Immunosuppressants (calcineurin inhibitors / CNIs)
- Tacrolimus/cyclosporine block calcineurin
- ↓ T-cell IL-2 transcription
- Core transplant immunosuppression
- Nephrotoxicity + hypertension are major limits
- Narrow therapeutic index → TDM
- CYP3A/P-gp DDIs can be dramatic
Class at a glance
- Tacrolimus/cyclosporine block calcineurin
Pharmacology
- CYP3A/P-gp DDIs can be dramatic
Practical pearls
- ↓ T-cell IL-2 transcription
- Narrow therapeutic index → TDM
Safety / monitoring
- Core transplant immunosuppression
- Nephrotoxicity + hypertension are major limits
Self-check
- What monitoring does the narrow therapeutic index of calcineurin inhibitors require?
Therapeutic drug monitoring (TDM). - What major toxicities limit calcineurin inhibitors?
Nephrotoxicity and hypertension.
Drugs in this class (4)
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