10/19/2023 0 Comments Statins and grapefruit cyp3a4![]() Grapefruit juice enhances the efficacy of certain statins by raising blood levels in so doing, it reduces LDL levels further and, as a result, reduces the risk of ischemic heart disease more.4 Comparing 2 doses of simvastatin, 40 and 20 mg, demonstrated that the rate of muscle injury with higher doses of statin was unlikely to be greater than 1 or 2 per 100,000 person-years. What about the potential negative corollary, rhabdomyolysis? A recent study enrolling 313,552 simvastatin users identified 29 individuals who developed rhabdomyolysis. ![]() 2 Using these calculations, and knowing that 10 mg of simvastatin reduces the ischemic heart disease risk by 61%, the authors conclude that adding grapefruit juice 12 hours before dosing would further reduce risk by 66%. 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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