Grapefruit has what effect on certain statins?

Grapefruit has what effect on certain statins?

• A. Decreases absorption of statins
• B. Has no effect on statins
• C. Blocks an intestinal enzyme, increasing absorption of certain statins
• D. Increases hepatic clearance of statins

Answer: (C)

Grapefruit juice blocks an intestinal enzyme, specifically CYP3A4, that normally metabolizes several statins as they are absorbed from the gut. By inhibiting this enzyme in the intestine, grapefruit reduces first-pass metabolism and increases the drug’s bioavailability, leading to higher plasma levels. This heightened exposure raises the risk of muscle-related side effects with these statins. Other statins that aren’t primarily metabolized by intestinal CYP3A4 aren’t affected as much.

Grapefruit juice blocks an intestinal enzyme, specifically CYP3A4, that normally metabolizes several statins as they are absorbed from the gut. By inhibiting this enzyme in the intestine, grapefruit reduces first-pass metabolism and increases the drug’s bioavailability, leading to higher plasma levels. This heightened exposure raises the risk of muscle-related side effects with these statins. Other statins that aren’t primarily metabolized by intestinal CYP3A4 aren’t affected as much.