Pharmacology: Antineoplastics IV/V - 2

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kyleannkelsey
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271156
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Pharmacology: Antineoplastics IV/V - 2
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2014-04-19 19:15:54
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Pharmacology Antineoplastics IV
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Pharmacology: Antineoplastics IV/V - 2
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Pharmacology: Antineoplastics IV/V - 2
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  1. What is SERM?
    • Selective Estrogen Receptor Modulators
    • designer estrogens—
    • Exert both estrogenic and antiestrogenic actions on ER positive breast tumors
  2. What are the SERMs?
    • tamoxifen
    • fulvestrant
    • toremifene
    • raloxifene
  3. What SERMs have both estrogenic and anti-estrogenic activity?
    Tamoxifen, toremifene, and raloxifene
  4. What SERMs are only anti-estrogenic?
    Fulvestrant
  5. By what route is Tamoxifen (Nolvadex) given?
    Oral
  6. What I steh MOA of Tamoxifen (Nolvadex)?
    • Non-steroidal antiestrogen with both estrogen receptor antagonist and agonist properties ON BREAST CANCER TISSUES
    • Antagonist: prevents receptor stimulation by estradiol
  7. Why would some people be Tamoxifen (Nolvadex) resistant?
    They have PM expression of CYP2D6
  8. What are the Pharmacokinetics of Tamoxifen (Nolvadex)?
    • PRODRUG: CYP2D6 to active metabolites
    • Phenytoin accelerates metabolism
    • Ketoconazole, erythromycin inhibit metabolism
  9. What are the indications for Tamoxifen (Nolvadex)?
    • Pre- and post-menopausal breast cancer if estrogen receptors are present
    • Breast cancer prophylaxis
  10. What are the SE for Tamoxifen (Nolvadex)?
    • menopausal symptoms:
    • estrogen deficiency
    • nausea
    • hot flashes
    • Others (estrogenic effects):
    • thromobophlebitis,
    • endometrial cancer
    • maintain bone mineral density
  11. What is the route of administration for Fulvestrant (Faslodex)?
    IM
  12. What is the MOA for Fulvestrant (Faslodex)?
    • “Pure antiestrogen” –steroid structure
    • Derivative of tamoxifen
    • Binds to estrogen receptors which causes:
    • Prevention of estrogen binding
    • Downregulation
  13. What are the indications for Fulvestrant (Faslodex)?
    • Active against tamoxifen resistant strains.
    • Metastatic breast cancer in postmenopausal women
  14. What are the Side effects for Fulvestrant (Faslodex)?
    • GI disturbances
    • hot flashes
    • no thromboembolism
  15. How does Fulvestrant (Faslodex) compare to anaastrazole?
    As effective as anastrozole
  16. Does Fulvestrant (Faslodex) cause thromboembolism?
    No
  17. What is the route of administration for toremifene (Farston)?
    Oral
  18. What is the Mechanism of Action for toremifene (Farston)?
    Anti-estrogen receptor analog of tamoxifen
  19. What metabolizes toremifene (Farston)?
    CYP 450
  20. What are the indications for toremifene (Farston)?
    Postmenopausal metastatic breast cancer ER +
  21. What are the SEs for toremifene (Farston)?
    • Hot flashes
    • Thrombophlebitis
    • Endometrial cancer
    • Cross-resistance with other anti-estrogens
  22. Is toremifene (Farston) a good choice for a patient who is resistant to other SERMs?
    No, cross-resistant
  23. What is the MOA of raloxifene (Evista)?
    Blocks estrogen receptors on breast cancer cells thereby preventing receptor stimulation by estradiol
  24. What are the important pharmacokinetic parameters of raloxifene (Evista)?
    Extensive first-pass metabolism
  25. What are the indications for raloxifene (Evista)?
    • Osteoporosis
    • Approved as a postmenopausal prophylactic for breast cancer
  26. What are the SEs for raloxifene (Evista)?
    Hot flashes, thromboembolism, fetal abnormalities, no endometrial cancer
  27. What are the Aromatase Inhibitors?
    • anastrozole—nonsteroidal
    • letrozole—nonsteroidal
    • exemestane—steroidal
  28. Which Aromatiase inhibitors are steroidal?
    Exemestane
  29. Which Aromatiase inhibitors are non-steroidal?
    • anastrozole
    • letrozole
  30. What are the drug types used for Breast cancers?
    • SERMs
    • Aromatase Inhibitors
    • HER-2 receptor inhibitors
    • Anti-mitotic breast cancer drugs
  31. Why can’t you use Aromatase inhibitors in pre-menopausal women?
    They reduce estrogen and thus cause the Hypothalamus and pituitary to produce more LH, FSH and GTRH
  32. Can you use Aromatase inhibitors in pre- or post-menopausal women?
    ONLY POST
  33. What is the route of administration for anastrozole (Arimidex) and letrozole (Femara)?
    Oral
  34. What is the indication for anastrozole (Arimidex) and letrozole (Femara)?
    Approved for use against breast cancer in post menopausal women with ER positive breast tumors
  35. What is the MOA for anastrozole (Arimidex) and letrozole (Femara)?
    Interfere with aromatase which plays a critical role in the production of estrogen in postmenopausal women from androgen produced in the adrenal gland (not from ovaries)
  36. What are the Side effects of anastrozole (Arimidex) and letrozole (Femara)?
    • nausea,
    • hot flashes,
    • headache,
    • fewer adverse effects than tamoxifen (no estrogenic activity)
    • no significant thromboembolism,
    • arthritis,
    • bone density
    • Hypercholesteremia
  37. Do anastrozole (Arimidex) and letrozole (Femara) cause endometrial cancer?
    No
  38. Exemestane (Aromasin) has what route of administration?
    Oral
  39. What is the MOA for Exemestane (Aromasin)?
    • Irreversible, “suicide” inhibitor of aromatase,
    • LACK of cross-resistance with other non-steroidal aromatase inhibitors, anastrozole and letrozole
  40. If a patient is not successful on anastrazole or letrozole, could they use Exemestane (Aromasin)?
    Yes, not cross resistant
  41. What are the indications for Exemestane (Aromasin)?
    Metastatic breast cancer in postmenopausal women, ER+
  42. What are the SEs for Exemestane (Aromasin)?
    • Similar to other aromatase inhibitors:
    • nausea,
    • hot flashes,
    • headache,
    • fewer adverse effects than tamoxifen (no estrogenic activity)
    • no significant thromboembolism,
    • arthritis,
    • bone density
    • Hypercholesteremia
  43. What does HER-2 stand for?
    Human Epidermal Growth Factor Receptor 2
  44. What is the general mechanism of HER-2 inhibitors?
    • Biological Response Modifiers
    • Signal Transduction Inhibition Targeted Drug Therapy
  45. What HER2 inhibitors are available?
    • trastuzumab
    • lapatinib
  46. How is trastuzumab (Herceptin) administered?
    Infused
  47. What is the MOA of trastuzumab (Herceptin)?
    • Monoclonal antibody against the HER2 protein
    • Inhibits growth-promotion
    • Ligand for the HER-2/neu receptor found in 30% of breast cancer cells
    • Interferes with signal transduction and causes apoptosis
  48. What are the indications fro trastuzumab (Herceptin)?
    Breast cancer HER2 receptor positive
  49. What are the SE for trastuzumab (Herceptin)?
    • Flu like symptoms (fever, chill)
    • Cardiotoxicity (Main one to worry about)
    • Pulmonary events and potentially fatal allergic reactions
  50. Does trastuzumab (Herceptin) cause Bone marrow suppression?
    No
  51. Does trastuzumab (Herceptin) cause alopecia?
    No
  52. trastuzumab (Herceptin) is often used in combination with what other drugs and why?
    • trastuzumab, doxorubicin and cyclophosphamide followed by paclitaxel
    • Good SE complementation
  53. What is the route of administration for lapatinib (Tykerb)?
    Oral
  54. What is the MOA for lapatinib (Tykerb)?
    • Tyrosine kinase signal transduction inhibitor
    • Binds to the intracellular domain of the EGFR (ErbB1) and HER-2/neu (ErbB2) receptors and competes with ATP
    • Prevents phosphorylation = prevents receptor activation
    • Causes apoptosis and suppression of tumor cell growth
  55. What are the indications for lapatinib (Tykerb)?
    Breast cancer HER2 receptor positive
  56. What are the SE for lapatinib (Tykerb)?
    • GI (diarrhea)
    • skin
    • less cardiotoxicity than trastuzumab
    • myelosuppression
    • Drug-drug interactions with inducers and inhibitors of the CYP3A4

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