Pharmacology: Antineoplastics III - 1

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  1. What are the antineoplastic glucocorticoid receptor specific hormones?
    • Prednisone
    • Dexamethasone (Decadron)
  2. What is the MOA for Glucocorticoid antineoplastics (prednisone and dexamethasone)?
    • Repress of activate transcription through a nuclear binding process
    • Cause apoptosis of lymphocytes
    • Have Lympholytic effects
  3. What are the indications for Glucocorticoid antineoplastics?
    • Acute and chronic leukemias
    • Breast cancer
    • Hodgkin’s Lymphoma
    • Non-Hodgkin’s Lymphoma
  4. What are the SE’s of glucocorticoid antineoplastics?
    Truncal obesity, moon face, fragile skin, susceptibility to infections
  5. How do you D/C Glucocorticoid antineoplastics?
    Slowly to avoid adrenal insufficiency
  6. What is the mechanism of action of Cetuximab?
    • Inhibits Tyrosine kinase through inhibition of EGFR receptors
    • Eventually causes apoptosis and growth inhibition
  7. Cetuximab brand name:
  8. What are the indications for Cetuximab?
    • EGFR positive colorectal, head and neck cancers
    • Investigational for EGFR over-expressing tumors
  9. What is Cetuximab (Erbitux) often used in combo wuth>
  10. What are the major toxicities of Cetuximab (Erbitux)?
    • Severe infusion reactions (b/c giving an antibody)
    • Acne-like rash
    • Interstitial lung disease
  11. How do you prevent infusion reactions by Cetuximab (Erbitux)?
    Pretreat with an antihistamine
  12. What type of antibody is Panitumumab (Vectibix)?
    Full human
  13. What is the MOA for Panitumumab (Vectibix)?
    • Inhibits Tyrosine kinase through inhibition of EGFR receptors
    • Eventually causes apoptosis and growth inhibition
  14. What is the brand name for Panitumumab?
  15. What are the side effects of Panitumumab (Vectibix)?
    Rare infusion reaction and interstitial lung disease
  16. What is the only indication for Panitumumab (Vectibix)?
    Colorectal cancer
  17. Why does Panitumumab (Vectibix) have fewer infusion reactions than Cetuximab?
    Panitumumab (Vectibix) is a human antibody and Cetuximab is a mouse
  18. Elortinib (Tarceva) is given by what route?
  19. What DDIs does Elortinib (Tarceva) have?
    CYP3A4 related
  20. What is the MOA of Elortinib (Tarceva)?
    Cystolic inhibitor of EGFR-TK
  21. What group of patients does Elortinib (Tarceva) work best in?
    Female non-smokers
  22. What is the indication or Erlotinib?
    Non-small cell lung cancer w/ a specific mutation
  23. What is the black box warning for Erlotinib (Tarveca)?
    • GI perforation
    • Must stop the drug if this occurs
  24. Does Erlotinib (Tarveca) cause bone marrow suppression?
  25. What are the SE of Erlotinib (Tarveca)?
    • SE are mild
    • Mild rash and diarrhea
    • Only worrisome one = GI perforation (BB)
    • CI in pregnancy
  26. What drugs work extracellularly on the EGFR?
    Pantumamab, Cetuximab and Trastuzimab
  27. What drugs work intracellularly on the EGFR?
    Lapatinib, Gefitinib and Erlotinab
  28. What are the drugs that act on ABL used for?
    Chronic myolegenous leukemia
  29. What drugs act on ABL?
    Imatinib, Nilotinib and Dasatinib
  30. Imatinib, Nilotinib, Dasatinib are metabolized by what enzyme?
  31. What is the MOA for imatinib (Gleevac)?
    Competitive inhibition of ATP binding site on C-ABL, C-Kit ad PDGFR
  32. What is the route of administration of imatinib (Gleevac)?
  33. What are the DDIs associated with imatinib (Gleevac)?
    CYP3A4 related
  34. What are the indications for imatinib (Gleevac)?
    • Chronic myelogenous leukemia (CML)
    • GI stromal cell tumors expressing C-KIT
  35. What are the SE for Imatinib (Gleevec)?
    • GI, hepatotoxic, rashes, fatigue, Fluid retention
    • Neutropenia/thrombocytopenia (myelosupression)
  36. What is the MOA of Nilotinib (Tasigna)?
    Binds inactive BCR-ABL
  37. How does the binding affinity of Nilotinib (Tasigna) compare to imatinib (Gleevac)?
    Nilotinib (Tasigna) has greater binding affinity
  38. What are the indicatios for Nilotinib (Tasigna)?\
    • CML
    • Used against all imatinib resistant clones EXCEPT T3151 mutations
  39. What are the SE of Nilotinib (Tasigna)?
    • Prolongs QT
    • (less severe SE overall than imatinib)
  40. What is the MOA of dasatinib (Sprycel)?
    • Binds variety of PKs
    • Binds inactive OR active BCR-ABL
  41. How does the binding affinity of dasatinib (Sprycel) compare to imatinib (Gleevac)?
    dasatinib (Sprycel) has greater binding affinity
  42. What are the indications for dasatinib (Sprycel)?
    • CML
    • Used against all imatinib resistant clones EXCEPT T3151 mutations
  43. What are the SE’s for dasatinib (Sprycel)?
    • Prolong QT
    • Similar to imatinib
    • Myelosupression
  44. What are the RAS-MAP kinase inhibitors?
    • sorafenib
    • sunitinib
    • vemurafenib
    • pazopanib
    • vandetanib
  45. What is the MOA of Sorafenib (Nexavar)?
    • Inhibits multiple Tyrosine kinases via inhibition of phosphorylation
    • Results in angiogenesis (capillary growth) and metastasis
  46. What is the indication for Sorafenib (Nexavar)?
    Advanced renal cell carcinoma
  47. What are the SE for Sorafenib (Nexavar)?
    GI, rash, fatigue, hand-and-foot syndrome, HTN
  48. What are the DDIs for Sorafenib (Nexavar)?
    CYP3A4 DDIs
  49. Does Sorafenib (Nexavar) cause myelosupression?

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Pharmacology: Antineoplastics III - 1
2014-04-19 19:33:30
Pharmacology Antineoplastics III
Pharmacology: Antineoplastics III - 1
Pharmacology: Antineoplastics III - 1
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