Antineoplastics #4

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mp
ID:
215243
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Antineoplastics #4
Updated:
2013-04-22 23:58:04
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Med Chem III Antineoplastics
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Antineoplastics #4
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  1. Topoisomerase Inhibitors
    create torsional stress, fragments DNA chains and destroys the cell
  2. Etoposide -- Etopophos and Teniposide -- Vumon
    • cell cycle specific
    • inhibits DNA topoisomerase II
    • prodrug -- 3A4
  3. Irinotecan -- Camptosar
    • inhibits topoisomerase I
    • 2000X more active metabolite
    • severe N/V
    • UGT1A1*28 -- will accumulate
  4. topotecan -- Hycamtin
    • inhibits topoisomerase I
    • don't give to pts with <1500 baseline neutrophil counts
  5. Hormone and Hormone Antagonists -- classes
    • androgens -- progestin
    • antiandrogens
    • GnRH analogs
    • Estrogens -- antiestrogens
    • Aromatase inhibitors
  6. Bicalutamide -- Casodex
    • antiandrogen
    • advanced prostate cancer
    • non-steroid competitive inhibitor
    • inhibits testosterone in peripheral tissue
    • causes gynecomastia
  7. Nilutamide -- Nilandron
    • antiandrogen
    • non-steroid that inhibits cellular uptake of T and nuclear binding
  8. Megesterol -- Megace
    • progestin
    • anti-leutinizing effect mediated by pituitary (centrally acting)
    • appetite stimulant in HIV related cachexia
  9. Medroxyprogesterone -- Depo-Provera
    • progestin
    • inhibits secretion of pituitary gonadotropin
  10. GnRH analogs -- drugs (4)
    • Leuprolide -- Lupron
    • Goserelin -- Zoladex
    • Triptorelin -- Trelstar Depot
    • Degarelix -- Firmagon
  11. Leuprolide -- Lupron
    • GnRH analog
    • decreased androgen production
    • add Casodex for peripheral inhibition
  12. Goserelin -- Zoladex and Triptorelin -- Trelstar Depot
    Advanced prostate cancer
  13. Degarelix -- Firmagon
    • prostate cancer
    • GnRH receptor antagonist
  14. Estermustine -- Emcyt
    • prodrug mustard alkylating agent
    • estrogen delivers site specific alkylating agent
  15. Anti-estrogens -- drugs
    • Tamoxifen -- Soltamox
    • Toremifene -- Fareston
    • Fulvestrant -- Faslodex
  16. Tamoxifen -- Soltamox
    • non-steroid anti-estrogen that competes with estradiol for estrogen receptors
    • most widely used RX for breast cancer
    • metab -- CYP2D6 (SSRIs)
  17. Toremifene -- Fareston
    • breast cancer
    • nonsteroid anti-estrogen that competes with estradiol for estrogen receptors
    • metab -- 3A4
  18. Fluvestrant -- Faslodex
    • steroidal estrogen antagonist -- down regulatesthe estrogen receptor protein
    • metab --3A4
  19. Aromatase inhibitors -- drugs (3)
    • Letrozole -- Femara
    • Anastrozole -- Arimidex
    • Exemestane -- Aromasin
  20. Aromatase inhibitors -- info
    • inhibitors of the aromatase enzyme
    • NO cross resistance -- can use exemestane if resistant to other 2
    • exemestane is a suicide substrate
    • exemestane is steroidal
  21. anastrozole -- Arimidex
    • gold standard
    • not effective for ER negative tumors
    • used when tamoxifen fails
  22. Sodium iodide (131I) -- Hicon
    • thyroid cancer and tx of hyperthyroidism
    • have to deplete iodine stores
  23. Sodium iodine (123I)
    • thyroid evaluation
    • electron capture decay -- diagnostic, short acting
  24. Strontium-89 Chloride -- Metastron
    • use normal toilet, no urinals to decrease transmission of radioactivity
    • mimics Ca2+, used for bone type cancers
  25. Brachytherapy -- radioactive implants
    • Pharmaseed
    • contain either Iodine-125 or Palladium-103
    • prostate cancer -- localized delivery

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