Pharmacolcogy Immunopharm

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ljmtf3
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62603
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Pharmacolcogy Immunopharm
Updated:
2011-01-29 17:38:06
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Pharmacology Immunopharm
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Pharmacology, Immunopharm
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  1. Glucocorticoids
    • 1st hormonla agent with lympholytic properties
    • reduces size and lymphoid content of LN and spleen
    • interfere with lymphocyte cell division
    • No effect on myeloid and erythroid stem cells
    • Effect on CMI>HMI
    • Prednisone!!!!: idiopathic thrombocytopenic pupura, rheumatoid arthritis, autoimmune hemolytic anemia, asthma, organ and bone marrow transplant
  2. Cyclosporine
    • calcineurin inhibitors
    • peptide antibiotic
    • oral, IV, used alone or in combo
    • used for organ transplant, evere dry eye syndrome
  3. Cyclosporine mech of action
    binds to cyclophilin for form complex, which inhibits calcineurin, which is responsible for T cell transcription factor for synthesis of IL2
  4. Cyclosporine side effects
    • NEPHROTOXIC
    • hypertension
    • hyperglycemia
    • liver dysfunction
    • seizure
    • metastiasis
  5. Tacrolimus
    • calcineurin inhibitor
    • macrolide antibiotic
    • not related to CSA but mech is same (binds with FK binding protein that inhibits calcineurin)
    • 10-100 times more potent than CSA
    • organ transplant
    • Metabolized by CYP450
    • T1/2 9-12 h
    • NEPHROTOXIC
  6. Sirolimus and Everoliumus
    • Proliferation signal inhibitors
    • binds with FKBP and targets mTOR --> inhibits T cell proliferation
    • metabolized through CYP450(drug interaction with CSA)
    • Sirolimus t1/2: 60 hr
    • Everolimus t1/2: 43 hr
    • prevents graft rejection
    • uveoretnitis with CSA
    • Toxicity: myelosupression, hepatotoxicity, diarrhea, NO NEPHROTOXICITY (good alternative to CSA)
  7. Mycophenolate mofetil
    • semi synthetic derivative of mycophenolic acid
    • Inhibits T and B cell proliferation in tissue culture (purine synthesis inhibition (adenine and quanine))
    • Oral and IV
    • for solid organ transplant, RA, and IBD
    • Toxic: gi problems, ha, hypertension, reversible myelosuppression
  8. Thalidomide
    • sedative drug, teratogenicity in pregnant women
    • immunomodulator
    • inhibits angiogenesis, antiinflammatory, multiple myeloma, solid tumor, lupus erythematosus
    • Inhibits TNF-alpha, reduce phagocytosis by neutrophils, increase IL10, enhanced CMI
    • Toxic: tertogenesis, peripheral neuropathy, rash, constipation, fatigue, deep vein thrombosis
  9. Azathroprine
    • cytotoxic agent
    • percaptopurine prodrug
    • GI absoption
    • Xanthine oxidase converts active compound into 6-thiouric acid-excreted through urine
    • interferes with purine metabolism
    • good for renal allografts, RA, crohn disease, MS
    • Toxic: bone marrow suppression, thrombocytopenia, rash, fever, nausea, hepatic dysfunction
  10. Cyclophosphamide
    • cytotoxic agents
    • One of most efficacious immunosuppressive drugs
    • destoys dividing lymphoid cells , but also effects resting cells
    • Good for SLE, autoimmune hemolytic anemia
    • Toxic: n/v, cardiac, electrolyte imbalance
  11. Leflunomide
    • cytotoxic agents
    • Inhibitor of pyrimidine synthesis
    • long half life
    • orally active
    • good for RA
    • Toxic: liver enzyme, renal impairment, teratogenic
  12. Hydroxychloroquine
    • cytotoxic agent
    • antimalarial
    • affects intracellular antigen processing and loading of epitope on MHC classII
    • Used for RA and SLE
  13. Fingolimod
    • oral drug for relapsing MS
    • Sphingosine 1-phosphate receptor modulator
    • reduces lymphocyte migration from lymph node to brain
    • reduces counts 20-30%
    • Side effects: decrease heart rate, slight increase in bp, fetal harm
  14. ALG and ATG
    • anti lymphocyte or thymocyte antibodies
    • used in transplants
  15. ALG/ATG+CSA
    • antilymphocyte or thymocyte antibodies
    • used for bone marrow transplant
  16. Toxicity of ALG and ATG
    local pain, erythema, type3 hypersensitivity
  17. Immunoglobulin
    • IGIV prepared form healthy volunteers
    • Kawasaki disease: prevents coronary artery aneurysm
    • Helps in SLE, and ITP (idiopathic thromocytopenic purpura
    • Mech of action unclear
  18. Adalimumab (humira)
    • Target: TNF-alpha
    • Disease: auto-immune
  19. Basiliximab
    • Target: CD25
    • Disease: transplant rejection
  20. Daclzumab
    • CD25
    • Transplant rejection
  21. Efalizumab
    • CD11a
    • psoriasis
  22. Infliximab
    • TNF-alpha
    • arthritis and crohns
  23. mepolizumab
    • IL-5
    • hypereosinophilic syndrome
  24. natalizumab
    • a4 integrin
    • MS
    • crohns disease
  25. Omalizumab
    • IgE
    • allergy
  26. ranibizumab
    • VEGF-A
    • macular degeneration
  27. Macrophages
    • phagocytosis
    • activation of bact mech
    • antigen presenting
  28. dendritic cell
    • antigen uptake in periphery
    • antigen presenting in lymph node
  29. neutrophil
    • phagocytosis
    • activation of bact mech

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