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B&L: Immunosuppressants by Mind Map: B&L: Immunosuppressants
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B&L: Immunosuppressants

Glucocorticoids: Prednisone


Prevention and treat of rejection and GVHD

DOC: autoimmune Dz


wipes out entire immune system; decreases all lymphocyte & cytokine levels

inhib IL-2 production -> inhib T-cell proliferation

Side effects

Thinning of skin/purpura

Cushing-like syndrome


GI, Gastritis, peptic ulcers, bleeding

Fluid retention, d/t electrolyte imbalances, Usually only a problem for pts w/ previous heart and kidney Dz


Amenorrheoa; infertility


Muscle weakness, weakness in extremities d/t catabolism of skeletal muscle


Psychiatric, depression, panic attacks, Phobias


Hyperglycemia, leads to Diabetes

Increases susceptibility to infxn

Calcineurin Inhibitors


Uses, Prevention only!!!

MOA, Binds cyclophilin, Drug-cyclophilin complex bind calcineurin, Inhibits IL-2 & IL-2 dependent T-cell proliferation

PK, Narrow TI, Eliminated by CYP3A4, D-D interaxn: azoles and erythromycin inhib CYP3A4

Side Effects, Nephrotoxicity, Must distinguish btwn tox and kidney transplant rejection! Biopsy only definitive Dx test., Neuro and hepatic tox, Gingival hyperplasia, Hirsutism, Hyperkalemia!, DON'T give with ACEi!!! They decrease aldosterone release


MOA, Similar to cyclo except Tacro-FKBP complex binds calcineurin

Side Effects, Similar to cyclo, NO hirsutism or gingival hyperplasia!!!

Antiproliferative Agents (Anti-cancer drugs)


Use, Prophylaxis (in combo) only!!, + Calc inh + steroid

MOA, Binds FKBP (like Tacro), but..., Siro-FKBP complex binds mTOR down stream of calcineurin (i.e. DOESN'T block IL-2 production, Inhibits cell proliferation

Side effects, Hyperlipidemia, Profound BMD, NO RENAL TOX!!!

PK, Metabolized in liver by CYP3A4


MOA, Prodrug, purine antimetabolite, Interferes w/ purine necleotide de novo synthesis -> inhib DNA synthesis, Cytotoxic to proliferating cells, esp. T-cells

PK, Inactivated by xanthine oxidase, reduce dose when allopurinol is being used

Side effects, BMD

Mycophenolate mofetil

MOA, Selective non-competative inhibitor of IMPDH (needed for de novo G synthesis, Used in combo: MM + Calc inh + steroid

SE, BMD; but less than with azathioprine


Use, GVHD, RA, Psoriasis


Always used in combo, usually in acute transplant rejection episodes


Use, Kidney transplants

MOA, polyclonal anti-lymphocyte globulin

Use and SE: same as ATF


Use, Used to Tx donor BM prior to transplant to destroy T-cells and avoid GVHD, SE: alleric rxns; eventually body with reject Ab as foreign, Acute rejection episodes

MOA, polyclonal anti-thymocyte globulin

Muromonab (OKT3)

MOA, T-cell specific murine monoclonal Ab, Directed against CD3 thymocytes and T-cells, Shuts down activation of T-cell prolif and impairs CD8 function

Use, Acute rejection episodes, Tx donor BM to prevent GVHD

SE, Cytokine storm! Usually w/ 1st doses, Body will make Ab against OKT3. Only get one shot w/ this one!


MOA, Ab to CD25 receptor on IL-2; acts as IL-2 antagonist, No t-cell depletion

Use, Prophylaxis and Tx of AREs

SE, Allergic Sx and infxn