Greater impact of oral fluconazole on drug interaction with intravenous calcineurin inhibitors as compared with intravenous fluconazole

Ai Mihara, Takehiko Mori, Yoshinobu Aisa, Rie Yamazaki, Osamu Iketani, Yusuke Tanigawara, Yasuo Ikeda, Shinichiro Okamoto

Research output: Contribution to journalArticle

23 Citations (Scopus)

Abstract

Objective: Although the drug interaction between fluconazole and calcineurin inhibitors has been established, the influence of the route of fluconazole administration on its drug interaction with calcineurin inhibitors has yet to be fully examined. The aim of the present study is to examine whether different routes of fluconazole administration alter its drug interactions with intravenous calcineurin inhibitors. Methods: In 53 recipients of allogeneic hematopoietic cell transplantation receiving calcineurin inhibitors intravenously, steady-state whole-blood levels of cyclosporine A (CsA) or tacrolimus were measured after the route of fluconazole (200 mg/day) administration was switched from intravenous to oral. Results: The mean steady-state whole-blood level of CsA or tacrolimus significantly increased after the route of fluconazole administration was switched from intravenous to oral (CsA: to 394±28.4 from 362±17.8 ng/mL; tacrolimus: to 18.8±0.64 from 17.4±0.39 ng/mL, P<0.05). Conclusion: This finding strongly suggests that oral fluconazole has a greater impact on its drug interactions with intravenous calcineurin inhibitors than intravenous fluconazole. Monitoring of blood levels of intravenous calcineurin inhibitors is recommended when the route of fluconazole administration is switched from intravenous to oral.

Original languageEnglish
Pages (from-to)89-91
Number of pages3
JournalEuropean Journal of Clinical Pharmacology
Volume64
Issue number1
DOIs
Publication statusPublished - 2008 Jan

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Fluconazole
Drug Interactions
Tacrolimus
Cyclosporine
Calcineurin Inhibitors
Cell Transplantation

Keywords

  • Calcineurin inhibitors
  • Cyclosporine A
  • Drug interaction
  • Fluconazole
  • Tacrolimus

ASJC Scopus subject areas

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

Cite this

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abstract = "Objective: Although the drug interaction between fluconazole and calcineurin inhibitors has been established, the influence of the route of fluconazole administration on its drug interaction with calcineurin inhibitors has yet to be fully examined. The aim of the present study is to examine whether different routes of fluconazole administration alter its drug interactions with intravenous calcineurin inhibitors. Methods: In 53 recipients of allogeneic hematopoietic cell transplantation receiving calcineurin inhibitors intravenously, steady-state whole-blood levels of cyclosporine A (CsA) or tacrolimus were measured after the route of fluconazole (200 mg/day) administration was switched from intravenous to oral. Results: The mean steady-state whole-blood level of CsA or tacrolimus significantly increased after the route of fluconazole administration was switched from intravenous to oral (CsA: to 394±28.4 from 362±17.8 ng/mL; tacrolimus: to 18.8±0.64 from 17.4±0.39 ng/mL, P<0.05). Conclusion: This finding strongly suggests that oral fluconazole has a greater impact on its drug interactions with intravenous calcineurin inhibitors than intravenous fluconazole. Monitoring of blood levels of intravenous calcineurin inhibitors is recommended when the route of fluconazole administration is switched from intravenous to oral.",
keywords = "Calcineurin inhibitors, Cyclosporine A, Drug interaction, Fluconazole, Tacrolimus",
author = "Ai Mihara and Takehiko Mori and Yoshinobu Aisa and Rie Yamazaki and Osamu Iketani and Yusuke Tanigawara and Yasuo Ikeda and Shinichiro Okamoto",
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T1 - Greater impact of oral fluconazole on drug interaction with intravenous calcineurin inhibitors as compared with intravenous fluconazole

AU - Mihara, Ai

AU - Mori, Takehiko

AU - Aisa, Yoshinobu

AU - Yamazaki, Rie

AU - Iketani, Osamu

AU - Tanigawara, Yusuke

AU - Ikeda, Yasuo

AU - Okamoto, Shinichiro

PY - 2008/1

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N2 - Objective: Although the drug interaction between fluconazole and calcineurin inhibitors has been established, the influence of the route of fluconazole administration on its drug interaction with calcineurin inhibitors has yet to be fully examined. The aim of the present study is to examine whether different routes of fluconazole administration alter its drug interactions with intravenous calcineurin inhibitors. Methods: In 53 recipients of allogeneic hematopoietic cell transplantation receiving calcineurin inhibitors intravenously, steady-state whole-blood levels of cyclosporine A (CsA) or tacrolimus were measured after the route of fluconazole (200 mg/day) administration was switched from intravenous to oral. Results: The mean steady-state whole-blood level of CsA or tacrolimus significantly increased after the route of fluconazole administration was switched from intravenous to oral (CsA: to 394±28.4 from 362±17.8 ng/mL; tacrolimus: to 18.8±0.64 from 17.4±0.39 ng/mL, P<0.05). Conclusion: This finding strongly suggests that oral fluconazole has a greater impact on its drug interactions with intravenous calcineurin inhibitors than intravenous fluconazole. Monitoring of blood levels of intravenous calcineurin inhibitors is recommended when the route of fluconazole administration is switched from intravenous to oral.

AB - Objective: Although the drug interaction between fluconazole and calcineurin inhibitors has been established, the influence of the route of fluconazole administration on its drug interaction with calcineurin inhibitors has yet to be fully examined. The aim of the present study is to examine whether different routes of fluconazole administration alter its drug interactions with intravenous calcineurin inhibitors. Methods: In 53 recipients of allogeneic hematopoietic cell transplantation receiving calcineurin inhibitors intravenously, steady-state whole-blood levels of cyclosporine A (CsA) or tacrolimus were measured after the route of fluconazole (200 mg/day) administration was switched from intravenous to oral. Results: The mean steady-state whole-blood level of CsA or tacrolimus significantly increased after the route of fluconazole administration was switched from intravenous to oral (CsA: to 394±28.4 from 362±17.8 ng/mL; tacrolimus: to 18.8±0.64 from 17.4±0.39 ng/mL, P<0.05). Conclusion: This finding strongly suggests that oral fluconazole has a greater impact on its drug interactions with intravenous calcineurin inhibitors than intravenous fluconazole. Monitoring of blood levels of intravenous calcineurin inhibitors is recommended when the route of fluconazole administration is switched from intravenous to oral.

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KW - Tacrolimus

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