Grapefruit Juice and Drug Interactions

If you take cholesterol medication, like atorvastatin (Lipitor^®), your doctor probably told you to avoid fried foods, fatty foods, and sugar. Did he or she tell you also to avoid grapefruit and grapefruit juice?

You may be thinking, what? Grapefruit juice? How does that affect my cholesterol? Isn’t grapefruit a healthy citrus fruit – full of vitamin C – that should be part of a balanced diet? 

The reason to avoid grapefruit is not that it is unhealthy. Grapefruit juice interacts with certain medications, which can lead to unwanted consequences. Continue reading to learn all about grapefruit juice and drugs.

How Does Grapefruit Juice Interact with Medications?

Many drugs are processed by an enzyme called cytochrome P450 3A4 (CYP3A4). Grapefruit juice inhibits this enzyme. When the enzyme can’t process the medication as efficiently, the drug levels can build up, causing worsened or more severe side effects. 

If too much atorvastatin or another statin builds up in your body, you can suffer from liver and muscle damage and even kidney failure. 

Because everyone has a different amount of CYP3A4 in their intestines, grapefruit juice may affect people differently. 

What Medications Interact with Grapefruit Juice?

Keep in mind that the extent of the interaction varies by person, medicine, and the amount of grapefruit juice you drink. 

The following drugs can interact with grapefruit juice:

Statins (used to treat high cholesterol):

• Lipitor^® (atorvastatin)
• Zocor® (simvastatin)
• Mevacor® (lovastatin) 

Calcium channel blockers (used to treat high blood pressure)

• Procardia^® (nifedipine)
• Adalat^® CC (nifedipine)
• Plendil^® (felodipine)
• Calan^® (verapamil)

Organ transplant rejection drugs:

• Sandimmune^® (cyclosporine)
• Neoral^® (cyclosporine)
• Prograf^® (tacrolimus)

Psychiatric drugs:

• BuSpar^® (buspirone)
• Valium® (diazepam)
• Desyrel^® (trazodone)
• Sonata^® (zaleplon)

Other drugs:

• Entocort^® EC and Uceris^® (both contain budesonide)
• Pacerone^® (amiodarone): used to treat abnormal heart rhythm
• Allegra® (fexofenadine): over-the-counter (OTC) allergy medicine
• Estrogen, oral contraceptives (birth control pills)

Other drug interactions with grapefruit juice (or other juices) may occur. Consult your healthcare provider to determine if grapefruit juice is safe with all medicines (prescription and OTC) you take. Never stop taking any of your medications without speaking with your healthcare provider first, as it may cause serious harm.

Statins and Grapefruit Juice

Since the topic of grapefruit juice and statins seem to come up quite a bit, let’s dive a little deeper into this interaction by looking at some of the most common statins involved in grapefruit juice interactions.

• Atorvastatin (Lipitor^®): Levels of atorvastatin can increase when you drink an excessive amount (≥ 750 ml to 1.2 liters) of grapefruit juice per day. Atorvastatin levels can also increase (but not as much) when you drink as little as an 8-ounce cup of grapefruit juice daily. The combination of atorvastatin and grapefruit juice can increase the risk of muscle pain, tenderness, and weakness or can even cause liver and kidney problems.
• Simvastatin (Zocor^®): The manufacturer’s information for simvastatin states that you should avoid large quantities (>1 quart daily) of grapefruit juice in combination with simvastatin. The combination can increase the risk of muscle pain and breakdown of muscle tissue. 
• Grapefruit juice also affects lovastatin (Mevacor^®). Grapefruit juice has much less of an effect on pitavastatin (Livalo^®) and pravastatin (Pravachol^®). The rosuvastatin (Crestor®) manufacturer’s information does not mention a grapefruit juice interaction. 
• If you are interested in drinking or eating grapefruit, it’s best to ask your healthcare provider first, who can consider your personal medical history, the dose of medication, and how much grapefruit juice you drink. 

Can I Drink Other Juices with My Medicine?

Although grapefruit juice is known for causing medicine levels to increase, some studies have found the opposite effect on certain drugs. Instead of affecting enzyme CYP3A4, this effect is due to grapefruit juice’s impact on drug transporters. In these instances, less medicine gets into your system, and the medicine may not work as well. 

Shiew-Mei Huang, Ph.D., of the United States Food and Drug Administration (FDA) reports that grapefruit juice can lower levels of the allergy medicine fexofenadine (Allegra®). 
Fexofenadine also should not be taken with orange, grapefruit, or apple juice. Based on 3 clinical studies results, the manufacturer’s information recommends taking fexofenadine with water, not fruit juice. 

In addition, orange juice can lower levels of another beta-blocker called atenolol (Tenormin^®) and the antibiotic ciprofloxacin (Cipro^®). Orange and apple juice can also reduce the effects of the blood pressure medication aliskiren (Tekturna^®). 

Grapefruit juice also lowers levels of the medicine acebutolol, which is a beta-blocker used for high blood pressure, chest pain, and irregular heartbeat. Grapefruit juice also lowers levels of levothyroxine, a thyroid replacement medication. 

How Do I Know if I Should Avoid Grapefruit or Other Fruit Juices with My Medication? 

• Talk to your doctor or pharmacist. Ask if you can drink grapefruit or other fruit juices with your medications.
• If you purchase OTC medicine, read the Drug Facts label to see if it interacts with fruit juices.
• If you take a medicine that is not compatible with grapefruit juice, check the labels of any juices you drink to see if grapefruit juice is an ingredient. 
• If your medicine interacts with grapefruit juice, also avoid Seville oranges, pomelos, and tangelos. These citrus fruits have the same effect on medications as grapefruit juice. 
• Many experts believe that even if grapefruit juice interacts with your medication, it may be safe to drink a small amount. However, it is best to check with your healthcare provider for personalized medical advice because everyone’s body is different and could react differently. 
• If your medicine interacts with grapefruit juice, but you absolutely love all things grapefruit and regularly consume large quantities, ask your healthcare provider if an alternative treatment may be more appropriate for you.  

The Bottom Line

Grapefruit juice, as well as other fruit juices, may affect other medicines you take. Talk to your healthcare provider about all of the medications you take (prescription and OTC) and if fruit juices can affect them.

References:

1. Grapefruit Juice and Some Drugs Don’t Mix. FDA Website. Available at https://www.fda.gov/consumers/consumer-updates/grapefruit-juice-and-some-drugs-dont-mix Accessed September 12, 2020.
2. By the way, doctor: Is it okay to drink grapefruit juice, as long as I don’t take my statin at the same time? Harvard Women’s Health Watch. Available at https://www.health.harvard.edu/newsletter_article/is-it-okay-to-drink-grapefruit-juice-as-long-as-i-dont-take-my-statin-at-the-same-time Accessed September 12, 2020.
3. Allegra Prescribing Information. FDA. Available at https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/020872s018,021963s002lbl.pdf Accessed September 12, 2020. 
4. Lipitor Prescribing Information. FDA Label. Available at https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020702s056lbl.pdf Accessed September 12, 2020.
5. Zocor Prescribing Information. FDA Label. Available at https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019766s085lbl.pdf Accessed September 12, 2020. 
6. Ando H, Tsuruoka S, Yanagihara H, et al. Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin. Br J Clin Pharmacol. 2005;60(5):494-497. DOI:10.1111/j.1365-2125.2005.02462.x
7. Pravachol Prescribing Information. FDA Label. Available at https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019898s062lbl.pdf Accessed September 12, 2020. 
8. Crestor Prescribing Information. FDA Label. Available at https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021366s016lbl.pdf Accessed September 12, 2020. 
9. Bailey DG. Fruit juice inhibition of uptake transport: a new type of food-drug interaction. Br J Clin Pharmacol. 2010;70(5):645-655. DOI:10.1111/j.1365-2125.2010.03722.x
10. Tapaninen T, Neuvonen PJ, Niemi M. Orange and apple juice greatly reduce the plasma concentrations of the OATP2B1 substrate aliskiren. Br J Clin Pharmacol. 2011;71(5):718-726. DOI:10.1111/j.1365-2125.2010.03898.x

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