
AU - Park, Ji-Young
PY - 2005/8/1
Y1 - 2005/8/1
N2 - 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.
AB - 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.
KW - Cytochrome P450 2C8 (CYP2C8)
KW - Drug interaction
KW - Quercetin
KW - Rosiglitazone
UR - http://www.scopus.com/inward/record.url?scp=23044511374&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=23044511374&partnerID=8YFLogxK
U2 - 10.1177/0091270005278407
DO - 10.1177/0091270005278407
M3 - Article
VL - 45
SP - 941
EP - 946
JO - Journal of Clinical Pharmacology
JF - Journal of Clinical Pharmacology
SN - 0091-2700
IS - 8
ER -