Tacrolimus + CYP3A inducer/inhibitor
- Tacrolimus = very sensitive CYP3A/P-gp victim
- Inhibitors can raise exposure several-fold
- azoles/macrolides; ritonavir can be extreme
- Inducers can collapse levels → rejection
- Use trough-guided dosing after every change
Interaction at a glance
- Inhibitors can raise exposure several-fold
- azoles/macrolides; ritonavir can be extreme
Mechanism
- Tacrolimus = very sensitive CYP3A/P-gp victim
Magnitude / time course
- Inhibitors can raise exposure several-fold
- azoles/macrolides; ritonavir can be extreme
- Inducers can collapse levels → rejection
Mechanism / modifiers
- Use trough-guided dosing after every change
Self-check
- Which pathways make tacrolimus highly interaction-sensitive?
CYP3A and P-gp.
- How should tacrolimus dosing be managed after interacting-drug changes?
Use trough-guided dosing.
Drugs in this interaction (42)
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