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 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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