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34 Cards in this Set
- Front
- Back
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cyclosporin
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binds cyclophilin inside the cell and inhibits calcineurin activation; calcineurin is a phosphatase that normally dephosphorylates NF-AT so that it can enter the cell and increase IL-2 production
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cyclosporin interactions
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metabolized by CYP3A4
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tacrolimus
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binds FKBP12 (FKBP is a immunophilin similar to cyclophilin) and inhibits calcineurin
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cyclosporin side effects
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"This cycle belongs to the NIH"-nephrotoxic, neurotoxic, increased cholelithiasis, HTN, hyperlipidemia, hyperglycemia, hyperplasia of gums, and hirsutism, HUS AND GOUT
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tacrolimus interactions
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metabolized by CYP3A4
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sirolimus and transport and interactions
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binds FKBP12 (an immunophilin) that inhibits mTOR (a tyr kinase) which slows IL-2 production; transported by P-glycoprotein in feces; metabolized by CYP3A4
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everolimus and interactions
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binds FKBP12 (an immunophilin) that inhibits mTOR (a tyr kinase) which slows IL-2 production; metabolized by CYP3A4
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sirolimus side effects
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thrombocytopenia, hyperlipidemia, poor wound healing-breakdown of anastomoses, interstitial lung dz
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everolimus side effects
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thrombocytopenia, poor wound healing-breakdown of anastomoses, interstitial lung dz, hyperlipidemia
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mycophenolate and side effects
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inhibits inosine monophosphate dehydrogenase which leads to feedback inhibition on purine synth; cause diarrhea and anemia (only drug of the immunosuppressants that cause these probs)
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Which classes of immunosuppressives should you measure drug levels for?
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calcineurin inhibitors (cyclosporin and tacrolimus) and mTOR inhibitors (sirolimus and everolimus); don't have to measure levels of azathioprine but can measure levels of mycophenolate
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Which classes of immunosuppressants should you measure WBC count for?
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Cell cycle inhibitors (mycophenolate and azathioprine)
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glucocorticoids MOA acutely; main MOA
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acute: it can lyse lymphocytes when given at HIGH doses; normal MOA: binds to cytosloic receptor and increases IkB and decreases NF-kB
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side effects of glucocorticoids
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"I'm the PRESident's SON" (prednisone) and "I'M the HOPE"-iatrogenic cushing's, myopathy, hyperglycemia, HTN, hypokalemia, osteoporosis, osteonecrosis, peptic ulcer, pancreatitis, ecchymosis, eye disorder (cataracts)
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azathioprine
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prodrug for 6-MP which inhibits purine synth
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Which immunosupressant is a pro-drug?
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azathioprine; prodrug for 6-MP
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Which immunosupressant drug do we have to worry about a genetic deficiency in its metabolizing ez? What happens if this drug accumulates?
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azathioprine can cause BM toxicity; the ez that can be deficient is thiopurine methyltransferase
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Which of these immunosuppressive drugs can cause diarrhea and anemia?
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mycophenolic acid
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anti-thymocyte globulin S/E
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lymphocytopenia for > 1 yr
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anti-CD3; source of Ab; duration of action
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mouse ab; depletes T cells for 1 week
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daclizumab
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anti-CD25 (IL-1R); targets only activated T cells so non-depleting
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alemtuzamab; source of Ab; duration of effects; S/E
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anti-CD52; mouse and human hybrid; lymphocytopenia for 3 yrs (longest depletion of the induction immunosupressants); neutropenia and anemia
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basiliximab
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anti-CD25 (IL-1R); targets only activated T cells so non-depleting
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serum sickness
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anti-thymocyte globulin; 1 yr span
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hyperlipidemia
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calcineurin inhibitors and mTOR inhibitors
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thrombocytopenia and poor wound healing
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mTOR inhibitors
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DM2
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calcineurin inhibitors (mostly tacrolimus)
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tremor
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calcineurin inhibitors
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HTN
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cyclosporin
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hirsutism
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cyclosporin
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diarrhea
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MPA
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BM supression-leukopenia
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azathioprine
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gum hyperplasia
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cyclosporin
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What are your 3 choices for cellular mediated acute rejection of a graft?
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methylprednisone, anti-thymocyte, and anti-CD52
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