Grapefruit interaction
- Grapefruit inhibits intestinal CYP3A
- Oral CYP3A substrates can show higher exposure
- Effect can persist after the juice is gone
- Furanocoumarins—not acidity—drive interaction
- Magnitude depends on intestinal first-pass dependence
Interaction at a glance
- Grapefruit inhibits intestinal CYP3A
Magnitude / time course
- Grapefruit inhibits intestinal CYP3A
- Oral CYP3A substrates can show higher exposure
Mechanism
- Effect can persist after the juice is gone
- Furanocoumarins—not acidity—drive interaction
Mechanism / modifiers
- Magnitude depends on intestinal first-pass dependence
Self-check
- What determines grapefruit interaction magnitude?
Intestinal first-pass dependence. - Which grapefruit constituents drive the interaction?
Furanocoumarins, not acidity.
Drugs in this interaction (17)
All interaction examples · Open Grapefruit interaction in the interactive console ↗