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Statins and grapefruit cyp3a411/27/2023 ![]() through over-exposure to CYP3A4 substrates.ĬYPs Clementine Drug transporters Grapefruit HPLC-DAD-ESI-MS-MS Mandarin.Ĭopyright © 2016 Elsevier B.V. Our data indicate that clementine juice similar to grapefruit juice bears the potential for profound interactions with drugs potentially leading to adverse drug effects e.g. Taken together, our data indicate that clementine juice as well as grapefruit juice and to a lesser extent also mandarin juice can induce several important drug metabolising enzymes and drug transporters, but also inhibit some of these proteins. Apparently, grapefruits specifically a bioactive compound within the fruit called furanocoumarin are inhibitors of CYP3A4. Thus, inhibition of CYP3A4 is presumably the underlying reason for the observed increase in the concentrations of the CYP3A4 substrate tacrolimus in the patient. For example, concurrent grapefruit juice (a CYP3A4 inhibitor) increased the mean area under the concentrationtime curve (AUC024) of atorvastatin by 83. This interaction enhances systemic drug concentration through impaired drug metabolism. 1 3 Currently, more than 85 drugs, most of which are available in Canada, are known or predicted to interact with grapefruit. Even one glass of grapefruit juice, taken daily, considerably increases the plasma concentrations of simvastatin and simvastatin acid. ![]() Using an enzymatic activity assay, we demonstrated that at least in vitro CYP3A4 inhibition prevails for both grapefruit and clementine juice, whereas for CYP1A2 induction appears to predominate. Our research group discovered the interaction between grapefruit and certain medications more than 20 years ago. CYP3A4, raising the question which effect prevails in vivo. 156-fold and 34-fold induction of cytochrome P450 (CYP) 3A4 mRNA by grapefruit juice and clementine juice, respectively). All citrus juices profoundly induced several drug transporters and drug metabolising enzymes, whereas the effects of grapefruit juice were most pronounced (e.g. We observed substantially increased tacrolimus trough concentrations in a renal transplant patient consuming high clementine amounts and, thus, scrutinised the effects of clementine juice on drug metabolism and drug transporters in vitro and compared it to the effects of mandarin and grapefruit juice. ![]() Similar issues have not been reported for clementines and available data is scarce, despite of genetic descent. Adverse drug interactions due to grapefruit juice are well known prompting warnings even in drug labels. ![]()
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