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fallcloud13
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corticosteroids (Medrol)
-predinosone
-methylprednisolone
-dexamethasone
- 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
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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
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tacrolimus (FK506)
- macrolide
- MAO: binds to immunophilin(FKBP-12), decrease IL-2, INF-y
- Indications: allogeneic liver, kidney, heart transplants, atopic dermatitis (eczema)
- CYP3A
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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
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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
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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
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temsirolimus
- macrolide
- MAO: binds to mTOR (regulatory kinase)
- Indications: renal cell carinoma(RCC)
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zotarolimus
- 40-Epi-(N1-tetrazolyl)-rapamcin; ABT-578
- MAO: binds to mTOR (regulatory kinase)
- Indications: dru-eluting coronary stent
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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,
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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
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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)
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methotrexate
- MAO: antimetabolite of folic acid-blocks dihydrofolate reductase-blocks de novo
- Indications: antineoplastic chemotherapy, psoriasis, RA
- oral is preferred, birth defects
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anti-thymocyte globulin(rabbit)
- MAO: polyclonal rabbit antiserum agains T-cells
- Indications: acute renal transplant rejection
- viral infection
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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
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hydroxychloroquine
- MAO: alkaloid in lysosomes raise APC's vesicular pH causing MHC II altering
- Indications: malaria, lupus erythematosus, RA
- Irreversible retinal damage, psoriasis, prophyria
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sulfasalazine
- 5-aminosalacylic acid
- MAO: inhibits COX, 5-LOX
- Indications: ulcerative colitis, RA, JRA, IBD
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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
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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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