Why you should avoid mixing Lipitor and grapefruit

How do statins work? | What happens if you eat grapefruit while on statins? | Which statins are safe with grapefruit? | Can I eat grapefruit in the morning and take Lipitor at night? | Other grapefruit-drug interactions

Statins are a class of drugs used to lower cholesterol levels. They work by inhibiting the enzyme in the liver responsible for making cholesterol, known as HMG-CoA reductase. Statins are some of the most prescribed drugs in the United States, and they’re generally considered safe and effective.

While effective, one potential downside to statin drugs is their ability to interact with grapefruit. Grapefruit contains a chemical called furanocoumarin, which inhibits the enzyme that breaks down statins. This causes an increase in the levels of statins in the blood, which can increase the risk of side effects, most notably muscle problems.

If you’re taking a statin to help lower your cholesterol levels, it’s important to understand the potential grapefruit interaction. Read on to learn more about how statins work, their interaction with grapefruit, and what you can do to avoid problems.

RELATED: Statins: Uses, common brands, and safety info

How do statins work?

When you have high cholesterol, it means there’s too much low-density lipoprotein (LDL) cholesterol (the “bad” cholesterol) in your blood. This leads to a build-up of plaque on the walls of your arteries, which can narrow them and make it difficult for blood to flow through. The plaque build-up also increases your risk of cardiovascular disease, heart attack, stroke, and other health problems.

Statin medications work by inhibiting HMG-CoA reductase, an enzyme in the liver responsible for making cholesterol. In turn, the liver increases LDL receptors, which pull LDL cholesterol out of the bloodstream, and the amount of LDL cholesterol in the blood decreases—reducing plaque build-up in the arteries and lowering the risk of heart disease and other related medical conditions.

RELATED: 4 possible side effects of statins | Do statins and alcohol consumption mix?

What happens if you eat grapefruit while on statins?

Grapefruit is a citrus fruit that’s known for its bitter taste and high levels of vitamin C. As mentioned, it also contains a chemical called furanocoumarin. Furanocoumarin inhibits CYP3A4, the same enzyme that metabolizes statins.

When grapefruit and certain statins are both consumed, the level of statins in the blood can increase. This can increase the likelihood of side effects, such as muscle pain and weakness.

Grapefruit isn’t the only fruit that should be avoided while taking statins. There are several other fruits with high concentrations of furanocoumarin—meaning they too may need to be avoided while taking statins.

Consider avoiding these citrus fruits while taking certain statins:

• Grapefruit
• Bitter oranges
• Pomelos
• Limes
• Seville oranges

Citrus fruits safe to eat while taking statins include:

• Clementine
• Lemons
• Blood oranges
• Navel oranges
• Mandarins
• Tangerines

RELATED: The best diet for heart health

Grapefruit and statins side effects

Eating grapefruit or drinking grapefruit juice while taking certain statins can increase the statin drug level in your blood, which can increase the chance of side effects. The list of potential adverse effects from statins includes:

• Digestive problems
• Nausea and vomiting
• Diarrhea
• Headache
• Dizziness
• Fatigue
• Muscle pain
• Kidney damage
• Liver damage

In rare cases, the interaction between grapefruit and some members of the statin class can be serious, including muscle breakdown (rhabdomyolysis), which can lead to permanent kidney injury or even death. If you experience any of these side effects while taking statins, seek medical help immediately.

RELATED: Lipitor side effects

Which statins are safe with grapefruit?

Some statins are less likely to interact with grapefruit than others, so there are other options for lowering cholesterol levels. If you can’t avoid grapefruit or need a source of vitamin C, ask a healthcare provider about other statins that don’t interact with grapefruit, other ways to lower cholesterol, and vitamin C supplements that are safe to take with statins.

The statins that are the safest to take with grapefruit include:

• Pravachol (pravastatin)
• Crestor (rosuvastatin)
• Lescol (fluvastatin)
• Livalo (pitavastatin)

Related: Atorvastatin vs. simvastatin

Can I eat grapefruit in the morning and take Lipitor (atorvastatin) at night?

Because each person’s body and metabolism are different, it’s difficult to say how much grapefruit is safe while taking statins. In general, experts recommend avoiding grapefruit altogether while taking a statin.

“The greatest hazards may come from consuming grapefruit repeatedly during the day, which can cause a further increase in blood levels of affected drugs,” says Morton Tavel, MD, a retired physician specialist and author of Health Tips, Myths and Tricks: A Physician’s Advice.

According to a 2016 review published in The American Journal of Medicine, a once-daily glass of grapefruit juice raised simvastatin and lovastatin blood levels by about 260% when taken at the same time. When taken 12 hours apart, there was still a significant increase in blood levels—around 90%. Levels of atorvastatin increased by about 80%, regardless of the time taken, in the same study.

Because of this, it’s best to avoid grapefruit or grapefruit juice consumption altogether while taking medications that could react to citrus fruits containing high levels of furanocoumarin, including grapefruit. If you can’t avoid grapefruit, talk to your doctor about other options for lowering your cholesterol. They may suggest another statin that won’t react to grapefruit or other cholesterol-lowering medications, such as Zetia, bile acid sequestrants, fibrates, or PCSK9 inhibitors.

RELATED: 13 things you might not know about Lipitor | Lipitor dosage

Other grapefruit-drug interactions

According to Dr. Tavel, researchers estimate that grapefruit consumption creates a nutrient-drug interaction with more than 85 different medications. This includes drugs used to treat high blood pressure, heart conditions, anxiety, and even some forms of cancer.
According to the U.S. Food and Drug Administration (FDA), other specific grapefruit-drug interactions include:

• High blood pressure medications: Procardia (nifedipine)
• Anti-anxiety drugs: BuSpar (buspirone)
• Corticosteroids: Entocort EC and Uceris (budesonide)
• Antihistamines: Allegra (fexofenadine)
• Organ-transplant rejection drugs: Neoral and Sandimmune (cyclosporine)
• Antiarrhythmic medications: Pacerone and Cordarone (amiodarone)

This is only a partial list, as there are several other drugs that may interact with grapefruit. So, if you’re taking any medications—not just statins—it’s important to seek medical advice from your provider or pharmacist to learn more about your medications and potential adverse effects. Be upfront with your healthcare provider about everything you eat and drink—including grapefruit.

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Sources

• Do your statins and grapefruit safely mix, Cleveland Clinic
• Furanocoumarin, Science Direct
• Types of cholesterol-lowering medicine, Centers for Disease Control and Prevention
• LDL & HDL: Good & bad cholesterol, Centers for Disease Control and Prevention
• Grapefruit juice and statins, Harvard Health
• Grapefruit juice and statins, The American Journal of Medicine
• Grapefruit juice and some drugs don’t mix, FDA