Cancer Chemotherapy Part 2 - Chapter 54

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PA_Flash
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204756
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Cancer Chemotherapy Part 2 - Chapter 54
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2013-03-05 13:33:07
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Cancer Chemotherapy Pharmacology
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Cancer Chemotherapy Part 2 - Chapter 54
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  1. What are the names of the two ANTITUMOR ANTIBIOTICS?
    • Doxorubicin,
    • Bleomycin
  2. What is the brand name for Doxorubicin?
    Adriamycin
  3. Doxorubicin - MOA
    An anthracycline which can intercalate between base pairs, inhibit topoisomerase II, and generate free radicals, binding to cellular membranes to alter fluidity and ion transport

    • Blocks the synthesis of RNA and DNA
    •   and causes DNA strand scission.
  4. Doxorubicin - CCNS or CCS?
    CCNS
  5. Doxorubicin – Pharmacokinetics
    •Must be given IV. 

    • •Metabolized in the liver and excreted in
    • the urine, imparting to it a red color.
  6. Doxorubicin - Clinical use
    • Lymphoma,
    • sarcoma,
    • acute leukemia,
    • breast,
    • lung,
    • testes,
    • thyroid,
    • and ovary
  7. Doxorubicin – Toxicity
    • Myelosuppression,
    • GI distress,
    • and alopecia.
    • Unique side effect is cardiotoxicity.
  8. Bleomycin - MOA
    • acts by binding to DNA, which results in
    • single-strand and double-strand breaks following free radical formation, and inhibition of DNA biosynthesis

    • Cell cycle-specific drug that causes
    • accumulation of cells in the G2 phase of the cell cycle.
  9. Bleomycin - Clinical treatment of
    • Hodgkin's and non-Hodgkin's lymphomas,
    • germ cell tumor,
    • head and neck cancer,
    • and squamous cell cancer of the skin, cervix, and vulva.
  10. Bleomycin - Pharmokinetics
    May be given IV, IM, or SQ
  11. Bleomycin - Toxicity
    pneumonitis
  12. Plant Alkaloids are CCS drugs which include?
    • vinca alkaloids,
    • the podophyllotoxins,
    • and the taxenes.
  13. Brand name for Vincristine?
    Oncovin
  14. Vincristine - MOA
    A spindle poison derived from the periwinkle plant.  Prevents the assembly of tubulin dimers into microtubules, and blocks the formation of the mitotic spindle.

    Acts on the M phase of the cell cycle
  15. Vincristine – Resistance
    occurs as a result of increased efflux from the cell by a transporter molecule.
  16. Vincristine – Pharmacokinetics
    • Given IV. 
    • Good tissue penetration except into the CSF. 

     - Cleared mainly by biliary excretion
  17. Vincristine - Clinical use
    • Lymphoma,
    • Hodgkin’s disease,
    • Wilm’s tumor,
    • childhood acute leukemia
  18. Vincristine – Toxicity
    • GI distress,
    • alopecia,
    • myelosuppression,
    • Peripheral neuropathy.
  19. What type of plant alkaloid is Etoposide?
    • a podophyllotoxin
    • derived from the May apple  plant
  20. Etoposide - MOA
    • Interacts with Topoisomerase II to increase the degradation of DNA
    •  - Most active in the late S and early G2 phases.
  21. Etoposide – Pharmacokinetics
    • Good oral absorption,
    • eliminated via the kidney
  22. Etoposide – Toxicity
    • GI,
    • alopecia,
    • myelosuppression
  23. Etoposide - Clinical use
    • treat germ cell cancers,
    • small cell and non-small cell lung cancers,
    • Hodgkin’s and non-Hodgkin’s lymphomas,
    • and gastric cancer.
  24. Brand name for Paclitaxel?
    Taxol
  25. Paclitaxel - What type of plant alkaloid is it?
    • A taxane
    • derived from the Pacific yew tree.
  26. Paclitaxel - MOA
    • Mitotic spindle poison,
    • M phase specific

    •given IV
  27. Paclitaxel - Clinical use
    Breast and ovarian cancer
  28. Paclitaxel – Toxicity
    • Myelosuppression,
    • neuropathy,
    • and hypersensitivity reactions
  29. What are SERM’s?
    SERM’s are mixed estrogen agonists that act as antagonists in certain tissues
  30. Name two hormones used in the treatment of cancer.
    • Prednisone,
    • Tamoxifen (Nolvadex)
  31. Prednisone is used to treat?
    • acute leukemia,
    • Hodgkin’s disease,
    • and lymphoma
  32. Brand name for Tamoxifen?
    Nolvadex
  33. Tamoxifen - MOA
    • Selective Estrogen Receptor Modifier
    • (SERM) which blocks the binding of estrogen to receptors of estrogen-sensitive cancer cells in breast tissue.
    • acts as an antagonist in hormone-responsive breast cancers where it prevents receptor activation by endogenous estrogen.
  34. Tamoxifen - Clinical use
    - Used in the treatment of receptor-positive breast cancers and may help prevent cancer in high risk women.

     - has more agonist than antagonist action on bone and thus helps to prevent osteoporosis.
  35. Tamoxifen - Toxicity
    • nausea,
    • vomiting,
    • hot flushes,
    • vaginal bleeding,
    • hypercalcemia,
    • and peripheral edema.
  36. Interferon alfa-2  -  MOA
    • Made by lymphocytes,
    • inhibits cell proliferation,
  37. Interferon alfa-2  -  Clinical use
    • hairy cell leukemia,
    • Kaposi’s sarcoma,
    • and hepatitis.
  38. Interferon alfa-2  -  Side effects
    • –Causes flu-like symptoms,
    • fatigue,
    • depression,
    • NVD
  39. Imatinib - MOA
    - the first member of a new class of drugs that act by specifically inhibiting an enzyme that is characteristic of a cancer cell rather than non-specifically killing all rapidly dividing cells.

     - inhibitor of the tyrosine kinase domain of the Bcr-Abl oncoprotein
  40. Imatinib - Clinical use
    Indication - chronic myelogenous leukemia (CML),

    •  - Given orally,
    •  - Metabolized by CYP3A4
  41. What does EGFR stand for?
    Epidermal growth factor receptor
  42. What is the anticancer drug classified as an
    Epidermal growth factor receptor inhibitor?
    Cetuximab
  43. Cetuximab - Clinical use
    metastatic colon cancer
  44. Cetuximab - Toxicity
    • Acneiform skin rash,
    • hypersensitivity,
    • and hypomagnesemia
  45. What does VEGF stand for?
    vascular endothelial growth factor

    •  - (VEGF) is one of the most important angiogenic growth factors. The growth of both primary and metastatic tumors requires an
    • intact vasculature. As a result, the VEGF-signaling pathway represents an
    • attractive target for chemotherapy.
  46. Bevacizumab - MOA
    • Bevacizumab is a recombinant humanized monoclonal antibody that targets all forms of VEGF-A.
    • This antibody binds to and prevents VEGF-A from interacting with the target VEGF receptors.
  47. Bevacizumab - Clinical use
    - can be safely and effectively combined with 5-FU-, irinotecan-, and oxaliplatin-based chemotherapy

    •   - in the treatment of 
    • metastatic colorectal cancer.
  48. Name 3 drugs used to treat renal cell cancer.
    • Sorafenib,
    • Sunitinib,
    • Pazopanib

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