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15 Cards in this Set
- Front
- Back
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Cyclosporine Mechanism
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Binds to cyclophilins.
Cyclophilin + Cyclosporine complex inhibits Calcineurin, thus preventing PRODUCTION of IL-2 and its receptor. IL-2 required for differentiation and activation of T cells -helper and cytotoxic |
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Cyclosporine Clinical Use
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Suppresses organ rejection after transplantation
Selected autoimmune disorders |
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Cyclosporine Toxicity
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Viral illness and lymphoma.
Nephrotoxicity (preventable with mannitol) Gout |
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Tacrolimus Mechanism
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aka FK506
Similar to Cyclosporine (affects IL-2) Binds to FK binding protein, inhibiting secretion of IL-2 and other cytokines. |
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Tacrolimus Clinical Use
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Potent immunosuppressive used in organ transplant rejection (Like cyclosporine, since the mechanisms are similar)
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Tacrolimus Toxicity
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Significant toxicity
Nephrotoxicity - Can be used in kidney transplant, and can also CAUSE nephrotoxicity Peripheral Neuropathy Pleural effusion Hypertension Hyperglycemia N pH pH |
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Sirolimus aka? Mechanism?
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Rapamycin
Inhibits mTOR which inhibits the T-cell proliferation response to IL-2. |
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Sirolimus Clinical use?
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Used SPECIFICALLY in KIDNEY transplant as a combo therapy with cyclosporine and corticosteroids.
Also used with drug-eluting stents. |
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Sirolimus Toxicity?
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Hyperlipidemia
Thrombocytopenia Leukopenia |
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Daclizumab Mechanism
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Monoclonal antibody with a high affinity for the IL-2 receptor on activated T cells.
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Azathioprine Mechanism
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Toxic to proliferating lymphocytes which requires lots of nucleotides (rapidly dividing)
Azathioprine is a precursor of 6-Mercaptopurine which interferes with metabolism and synthesis of nucleic acids. |
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Azathioprine Clinical Use
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Kidney Transplantation
Autoimmune disorders (Including Glomerulonephritis and hemolytic anemia) |
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Azathioprine Toxicity
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Bone marrow suppression
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Azathioprine toxicity is worsened by? Why?
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Allopurinol. Azathioprine metabolite is mercaptopurine which is metabolized by xanthine oxidase.
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Muromonab-CD3 Mechanism?
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Monoclonal murine(mouse) antibody that binds to CD3 (epsilon chain) on surface of T cells thus blocking T cell signal transduction.
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