David Cohen, M.D.·Published 12 March 2012·9 min read
Key points
Grapefruit is a wonderfully healthy food, providing people with a rich source of vitamin C.
Buspirone (BuSpar) interacts with GRAPEFRUIT Grapefruit juice might increase how much buspirone (BuSpar) the body absorbs.
Grapefruit juice might increase how much carbamazepine (Tegretol) the body absorbs.
The body breaks down carvedilol (Coreg) to get rid of it.
Grapefruit is a wonderfully healthy food, providing people with a rich source of vitamin C. However, compounds found in this fruit that can lead to potentially serious outcomes.
A recent consumer update press release from the FDA warns that compounds found in fresh grapefruit and grapefruit juice can act on an enzyme found in the intestines. This enzyme is an integral part of drug metabolism and can lead to potentially hazardous effects when combined with certain pharmaceutical and over-the-counter drugs..
If this enzyme cannot do its job properly, taking certain drugs can lead to toxicity because too much of the drug will enter the body.
The compounds in question are two chemicals in the class called furanocoumarins. One is the compound bergamottin, the other is a related compound called dihydroxybergamottin. These compounds prevent an enzyme called CYP3A4 from performing its proper function in digestion.
One of the jobs of CYP3A4 is to help the body process certain drugs. If the grapefruit compounds interfere with its ability to do its job, some of drugs you may be taking will not be broken down at the usual rate.
When manufacturers set the amounts of drug dosages, they are taking into account what CYP3A4 will be doing. If CYP3A4 is not working right, it may be possible for the person to end up with toxic levels of the drugs in their blood stream.
Grapefruit Juice and Medication Can Be a Dangerous Mix Grapefruit juice can be dangerous for people on certain medications, nurse researchers remind doctors, nurses, and everyone who takes medicine and enjoys grapefruit juice, in a paper in the American Journal of Nursing, a journal of the American Nurses Association.
Amy Karch, R.N., M.S., of the School of Nursing at the University of Rochester Medical Center reported on a man from a northern climate who moved to Florida for the winter – one of tens of thousands of “snowbirds” who head south each winter – and began drinking two to three glasses of grapefruit juice each day. The man became critically ill as a result of an interaction between grapefruit juice and his cholesterol-lowering medication.
Karch’s paper, “The Grapefruit Challenge: The juice inhibits a crucial enzyme, with possibly fatal consequences,” appears in the December 2004 issue of the journal.
Interactions between grapefruit juice and medications have long been recognized. Last year, the Medical Letter on Drugs and Therapeutics devoted an entire issue to grapefruit juice and the dangerous drug interactions that can result. The U.S. Food & Drug Administration requires all prospective new drugs that are thought to interact with this enzyme system to be tested for interactions with grapefruit juice. And a warning about grapefruit juice is included in the “food-drug interactions” that come with dozens of medications. Nevertheless, Karch says many health-care professionals and patients don’t know about the risk.
Written and revised by
David Cohen, M.D.
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“The potential of drug interactions with grapefruit juice has been out there a long time, but most people just aren’t aware of it,” says Karch, a clinical associate professor of nursing. “There is so much information bombarding people all the time, that a lot of people may have heard this but forgotten it. But the problems can be life-threatening.”
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University of Rochester Medical Center
According to the FDA press release, drugs metabolized by CYP3A4 include statin cholesterol medications, such as Zocor (simvastatin), Lipitor (atorvastatin) and Pravachol (pravastatin).
Breast cancer: There is concern about the safety of drinking excessive amounts of grapefruit juice. Some research suggests that postmenopausal women who consume a quart or more of grapefruit juice every day have a 25% to 30% increased chance of developing breast cancer. Grapefruit juice decreases how estrogen is broken down in the body and might increase estrogen levels in the body. More research is needed to confirm these findings. Until more is known, avoid drinking excessive amounts of grapefruit juice, especially if you have breast cancer or are at higher than usual risk for developing breast cancer.
Also on this list are some blood pressure medications, such as Nifediac and Afeditab (both nifedipine) and some immune-suppressant medications, such as Sandimmune and Neoral (both cyclosporine).
Anti-anxiety medications, such as BuSpar (buspirone), and some anti-arrhythmia medications, such as Cordarone and Nexterone (both amiodarone) are also have risk for interference from the grapefruit compounds.
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Although these are not all the drugs that could be affected, they are some of the more common ones that could cause problems if taken with grapefruit. The chemical bergamottin from grapefruit can cause another problem in the small intestines if a person is taking certain drugs. It can prevent transporter proteins from carrying certain medications through the body.
If these proteins can’t do their job, neither can the drugs that are transported by them. An example of a medicine that is transported by these proteins is Fexofenadine (Allegra), which is a common allergy medicine.
Drugs that Interact with Grapefruit Juice:
(from the December 2004 issue of the American Journal of Nursing)
Buspirone (BuSpar) interacts with GRAPEFRUIT Grapefruit juice might increase how much buspirone (BuSpar) the body absorbs. Drinking grapefruit juice while taking buspirone (BuSpar) might increase the effects and side effects of buspirone (BuSpar).
Carbamazepine (Tegretol) interacts with GRAPEFRUIT
Grapefruit juice might increase how much carbamazepine (Tegretol) the body absorbs. Drinking grapefruit juice while taking carbamazepine (Tegretol) might increase the effects and side effects of carbamazepine (Tegretol).
Carvedilol (Coreg) interacts with GRAPEFRUIT
The body breaks down carvedilol (Coreg) to get rid of it. Grapefruit juice seems to decrease how quickly the body breaks down carvedilol (Coreg). Drinking grapefruit juice while taking carvedilol (Coreg) might increase the effects and side effects of carvedilol (Coreg).
Cisapride (Propulsid) interacts with GRAPEFRUIT
Grapefruit juice might decrease how quickly the body gets rid of cisapride (Propulsid). Drinking grapefruit juice while taking cisapride (Propulsid) might increase the effects and side effects of cisapride (Propulsid).
Clomipramine (Anafranil) interacts with GRAPEFRUIT
The body breaks down clomipramine (Anafranil) to get rid of it. Grapefruit juice might decrease how quickly the body gets rid of clomipramine (Anafranil). Taking grapefruit juice along with clomipramine (Anafranil) might increase the effects and side effects of clomipramine (Anafranil).
Cyclosporine (Neoral, Sandimmune) interacts with GRAPEFRUIT
Grapefruit might increase how much cyclosporine (Neoral, Sandimmune) the body absorbs. Drinking grapefruit juice while taking cyclosporine (Neoral, Sandimmune) might increase the side effects of cyclosporine.
Dextromethorphan (Robitussin DM, and others) interacts with GRAPEFRUIT
The body breaks down dextromethorphan (Robitussin DM, others) to get rid of it. Grapefruit might decrease how quickly the body breaks down dextromethorphan (Robitussin DM, others). Drinking grapefruit juice while taking dextromethorphan (Robitussin DM, others) might increase the effects and side effects of dextromethorphan (Robitussin DM, others).
Estrogens interacts with GRAPEFRUIT
The body breaks down estrogens to get rid of them. Grapefruit juice seems to decrease how quickly the body breaks down estrogens and increase how much estrogen the body absorbs. Drinking grapefruit juice while taking estrogens might increase estrogen levels and side effects associated with estrogen such as breast cancer.
Some estrogen pills include conjugated equine estrogens (Premarin), ethinyl estradiol, estradiol (Climara, Vivelle, Estring), and others.
Etoposide (VePesid) interacts with GRAPEFRUIT
Grapefruit might decrease how much etoposide (VePesid) the body absorbs. Drinking grapefruit juice while taking etoposide (VePesid) might decrease the effectiveness of etoposide (VePesid).
Itraconazole (Sporanox) interacts with GRAPEFRUIT
Itraconazole (Sporanox) is used to treat fungal infections. Grapefruit juice might decrease how much itraconazole (Sporanox) the body absorbs. Drinking grapefruit juice while taking itraconazole (Sporanox) might decrease the effectiveness of Itraconazole (Sporanox). Do not drink grapefruit juice if you are taking Itraconazole (Sporanox).
Medications changed by the liver (Cytochrome P450 3A4 (CYP3A4) substrates) interacts with GRAPEFRUIT Some medications are changed and broken down by the liver.
Grapefruit juice might decrease how quickly the liver breaks down some medications. Drinking grapefruit juice while taking some medications that are broken down by the liver can increase the effects and side effects of some medications. Before taking grapefruit, talk to your healthcare provider if you are taking any medications that are changed by the liver.
Some medications changed by the liver include lovastatin (Mevacor), ketoconazole (Nizoral), itraconazole (Sporanox), fexofenadine (Allegra), triazolam (Halcion), and many others.
Medications for high blood pressure (Calcium channel blockers) interacts with GRAPEFRUIT
Grapefruit juice might increase how much medication for high blood pressure the body absorbs. Drinking grapefruit juice while taking some medications for high blood pressure might cause your blood pressure to go too low.
Some medications for high blood pressure include nifedipine (Adalat, Procardia), verapamil (Calan, Isoptin, Verelan), diltiazem (Cardizem), isradipine (DynaCirc), felodipine (Plendil), amlodipine (Norvasc), and others.
Medications used for lowering cholesterol (Statins) interacts with GRAPEFRUIT
The body breaks down some medications used for lowering cholesterol to get rid of them. Grapefruit juice might decrease how quickly the body breaks down some medications used for lowering cholesterol. Drinking grapefruit juice while taking some medications used for lowering cholesterol might increase the effects and side effects of these medications.
Some medications used for high cholesterol include lovastatin (Mevacor), simvastatin (Zocor), atorvastatin (Lipitor), cerivastatin (Baycol), and others.
However, grapefruit juice doesn't seem to affect pravastatin (Pravachol).
Methylprednisolone interacts with GRAPEFRUIT
The body breaks down methylprednisolone to get rid of it. Grapefruit juice can decrease how quickly the body gets rid of methylprednisolone. Drinking grapefruit juice while taking methylprednisolone might increase the effects and side effects of methylprednisolone.
Praziquantel (Biltricide) interacts with GRAPEFRUIT
The body breaks down praziquantel (Biltricide) to get rid of it. Grapefruit juice can decrease how quickly the body breaks down praziquantel (Biltricide). Drinking grapefruit juice while taking praziquantel (Biltricide) might increase the effects and side effects of praziquantel (Biltricide).
Quinidine interacts with GRAPEFRUIT
The body breaks down quinidine to get rid of it. Grapefruit juice might decrease how fast the body gets rid of quinidine. Drinking grapefruit juice while taking quinidine might increase the chance of side effects.
Scopolamine (Transderm Scop) interacts with GRAPEFRUIT
The body breaks down scopolamine to get rid of it. Grapefruit juice can decrease how fast the body breaks down scopolamine. Drinking grapefruit juice while taking scopolamine might increase the effects and side effects of scopolamine.
Sedative medications (Benzodiazepines) interacts with GRAPEFRUIT
Sedative medications can cause sleepiness and drowsiness. Grapefruit juice can decrease how quickly the body breaks down some medications. Drinking grapefruit juice while taking some sedative medications can increase the effects and side effects of some sedative medications.
Some sedative medications that might interact with grapefruit juice include clonazepam (Klonopin), diazepam (Valium), lorazepam (Ativan), and others.
Sildenafil (Viagra) interacts with GRAPEFRUIT
The body breaks down sildenafil (Viagra) to get rid of it. Grapefruit can decrease how quickly the body breaks down sildenafil (Viagra). Drinking grapefruit juice while taking sildenafil (Viagra) can increase the effects and side effects of sildenafil.
Terfenadine (Seldane) interacts with GRAPEFRUIT
Grapefruit can increase how much terfenadine (Seldane) that the body absorbs. Drinking grapefruit juice while taking terfenadine (Seldane) might increase the effects and side effects of terfenadine (Seldane).
This information comes from a press release by the FDA, published in February of 2012.