Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike
F, Takada Y, Inui K.Delayed effect of grapefruit juice on
pharmacokinetics and pharmacodynamics of Tacrolimus (FK506) in a
living-donor liver transplant recipient.
Drug Metab Pharmacokinet. 2006 Apr;21(2):122-5.
Department of Pharmacy, Kyoto University Hospital, Faculty of
Medicine, Kyoto University, Japan.
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.
PMID: 16702731
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