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Last updated August 20, 2020. 4 minute read

Lipitor and grapefruit: how dangerous is it to mix them?

Past research has warned that eating grapefruit or drinking grapefruit juice and taking statins for high cholesterol may increase your risk for complications such as rhabdomyolysis, the breakdown of muscle tissue that may lead to kidney damage, joint pain, and muscle pain. But some researchers aren’t so sure.

Linnea Zielinski Written by Linnea Zielinski
Reviewed by Dr. Yael Cooperman, MD

Lipitor and grapefruit

While grapefruit has kind of become the poster child when it comes to what you’re not allowed to combine with prescription drugs such as Lipitor (generic name atorvastatin), it turns out it’s not alone in that regard.

Vitals

  • Lipitor is a part of a family of drugs called statins, which help lower “bad” cholesterol by blocking its production.
  • Your body has an enzyme called CYP3A4 that breaks down statins. Grapefruit blocks the action of CYP3A4, resulting in a larger amount of the statin medication entering your bloodstream with every dose.
  • Even one grapefruit or one glass of grapefruit juice can cause this effect.
  • Seville oranges, limes, and pomelos also contain this chemical and should be avoided if you’re taking statins.

Grapefruit gets a bad reputation when it comes to drug interactions because it contains furanocoumarins. This family of chemicals impairs CYP3A4, an enzyme in our body that does a lot of the work breaking down drugs. But here’s the thing: grapefruit isn’t the only fruit that contains furanocoumarins. Other citrus fruits such as Seville oranges (which are often used in marmalades), as well as limes, and pomelos all contain this family of compounds. (In case you’re worried about your breakfast juice of choice, several common sweet orange varieties such as navel and valencia do not contain these compounds, so no worries there.) Grapefruit is simply the most widely studied of these fruits (Bailey, 2013).

What are the risks of mixing grapefruit and statins?

Drugs that are taken orally, like Lipitor, are absorbed into the bloodstream from the gastrointestinal (GI) tract and pass through the liver before being distributed to the rest of the body. During this process, your body uses certain enzymes to break down the drugs. CYP3A4 helps break down the medication in the small intestine, thereby reducing the amount that ever makes it into your blood. But furanocoumarins interfere with this process, which may lead to higher than expected levels of drugs in the body (Fukazawa, 2004).

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Drinking grapefruit juice has been shown in past studies to increase the blood levels of certain medications, including some statins, allergy medications, immunosuppressive drugs, and anti-HIV medications. Statins, also known as HMG-CoA reductase inhibitors, work to lower cholesterol by—as the name suggests—inhibiting HMG-CoA reductase, an enzyme that controls the rate at which cholesterol is made by the body. If there’s a higher concentration of these drugs in your body, they’re able to block more cholesterol from being made. While this has been shown to hold true for simvastatin (FloLipid, Zocor), lovastatin (Altoprev), and atorvastatin (Lipitor), grapefruit juice is not associated with higher blood concentrations of pravastatin (Pravachol), which is why it’s sometimes viewed as the safest statin (Fukazawa, 2004).

Past research has warned that eating grapefruit or drinking grapefruit juice and taking statins for high cholesterol may increase your risk for complications such as rhabdomyolysis, the breakdown of muscle tissue that may lead to kidney damage, joint pain, and muscle pain. But some researchers aren’t so sure. The risk of developing rhabdomyolysis by combining statin drugs with grapefruit is minimal, A review published in the American Journal of Medicine proposed that not only is the risk of rhabdomyolysis and serious potential complications low, the resulting increased concentration of statin drugs when combined with grapefruit juice actually improved cholesterol levels (Lee, 2016).

How much grapefruit is okay when taking statins like Lipitor?

To be on the safe side, many researchers suggest you avoid consuming grapefruit entirely when taking statins such as Lipitor. Although past research has generally required participants to drink almost a liter of grapefruit juice a day to test how it affects liver enzymes that break down drugs, the amount it takes to affect that process appears to be far lower. Some studies have found that the amount of grapefruit that interferes with critical liver enzymes is small: about one whole grapefruit or a 200 mL (slightly under seven ounces) glass of grapefruit juice is enough (Bailey, 2013).

In the end, the consensus currently stands that consumption of 8 oz or less of grapefruit juice per day while taking statins is generally considered to be okay (Reddy, 2011), (UpToDate, 2020). With that being said, the U.S. Food and Drug Administration suggests that you not drink grapefruit juice if you’re taking a statin like Lipitor, reasoning that different people can respond differently to the combination, and instead, consult your healthcare provider to make a decision that is right for you (FDA, 2017).

What are statins, and can some be combined with grapefruit?

Statins are a class of medications that aim to reduce elevated cholesterol levels in people with a high risk of developing cardiovascular disease (also called heart disease), which may contribute to the development of heart attacks and strokes. They’re also called HMG-CoA reductase inhibitors because they lower LDL cholesterol by blocking HMG-CoA reductase, an enzyme that controls the rate at which cholesterol is made by the body. This class of medications includes:

  • atorvastatin (Lipitor)
  • fluvastatin (Lescol, Lescol XL)
  • lovastatin (Altoprev, Mevacor)
  • pitavastatin (Livalo)
  • pravastatin (Pravachol)
  • rosuvastatin (Crestor)
  • simvastatin (Zocor)

There are two types of statin drugs available: those marketed as single-ingredient products, like those listed above, and those that are combined with other medications to help further reduce cholesterol levels. These combined medications include (FDA, 2014):

  • Advicor (lovastatin/niacin extended-release)
  • Simcor (simvastatin/niacin extended-release)
  • Vytorin (simvastatin/ezetimibe)

Essentially, grapefruit increases your risk of experiencing the potential side effects of statins. Those adverse effects may include:

  • Rhabdomyolysis/muscle breakdown
  • Liver damage
  • Increased blood sugar
  • Problems with digestion
  • Joint or muscle pain
  • Neurological effects

If you’re put on any of these statins to improve your heart health, discuss with your prescribing healthcare professional whether grapefruit can be included in your diet.