Effects of single and multiple doses of itraconazole on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein

Mikiko Shimizu, Tsukasa Uno, Kazunobu Sugawara, Tomonori Tateishi

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

Aims: We determined whether or not the extent of drug interaction of fexofenadine by itraconazole is time-dependent. Methods: In a randomized two-phase crossover study, itraconazole was administered orally for 6 days, and, on days 1, 3 and 6, fexofenadine was administered simultaneously. On another occasion, fexofenadine was administered alone. Results: Itraconazole increased fexofenadine AUC(0, ∞), and the % change for difference was 178% (95% CI 1235, 3379), 205% (95% CI 1539, 3319) and 169% (95% CI 1128, 2987) on days 1, 3 and 6 of the 6 day treatment, respectively. Conclusions: The extent of drug interaction by itraconazole was not time-dependent.

Original languageEnglish
Pages (from-to)372-376
Number of pages5
JournalBritish Journal of Clinical Pharmacology
Volume62
Issue number3
DOIs
Publication statusPublished - 2006 Sep
Externally publishedYes

Fingerprint

fexofenadine
Itraconazole
P-Glycoprotein
Pharmacokinetics
Drug Interactions
Cross-Over Studies
Area Under Curve

Keywords

  • Drug interaction
  • Fexofenadine
  • Itraconazole
  • Pharmacokinetics
  • Treatment period

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Effects of single and multiple doses of itraconazole on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein. / Shimizu, Mikiko; Uno, Tsukasa; Sugawara, Kazunobu; Tateishi, Tomonori.

In: British Journal of Clinical Pharmacology, Vol. 62, No. 3, 09.2006, p. 372-376.

Research output: Contribution to journalArticle

Shimizu, Mikiko ; Uno, Tsukasa ; Sugawara, Kazunobu ; Tateishi, Tomonori. / Effects of single and multiple doses of itraconazole on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein. In: British Journal of Clinical Pharmacology. 2006 ; Vol. 62, No. 3. pp. 372-376.
@article{4d33c749bc4d40ecaed0a285594e8b9c,
title = "Effects of single and multiple doses of itraconazole on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein",
abstract = "Aims: We determined whether or not the extent of drug interaction of fexofenadine by itraconazole is time-dependent. Methods: In a randomized two-phase crossover study, itraconazole was administered orally for 6 days, and, on days 1, 3 and 6, fexofenadine was administered simultaneously. On another occasion, fexofenadine was administered alone. Results: Itraconazole increased fexofenadine AUC(0, ∞), and the {\%} change for difference was 178{\%} (95{\%} CI 1235, 3379), 205{\%} (95{\%} CI 1539, 3319) and 169{\%} (95{\%} CI 1128, 2987) on days 1, 3 and 6 of the 6 day treatment, respectively. Conclusions: The extent of drug interaction by itraconazole was not time-dependent.",
keywords = "Drug interaction, Fexofenadine, Itraconazole, Pharmacokinetics, Treatment period",
author = "Mikiko Shimizu and Tsukasa Uno and Kazunobu Sugawara and Tomonori Tateishi",
year = "2006",
month = "9",
doi = "10.1111/j.1365-2125.2006.02689.x",
language = "English",
volume = "62",
pages = "372--376",
journal = "British Journal of Clinical Pharmacology",
issn = "0306-5251",
publisher = "Wiley-Blackwell",
number = "3",

}

TY - JOUR

T1 - Effects of single and multiple doses of itraconazole on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein

AU - Shimizu, Mikiko

AU - Uno, Tsukasa

AU - Sugawara, Kazunobu

AU - Tateishi, Tomonori

PY - 2006/9

Y1 - 2006/9

N2 - Aims: We determined whether or not the extent of drug interaction of fexofenadine by itraconazole is time-dependent. Methods: In a randomized two-phase crossover study, itraconazole was administered orally for 6 days, and, on days 1, 3 and 6, fexofenadine was administered simultaneously. On another occasion, fexofenadine was administered alone. Results: Itraconazole increased fexofenadine AUC(0, ∞), and the % change for difference was 178% (95% CI 1235, 3379), 205% (95% CI 1539, 3319) and 169% (95% CI 1128, 2987) on days 1, 3 and 6 of the 6 day treatment, respectively. Conclusions: The extent of drug interaction by itraconazole was not time-dependent.

AB - Aims: We determined whether or not the extent of drug interaction of fexofenadine by itraconazole is time-dependent. Methods: In a randomized two-phase crossover study, itraconazole was administered orally for 6 days, and, on days 1, 3 and 6, fexofenadine was administered simultaneously. On another occasion, fexofenadine was administered alone. Results: Itraconazole increased fexofenadine AUC(0, ∞), and the % change for difference was 178% (95% CI 1235, 3379), 205% (95% CI 1539, 3319) and 169% (95% CI 1128, 2987) on days 1, 3 and 6 of the 6 day treatment, respectively. Conclusions: The extent of drug interaction by itraconazole was not time-dependent.

KW - Drug interaction

KW - Fexofenadine

KW - Itraconazole

KW - Pharmacokinetics

KW - Treatment period

UR - http://www.scopus.com/inward/record.url?scp=33747039299&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33747039299&partnerID=8YFLogxK

U2 - 10.1111/j.1365-2125.2006.02689.x

DO - 10.1111/j.1365-2125.2006.02689.x

M3 - Article

C2 - 16796706

AN - SCOPUS:33747039299

VL - 62

SP - 372

EP - 376

JO - British Journal of Clinical Pharmacology

JF - British Journal of Clinical Pharmacology

SN - 0306-5251

IS - 3

ER -