Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression¶
Lown. (1997). Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. Journal of Clinical Investigation.
Cited by¶
1 citation across 1 artifact.
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Domain-specific¶
- Enzyme Inhibition
- Because first-pass metabolism of felodipine is thereby destroyed, its oral exposure (AUC) climbs roughly two- to threefold at an unchanged dose.
This sourceThe study shows grapefruit juice cut intestinal CYP3A4 by 62% and raised felodipine AUC roughly two- to threefold at the same 10-mg dose; it does not show first-pass metabolism destroyed, since liver CYP3A4 was unchanged.
Supported in partVerified against the work's full text
“the concentration of CYP3A4 in small bowel epithelia (enterocytes) fell 62%”
- Because first-pass metabolism of felodipine is thereby destroyed, its oral exposure (AUC) climbs roughly two- to threefold at an unchanged dose.
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