Immunosuppressants
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| Complications of immunosuppressive therapy ? | * Suppression of immune system .... (lead to infections such as CMV)
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| Major classes of immunosuppressive agent classes ? | * Glucocorticoids -- Calcineurin inhibitors -- Cytotoxic agents -- Biologics
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| Glucocorticoids = ? | * Prednisone -- methylprednisolone -- dexamethasone
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| Gluco. Uses ? | * Prevent rejection - best if given at time of transplant ..... * high doses treat Acute Rejection phases ..... * helps supress/lower GVHD
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| Gluco. MOA ? | * Inhibits innate and acquired immunity by inhibiting T cell proliferation
and inhibits IL-2 production (which increase T-cells)
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| Gluco. SEs ? | * Steroid Man
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| Calcineurin inhibitors (antibiotics)= ? | * Cyclosporine and Tacrolimus
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| Cyclosporine use ? | * prophylaxis only - not effective in ongoing rejection
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| Cyclosporine MOA ? | * Binds to cyclophilin --> Cyclosporin-cyclophilin complex binds calcineurin --> prevents IL-2 from being activated (no T-cells)
.... * Prevents transcription factors from being made to activate IL-2
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| Cyclosporine pharmokinetics ? | * Narrow TI ….. Need enough dose to prevent rejection, but have to monitor as to not get toxicity
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| Cyclosporine SEs ? | * typical stuff and weird ones --> hirsutism and gingival bleeding ..... * Highly Nephrotoxic (give to prevent rejection, yet it is damaging to an organ you are trying to help) .... * Hyperkalemia - due to decreased K excretion
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| Tacrolimus MOA and SEs ? | * Similar MoA and Use as cyclosporine except binds FKBP rather than cyclophilin....
* No side effects like cyclosporine
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| Antiproliferative Agent - Sirolimus use and MOA ? | * USE: prophylaxis (usually in combo) -
+ calcineurin inhibitor + glucocorticoid ...... * Binds to FKBP like tacrolimus but Does NOT block IL-2 production, the Sirolimus-FKBP complex binds to mTOR which blocks kinases needed for genes
binds mTOR
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| MOA basics ? | * Interrupts T-cell activation downstream of IL-2 receptor
--> Inhibits proliferation bc stops cell proliferation at G1-S phase
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| Sirolimus SEs ? | * hyperlipidemia and myelosuppression --> (thrombocytopenia, anemia, leukopenia)
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| Antiproliferative - Azathioprine uses ? | * Prodrug converted to mercaptopurine..... * Primary cytotoxic agent used for immunosuppression to prevent and maintain transplant.... * CAN use in ongoing Rejection
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| Azathioprine MOA ? | * the active metabolite (6-MP) Interferes with purine nucleotide de novo synthesis --> inhibits DNA synthesis ..... acts just like the anti-cancer antimetab purine drugs by (-) TMP/IMP synthesis needed for G and A synthesis
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| Azathioprine pharmokinetics ? | * Metabolized (cleared) by the enzyme xanthine oxidase..... * So Azathioprine dose reduction required when allopurinol is being used
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| Azathioprine SEs ? | * bone marrow suppression -- leukopenia (most common)
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| Immunosupressant - Mycophenolate mofetil MOA and USE? | * Selective, noncompetitive inhibitor of IMPDH
--> Stops IMP from being made --> no pureines made ..... * Used w/ glucocorticoid + calcineurin inhibitor
--- Has mostly replaced azathioprine for maintenance immunosuppression
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| Methotrexate use ? | * Used extensively to treat GVHD
and Rheumatoid arthritis
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| Immunosuppressive Antibodies purpose ? | * lower/impair T-Cells, while keeping humoral immunity intact
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| Immunosuppressive Antibody ALG when to use ? | * is a Polyclonal anti-lymphocyte .... * Major use in kidney transplants after transplant .... *
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| ATG ? | * Polyclonal anti-thymocyte also.... *Used during acute rejection episodes...... * also be used in immunosuppression like ALG
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| ALG & ATG summary ? | * Used to treat donor BM prior to transplantation to destroy T cells to avoid GVHD
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| ALG AND ATG SEs ? | * allergic type reactions from body recognizing foreign particles and mounting a response to them
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| Muromonab-CD3 (OKT3) MOA? | * Directed against CD3 on surface of human thymocytes & mature T-cells
......... * Shuts down activation of T-cell proliferation
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| Muromonab-CD3 (OKT3) uses and SEs ? | * USES: -
Treat acute rejection episodes in combination with other drugs ---
Deplete donor BM of T-cells prior to BM transplant ...... * not really used anymore bc SEs...... * SEs: fever, chills,and Cytokine Storm ... * body can develop ABs to it also
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| Daclizumab & Basiliximab MOA ? | * Monoclonal antibodies to part of IL-2 receptor (CD25) … IL-2 antagonist ...... * prevents IL-2 from binding to lymphocytes...... ---- * Daclizumab – humanized IgG1
---- Basiliximab – chimeric mouse-human IgG1
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| Daclizumab & Basiliximab use ? | * Can use long term ..... * Primarily used for prophylaxis against acute rejection of renal transplants in combination with cyclosporine and corticosteroids
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| For a renal graft rejection, what Treatment (frequency of use) is most commonly used ? | * High dose corticosteroid pulse (76%)
- 1st line therapy in most centers
...... * Anti T-cell antibody therapy --
Thymoglobulin (ALG AND ATG)(28%)
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| GVHD Prophylaxis ? | * Methotrexate + cyclosporine and deplete T-Cells
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