by Chris Prakash, MD
Question: I take Lipitor for high cholesterol. I have been told by my doctor not to drink grapefruit juice. Can it be that harmful?
Answer: Believe it or not, Your doctor is right! Grapefruit juice sounds very healthy, but can cause severe drug interactions, and can even lead to life threatening consequences. Lipitor is one of major drugs that has adverse effects when combined with grapefruit juice.
The mechanism by which grapefruit juice causes the drug interaction, can be explained by the fact that grapefruit juice is a potent inhibitor of the function of an enzyme called Cytochrome P (CYP3A4). Many medications are metabolized by the CYP 3A4 enzymatic process and it has been shown that grapefruit juice can reduce the intestinal CYP 3A4 function by nearly 50%. The consequence of decreased CYP 3A4 function is that the intestinal absorption of Lipitor may be significantly increased in a person who also drinks grapefruit juice. This leads to increased bioavailability of the drug (higher levels) leading to some of the more serious side effects, such as rhabdomyolysis (muscle damage and pain) and can even lead to kidney failure.
The inhibition of the CYP 3A4 enzyme by grapefruit juice is irreversible. This means that a person who drinks grapefruit juice in the morning, will have interaction with Lipitor even if taken in the evening. In fact the effect of the inhibition of the CYP 3A4 enzyme is felt to be significant for up to 72 hours. So, do not think that you are safe if you drink grapefruit juice in the morning and take lipitor at night.
If you just cannot stay away from grapefruit juice, most experts recommend using an alternative medication in the statin class such as Pravastatin (Pravachol), Rosuvastatin (Crestor) or Fluvastatin (Lescol).
Grapefruit juice can have negative interactions with about 50 different medications. Therefore check the label on your prescription carefully to make sure it does not interact with grapefruit juice. Or, you may just have to find a new favorite juice, as grapefruit juice is the only fruit juice that reacts negatively with medications.
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