Pharm immunomodulators

Card Set Information

Author:
USUHS14
ID:
152417
Filename:
Pharm immunomodulators
Updated:
2012-05-05 22:21:34
Tags:
immunomodulators
Folders:

Description:
immunomodulators
Show Answers:

Home > Flashcards > Print Preview

The flashcards below were created by user USUHS14 on FreezingBlue Flashcards. What would you like to do?


  1. Cyclosporine
    • Mechanism: inhibits calcineurin, preventing expression of IL-2, thereby inhibiting activation of CD4+ and CD8+ T-cells
    • Pharmacology: variable absorption leading to unpredictable bioavailability; metabolized by CYP3A4
    • Uses: organ transplants; GVHD; selected autoimmune diseases
    • Toxicity: nephrotoxicity, neurotoxicity, hypertension, hirsutism, hyperlipidemia, gingival hyperplasia
  2. Tacrolimus
    • Mechanism: inhibits calcineurin, preventing expression of IL-2, thereby inhibiting activation of CD4+ and CD8+ T-cells
    • Pharmacology: metabolized in liver
    • Uses: prophylaxis after liver and kidney transplants; rescue therapy in graft rejection
    • Toxicities: nephrotoxicity; neurotoxicity; hypertension; inhibition of beta cell function; increased risk fro malignant lymphoma
  3. Sirolimus
    • Mechanism: inhibits mTOR, preventing transcription and translation of genes involved in cellular proliferation thereby inhibiting B and T cell proliferation
    • Pharmacology: metabolized by CYP3A4
    • Uses: prevention of acute transplant rejection; prevents neointimal proliferation and restenosis after stent placement
    • Toxicity: anemia, thrombocytopenia, and hyperlipidemia; contraindicated after liver transplantation; no risk of lymphoma
  4. Mycophenolate mofetil
    • Mechanism: inhibits de novo purine synthesis
    • Pharmacology: prodrug; should not be administered with antacids containing magnesium or aluminium hydroxide
    • Uses: solid organ transplant as a single agent or in combination
    • Toxicity: diarrhea, leukopenia
  5. Leflunomide
    • Mechanism: inhibits de novo pyrimidine synthesis
    • Pharmacology: prodrug; extremely long half-life
    • Uses: active rheumatoid arthritis
    • Toxicity: diarrhea, nausea, myelosuppression, severe hepatotoxicity (rare)
  6. Thalidomide
    • Mechanism: unknown
    • Uses: multiple myeloma, erythema nodosum leprosum
    • Toxicity: peripheral neuropathy, teratogenicity
  7. Fingolimod
    • Mechanism: binds to sphingosine-1 phosphate receptors to block migration of lymphocytes out of lymph nodes
    • Uses: MS
    • Toxicity: fatal infections
    • Pharmacology: must be phosphorylated by sphingosine kinase 2
  8. Daclizumab
    • Mechanism: humanized monoclonal antibody against alpha chain (CD25) of the high affinity IL-2 receptor, inhibiting IL-2 mediated T-cell activation
    • Use: in combo to reduce acute rejection in kidney and cardiac transplantation
  9. Basiliximab
    • Mechanism: chimeric monoclonal antibody against alpha chain (CD25) of the high affinity IL-2 receptor, inhibiting IL-2 mediated T-cell activation
    • Use: in combo to reduce acute rejection in kidney and cardiac transplantation
    • Toxicity: acute hypersensitivity reactions
  10. Muromonab
    • Mechanism: mouse monoclonal antibody directed against epsilon chain of the T-cell surface protein CD3, thereby blocking engagement of the T-ell receptor
    • Use: reversal of acute rejection of heart, liver, and kidney transplants
    • Toxicity: may non-specifically activate T cells upon first infusion; may cause hypersensitivity reactions
  11. Etanercept
    • Mechanism: neutralizes free TNF
    • Uses: rheumatoid arthritis, ankylosing spondylitis, plaque psoriasis
    • Toxicity: demyelinating disease
  12. Natalizumab
    • Mechanism: humanized monoclonal antibody against alpha4 subunit of integrin that inhibits lymphocyte migration through endothelial cells
    • Use: Crohn's, MS
    • Toxicity: significant risk for JC virus-induced PML
  13. Abatacept
    • Mechanism: binds to CD80 and CD86 to block binding of CD28 and prevent T cell activation
    • Uses: prevention of renal allograft rejection
  14. Infliximab
    • Mechanism: chimeric monoclonal antibody against TNF alpha
    • Uses: Crohn's, UC, rheumatoid arthritis, psoriatic arthritis, plaque psoriasis, ankylosing spondylitis
    • Toxicity: increased susceptibility to infection, reactivation of hepatitis B, malignancies, hepatotoxicity, development of anti-infliximab antibodies
  15. Anakinra
    • Mechanism: IL-1 receptor antagonist
    • Use: rheumatoid arthritis
    • Toxicity: increased susceptibility to serious bacterial infection
  16. Methotrexate
    Cytotoxic cancer chemotherapeutic used at lower concentrations to treat autoimmune disease
  17. Azathioprine
    • Mechanism: disrupts de novo purine synthesis; inhibits transcription
    • Use: rheumatoid arthritis (in combo with prednisone +/- cyclosporine/tacrolimus)
    • Toxicity: bone marrow suppression, GI distress
  18. Glatiramer
    • Mechanism: antigenically similar to myelin basic protein
    • Use: remitting-relapsing MS
  19. Antilymphocyte & antithymocyte globulin
    • Mechanism: depletes peripheral T cells by blocking cell surface receptors and direct cytotoxicity
    • Uses: prevention of transplant rejection, GVHD, aplastic anemia
    • Toxicity: fever, chills, leukopenia, thrombocytopenia, skin reactions
  20. Immune globulin (i.v.)
    • Uses: to confer passive immunity; treatment of autoimmune disorders (like ITP)
    • Mechanism: controversial/unknown
  21. INF-beta
    • Mechanism: exploit cells' natural anti-viral and anti-proliferative properties
    • Use: MS
  22. Epoetin alfa
    • Mechanism: erythropoietin analogue that stimulates formation of rbcs
    • Use: anemia
    • Toxicity: stroke, CV side effects
  23. Darbepoetin alfa
    • Mechanism: longer half-life form of erythropoietin analogue that stimulates formation of rbcs
    • Use: anemia
    • Toxicity: stroke, CV side effects

What would you like to do?

Home > Flashcards > Print Preview