Why Grapefruit and Statin Drugs Do Not Mix

If you have been prescribed a statin drug to treat high cholesterol, your healthcare provider or pharmacist may have advised you to avoid grapefruit or grapefruit juice while on treatment. While that may sound oddly specific, there is a good reason why you want to steer clear of this particular fruit. Not only can grapefruit alter the level of medication in your blood, but it can also increase the risk of side effects, some of which may be serious. There are other types of drugs that may be affected by grapefruit, too.

Grapefruit image
Arda Mutlu / EyeEm / Getty Images

The Concern

Statin drugs, also known as HMG-CoA reductase inhibitors, work by blocking the enzyme that your body needs to produce cholesterol. In addition to lowering "bad" LDL cholesterol and raising "good" HDL cholesterol, statin drugs can also decrease the level of triglycerides circulating in your blood.

The interaction is caused by an organic compound in grapefruit known as furanocoumarin. Furanocoumarins are found in other fruits and vegetables (such as celery, parsnips, and pomegranates), but are especially high in grapefruit and grapefruit juice.

The problem with furanocoumarins is that they deactivate an enzyme in the liver and intestines known as cytochrome P4503A4 (CYP3A4), which the body uses to break down certain drugs so that they can be excreted from the body. When this happens, the drug concentration can increase dramatically and, with it, the risk of side effects.

Of the seven statins approved for use in the United States, the drugs most affected by the consumption of grapefruit are:

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

Risks

The abnormal accumulation of atorvastatin, lovastatin, or simvastatin in the blood can lead to a rare but potentially serious side effect called rhabdomyolysis, a breakdown of muscle tissue that can lead to kidney failure and death

Other statin drugs remain largely unaffected by the consumption of grapefruit. These include:

  • Crestor (rosuvastatin)
  • Lesco (fluvastatin)
  • Pravachol (pravastatin)

This is because the two drugs are broken down by an entirely different enzyme known as CYP2C9. Pravastatin is metabolized by yet a different mechanism.

Safety and Considerations

There is a popular assumption that grapefruit may be safe if eaten before or after a dose of Lipitor, Mevacor, or Zocor. At present, no one really knows where the "safe" line is.

What is known is that statin drug levels can increase by anywhere from 80 percent to 260 percent if the medication is taken at the same time as grapefruit. If taken 12 hours apart, that drops to between 44 percent and 66 percent. The effect remains the same whether you cook the grapefruit or drink frozen or homogenized juice.

How this translates to the "safe" consumption of grapefruit remains unclear. Most healthcare providers will tell you that an occasional serving of juice or fruit will do you no harm. Most evidence suggests that serious problems are more likely to occur if you consume large quantities over an extended period of time.

Limit your consumption of grapefruit or switch to "safe" citrus fruits, such as blood oranges, clementines, lemons, limes, mandarins, navel oranges, and tangerines. Bitter oranges, pomelos, tangelos, and Seville oranges contain high levels of furanocoumarin and should also be avoided.

Other Drugs

Other drugs are equally affected by grapefruit and grapefruit juice. In some cases, the fruit can block enzymatic action and increase the concentration of the drug. In others, it can interfere with protein transporters in the blood, reducing the concentration and effect of the drug.

These include:

  • Certain anti-arrhythmia drugs, like amiodarone
  • Certain anti-anxiety drugs, like buspirone
  • Some antihistamines, like Allegra (fexofenadine)
  • Certain corticosteroids, like budesonide
  • Some hypertension medications, like nifedipine
  • Some organ transplant rejection drugs, like cyclosporine

Speak with your healthcare provider or pharmacist if you regularly consume grapefruit to ensure that it doesn't interfere with your medications.

A Word From Verywell

If you truly love grapefruit and can't do without it, ask your healthcare provider about switching to another statin or lowering your dose. If you consume grapefruit every now or then, it is unlikely to do any real harm. What is most important is that you avoid the regular consumption or overconsumption of furanocoumarin in any form. Switch to oranges or other safe fruits and save grapefruit for special occasions.

Frequently Asked Questions

  • Why should you avoid grapefruit when taking a statin?

    Grapefruit contains a compound known as furanocoumarin, which deactivates an enzyme that breaks down certain drugs, including statins. As a result, the drug concentration increases dramatically. This can cause a rare but serious condition that causes breakdown of muscle tissue and can lead to kidney failure.

  • What drugs interact with grapefruit?

    Grapefruit and grapefruit juice can negatively interact with medications in several different classes. However, not all drugs in each class of medications are affected. Some of the drugs that interact with grapefruit include: 

    • Allegra (fexofenadine), an allergy medication
    • Amiodarone, a heart arrhythmia drug sold under the brand names Pacerone and Cordarone 
    • Budesonide, a corticosteroid sold under the brand names Entocord EC and Uceris 
    • Buspar (buspirone), an anti-anxiety medication 
    • Cyclosporine, an organ-transplant anti-rejection drug sold under the brand Ames Neural and Sandimmune 
    • Lipitor (atorvastatin), a statin
    • Nifedipine, a high-blood-pressure medication sold under the brand names Procardia and Adalat CC
    • Zocor (simvastatin), a statin

    If you are uncertain whether or not you can eat grapefruit with a medication you are currently taking, read the label that came with the medication or talk to your pharmacist.

  • Which statins are safe to take with grapefruit?

    Some statins are less affected by grapefruit than others. Statins that are safe to take with grapefruit include: 

    • Crestor (rosuvastatin)
    • Lescol (fluvastatin)
    • Livalo (pitavastatin)
    • Pravachol (pravastatin)
6 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. Hung WL, Suh JH, Wang Y. Chemistry and health effects of furanocoumarins in grapefruit. J Food Drug Anal. 2017;25(1):71-83. doi:+10.1016/j.jfda.2016.11.008

  2. Mcdonnell AM, Dang CH. Basic review of the cytochrome p450 system. J Adv Pract Oncol. 2013;4(4):263-8. doi:10.6004/jadpro.2013.4.4.7

  3. Lee JW, Morris JK, Wald NJ. Grapefruit Juice and Statins. Am J Med. 2016;129(1):26-9. doi:10.1016/j.amjmed.2015.07.036

  4. Cleveland Clinic. Do your statins and grapefruit safely mix?

  5. US Food & Drug Administration. Grapefruit juice and some drugs don't mix.

  6. Harvard Health Letter. Grapefruit juice and statins.

Additional Reading

By Jennifer Moll, PharmD
Jennifer Moll, MS, PharmD, is a pharmacist actively involved in educating patients about the importance of heart disease prevention.