Drug Metabolism and Pharmacokinetics
Online ISSN : 1880-0920
Print ISSN : 1347-4367
Regular Articles
Delayed Effect of Grapefruit Juice on Pharmacokinetics and Pharmacodynamics of Tacrolimus in a Living-Donor Liver Transplant Recipient
Sachio FUKATSUMasahide FUKUDOSatohiro MASUDAIkuko YANOToshiya KATSURAYasuhiro OGURAFumitaka OIKEYasutsugu TAKADAKen-ichi INUI
Author information
JOURNALS FREE ACCESS

2006 Volume 21 Issue 2 Pages 122-125

Details
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.

Information related to the author

This article cannot obtain the latest cited-by information.

© 2006 by The Japanese Society for the Study of Xenobiotics
Previous article Next article
feedback
Top