furanocoumarin
7 interactions related to furanocoumarin
pomelo + tacrolimus
Pomelo contains furanocoumarins that inhibit intestinal CYP3A4 and P-glycoprotein, the two systems that limit tacrolimus absorption. A documented case in a renal transplant patient showed pomelo consumption nearly doubled tacrolimus blood levels, risking nephrotoxicity and neurotoxicity given tacrolimus's narrow therapeutic window.
seville orange + atorvastatin
Seville (bitter) orange contains the same furanocoumarins as grapefruit, including bergamottin and 6',7'-dihydroxybergamottin, which irreversibly inhibit intestinal CYP3A4. A landmark crossover study showed Seville orange juice raised felodipine AUC by 76%, comparable to grapefruit, and atorvastatin shares the same CYP3A4 metabolic pathway, raising the risk of statin-induced myopathy.
seville orange + cyclosporine
Seville orange juice contains furanocoumarins that reduce enterocyte CYP3A4 expression by approximately 40%, although a controlled human study found no significant change in cyclosporine AUC, likely because cyclosporine disposition also depends on intestinal P-glycoprotein, which Seville orange does not inhibit as strongly as grapefruit.
blood orange + simvastatin
Blood orange (Citrus sinensis var.) is a sweet orange and does not contain the furanocoumarins (bergamottin, 6',7'-dihydroxybergamottin) that drive the grapefruit-statin interaction. Published reviews of citrus furanocoumarin content list blood orange among the sweet oranges as essentially free of clinically significant CYP3A4-inhibiting compounds.
bergamot + statins
Bergamot orange (Citrus bergamia) is the source of bergamottin, the prototype furanocoumarin that irreversibly inhibits CYP3A4. Bergamot juice and high-dose bergamot polyphenol supplements (BPF), often marketed for cholesterol, can theoretically raise levels of CYP3A4-metabolized statins (simvastatin, atorvastatin, lovastatin), though human pharmacokinetic data with statins are limited.
pomelo + simvastatin
Pomelo (Citrus maxima) contains furanocoumarins that irreversibly inhibit intestinal CYP3A4, the enzyme that metabolizes simvastatin during first-pass absorption. With CYP3A4 disabled, simvastatin plasma concentrations rise substantially, increasing the risk of myopathy and rhabdomyolysis.
alprazolam + grapefruit
Grapefruit juice contains furanocoumarins that inhibit intestinal CYP3A4, the enzyme that partially metabolizes alprazolam. The interaction can raise alprazolam blood levels and prolong sedation, although the magnitude is modest compared to other benzodiazepines because alprazolam has high oral bioavailability.