British journal of clinical pharmacology
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Br J Clin Pharmacol · Jun 2013
Randomized Controlled TrialGrapefruit juice markedly increases the plasma concentrations and antiplatelet effects of ticagrelor in healthy subjects.
This study examined the effects of grapefruit juice on the new P2Y12 inhibitor ticagrelor, which is a substrate of CYP3A4 and P-glycoprotein. ⋯ Grapefruit juice increased ticagrelor exposure by more than two-fold, leading to an enhanced and prolonged ticagrelor antiplatelet effect. The grapefruit juice-ticagrelor interaction seems clinically important and indicates the significance of intestinal metabolism to ticagrelor pharmacokinetics.