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Pharmacology 2 > 3 - Antineoplastic Drugs > Flashcards

3 - Antineoplastic Drugs Flashcards

1
Q

What are the 3 steps of carcinogenesis?

A
  1. Tranformation
  2. Proliferation
  3. Metastasis
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2
Q

What’s the challenge in dose-limiting toxicities?

A

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

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3
Q

What’s the mechanism of action for chemotherapy?

A
  • Interfere with cell proliferation
  • Relative selectivity against cancer cells
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4
Q

What is p53?

A
  • 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)
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5
Q

What are the benefits of using combination chemotherapy?

A
  • Some regimens offer synergistic benefits
  • Typically use intermittent dosing
  • Reduces emergence of drug resistance
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6
Q

What are some examples of cancers that require combination chemotherapy?

A
  • Hodgkin’s disease
  • Testicular cancer
  • Breast cancer
  • Ovarian cancer
  • Cervical cancer
  • Bladder cancer
  • Lung cancer
  • Cancer of the head and neck
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7
Q

What is the current emphasis on cancer chemotherapy on?

A

The use of drug combination therapy

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8
Q

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

A
  • Cell-cycle specific - drug affects one phase
  • Cell-cycle non-specific - drug affects any/all phases
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9
Q

What are some important characteristics of chemotherapy drugs?

A
  • Not safe
  • Lack of specificity - affects normally proliferating cells (bone marrow, skin, intestinal mucosa)
  • Signs of toxicity appear in those areas
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10
Q

What are the alkylating agents mechanism of action?

A

Transfer alkyl groups to important cell constituents

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11
Q

What are some examples of Alkylating Agents?

A
  • cyclophosphamide (Cytoxan) - multiple cancers, bone marrow transplants
  • ifosfamide (Ifex) - nitrogen mustard - multiple cnacers
  • procarbazine (Matulane) - Hodgkin’s disease
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12
Q

What do Antimetabolites do?

A
  • Serve as fraudulent substrates for biochemical interactions
  • S Phase specific
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13
Q

What are the different classes of Antimetabolites?

A
  • Folic acid antagonists
  • Purine antagonists
  • Pyrimidine antagonists
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14
Q

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

A
  • Inhibits DNA synthesis
  • Cell-cycle specific = S phase
  • **methotrexate **(Rheumatrex, Trexall)
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15
Q

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

A
  • Inhibits enzymes that convert hypoxanthine ribonucleotide to adenine and xanthine ribonucleotide
  • Cell-cycle specific = S phase
  • mercaptopurine (Purinethol)
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16
Q

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

A
  • 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
Q

What are the common preps of Platinum complexes?

A
  • carboplatin (Paraplatin)
    • small-cell lung cancer, ovarian cancer
  • cisplatin (Platinol)
    • bladder, testicular, ovarian cancers
18
Q

What are the toxicities associated with platinum-derived compounds?

A
  • Myelosuppression
  • Nephrotoxicity
  • Neurotoxicity
  • Ototoxicity
  • Nausea/vomiting
19
Q

What type of alkyloids are derived from the periwinkle plants?

A

Vinca Alkyloids

20
Q

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

A
  • Inhibit mitotic division
  • M and S Phases (cell-cycle specific)
  • vinblastine (Valban)
  • vincristine (Oncovin)
21
Q

Where to hormonal agents act?

A

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

22
Q

What are the different types of hormonal agents?

A
  • Estrogens - prostate/mammary CA
  • Androgens - mammary CA postmenopausal
  • Progestins - renal and endometrial CA
  • Glucocorticoids - hematologic, lymphomas
    • Prednisone
23
Q

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

A
  • Anti-estrogen, breast CA treatment/prevention
  • G0 & G1 phases
  • tamoxifen (Nolvadex)
24
Q

What do antibiotics do in the chemotherapy drugs?

A
  • 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
Q

What are the selected agents of antibiotics preparations?

A
  • bleomycin (Blenoxane)
    • G2, M
  • doxorubicin (Adriamycin)
    • S phase, Kaposi’s sarcoma
  • daunorubicin citrate (DaunoXome) = HIV-associated Kaposi’s sarcoma
26
Q

How do other antibiotic agents work?

A
  • Inhibit DNA and RNA synthesis
27
Q

What are the indications for thalidomide (Thalomid)?

A
  • Multiple myeloma
  • Crohn’s
  • AIDS-related aphthous lesions
  • Classic model drug for teratogensis
28
Q

What are the systemic effects of chemotherapy?

A
  • Suppression of bone marrow
  • GI disturbances
  • Dermatological reactions
  • Hepatotoxicity
  • Nephrotoxicity
  • Neurotoxicity
  • Immune deficiencies
  • Infertility
29
Q
A

Pharmacology 2 (21 decks)

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