Immunosuppressants Drug Introduction Immunosuppressants medications can be broken down into the following categories corticosteroids calcineurin Inhibitors monoclonals antimetabolites others Immunosuppressants Drug Table Corticosteroids Name Mechanism of Action Key Indication Key Toxicity Prednisone Glucocorticoid receptor agonist Phospholipase A2 inhibitor → ↓ COX expression NFκB inhibitor Adrenal insuffiency Asthma Autoimmune disease to achieve immunosuppression Organ transplantation Certain hematologic cancers Drug-induced Cushing-like symptoms Hyperglycemia Osteoporosis Mood alterations Calcineurin Inhibitors Name Mechanism of Action Key Indication Key Toxicity Cyclosporine Calcineurin inhibitor via cyclosporine-cyclophilin complex Organ transplantation Certain autoimmune diseases Nephrotoxicity Neurotoxicity Hypertension Gingival hyperplasia Hirsutism FK506 (tacrolimus) Calcineurin inhibitor via FK506 immunophilin Prophylaxis for organ transplant rejection Nephrotoxicity Neurotoxicity Hypertension Monoclonals Name Mechanism of Action Key Indication Key Toxicity OKT3 (muromonab) CD3 receptor monoclonal antibody Allograft rejection Pyrexia Diarrhea Basiliximab CD25 subunit of IL-2 receptor antibody Renal transplant rejection Hypertension Edema Hypercholesterolemia Hyperglycemia Hyperuricemia Hypophosphatemia Antimetabolites Name Mechanism of Action Key Indication Key Toxicity Azathioprine Precursor to 6-mercaptopurine leads to inhibition of lymphocytic proliferation perhaps by inhibiting nucleotide synthesis Transplant rejection prophylaxis Autoimmune diseases Pancytopenia Increased toxicity when used with allopurinol Mycophenolic acid Inosine monophosphate dehydrogenase inhibitor Cytostatic effect on lymphocytes lymphocytes do not have enzymes involved in salvage pathway, and thus why they are preferentially affected Transplant rejection GI distrubances Pancytopenia CMV infection Less nephro- and neurotoxic Others Name Mechanism of Action Key Indication Key Toxicity Rapamune (sirolimus) mTOR inhibitor via sirolimus-FK506 complex Impairs lymphocyte response to IL-2 activation Kidney transplant prophylaxis Pancytopenia Insulin resistance Hyperlipidemia