furanocoumarin
8 interactions related to furanocoumarin
seville orange + red yeast rice
Seville orange contains furanocoumarins that inhibit intestinal CYP3A4, the enzyme that clears the monacolin K in red yeast rice. Because monacolin K is chemically identical to the statin lovastatin and depends on CYP3A4 for its first-pass breakdown, blocking that enzyme raises systemic exposure to the active statin, increasing the risk of muscle-related side effects such as myopathy and, rarely, rhabdomyolysis.
pomelo + red yeast rice
Pomelo, like grapefruit, contains furanocoumarins that inhibit the intestinal CYP3A4 enzyme. Red yeast rice's active constituent, monacolin K, is chemically identical to the statin lovastatin, which depends on CYP3A4 for its breakdown. When pomelo blocks that enzyme, more of the monacolin K reaches the bloodstream, amplifying the dose-dependent statin-type risks of muscle injury and, rarely, liver enzyme elevation. Because furanocoumarin inhibition can persist for days, the effect is not reliably avoided by taking the two at different times of day.
pomelo + tacrolimus
Pomelo contains furanocoumarins that inhibit intestinal CYP3A4 and P-glycoprotein, the systems that limit how much tacrolimus is absorbed. A documented case in a renal transplant patient showed pomelo consumption raised tacrolimus blood levels, and tacrolimus has a narrow therapeutic window where small swings can cause kidney or nervous-system toxicity, or under-immunosuppression and rejection.
seville orange + atorvastatin
Seville (bitter) orange contains the same furanocoumarins as grapefruit, including bergamottin and 6',7'-dihydroxybergamottin, which inactivate intestinal CYP3A4. A randomized crossover study showed Seville orange juice raised levels of the CYP3A4 drug felodipine to a degree comparable with grapefruit juice, while ordinary sweet orange juice had no effect. Because atorvastatin is metabolised by the same CYP3A4 pathway, Seville orange can raise atorvastatin levels and increase the risk of statin-related muscle injury.
seville orange + cyclosporine
Seville orange (bitter orange, Citrus aurantium) contains furanocoumarins that inhibit intestinal CYP3A4, the enzyme that breaks down cyclosporine in the gut wall. Unlike grapefruit, however, a controlled human study found that Seville orange juice did not meaningfully raise cyclosporine blood levels, because cyclosporine absorption also depends on intestinal P-glycoprotein, which Seville orange spares. Most transplant teams still advise avoiding bitter orange products as a precaution given variable furanocoumarin content and the high stakes of altered immunosuppressant levels.
blood orange + simvastatin
Blood orange (Citrus sinensis var.) is a sweet orange and does not contain the furanocoumarins (such as bergamottin and 6',7'-dihydroxybergamottin) that drive the grapefruit-statin interaction. Reviews of citrus furanocoumarin content place blood orange among the sweet oranges that are essentially free of clinically significant CYP3A4-inhibiting compounds, so it is not expected to meaningfully affect simvastatin levels.
bergamot + statins
Bergamot orange (Citrus bergamia) is the source of bergamottin, the prototype furanocoumarin that inactivates CYP3A4. Bergamot juice and concentrated bergamot polyphenol supplements (often marketed for cholesterol) could in theory raise levels of CYP3A4-metabolized statins (simvastatin, atorvastatin, lovastatin). The mechanism is well established in the lab and in animals, but no direct human pharmacokinetic studies of bergamot with statins exist, so the real-world magnitude is uncertain.
pomelo + simvastatin
Pomelo (Citrus maxima) contains furanocoumarins that inhibit intestinal CYP3A4, the enzyme that breaks down simvastatin during first-pass absorption. With that enzyme suppressed, more simvastatin reaches the bloodstream, raising the risk of muscle-related side effects. This is the same mechanism behind the well-established grapefruit-simvastatin interaction, since pomelo is the parent species of grapefruit and shares its furanocoumarins.