Immunosuppressants Flashcards
Cyclosporine
Calcineurin inhibitor that binds cyclophilin. Blocks dephosphorylation of NFAT-P. Without this, no NFAT binding and transcription of IL-2. No T-cell activation
Use for transplant rejection prophylaxis, psoriasis, and RA
Cyclosporine Toxicity
VERY nephrotoxic.
Also can cause HTN, tremor, gingival hyperplasia.
Tacrolimus
Calcineurin Inhibitor that binds FKBP. Prevents NFAT from transcribing IL-2. No T cell activation.
Used to prevent organ transplant rejction
Tacrolimus toxicity
NEPHROTOXIC.
Increased risk of diabetes and neurotoxicity. No gingival hyperplasia.
Sirolimus/rapamycin
Blocks M-TOR which transduces signal of IL2 activation. Prevents T cell activation and B-cell differentiation.
Sirolimus/rapamycin
Blocks M-TOR by binding FKBP which transduces signal of IL2 activation. Prevents T cell activation and B-cell differentiation.
Used for prevention of kidney transplant rejection
Sirolimus toxicity
NOT nephrotoxic, but can cause pancytopenia.
Basiliximab
Monoclonal antibody that blocks IL2R.
Used in kidney transplant rejection prophylaxis.
Basiliximab toxicity
Edema, hypertension, tremor
Azathioprine
Precursor to 6MP. Purine analog that prevents de novo purine synthesis.
Use in transplant rejection, RA, Crohns. Don’t use with allopurinol.
Glucocorticoids
Block NFkB which decreases B and T cell function.
Used to prevent transplant rejection.
Oprelvekin
Recombinant IL11 used in thrombocytopenia.
Alemtuzumab
CD52 MAb used for CLL.
Bevacizumab
VEGF MAb used for colorectal cancer and renal cell carcinoma
Cetuximab
EGFR monoclonal antibody. Stage IV colorectal cancer
