1. corticosteroids (Medrol)
    • MOA: lymphocyte sequestration, diminished lymphocyte proliferation, reduced macrophage activity (MHCII, IL-2), lipocortin (annexin) production (phosphlipase A2)
    • stabilize lysosome
    • diminished expression of COX-II
    • Indications: multiple inflammatory or oncology
    • Infections, water retention, hypokalemia, long-term adverse effects
  2. cyclosprin A
    • MAO: binds to immunophilin(cyclophilin), decrease IL-2, IL-3, INF-y
    • Indications: allogeneic transplants, RA, severe recalcitrant psoriasis, dry eye syndrome(keratoconjunctivitis sicca)
    • CYP3A in liver, grape fruit, nephrotoxicity, hepatic toxicity
  3. tacrolimus (FK506)
    • macrolide
    • MAO: binds to immunophilin(FKBP-12), decrease IL-2, INF-y
    • Indications: allogeneic liver, kidney, heart transplants, atopic dermatitis (eczema)
    • CYP3A
  4. pimecrolimus
    • macrolide
    • MAO: binds to FKBP-12, calcineurin decrease IL-2, IFN-y from TH1, IL-4, IL-10 from TH2), prevents mast cell degranulation
    • Indications: atopic dermatitis(eczema)
    • Twice daily, lack of safety, contact doctor after 6 weeks, not for immunocompromised patients
  5. sirolimus
    • rapamycin
    • macrolide
    • MAO: binds to mTOR (regulatory kinase)
    • Indications: renal transplants, drug-eluting coronary stents for re-stenosis, psoriasis
    • CYP3A4, not for liver-HAT(hepatic artery thrombosis), not for lung-dehiscence
  6. everolimus
    • macrolide
    • MAO: binds to mTOR (regulatory kinase)
    • Indications: advanced renal cell carcinoma(RCC), subependymal giant cell astrocytoma(SEGA), pancreatic neuroendocrine tumor(PNET), transplants, drug-eluting coronary stent
    • more lipophilic, shorter t1/2
  7. temsirolimus
    • macrolide
    • MAO: binds to mTOR (regulatory kinase)
    • Indications: renal cell carinoma(RCC)
  8. zotarolimus
    • 40-Epi-(N1-tetrazolyl)-rapamcin; ABT-578
    • MAO: binds to mTOR (regulatory kinase)
    • Indications: dru-eluting coronary stent
  9. mycophenolate mofetil
    • semi-synthtic from Penicillium mold
    • metabolized to MPA(mycophenolic acid)-active drug
    • MAO: selective, uncompetitive, reversible inhibitor of inosine monophosphate dehydrogenase-blocks de novo of guanosine
    • Indications: allogenei renal, cardiac, hepatic trnasplants, uveitis, Churg-Strauss syndrome,
  10. azathioprine
    • imidazoyle drivative of mercaptopurine
    • MAO: metabolized to 6-mercaptopurine-antimetabolite of purine
    • Indications: renal allograft, RA
    • with allopurinol use only 25-33$of the typical dose
    • mutagenic, hematologic toxicities, neoplasia
  11. cyclophosphamide
    • MAO: nitorgen mustard alkylating antineoplastic agent-cytotoxic to rapidly dividing cells
    • Indications: malignant disease and nephrotic syndrome in children
    • leukopenia, carcinogenesis, alopecia(hair loss)
  12. methotrexate
    • MAO: antimetabolite of folic acid-blocks dihydrofolate reductase-blocks de novo
    • Indications: antineoplastic chemotherapy, psoriasis, RA
    • oral is preferred, birth defects
  13. anti-thymocyte globulin(rabbit)
    • MAO: polyclonal rabbit antiserum agains T-cells
    • Indications: acute renal transplant rejection
    • viral infection
  14. lymphocyte immuno globulin, anti-thymocyte globulin(equine)
    • MAO: polyclonal antiserum from horses(equine), antibodies works as hypersensitivity type II
    • Indications: acute renal transplant rejection, aplastic anemia
    • IV infusion in NO LESS than 4hrs
  15. hydroxychloroquine
    • MAO: alkaloid in lysosomes raise APC's vesicular pH causing MHC II altering
    • Indications: malaria, lupus erythematosus, RA
    • Irreversible retinal damage, psoriasis, prophyria
  16. sulfasalazine
    • 5-aminosalacylic acid
    • MAO: inhibits COX, 5-LOX
    • Indications: ulcerative colitis, RA, JRA, IBD
  17. leflunomide
    • MAO: inhibits dihydroorotate dehydrogenase(de novo pyrimidine synthesis) located in mitochondria
    • Indications: RA 100mgDL, 20mg DM
    • M1, (A77 1726), t1/2: 2 weeks - pregnancy
    • immunosuppression, hepatotoxicity
  18. anakinra
    • MAO: recombinant, non-glycosylated synthetic IL-1Ra
    • Indications: RA, ulcerative colitis
    • E. Coli, no combo with TNF-a, 100mg daily subQ
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