on 17.3.09 with 0 comments

  • azathioprine

    • has been used for longer than the other antiproliferative agents—40, 50 years

    • mercaptopurine analog; inhibits purine synthesis and decreases cell proliferation

    • formerly used in conjunction with prednisone for solid organ transplants; also used for rheumatoid arthritis

    • no longer a first-line drug for organ transplants

    • major side effect = bone marrow suppression (white cells > red cells > platelets)

  • Mycophenolate mofetil

    • newer drug; is a prodrug

    • metabolized to mycophenolic acid, the active drug

    • inhibits inosine monophosphate dehydrogenase, part of guanine nucleotide synthesis

    • in B and T cells, there is no salvage pathway for guanine nucleotides. this is why mcophenolate mofetil is relatively selective as an immunosuppressive

    • decreases lymphocyte proliferation

    • used to prevent organ transplant rejection in conjunction with glucocorticoids and calcineurin inhibitors

    • cardinal side effects: diarrhea, bone marrow suppression

  • Sirolimus

    • isolated from a handful of dirt from Easter Island

    • binds to FKBP-12; blocks mTOR (mammalian target of rapamycin), a kinase that promotes the cell cycle

    • this blocks the effects of IL-2

    • so you can use it in conjunction with calcineurin inhibitors as a double-whammy against lymphocytes

    • also, spares the side effects of calcineurin inhibitors, including nephrotoxicity

    • cardinal side effect = bone marrow suppression

Category: Medical Subject Notes , Pathology Notes



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