CYP metabolism (autoinhibition)
- Drug inhibits an enzyme involved in its own clearance
- Exposure can rise nonlinearly as dose/time increase
- Steady state may be less predictable
- Other inhibitors can magnify the effect
- Dose proportionality may fail
Interaction at a glance
- Drug inhibits an enzyme involved in its own clearance
Magnitude / time course
- Drug inhibits an enzyme involved in its own clearance
Mechanism
- Steady state may be less predictable
- Other inhibitors can magnify the effect
Management
- Exposure can rise nonlinearly as dose/time increase
- Dose proportionality may fail
Self-check
- Can autoinhibition make steady state less predictable?
Yes. - How can exposure change during autoinhibition as dose/time increases?
Rise nonlinearly.
Drugs in this interaction (3)
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