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Kaplan Section 8 - Cancer

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Question
Answer
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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