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48 Cards in this Set
- Front
- Back
What is the pneumonic for the immunopharm drugs?
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Many Cytotoxic Agents May Predispose Cell To Suicide
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What is prednisolone?
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corticosteroid
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What does prednisolone do to cell trafficking?
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lymphocytopenia & monocytopenia due to sequesteration
prevents neutorphil adherence inhibits chemoattactant factors |
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What does prednisolone do to cell function?
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interferes w MP Ag processing
blocks action of lymphokines inhibits binding to Fc receptor |
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What is prednisolone used to treat?
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autoimmune disease
prevents graft rejection |
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What side effects are there with prednisolone?
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acute adrenal insufficiency
cushing syndrome |
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What is prednisolone contraindicated in?
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pre-existing infections
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What do the cytotoxic drugs do?
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kill rapidly proliferating cells
best if used at time of initial exposure |
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What are the first generation cytotoxic drugs?
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Many Cytotoxic Agents
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What are the first generation cytotoxic drugs?
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Methotrexate
cyclophosphamide azathiprine |
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What is the mechanism of action of azathioprine?
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purine anti-metabolite that inhibits purine biosythesis & therefore DNA synthesis
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What is azathioprine used to treat?
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RA & autoimmune disease
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What are the uses for azathioprine?
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inhibits rejection of transplanted organs
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What are the SE of azathioprine?
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BM depression!
GI & hepatotoxicity inc risk of infection |
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What is the mechanism of action of cyclophosphamide?
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alkylating agent that results in cross-linking of dsDNA
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Where are the toxic effects of cyclophosphamide more pronounced?
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B-cells so suppresses humoral immunity
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How do you take cyclophosphamide?
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orally
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What is cyclophosphamide used to treat?
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autoimmune disease
not effective in preventing graft rejection |
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What are the SE of cyclophosphamide?
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BM suppression
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What is the mechanism of action of methotrexate?
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inhibitor of difolate reductase - inhibits folate dependent purine synthesis
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What is methotrexate used to treat?
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autoimmune dz
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What are the SE of methotrexate?
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hepatic toxicity
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What is the second generation cytotoxic drugs?
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mycophenolate mofetil
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What is the mechanism of action of mycophenolate mofetil?
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inhibits DE NOVO pathway only by metabolism to active mycophenolic acid
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What does mycophenolate mofetil do?
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inhibits IMP dehydrogenase that is required for purine synthesis
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What is special about mycophenolate mofetil?
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selective for lymphocytes
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How do you take mycophenolate mofetil?
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orally
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Why do you take mycophenolate mofetil & corticosteroids & cyclosporine?
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prevent renal allograft rejection
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What else do you use mycophenolate mofetil to treat?
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autoimmune disease
RA, refractory psoriasis |
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Who should you be careful with mycophenolate mofetil?
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pts w active GI dz, reduced renal functions, infections, pregnant women
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What are the SE of mycophenolate mofetil?
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infection, leukopenia, anemia
nausea, diarrhea, stomach cramping |
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What are the drugs used to prevent rejection of transplanted organs?
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cyclosporin
tacrolimus sirolimus |
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What does cyclosporin bind to?
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cyclophilin
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What does cyclosporin inhihibit?
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clacineurin - a calcium dependent phosphatase
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What does the inhibition of calcinurin by cyclosporin lead to?
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inactivation of TF NFAT that is necessary for IL-2 production
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What is cyclosporin used to treat?
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prevents rejection
some autoimmune |
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How do you take cyclosporin?
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orally
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What are the SE of cyclosporin?
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nephrotoxicity!
hepatotoxicity |
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What does tacrolimus bind to?
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FK binding protien (cyclophilin related protein)
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What does binding to FKBP by tacrolimus inhibit?
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calcineurin - ca dependent phosphatase
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What does inhibiting calcineurin cause?
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blocks activation of TF NFAT that is required for the production of IL-2 to help T cells
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How potent is tacrolimus compared to cyclosporin?
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much more
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What are the SE fo tracrolimus?
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less nephro & hepatotoxcitity but fever as well
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What does sirolimus bind to?
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FKBP
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What does binding to FKBP by sirolimus cause?
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inhibits mTOR
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What does mTOR do?
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kinase involved in cell cycle progression, when blocked cells cannot progress from G1 to S
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Overall, what does sirolimus do?
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inhibits T cell activation & proliferation downstream of IL-2
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What are the uses of sirolimus?
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prevent rejection
some autoimmune dz coating of cardiac stents |