Immunosuppressant CMV Drugs

  1. What is the MOA of cyclosporine?
    • Binds cyclophilin to inhibit calcineurin
    • Thereby blocking T cell activation by inhibiting IL2 production
  2. What are adverse effects of cyclosporine?
    • Nephrotoxicity
    • Neurotoxicity
    • Hirsutism
    • Gingival hyperplasia
  3. What is the therapeutic use of cyclosporine?
    Prevent organ transplant rejection
  4. What is the MOA of tacrolimus?
    • binds FKBP which will inhibit calcineurin
    • Thereby blocking T cell activation by inhibiting production of IL2
  5. True/false: cyclosporine inhibits action of calcineurin by binding to FKBP
    False; cyclosporine binds to cyclophilin which will then inhibit calcineurin
  6. True/false: tacrolimus inhibits the action of calcineurin by bidning to FKBP
    True
  7. What are the agents of calcineurin inhibitors?
    • Cyclosporine
    • Tacrolimus
  8. What is an agent of proliferation signal inhibitor?
    Sirolimus
  9. What is the MOA of sirlolimus?
    Blocks IL2 signaling needed for T cell proliferation by inhibiting nTOR which causes cell cycle to arrest at G1 phase
  10. What is the therapeutic use for sirolimus
    Prevent transplant kidney rejection
  11. What are adverse effects of sirolimus?
    • Bone marrow suppression
    • Pneumonitis
    • Hypertriglyceridemia
  12. What are agents of antimetabolites?
    • Azathioprine
    • Mycophenolate mofetil
  13. What is the MOA of azathioprine?
    Inhibit nucleotide synthesis by interfering with purine nucleic acid metabolism and thereby inhibit lymphocyte proliferation
  14. What are adverse effects of azathioprine?
    Bone marrow suppression
  15. What should the azathioprine dose adjustment be for gout patients taking allopurinol?
    Reduce dose of azathioprine
  16. True/false: high plasma level of azathioprine is toxic to the body
    True
  17. What is the MOA of mycophenolate mofetil?
    • Inhibits inosine monophosphate dehydrogenase, an enzyme involved in guanosine metabolism
    • Inhibits de novo synthesis of purines
    • Thereby inhibiting T and B cells response
  18. What are nucleotide/nucleoside analogues?
    Compete with natural triphosphate substrates of viral polymerases and can lead to termination of viral DNA synthesis
  19. What are agents of nucleoside analogs?
    • ganiciclovir/ valganciclovir
    • Foscarnet
    • Cidofovir
  20. What is the MOA of ganciclovir/valganciclovir?
    Inhibit viral DNA polymerase from the get go
  21. What are adverse effect of ganciclovir/valganciclovir?
    Bone marrow suppression
  22. What is preemptive prophylaxis of GCV/VGC?
    Given to high risk pt
  23. What is universal prophylaxis of GCV/VGC?
    Given to all transplant pt
  24. What is the MOA of foscarnet?
    binds to pyrophosphate binding site and inhibit herpes viral DNA polymerases and RNA polymerase
  25. Which antiviral CMV drug does not require activation by phosphorylation?
    Foscarnet
  26. What are adverse effects of foscarnet?
    • Nephrotoxicity
    • CNS toxicity
  27. What is the MOA of cidofovir?
    Inhibit viral DNA polymerase, no forming of diphosphate
  28. True/false: cidofovir must be administered with oral probenecid
    True
  29. True/false: foscarnet must be administered with oral probenecid
    False; it is cidofovir that needs to be administered with probenecid
  30. What is a contraindication of cidofovir?
    Renal insufficiency
Author
lykthrnn
ID
346247
Card Set
Immunosuppressant CMV Drugs
Description
Renal Midterm- Pharmacology
Updated