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Immunosuppressants

DrugFamilyMechanismSide Effects
Prednisone - sone / Glucocorticoids / Antagonizes insulin action & promotes gluconeogenesis / Increases muscle catabolism / Augments growth hormone action on lipolysis / Decreases inflammatory response / Reduces cytokine release inhibit NFkB. Binds intracellularly to a Type II glucocorticoid receptor and is transported into the nucleus. The complex binds to a so-called response element (DNA sequence) which up-regulates or down-regulates the transcription / expression of genes. Increased susceptibility to infections / Cushing's Syndrome (moon face) / Myopathy
Cyclosporine A Calcineurin inhibitors / Inhibitors of T-cell mediated immunity Inhibition of T-lymphocyte activation, thus reduced IL-2 production. / Extensively metabolized by CYP450 3A / Interacts with drugs that also use CYP450 3A. Including Grapefruit juice TDM needed because of high potential for nephrotoxicity
Tacrolimus Calcineurin inhibitors / Tacrolimus more potent than cyclosporine A Inhibition of T-lymphocyte activation, thus reduced IL-2 production. / Extensively metabolized by CYP450 3A / Interacts with drugs that also use CYP450 3A. Including Grapefruit juice TDM needed because of high potential for nephrotoxicity
Sirolimus Antiproliferatives / Anti-metabolites / Lymphocyte signaling inhibitor / Prophylaxis in organ transplantation Blocks IL-2 receptor signaling and arrests cell division by blocking kinase mTOR. Prevents IL-2 mediated signal transduction to cell nucleus. / Extensively metabolized by CYP450 3A not nephrotoxic / lung toxicity (interstitial pneumonitis)
Azathioprine Antiproliferatives / Anti-metabolites / Purine antimetabolite that inhibits proliferation of T cells and B cells. rapidly, non enzymatically cleaved into 6-mercaptopurine (6-MP) which acts as a purine analogue (adenine & guanine) causing inhibition of DNA synthesis (false nucleotide incorporation) and thus inhibition of proliferation of T cells and B cells. myelosuppression (bone marrow suppression) causing anemia and/or increased susceptibility to infection / nausea, vomiting
Methotrexate Antiproliferatives / Anti-metabolites / Competitive analog of folate Inhibits the metabolism of folate by inhibiting dihydrofolate reductase, blocking purine biosynthesis and leading to accumulation of adenosine and inhibition of T cell activation. Hepatotoxicty, anemia, azotemia / Penicillin may increase elimination.
Mycophenolic Acid Antiproliferatives / Anti-metabolites / Inhibits the de novo synthesis of lymphocyte purine nucleotides prevents production of guanosine nucleotides required for DNA synthesis thus, it prevents the proliferation of T-cells, lymphocytes, and the formation of antibodies from B-cells; it also may inhibit recruitment of leukocytes to inflammatory sites high blood sugars, increased blood cholesterol levels
Muromonab-CD3 (OKT3) Biologics / Biological modifiers / Mouse monoclonal antibody against the human CD3 receptor, a membrane protein on the surface of T cells Prevents T cell activation and proliferation by binding the T cell receptor complex present on all differentiated T cells (causing apoptosis) Cytokine release syndrome / Repeated administration can cause tachyphylaxis / Not approved for prophylaxis
Anti-thymocyte Globulin (ATG) Biologics / Biological modifiers / polyclonal antibodies (derived from rabbit or horse) against human T-cells (CDs) cytokine release syndrome
Daclizumab Biologics / Biological modifiers / humanized anti-CD25 (anti-IL-2α) mouse monoclonal antibody bind to IL-2α receptor on activated T-cells and block IL-2 mediated T-cell activation / expansion of activated lymphocytes and shortening their survival
Basiliximab Biologics / Biological modifiers / humanized anti-CD25 (anti-IL-2α) mouse monoclonal antibody bind to IL-2α receptor on activated T-cells and block IL-2 mediated T-cell activation / expansion of activated lymphocytes and shortening their survival
Created by: carchase