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Flashcards in 3 - Antineoplastic Drugs Deck (29):

What are the 3 steps of carcinogenesis?

  1. Tranformation
  2. Proliferation
  3. Metastasis


What's the challenge in dose-limiting toxicities?

To give an adequate dose to kill cancer cells without killing too many healthy cells


What's the mechanism of action for chemotherapy?

  • Interfere with cell proliferation
  • Relative selectivity against cancer cells


What is p53?

  • Transcription factor that regulates the cell cycle
  • Functions as a tumor suppressor
  • Cancers that express p53 are highly responsive to chemo (leukemias, lymphomas, testicular cancer)


What are the benefits of using combination chemotherapy?

  • Some regimens offer synergistic benefits
  • Typically use intermittent dosing
  • Reduces emergence of drug resistance


What are some examples of cancers that require combination chemotherapy?

  • Hodgkin's disease
  • Testicular cancer
  • Breast cancer
  • Ovarian cancer
  • Cervical cancer
  • Bladder cancer
  • Lung cancer
  • Cancer of the head and neck


What is the current emphasis on cancer chemotherapy on?

The use of drug combination therapy


How can drugs be broken down by the cell cycle they affect?

  • Cell-cycle specific - drug affects one phase
  • Cell-cycle non-specific - drug affects any/all phases


What are some important characteristics of chemotherapy drugs?

  • Not safe
  • Lack of specificity - affects normally proliferating cells (bone marrow, skin, intestinal mucosa)
  • Signs of toxicity appear in those areas


What are the alkylating agents mechanism of action?

Transfer alkyl groups to important cell constituents 


What are some examples of Alkylating Agents?

  • cyclophosphamide (Cytoxan) - multiple cancers, bone marrow transplants
  • ifosfamide (Ifex) - nitrogen mustard - multiple cnacers
  • procarbazine (Matulane) - Hodgkin's disease


What do Antimetabolites do?

  • Serve as fraudulent substrates for biochemical interactions
  • S Phase specific


What are the different classes of Antimetabolites?

  • Folic acid antagonists
  • Purine antagonists
  • Pyrimidine antagonists


What are the characteristics of Folic Acid Antagonists and whats the common preparation?

  • Inhibits DNA synthesis
  • Cell-cycle specific = S phase
  • methotrexate (Rheumatrex, Trexall)


What are the characteristics of Purine Antagonists and what's the common preparation?

  • Inhibits enzymes that convert hypoxanthine ribonucleotide to adenine and xanthine ribonucleotide
  • Cell-cycle specific = S phase
  • mercaptopurine (Purinethol)


What are the characteristics of Pyrimidine Antagonists and what are the common preparations?

  • Inhibit pyrimidine synthesis
  • fluorouracil (Adrucil) "5-FU" - many cancers
    • Interferes with DNA synthesis
  • cytarabine (Cytosar-U) "Ara-C" - blood cancers
    • Cell cycle specific = S phase


What are the common preps of Platinum complexes?

  • carboplatin (Paraplatin)
    • small-cell lung cancer, ovarian cancer
  • cisplatin (Platinol) 
    • bladder, testicular, ovarian cancers


What are the toxicities associated with platinum-derived compounds?

  • Myelosuppression
  • Nephrotoxicity
  • Neurotoxicity
  • Ototoxicity
  • Nausea/vomiting


What type of alkyloids are derived from the periwinkle plants?

Vinca Alkyloids


How do Vinca Alkyloids act? What are the common preps?

  • Inhibit mitotic division
  • M and S Phases (cell-cycle specific)
  • vinblastine (Valban)
  • vincristine (Oncovin)


Where to hormonal agents act?

Hormones interrupt cells in the G phase - reduction in the amount of circulating hormones


What are the different types of hormonal agents?

  • Estrogens - prostate/mammary CA
  • Androgens - mammary CA postmenopausal
  • Progestins - renal and endometrial CA
  • Glucocorticoids - hematologic, lymphomas
    • Prednisone


What type of drug is tamoxifen and what does it do?

  • Anti-estrogen, breast CA treatment/prevention
  • G0 & G1 phases
  • tamoxifen (Nolvadex)


What do antibiotics do in the chemotherapy drugs?

  • bind with DNA to inhibit cell division
  • Attack cells in different phases:
    • non-cell cycle specific
    • cell cycle specific
  • Most effective for solid mass tumors


What are the selected agents of antibiotics preparations?

  • bleomycin (Blenoxane)
    • G2, M
  • doxorubicin (Adriamycin)
    • S phase, Kaposi's sarcoma
  • daunorubicin citrate (DaunoXome) = HIV-associated Kaposi's sarcoma


How do other antibiotic agents work?

  • Inhibit DNA and RNA synthesis


What are the indications for thalidomide (Thalomid)?

  • Multiple myeloma
  • Crohn's
  • AIDS-related aphthous lesions
  • Classic model drug for teratogensis


What are the systemic effects of chemotherapy?

  • Suppression of bone marrow
  • GI disturbances
  • Dermatological reactions
  • Hepatotoxicity
  • Nephrotoxicity
  • Neurotoxicity
  • Immune deficiencies
  • Infertility