Pharmacology: Antineoplastics I - 2

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Pharmacology: Antineoplastics I - 2
2014-04-18 13:00:02
Pharmacology Antineoplastics

Pharmacology: Antineoplastics I - 2
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  1. What is the indication for Bisulfan (important to know)?
    • Used in combo w/ cyclophosphamide
    • For allogenic bone marrow transfers in chronic myelogenous leukemia
  2. What is the MOA of Bisulfan?
    • Cross links DNA
    • Like an alkylating agent
  3. What are the SEs for Bisulfan?
    • Bone marrow suppression
    • Pulmonary toxicity = fibrosis
  4. What is the MOA of carmustine (BiCNU)?
    • Alyklyates DNA
    • Carbamoylates proteins
  5. What are the side effects of Carmustine (BiCNU)?
    • N/V
    • Pulmonary fibrosis
    • BONE MARROW TOXICITY (thrombocytopenia, leukocytopenia)
  6. Why can Carmustine be used for Brain Cancer?
    • Highly lipophilic
    • Crosses the BBB
  7. What is the route of administration for Carmustine?
  8. What are the Nitrosureas?
    Camustine and Lomustine
  9. Can Bisulfan penetrate the BBB?
    Yes, but Brain cancer is not a normal indication
  10. What are the side effects of Bidulfan and the Nitrosureas?
    • Acute: N/V
    • Delayed: Myelosuppression, teratogenic, reproductive organ inhibition, high dose pulmonary toxicity (fibrosis)
  11. What treatment regimens is Dacarbazine (DTIC-Dome) used in?
    CHOP (C) and ABCD (D)
  12. What is the MOA for Dacarbazine (DTIC-Dome)?
    Metabolite is a Non-cell cycle specific alkylating agent
  13. By what route is Dacarbazine (DTIC-Dome) given?
  14. How is Dacarbazine (DTIC-Dome) activated?
    By liver microsomal enzymes
  15. What is Dacarbazine (DTIC-Dome) mainly used for?
    Melanoma, especially in combo with newer drugs
  16. What is the MOA for Temozolomide (Temodar)?
    • Metabolite acts as a non-cell cycle specific alkylating agent
    • (same as Dacarbazine)
  17. How is Temozolomide (Temodar) administered?
  18. What physiological functions need to be competent for Temozolomide (Temodar) to be activated?
    Liver microsomal enzymes
  19. What is the indication for Temozolomide (Temodar) and why?
    Lipophilic = brain tumors/cancer
  20. What is Bendamustine (Treanda) a derivative of?
  21. What is the MOA of Bendamustine (Treanda)?
    Alkylating agent that inhibits mitotic check points ( stops cell from entering mitosis)
  22. How is Bendamustine (Treanda) administered?
  23. What are the general indications for Bendamustine (Treanda)?
    Lymphoma and Leukemia
  24. Is Bendamustine (Treanda) a prodrug or active as is?
  25. Of Decarbazine, bendamustine and temozolamide, which has the longest half life?
  26. What are the Platinum coordination complexes (Alkylating-like agents)?
    • cisplatin (Platinol)
    • oxaliplatin (Eloxatin)¬†
    • carboplatin (Paraplatin)
  27. How are the Platinum coordination complexes (Alkylating-like agents) administered?
  28. What is the MOA of the platinum coordination complexes?
    • Pt- guanine DNA crosslinking
    • Inhibit DNA and RNA polymerase
  29. What is the main indication or Oxaliplatin?
    Colorectal cancer
  30. What two platinum coordination complexes have essentially the same indications?
    Carboplatin and Cisplatin
  31. What general type of cancers are platinum coordination complexes intended for?
    Solid tumors
  32. What is  common drug combination with platinum coordination complexes?
    • Cisplatin and 5-FU
    • Together they penetrate the BB well
  33. Dose Cisplatin penetrate the BBB well?
    No, needs 5-FU to open the membranes for it.