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ALL / Pharmacology
Tacrolimus
Tacrolimus
Tacrolimus is a calcineurin inhibitor used as an immunosuppressant to prevent transplant rejection. It has a very similar action to ciclosporin.Mechanism of action
- decreases clonal proliferation of T cells by reducing IL-2 release
- binds to FKBP forming a complex which inhibits calcineurin, a phosphotase that activates various transcription factors in T cells
- this contrasts with ciclosporin, which binds to cyclophilin rather than FKBP
Adverse effects
- nephrotoxicity (impaired renal function, raised creatinine) – dose-related and very common
- neurotoxicity (tremor, headache, paraesthesia, seizures in severe cases)
- hypertension
- hyperglycaemia / diabetes mellitus (post-transplant diabetes)
- hyperkalaemia
Tacrolimus is more potent than ciclosporin and hence the incidence of organ rejection is less. However, nephrotoxicity and impaired glucose tolerance is more common.
+PassMedicine Notes
Tacrolimus is a calcineurin inhibitor used as an immunosuppressant to prevent transplant rejection. It has a very similar action to ciclosporin.
Mechanism of action- decreases clonal proliferation of T cells by reducing IL-2 release
- binds to FKBP forming a complex which inhibits calcineurin, a phosphotase that activates various transcription factors in T cells
- this contrasts with ciclosporin, which binds to cyclophilin rather than FKBP
- nephrotoxicity (impaired renal function, raised creatinine) – dose-related and very common
- neurotoxicity (tremor, headache, paraesthesia, seizures in severe cases)
- hypertension
- hyperglycaemia / diabetes mellitus (post-transplant diabetes)
- hyperkalaemia
Tacrolimus is more potent than ciclosporin and hence the incidence of organ rejection is less. However, nephrotoxicity and impaired glucose tolerance is more common.
