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17 Cards in this Set
- Front
- Back
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When are immunosuppresants used?
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Immune mediated disease: inappropriate/overzealous immune response
* Ex. IMHA, IMT, Lupus, Pemphigus |
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What types of drugs are considered to be immunosuppresants?
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1. Glucocorticoids
2. Calcineurin inhibitors 3. Antiproliferative (cytotoxic) drugs 4. Antimetabolites |
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How can glucocorticoids function as an immunosuppressive drug?
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They decrease gene expression of genes that affect neutrophil trafficking, suppress macrophage function, and lower lymphocyte activity (esp T-cells)
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How can a calcineurin inhibitor function as an immunosuppressive drug?
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***Inhibit normal T-cell transduction***
* Blocks calcineurin phosphatase activity * Normally, calcineurin dephosphorylates NFAT – allowing it to move to nucleus * NFAT induces cytokine genes s/a IL-2 (T-cell growth and differentiation factor) |
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What are 2 commonly used immunosuppresent calcineurin inhibitors?
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Cyclosporine, Tacrolimus
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What is the adverse effects of Cyclosporine?
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GI effects, Gingival hyperplasia
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What antiproliferative (cytotoxic) drugs act as immunosuppressive drugs? MOA?
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Cyclophosphamide and Chlorambucil
** MOA: Alkylating agents – prevents cell from reproducing |
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What is the major adverse effect of Cyclophosphamide and Chlorambucil (Antiproliferative (cytotoxic) drugs)?
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Bone marrow suppression
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What are the 2 antimetabolite drugs used as immunosuppresive drugs?
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Azathioprine and Mycophenolate
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MOA of Azathioprine
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*Purine analog*
Inhibits purine synthesis leading to decreased lymphocyte proliferation |
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MOA of Mycophenolate
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Inhibits enzyme involved in purine synthesis leading to decreased lymphocyte proliferation
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Adverse effects of Azathioprine
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Bone marrow suppression
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Adverse effects of Mycophenolate
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GI effects
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MOA of Dasprone
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Alters folic acid synthesis, decreases neutrophil chemotaxis, complement activation, antibody production, lysosomal enzyme synthesis
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Adverse Effects of Dasprone
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Hepatotoxicity, hemolytic anemia, thrombocytopenia, neutropenia, GI effects, neuropathies, cutaneous drug eruptions, photosensitivity, carcinogen
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MOA of Methotrexate
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Inhibits folic acid reductase, affecting production of purines and pyrimidines
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Adverse Effects of Methotrexate
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GI effects, listlessness, mucosal sloughing, hematopoietic toxicity, hepatopathy, renal tubular necrosis
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