Anticancer Agents and Pharmacology
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Questions and Answers

What is the primary source of estrogen in postmenopausal women?

  • Pituitary gland
  • Peripheral aromatization (correct)
  • Adrenal glands
  • Ovarian synthesis
  • What is the effect of aromatase inhibitors on estrogen synthesis in postmenopausal women?

  • Increase estrogen synthesis
  • Totally eliminate estrogen synthesis
  • Have no effect on estrogen synthesis
  • Decrease estrogen synthesis (correct)
  • What is the mechanism of action of Trastuzumab?

  • It inhibits the expression of HER2 protein
  • It binds to HER2 sites and promotes cell proliferation
  • It stimulates the production of HER2 protein
  • It binds to HER2 sites and inhibits cell proliferation (correct)
  • What percentage of patients with metastatic breast cancer overexpress the HER2 protein?

    <p>25% to 30%</p> Signup and view all the answers

    What is the advantage of targeted therapy in cancer treatment?

    <p>It can attack specific cancer cells without harming normal cells</p> Signup and view all the answers

    What is the function of Anastrozole?

    <p>It inhibits the production of estrogen</p> Signup and view all the answers

    Where does peripheral aromatization take place?

    <p>Liver, fat, muscle, skin, and breast tissues</p> Signup and view all the answers

    What is the effect of Trastuzumab on cell proliferation?

    <p>It decreases the number of cells in the S-phase</p> Signup and view all the answers

    What is the advantage of using targeted therapy in combination with traditional chemotherapy?

    <p>It results in fewer severe adverse effects</p> Signup and view all the answers

    What is the target of Trastuzumab in breast cancer cells?

    <p>HER2 growth receptor</p> Signup and view all the answers

    Study Notes

    Anticancer Agents

    • Antimetabolites are structurally related to normal compounds that exist within the cell and interfere with the availability of normal purine or pyrimidine nucleotide precursors.

    Methotrexate

    • Mechanism: inhibits mammalian dihydrofolate reductase (DHFR), the enzyme that converts folic acid to its active, coenzyme form, tetrahydrofolic acid
    • Therapeutic uses: effective against acute lymphocytic leukemia, breast cancer, bladder cancer, and head and neck carcinomas, as well as inflammatory diseases such as severe psoriasis, rheumatoid arthritis, and Crohn disease
    • Adverse effects: depression, nausea, vomiting, bone marrow suppression

    Cyclophosphamide

    • Mechanism: alkylating agents that covalently bind to nucleophilic groups on various cell constituents, leading to DNA alkylation and cytotoxicity
    • Therapeutic uses: useful in many solid tumors due to its prominent immunosuppressant property
    • Adverse effects: alopecia, cystitis (due to acrolein)

    Doxorubicin

    • Mechanism: disrupts DNA function, inhibits topoisomerases (I and II), and produces free radicals
    • Adverse effects: irreversible, dose-dependent cardiotoxicity

    Vincristine

    • Mechanism: binds to microtubular protein-tubulin, prevents its polymerization and assembly of microtubules, causing disruption of mitotic spindle and interference with cytoskeletal function
    • Therapeutic uses: induces remission in childhood acute lymphoblastic leukemia
    • Adverse effects: peripheral neuropathy, alopecia

    Prednisone

    • Mechanism: potent, synthetic, anti-inflammatory corticosteroid
    • Therapeutic uses: induces remission in acute lymphocytic leukemia, and treats both Hodgkin and non-Hodgkin lymphomas

    Tamoxifen

    • Mechanism: estrogen antagonist with some estrogenic activity, classified as a selective estrogen receptor modulator (SERM)
    • Therapeutic uses: first-line therapy for estrogen receptor-positive (ER+ve) breast cancer, and prophylactically reduces breast cancer occurrence in high-risk women

    Anastrozole

    • Mechanism: aromatase inhibitor, decreases estrogen production in postmenopausal women
    • Therapeutic uses: treats estrogen receptor-positive breast cancer

    Targeted Therapy

    • Mechanism: targets specific pathways, processes, and proteins uniquely disrupted in cancer cells or the tumor microenvironment
    • Advantages: more effective treatments that can attack specific breast cancer cells without harming normal cells, with fewer severe adverse effects

    Trastuzumab

    • Mechanism: humanized monoclonal antibody, specifically targets the extracellular domain of the HER2 growth receptor
    • Therapeutic uses: treats HER2-overexpressing breast cancer and gastric cancer

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    Description

    Learn about different types of anticancer agents, including their mechanisms of action, clinical uses, and adverse effects. This quiz covers Methotrexate, Doxorubicin, Cyclophosphamide, Vincristine, Prednisone, Tamoxifen, and Anastrozole.

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