statin interactions
8 interactions related to statin interactions
pravastatin + grapefruit
Unlike simvastatin, lovastatin, and atorvastatin, pravastatin is not significantly metabolized by CYP3A4, so grapefruit juice does not meaningfully change its plasma exposure. Clinical pharmacokinetic studies show no significant effect of grapefruit juice on pravastatin disposition.
rosuvastatin + berberine
Rosuvastatin is taken into liver cells by the OATP1B1 transporter, and berberine has been shown to upregulate OATP1B1 in hepatocyte studies, increasing hepatic uptake of rosuvastatin. The clinical net effect (more LDL lowering vs. higher muscle/liver risk) is not well established in humans.
lovastatin + grapefruit
Grapefruit juice blocks intestinal CYP3A4, dramatically increasing lovastatin and lovastatin acid exposure. A controlled study showed lovastatin Cmax rose ~12-fold and AUC ~15-fold after high-dose grapefruit juice, sharply raising the risk of myopathy and rhabdomyolysis.
atorvastatin + vitamin d
Vitamin D's active metabolite (calcitriol) can induce CYP3A4, which metabolizes atorvastatin. Small studies show vitamin D supplementation may reduce atorvastatin and metabolite plasma levels by up to ~55%, although LDL-lowering efficacy appears largely preserved.
simvastatin + berberine
Simvastatin is extensively metabolized by CYP3A4, and berberine inhibits CYP3A4 in vitro, which can raise simvastatin levels and increase the risk of myopathy and rhabdomyolysis. The interaction is bidirectional in some models (induction is also possible), making net effect unpredictable.
simvastatin + st. john's wort
St. John's wort induces intestinal and hepatic CYP3A4 and P-glycoprotein, sharply increasing simvastatin's first-pass metabolism. In a crossover study of healthy adults, the AUC of active simvastatin hydroxy acid was cut roughly in half (to about 48% of placebo).
atorvastatin + st. john's wort
St. John's wort potently induces hepatic and intestinal CYP3A4, accelerating atorvastatin's first-pass metabolism. A controlled study showed roughly a 12% drop in atorvastatin AUC and meaningful increases in LDL and total cholesterol over 4 weeks of co-administration.
atorvastatin + berberine
Berberine inhibits CYP3A4 in vitro and can raise plasma levels of CYP3A4 substrates, including atorvastatin, which may increase the risk of muscle pain, liver enzyme elevation, and rhabdomyolysis. The interaction direction is complex — some animal data also show induction — but co-use is unpredictable.