Lipitor and Grapefruit Juice: Much has been written about the interaction of grapefruit juice and large number of medications. Lipitor is among the most frequently mentioned of the medications where grapefruit juice can significantly impact the bioavailability of a medication. The mechanism of action of grapefruit juice in altering medication bioavailability lies in the fact that grapefruit juice is a moderately potent inhibitor of intestinal CYP3A4 function. 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 three A4 function is that the intestinal absorption of Lipitor may be significantly increased in a person who also drinks grapefruit juice. The inhibition of the CYP 3A4 enzyme by grapefruit juice is irreversible. This means that a person who drinks grapefruit juice in the morning can have significant increase in the absorption of the Lipitor they take an evening. The effect of the inhibition of the CYP 3A4 enzyme is felt to be significant for up to 72 hours.

Lipitor is among the most popular medications used in America and Lipitor side effects may be significantly increased in people who use Lipitor and grapefruit juice together. Unfortunately the predictability of the Lipitor and grapefruit juice interaction is not enough to allow physicians to prescribe lower doses of Lipitor along with grapefruit juice to get predictable results. Most experts recommend using an alternative medication the statin class such as pravastatin or Crestor, but simvastatin also has a similar interaction with alcohol making it a poor choice as a substitute for Lipitor and grapefruit juice.

This whole Lipitor grapefruit juice interaction and the CYP 3A4 enzyme inhibition by grapefruit juice is widely misunderstood. This information has been given to patients suggesting that as long as they take the Lipitor in the evening and don’t drink grapefruit juice other than the morning they should be okay. The irreversible nature of the CYP 3A4 inhibition by grapefruit juice makes this not the case.

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