Immunosuppressants Flashcards
Immunosuppressants that Block T-cell activation by preventing IL-2 transcription
Cyclosporine and Tacrolimus
Calcinuerin inhibitor that bind FK506
Tacrolimus
Calcinuerin inhibitor that binds cyclophilin
Cyclosporine
mTOR inhibitor that binds FKBP
Sirolimus (Rapamycin)
Immunosuppresant that blocks T-cell activation and differentiation of B-cells by preventing response to IL-2
Sirolimus (Rapamycin)
Sirolimus (Rapamycin) mechanism
Blocks T-cell activation and B-cell differentiation by preventing response to IL-2
Tacrolimus mechanism
Calcineurin inhibitor that binds FK506 preventing IL-2 transcription which blocks T-cell activation
Cyclosporine mechanism
Calcineurin inhibitor that binds cyclophilin preventing IL-2 transcription which blocks T-cell activation
Nephrotoxic immunosuppressant
Both calcineurin inhibitors are nephrotoxic but cyclosporine > tacrolimus
Tacrolimus inhibits what
Calcineurin
Cyclosporine inhibits what
Calcinuerin
Sirolimus (Rapamycin) inhibits what
mTOR
Sirolimus
mTOR inhibitor that binds FKBP preventing IL-2 response and blocking T-cell activation and B-cell differentiation
Indications for Sirolimus (Rapamycin)
Kidney transplant rejection prophylaxis
Immunosuppressant given to synergistically with cyclosporine
Sirolimus (Rapamycin)
Immunosuppressant used in drug-eluding stents
Sirolimus (Rapamycin)
Immunosuppresant that spares the kidney
Sirolimus (Rapamycin)
Other indications for cyclosporine
Psoriasis, rheumatoid arthritis
Toxicities associated with cyclosporine
Nephrotoxicity, hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism
Toxicities associated with tacrolimus
Increased risk of diabetes and neurotoxicity; NO gingival hyperplasia or hirsutism