Delayed Effect of Grapefruit Juice on Pharmacokinetics and Pharmacodynamics of Tacrolimus in a Living-Donor Liver Transplant Recipient

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Author(s)

    • FUKATSU Sachio
    • Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University
    • FUKUDO Masahide
    • Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University
    • MASUDA Satohiro
    • Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University
    • YANO Ikuko
    • Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University
    • KATSURA Toshiya
    • Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University
    • OGURA Yasuhiro
    • Department of Transplantation and Immunology, Graduate School of Medicine, Kyoto University
    • OIKE Fumitaka
    • Department of Transplantation and Immunology, Graduate School of Medicine, Kyoto University
    • TAKADA Yasutsugu
    • Department of Transplantation and Immunology, Graduate School of Medicine, Kyoto University
    • INUI Ken-ichi
    • Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University

Abstract

  Tacrolimus is a calcineurin inhibitor that has been widely used to prevent allograft rejection after transplantation. We report a case of a living-donor liver transplant recipient experiencing a considerable increase in the trough blood concentration of tacrolimus after concomitant ingestion of grapefruit juice (250 mL) 4 times for 3 days. The trough blood concentrations of tacrolimus were not changed during or immediate after the repeated intake of grapefruit juice. However, almost 1 week after the final ingestion, the blood concentration of tacrolimus markedly increased to as much as 47.4 ng/mL from 4.7 ng/mL before the ingestion, resulting in a profound reduction of calcineurin phosphatase activity in peripheral blood mononuclear cells. Furthermore, headache and nausea, but not nephrotoxicity or hyperglycemia, took place throughout the period of the elevated blood concentrations. Grapefruit juice may have a clinically significant effect on the pharmacokinetics and pharmacodynamics of tacrolimus. It is recommended to avoid the consumption of grapefruit juice in transplant recipients treated with tacrolimus.<br>

Journal

  • Drug Metabolism and Pharmacokinetics

    Drug Metabolism and Pharmacokinetics 21(2), 122-125, 2006-04-27

    The Japanese Society for the Study of Xenobiotics

References:  11

Cited by:  2

Codes

  • NII Article ID (NAID)
    10017423156
  • NII NACSIS-CAT ID (NCID)
    AA1162652X
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    13474367
  • Data Source
    CJP  CJPref  J-STAGE 
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