Kaplan Section 8 - Cancer
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show | Anti-cancer drugs kill a fixed percentage of tumor cells (first order kinetics), not a fixed number per time. This is the rationale for drug combinations.
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show | FALSE. These drugs are more effective against tumors and cells that have a high growth fraction (cell POPULATIONS with a large percentage that is rapidly dividing -- e.g. bone marrow or active tumor cells).
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show | Drugs that act on cells that are actively proliferating.
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show | 66-CHEM: 6-mercaptopurine, 6-thioguanine, cytarabine, hydroxyurea, etoposide, methotrexate (cytotoxic to lymphocytes, used for RA)
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show | Bleomycin
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Name the drugs that are M-phase specific. | show 🗑
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Name the drugs that are G0-phase specific. | show 🗑
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What is the mechanism of methotrexate? | show 🗑
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How does the body develop resistance to methotrexate? | show 🗑
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What diseases would you use methotrexate for? | show 🗑
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Adverse effects of methotrexate | show 🗑
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What is leucovorin rescue? | show 🗑
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show | Alkylating agent - works in G0 Phase. A Prodrug that is converted to active forms in the liver. Forms DNA crosslinks between and within DNA strands at guanine N-7 positions --> dysfxnal DNA --> cell death.
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What would you use cyclophosphamide for? | show 🗑
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What are the adverse effects of cyclophosphamide? | show 🗑
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show | sudden onset of hematuria (blood in urine) combined with bladder pain and irritative bladder symptoms
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Why do pts get hemorrhagic cystitis on cyclophosphamide? | show 🗑
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show | Use Mesna (traps acrolein) or aggressive hydration for prophylaxis
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What is Cisplatin? | show 🗑
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show | 1. Traps the drug, 2. increases cell's ability to repair the damaged DNA.
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What would you use Cisplatin for? | show 🗑
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show | 1. Nausea, 2. Vomiting (use Odansetron), 3. Nephrotoxicity (use Amifostine), 4. Neurotoxicity (deafness)
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show | 1. An intercalator --> inhibition of macromolecular biosynthesis --> inhibits the progression of the enzyme topoisomerase II, which unwinds DNA for transcription --> stabilizes the topoisomerase II complex after it has broken the DNA chain for replication
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What would you use Doxorubicin for? | show 🗑
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Adverse effects of doxorubicin | show 🗑
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show | severe skin reaction that occurs when chemotherapy drugs (doxorubicin) administered during or soon after radiation treatment. The rash appears like a severe sun burn. Treatment = corticosteroids to reduce inflammation.
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show | A drug that protects from the cardiotoxic radical-formation effects of doxorubicin. It chelates iron and prevents the formation of free radicals.
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What is the mechanism of 6 mercaptopurine? | show 🗑
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How does the body develop resistance to 6-mercaptopurine? | show 🗑
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What would you use 6-mercaptopurine for? | show 🗑
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show | It's the prodrug that is metabolized to become 6-mercaptopurine
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What are the adverse effects of 6-mercaptopurine? | show 🗑
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show | Reduced activation of the prodrug.
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What is vincristine? | show 🗑
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What is vinblastine? | show 🗑
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show | 1. Hodgkin's lymphoma (ABVD, V = vinblastine), 2. testicular ca, 3.kaposi's sarcoma
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What diseases would you use vincristine for? | show 🗑
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show | 1. bone marrow suppression, 2. GI distress, 3. alopecia
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Adverse effects of vincristine. | show 🗑
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show | Anti-cancer drug. Complexing with Fe and O2 --> induce breaks in the DNA strand (G2 Phase)
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show | 1. Hodgkin's lymphoma (ABVD, B = bleomycin), 2. testicular ca, 3. head ca, 4. neck ca, 5. skin ca
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show | 1. pneumonitis, 2. pulmonary fibrosis, 3. mucocutaneous rxns (blisters), 4. alopecia, 5. hypersensitivity
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What is procarbazine? | show 🗑
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show | 1. decreased drug accumulation (by inc transports to get it out of cell OR by dec permeability to allow less in), 2. Production of chemicals that "trap" the drug
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For what disease would you use Procarbazine? | show 🗑
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show | 1. bone marrow suppression, 2. pulmonary toxicity, 3. hemolysis, 4. neurotoxicity, 5. leukemogenic
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show | Anti-cancer drug, anti-metabolite. Bioactivated --> inhibit thymidylate synthetase --> halt pyrimidine synthesis (can't make thymine)
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show | form enzymes that inactivate the drug
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What would you use 5-fluorouracil for? | show 🗑
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What are the adverse effects of 5-fluorouracil? | show 🗑
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show | 5-FdUMP
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What is Flucytosine? | show 🗑
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What parts of the body are most sensitive to cytotoxic cancer drugs? | show 🗑
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What is the cancer drug toxicity that is dose-limiting? | show 🗑
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Which drugs are particularly toxic to the kidneys? | show 🗑
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show | Cisplatin, Bleomycin, Vincristine, Asparaginase (B-VAC)
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Which drugs are particularly toxic to the liver? | show 🗑
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show | Bleomycin, Busulfan, Procarbazine
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Which drugs are particularly toxic to the heart? | show 🗑
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Which drugs are particularly toxic to the nerves? | show 🗑
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show | Cyclophosphamide, Cytarabine, Dactinomycin, Methotrexate
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Which drug causes hemorrhagic cystitis? | show 🗑
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Which drug causes secondary leukemia? | show 🗑
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show | Asparaginase
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