2 minute read
Central Research
Food and drug interactions. Statins and grapefruit juice
Having a high level of low-density lipoprotein cholesterol (LDL-C) can be dangerous to our health, contributing to the development of atherosclerosis (hardening of the arteries due to accumulation of fats, cholesterol, among other substances) and increasing the risk of coronary heart disease. Statins (for example, atorvastatin, lovastatin and simvastatin) are mainly used to regulate the level of LDL-C, being the most prescribed drugs in the world for this purpose.
Statins act as inhibitors of the activity of the enzyme HMG-CoA reductase, which contributes to the synthesis of cholesterol; in response to this enzyme inhibition, the formation of LDL cholesterol is regulated between 20% and 63%. These drugs are then metabolized or degraded in the intestines and liver via the cytochrome P450 (CYP) pathway.
Particularly atorvastatin, lovastatin and simvastatin are degraded by the cytochrome enzyme CYP3A4, thus reducing the amount of drug entering the bloodstream. This process of statin degradation may be slowed if grapefruit-based foods or beverages are consumed during treatment. Grapefruit has different components, among them are furanocoumarins, such as bergamotin (BGT) and 6,7-dihydroxybergamotine (DHB), these are also metabolized by CYP3A4 and the resulting compounds bind to the active site of this enzyme (CYP3A4), causing its inactivation.
This blockade in the enzymatic activity of CYP3A4 means that statins cannot be adequately degraded and accumulate in the body, which can trigger liver damage, kidney failure and increase the adverse effects caused by statins. Currently, more than 85 drugs are predicted to interact with grapefruit, increasing the systemic concentration of the drug in the body. Recovery of CYP3A4 activity may take from 24 hours to 3 days and will depend on the type and dose of statin; large amounts of grapefruit juice consumption can inhibit hepatic CYP3A4 leading to worse adverse effects.
As a recommendation, ask your trusted doctor what foods or beverages may interfere with your medication in a similar way to grapefruit juice.
Claudia MejIa Morales, PhD
Research and Development Analyst at Drox Health Science.
References
FDA (2021). Grapefruit Juice and Some Drugs Don’t Mix. Retrieved from: https://www.fda.gov/consumers/consumer-updates/grapefruit-juice-and-some-drugs-dontmix#:~:text=Many%20drugs%20are%20broken%20down,much%20drug%20in%20your%20body
Turner, R. M., & Pirmohamed, M. (2019). Statin-related myotoxicity: a comprehensive review of pharmacokinetic, pharmacogenomic and muscle components. Journal of Clinical Medicine, 9(1), 22.
