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48 Cards in this Set

  • Front
  • Back
What is the pneumonic for the immunopharm drugs?
Many Cytotoxic Agents May Predispose Cell To Suicide
What is prednisolone?
corticosteroid
What does prednisolone do to cell trafficking?
lymphocytopenia & monocytopenia due to sequesteration
prevents neutorphil adherence
inhibits chemoattactant factors
What does prednisolone do to cell function?
interferes w MP Ag processing
blocks action of lymphokines
inhibits binding to Fc receptor
What is prednisolone used to treat?
autoimmune disease
prevents graft rejection
What side effects are there with prednisolone?
acute adrenal insufficiency
cushing syndrome
What is prednisolone contraindicated in?
pre-existing infections
What do the cytotoxic drugs do?
kill rapidly proliferating cells
best if used at time of initial exposure
What are the first generation cytotoxic drugs?
Many Cytotoxic Agents
What are the first generation cytotoxic drugs?
Methotrexate
cyclophosphamide
azathiprine
What is the mechanism of action of azathioprine?
purine anti-metabolite that inhibits purine biosythesis & therefore DNA synthesis
What is azathioprine used to treat?
RA & autoimmune disease
What are the uses for azathioprine?
inhibits rejection of transplanted organs
What are the SE of azathioprine?
BM depression!
GI & hepatotoxicity
inc risk of infection
What is the mechanism of action of cyclophosphamide?
alkylating agent that results in cross-linking of dsDNA
Where are the toxic effects of cyclophosphamide more pronounced?
B-cells so suppresses humoral immunity
How do you take cyclophosphamide?
orally
What is cyclophosphamide used to treat?
autoimmune disease

not effective in preventing graft rejection
What are the SE of cyclophosphamide?
BM suppression
What is the mechanism of action of methotrexate?
inhibitor of difolate reductase - inhibits folate dependent purine synthesis
What is methotrexate used to treat?
autoimmune dz
What are the SE of methotrexate?
hepatic toxicity
What is the second generation cytotoxic drugs?
mycophenolate mofetil
What is the mechanism of action of mycophenolate mofetil?
inhibits DE NOVO pathway only by metabolism to active mycophenolic acid
What does mycophenolate mofetil do?
inhibits IMP dehydrogenase that is required for purine synthesis
What is special about mycophenolate mofetil?
selective for lymphocytes
How do you take mycophenolate mofetil?
orally
Why do you take mycophenolate mofetil & corticosteroids & cyclosporine?
prevent renal allograft rejection
What else do you use mycophenolate mofetil to treat?
autoimmune disease
RA, refractory psoriasis
Who should you be careful with mycophenolate mofetil?
pts w active GI dz, reduced renal functions, infections, pregnant women
What are the SE of mycophenolate mofetil?
infection, leukopenia, anemia
nausea, diarrhea, stomach cramping
What are the drugs used to prevent rejection of transplanted organs?
cyclosporin
tacrolimus
sirolimus
What does cyclosporin bind to?
cyclophilin
What does cyclosporin inhihibit?
clacineurin - a calcium dependent phosphatase
What does the inhibition of calcinurin by cyclosporin lead to?
inactivation of TF NFAT that is necessary for IL-2 production
What is cyclosporin used to treat?
prevents rejection
some autoimmune
How do you take cyclosporin?
orally
What are the SE of cyclosporin?
nephrotoxicity!
hepatotoxicity
What does tacrolimus bind to?
FK binding protien (cyclophilin related protein)
What does binding to FKBP by tacrolimus inhibit?
calcineurin - ca dependent phosphatase
What does inhibiting calcineurin cause?
blocks activation of TF NFAT that is required for the production of IL-2 to help T cells
How potent is tacrolimus compared to cyclosporin?
much more
What are the SE fo tracrolimus?
less nephro & hepatotoxcitity but fever as well
What does sirolimus bind to?
FKBP
What does binding to FKBP by sirolimus cause?
inhibits mTOR
What does mTOR do?
kinase involved in cell cycle progression, when blocked cells cannot progress from G1 to S
Overall, what does sirolimus do?
inhibits T cell activation & proliferation downstream of IL-2
What are the uses of sirolimus?
prevent rejection
some autoimmune dz
coating of cardiac stents