CYP metabolism (high first-pass)
- Large fraction is metabolized before systemic entry
- Oral bioavailability may be low/variable
- Enzyme inhibition can sharply raise oral exposure
- Route changes can bypass much first-pass loss
- Gut and hepatic CYP3A are common contributors
Interaction at a glance
- Large fraction is metabolized before systemic entry
Mechanism
- Large fraction is metabolized before systemic entry
- Oral bioavailability may be low/variable
Magnitude / time course
- Enzyme inhibition can sharply raise oral exposure
- Gut and hepatic CYP3A are common contributors
Mechanism / modifiers
- Route changes can bypass much first-pass loss
Self-check
- How can enzyme inhibition affect high-first-pass oral drugs?
Sharply raise exposure. - What can bypass much first-pass loss?
A change in route.
Drugs in this interaction (10)
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