Interaction of Statins with Grapefruit Juice

Abstract

Grapefruit juice, which discovered to interact with felodipine for the first time, is now known to interact with more that 80 drugs. Statins are among the drugs that interact with grapefruit juice. Grapefruit juice-statin interactions were first investigated in 1998 in human pharmacokinetic studies with lovastatin and simvastatin. The pharmacokinetic and pharmacodynamic basis of the interaction has been extensively investigated in studies. Flavonoids and furanocoumarins, the main components of grapefruit juice, have been reported to cause drug interactions. Furthermore, statin-grapefruit juice interactions occur mostly through inhibition of cytochrome-3A4 (CYP3A4), to a lesser extent through inhibition of P-glycoprotein (P-gp) and organic anion transporting polypeptides (OATPs). Changes in plasma drug levels as a result of interaction may increase the side-effect of statins or reduce their therapeutic efficacy. Therefore, patients using statins are generally advised to avoid grapefruit juice consumption.