The authors also note that a standard serving of grapefruit juice, taken at the same time as simvastatin, increases the effective dose of the drug 3.6-fold this increase would be 1.9-fold were the grapefruit product consumed 12 hours earlier. 2 They note that a meta-analysis 3 in 2003 estimated that 40 mg of simvastatin reduces low-density lipoprotein (LDL) cholesterol by 37%, but double this dosage and LDL drops by 43%. 2ĭespite the fact that the studies examining possible cause-and-effect relationships between statins and muscle necrosis were characterized by large doses of grapefruit juice, 2 a universal prohibition followed nonetheless: No grapefruits or grapefruit juice for users of atorvastatin, simvastatin, or lovastatin!įast-forward to 2016, where a Top Paper by Lee, Morris, and Wald reframes the grapefruit-statin interaction. 2 Drinking grapefruit juice with lovastatin, simvastatin, or atorvastatin also may induce rhabdomyolysis, a complication related to statin use in certain individuals (incidence of 4 per 100,000 person-years with these 3 statins). 2 Taking atorvastatin with grapefruit juice, for example, increases this statin’s blood level 1.8 times. Furanocoumarins in grapefruit juice inactivate CYP3A4, the enzyme responsible for metabolizing lovastatin, simvastatin, and atorvastatin (but not fluvastatin, rosuvastatin, or pravastatin). Later, grapefruit products were found to increase levels of many other drugs, including statins. Felodipine concentrations in the patients’ blood increased. In an experiment designed to determine the effect of ethanol on felodipine levels, 1 researchers used grapefruit juice to mask the taste of alcohol.
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