Pharmacology: Antineoplastics IV/V - 3

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  1. What drug is lapatinib (Tykerb) used in combo with?
  2. What are the Anti-Mitotic Breast Cancer Drugs?
    • ixabepilone (Ixempra)
    • eribulen mesylate (Halaven)
    • ixabepilone (Ixempra)
  3. What is the MOA for ixabepilone (Ixempra)?
    • Binds to beta tubulin subunits of microtubules
    • M phase cell-cycle specific
  4. What is the indication for ixabepilone (Ixempra)?
    Monotherapy or combo with capecitabine for metastatic breast cancer resistant to anthracyclines (like doxorubicin) and taxanes (like Paclitaxel or docetaxel)
  5. What are the side effects for ixabepilone (Ixempra)?
    • Myelosuppression (due to inhibition of mitosis)
    • GI
    • peripheral neuropathy
    • rash (hypersensitivity)
  6. What is the MOA for eribulen mesylate (Halaven)?
    • Microtubule inhibitor isolated from marine sponge
    • M phase specific
  7. What are the indications for eribulen mesylate (Halaven)?
    Metastatic breast cancer
  8. What are the SE for eribulen mesylate (Halaven)?
    Myelosuppression, GI, peripheral neuropathy
  9. What types of Prostate Cancer Drugs are availabale?
    • Androgen Receptor Antagonists
    • Gonadotropin Releasing Hormone agonist or Luteinizing Hormone-Releasing hormone agonists
    • Gonadotropin Releasing Hormone antagonist or Luteinizing Hormone-Releasing hormone antagonists
    • Non-hormonal drugs
  10. What are the Androgen receptor antagonists?
    • bicalutamide
    • flutamide
    • nilutamide
  11. What is the general mechanism of androgen receptor antagonists?
    • Stop testosterone from entering cells
  12. Which Androgen receptor antagonist binds the most tightly to angrogen receptors?
  13. Which Andorgen receptor has the longest half-life?
    bicalutamide (Casodex)
  14. Does bicalutamide or flutamide bind tighter to angrogen reeceptors?
    bicalutamide (Casodex) (though still less tightly than Nilutamide)
  15. What is the route of administration for bicalutamide (Casodex)?
    oral once a day
  16. bicalutamide (Casodex) is a derivative of what?
  17. What is the MOA of bicalutamide (Casodex)?
    Blocks androgen receptors primarily in prostate tumor cells depriving them of androgenic stimulation.
  18. What is the indication of bicalutamide (Casodex)?
    Metastatic prostate cancer
  19. What are the SE for bicalutamide (Casodex)?
    • Chemical castration:
    • Hot flashes, gynecomastia, vomiting, diarrhea, hepatotoxicity
  20. How is flutamide (Eulexin) taken?
    Orally 3 times a day
  21. What is the MOA of flutamide (Eulexin)?
    Blocks androgen receptors in tumor cells depriving them of androgenic stimulation
  22. What is the MOA of flutamide (Eulexin) ?
    Metastatic prostate cancer
  23. What are the SE for flutamide (Eulexin)?
    • Hot flashes,
    • gynecomastia
    • vomiting
    • diarrhea
    • hepatotoxicity
  24. What is the MOA for nilutamide (Nilandron)?
    Blocks all androgen receptors, including adrenal androgen receptors
  25. What is the indication for nilutamide (Nilandron)?
    Metastatic prostate cancer for patients with surgical castration
  26. Why is nilutamide (Nilandron) used in patients after surgical castration?
    Adrenal gland still produces testosterone
  27. What are the SE for nilutamide (Nilandron)?
    • GI
    • gynecomastia
    • hot flashes
    • difficulty in adapting to dark
    • pneumonia
  28. What are the Gonadotropin Releasing Hormone agonist or Luteinizing Hormone-Releasing hormone AGONISTS?
    • leuprolide (Lupron)
    • goserelin (Zoladex)
  29. What are the indications for leuprolide (Lupron) and goserelin (Zoladex)?
    Palliative care in Metastatic prostate cancer
  30. What is the MOA for leuprolide (Lupron) and goserelin (Zoladex)?
    • Suppresses androgen production in the testes
    • GnRH is continuously supplied
    • Inhibits the release of gonadotropin from the pituitary = downregulating testosterone synthesis
  31. Do leuprolide (Lupron) and goserelin (Zoladex) reduce adrenal androgens?
    No, only testicular
  32. Can you use leuprolide (Lupron) and goserelin (Zoladex) instead of surgical castration?
  33. Why would you want to use leuprolide (Lupron) and goserelin (Zoladex) with androgen receptor antagonist?
    To counteract testosterone flair
  34. What are the SE for leuprolide (Lupron) and goserelin (Zoladex)?
    Hot flashes, loss of libido, fatigue, nausea/vomiting, loss of muscle mass, increased adipose tissue, possible bone loss
  35. What hormone other than Testosterone do leuprolide (Lupron) and goserelin (Zoladex) inhibit?
  36. What is the Gonadotropin Releasing Hormone antagonist or Luteinizing Hormone-Releasing hormone ANTAGONIST?
    degarelix (Firmagon)
  37. What is the MOA for degarelix (Firmagon)?
    • Decreases production of testosterone
    • By blocking GnRH receptors in pituitary
    • Decreases release of LH and FSH
    • Deprives testes of stimulation needed for testosterone production
  38. What are the indications for degarelix (Firmagon)?
    Ppalliative advance prostate cancer in those patients not eligible for GnRH agonist or don’t want surgical castration
  39. What are the SE for degarelix (Firmagon)?
    No tumor flare, hot flashes, gynecomastia, POTENTIAL LONG QT SYNDROME, libido, impotence
  40. What are the Non-Hormonal Prostate Cancer Drugs?
    • estramustine (Estracyte)
    • ketoconazole
    • sipuleucel-T (Provenge)
  41. What is the MOA of estramustine (Estracyte)?
    • Conjugate of estradiol phosphate conjugated with a nitrogen mustard
    • Cell cycle specific in M phase
    • Inhibits microtubule structure, function and assembly
    • Active against estrogen receptor (-) tumor cells including prostate cancer cells
  42. Does estramustine (Estracyte) have alkylating activity?
  43. What are the indications for estramustine (Estracyte)?
    Hormone refractory, metastatic prostate cancer
  44. What is the MOA for sipuleucel-T (Provenge)?
    • Biological Response Modifier = Active Cellular Immunotherapy ( enhance immunoresponse)
    • Create an antigen presenting cell from patients own cells that present sipuleucel-T and reinfused back into the patient
    • Altered T Cells proliferate and attack cancer cells
  45. What are the SE for estramustine (Estracyte)?
    GI, thromboembolism (from the estradiol), gynecomastia
  46. What is the indication for sipuleucel-T (Provenge)?
    Asymptomatic or minimally symptomatic, metastatic, androgen-independent (hormone refractory) prostate cancer
  47. What are the SE for sipuleucel-T (Provenge)?
    Acute infusion reactions (fever, respiratory, fatigue, nausea, vomiting)
  48. What is the MOA of abiraterone acetate (Zytiga)?
    • Anti-androgen
    • Inhibits 17 α-hydroxylase (CYP17) more effectively than ketoconazole.
    • Enzyme required for androgen biosynthesis.
    • Inhibits in all tissues including testicles, adrenal gland and prostate tumors.
  49. abiraterone acetate (Zytiga) is used in combo with what else and why?
    • Prednisone due to increased mineralocorticoid levels from CYP17 inhibition
    • Co-administer with corticosteroid to counter increased production of mineralocorticoids
  50. What is the indication for abiraterone acetate (Zytiga)?
    Metastatic castration-resistant prostate cancer (androgen dependent), resistant to docetaxel.
  51. What is the pregnancy category of abiraterone acetate (Zytiga) ?
    Pregnancy category X
  52. What are the SE for abiraterone acetate (Zytiga)?
    Hypertension, hypokalemia, fluid retention, QT elongation, Joint and muscle discomfort
Card Set:
Pharmacology: Antineoplastics IV/V - 3
2014-04-19 23:17:35
Pharmacology Antineoplastics IV
Pharmacology: Antineoplastics IV/V - 3
Pharmacology: Antineoplastics IV/V - 3
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