Immunosuppressants Flashcards
Cyclosporine
MOA: Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.
Use: Transplant rejection prophylaxis, psoriasis, rheumatoid arthritis
Adverse Effects: Nephrotoxicity, hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism.
Tacrolimus (FK506)
MOA: Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T-cell activation by preventing IL-2 transcription.
Use: Transplant rejection prophylaxis.
Adverse Effects: Similar to cyclosporine, ↑ risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism.
Sirolimus (Rapamycin)
MOA: mTOR inhibitor; binds FKBP. Blocks T-cell activation and B-cell differentiation by preventing response to IL-2.
Use: Kidney transplant rejection prophylaxis.
Adverse Effects: Pancytopenia, insulin resistance, hyperlipidemia. NOT nephrotoxic
Daclizumab, basiliximab
MOA: Monoclonal antibodies; block IL-2R.
Use: Kidney transplant rejection prophylaxis.
Adverse Effects: Edema, hypertension, tremor.
Azathioprine
MOA: Antimetabolite precursor of 6-mercaptopurine. Inhibits lymphocyte proliferation by blocking nucleotide synthesis.
Use: Transplant rejection prophylaxis, rheumatoid arthritis, Crohn disease, glomerulonephritis, other autoimmune conditions.
Adverse Effects: Leukopenia, anemia, thrombocytopenia.
Mycophenolate motefil
MOA: Reversibly inhibits IMP dehydrogenase, preventing purine synthesis of B and T cells.
Use: Transplant rejection prophylaxis, lupus nephritis.
Adverse Effects: GI upset, pancytopenia, hyperension, hyperglycemia. Less nephrotoxic and neurotoxic.
Corticosteroids
MOA: Inhibit NF-κB. Suppress both B- and T-cell function by ↓ transcription of many cytokines. Induce apoptosis of T lymphocytes
Use: Transplant rejection prophylaxis, many autoimmune and inflammatory disorders.
Adverse Effects: Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, avascular necrosis (femoral head)
