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Why might grapefruit juice affect how Lipitor works? Grapefruit juice inhibits an enzyme called CYP3A4 in the small intestine. This enzyme normally breaks down atorvastatin, the active ingredient in Lipitor. When it is inhibited, more of the drug stays in the body, raising blood levels and increasing the chance of side effects. What happens if you drink grapefruit juice regularly with Lipitor? Regular consumption can lead to higher atorvastatin exposure. This increases the risk of muscle pain, weakness, or rhabdomyolysis, a rare but serious condition where muscle tissue breaks down and releases proteins into the blood that can damage the kidneys. Studies show levels of atorvastatin may rise up to threefold when combined with grapefruit juice. When does the risk become significant? The risk grows with the amount and timing of grapefruit juice consumed. Drinking more than 1.2 liters daily or drinking it within hours of taking Lipitor increases exposure. One study found that even a single glass can elevate blood levels of the drug for up to 72 hours because the enzyme inhibition lasts that lang.
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