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Flashcards in 3 - Antineoplastic Drugs Deck (29):
1

What are the 3 steps of carcinogenesis?

  1. Tranformation
  2. Proliferation
  3. Metastasis

2

What's the challenge in dose-limiting toxicities?

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

3

What's the mechanism of action for chemotherapy?

  • Interfere with cell proliferation
  • Relative selectivity against cancer cells

4

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)

5

What are the benefits of using combination chemotherapy?

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

6

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

7

What is the current emphasis on cancer chemotherapy on?

The use of drug combination therapy

8

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

9

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

10

What are the alkylating agents mechanism of action?

Transfer alkyl groups to important cell constituents 

11

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

12

What do Antimetabolites do?

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

13

What are the different classes of Antimetabolites?

  • Folic acid antagonists
  • Purine antagonists
  • Pyrimidine antagonists

14

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

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

15

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)

16

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

17

What are the common preps of Platinum complexes?

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

18

What are the toxicities associated with platinum-derived compounds?

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

19

What type of alkyloids are derived from the periwinkle plants?

Vinca Alkyloids

20

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

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

21

Where to hormonal agents act?

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

22

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

23

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

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

24

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

25

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

26

How do other antibiotic agents work?

  • Inhibit DNA and RNA synthesis

27

What are the indications for thalidomide (Thalomid)?

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

28

What are the systemic effects of chemotherapy?

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

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