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Multiple Choice

Which of the following has the strongest effect on statin absorption due to grapefruit juice?

Grapefruit juice contains furanocoumarins that inhibit the intestinal enzyme CYP3A4, which normally metabolizes many statins during absorption. When this enzyme is blocked in the gut, a larger fraction of the statin avoids first-pass metabolism, leading to higher oral bioavailability, higher blood levels, and a greater risk of toxicity such as myopathy. This interaction is especially pronounced for statins that are strong CYP3A4 substrates (like simvastatin and lovastatin), making grapefruit juice the strongest dietary factor affecting their absorption. The other options don’t produce this potent, gut-based CYP3A4 inhibition: apple juice affects CYP2D6 rather than the statin-metabolizing CYP3A4; orange juice does not have the same strong inhibitory effect on CYP3A4; and garlic is not known to cause a meaningful reduction in statin absorption.

Grapefruit juice contains furanocoumarins that inhibit the intestinal enzyme CYP3A4, which normally metabolizes many statins during absorption. When this enzyme is blocked in the gut, a larger fraction of the statin avoids first-pass metabolism, leading to higher oral bioavailability, higher blood levels, and a greater risk of toxicity such as myopathy. This interaction is especially pronounced for statins that are strong CYP3A4 substrates (like simvastatin and lovastatin), making grapefruit juice the strongest dietary factor affecting their absorption. The other options don’t produce this potent, gut-based CYP3A4 inhibition: apple juice affects CYP2D6 rather than the statin-metabolizing CYP3A4; orange juice does not have the same strong inhibitory effect on CYP3A4; and garlic is not known to cause a meaningful reduction in statin absorption.