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Pharmacology · Drug interactions: CYP3A4 and food
Sample itemA hypertensive patient on stable felodipine begins drinking a large glass of grapefruit juice every morning and develops flushing, ankle oedema and a low blood pressure. What is the mechanism?
Original practice item, not a recalled exam question. Nothing here is recorded.
The answer and the reasoning
A. Inhibition of intestinal CYP3A4, raising oral bioavailability
Furanocoumarins in grapefruit juice irreversibly inhibit CYP3A4 in the gut wall, reducing first-pass metabolism. Bioavailability of drugs such as felodipine rises and produces exaggerated vasodilatation. The effect lasts for a day or more because new enzyme must be synthesised.
Option by option
A. Inhibition of intestinal CYP3A4, raising oral bioavailability (correct)
Correct. Reduced gut-wall metabolism increases systemic exposure to felodipine.
B. Induction of hepatic CYP2D6, increasing drug activation
Felodipine is inactivated, not activated, by CYP3A4, and grapefruit inhibits rather than induces.
C. Displacement of felodipine from plasma albumin
Albumin displacement is not the cause, and would only transiently raise free drug.
D. Reduced tubular secretion of felodipine in the kidney
Felodipine is eliminated by hepatic metabolism, not by tubular secretion.
Source note: Original NextPrep sample item — pending expert review. This item is original practice material awaiting independent expert review, so confirm important facts in a standard textbook.
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