The Science of Sustainability

Think Before You Drink Grapefruit Juice

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photograph of grapefruit

Image courtesy of dullhunk via Wikimedia Commons

You follow the directions on your medication carefully, always taking the pills with the correct frequency and with or without food as directed. But have you discussed with your doctor or pharmacist whether ingesting grapefruit could cause an unintentional drug overdose?

A drug is normally metabolized in the gastrointestinal tract, but a liver enzyme called cytochrome P450 3A4 (CYP3A4) deactivates much of the drug so the body only absorbs about half of it. This process is taken into account when a doctor prescribes the necessary dose.

However, grapefruit, grapefruit juice, Seville bitter oranges (used in marmalade), limes and pomelos naturally contain chemicals called furanocoumarins. These furanocoumarins inhibit the CYP3A4 enzymes, causing the gut to absorb much more of the drug at a potentially toxic level. Sweet oranges, such as navel or Valencia, do not contain furanocoumarins.

David Bailey, Ph.D., a clinical pharmacologist at the Lawson Health Research Institute, discovered this interaction between grapefruit and some medications over 20 years ago. However, Bailey has recently released an updated list of medications affected by grapefruit in the peer-reviewed Canadian Medical Association Journal. The researchers say the number of drugs that interact with grapefruit has significantly increased to more than 85 as new drugs have come on the market, and 43 of these drugs could interact with grapefruit and lead to serious side effects, such as kidney damage, blood clots, respiratory depression, abnormal rapid heart beats (torsade de pointes) and sudden death.

The researchers provide a list of drugs predicted to interact with grapefruit, including:
Drugs used to treat cancer: crizotinib, dasatinib, erlotinib, everolimus, lapatinib, nilotinib, pazopanib, sunitinib, vandetanib, vemurafenib
Drugs used to treat or prevent infections: erythromycin, halofantrine, maraviroc, primaquine, quinine, rilpivirine
Drugs used to treat high cholesterol: atorvastatin, lovastatin, simvastatin
Drugs used to treat heart and blood vessel conditions: amiodarone, apixaban, clopidogrel, dronedarone, eplerenone, felodipine, nifedipine, quinidine, rivaroxaban, ticagrelor
Drugs affecting the central nervous system: oral alfentanil, buspirone, dextromethorphan, oral fentanyl, oral ketamine, lurasidone, oxycodone, pimozide, quetiapine, triazolam, ziprasidone
Drugs used to treat nausea: domperidone
Drugs used to suppress the immune system: cyclosporine, everolimus, sirolimus, tacrolimus
Drugs used to treat urinary tract conditions: darifenacin, fesoterodine, solifenain, silodosin, tamsulosin

How often such adverse reactions occur is under debate by scientists. Many cases may be missed because doctors don’t think to ask if patients have ingested grapefruit. The level of furanocoumarins in grapefruit also varies for different grapefruit crops or juice batches. The interaction may be affected by the frequency and timing of the citrus consumption. Some people are also more vulnerable to the interactions, depending on the levels of CYP3A4 enzymes normally present in their gut, their age and the medications that they take.

Even if serious reactions are rare, Bailey argues that these incidences are entirely avoidable. People can avoid ingesting the risky citrus or doctors may be able to prescribe an alternate drug. So it is important to carefully read the information leaflet that comes with your medication, as well as discuss with your doctor or pharmacist how your diet may affect your medication.

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Category: Blog, Chemistry, Food, Health

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Jennifer Huber

About the Author ()

Jennifer Huber is a medical imaging scientist at the Lawrence Berkeley National Laboratory with more than 20 years of experience in academic science writing. She received her Ph.D. in Physics from the University of California Santa Barbara. She is also a freelance science writer, editor and blogger, as well as a science-writing instructor for the University of California Berkeley Extension. Jennifer has lived in the San Francisco Bay Area most of her life and she frequently enjoys the eclectic cultural, culinary and outdoor activities available in the area. Read her previous contributions to QUEST, a project dedicated to exploring the Science of Sustainability.
  • http://grapefru.it/drugs/ Nakita Dasilua

    You can have grapefruit with medications but you should space out timing – have the grapefruit then wait a few hours before taking medications. Many people are unaware of the interactions and get repeat prescriptions without their doctors telling them about it. What effect is this having on grapefruit farmers?