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11 Cards in this Set
- Front
- Back
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Fractional Kill hypothesis:
3 log kill/1 log regrowth principle: Anti-metabolite chemo drugs are active in which part of the cell cycle? Which drug classes are non-cell cycle specific? |
each dose of chemo kills the same fraction, not absolute number of cells
one cycle of chemo kills 3 log kill, 1 log regrowth, need multiple rounds to eradicate tumor S phase nitrogen mustards, cyclophosphamide, -platins, Abx (doxorubicin, daunorubicin) |
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What should you consider with drug combinations for chemo?
Explain MDR. Major cause of SE's with chemo drugs? |
different MOA, toxicities, optimal dosages/timing
treatment confers resistance to that drug and other (same class or unrelated) - via P-gp, MRP-1 rapidly dividing cells affected - hair, GI, bone marrow, poor wound healing |
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Examples and MOA of alkylating agents:
Major toxicities? Dose-limiting? Maximum suppression? |
Nitrogen mustard (cyclophosphamide, chlorambucil), alkylsulfonate (busulfan), platinum analogs (-platins)
bind to DNA, cause breakage, abnormal pairing, depurination hematopoietic, GI, immunosuppression; dose limiting is myelosupression - max is 10 d-4 weeks post-tx |
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Drug associated with sterile hemorrhagic cystitis:
Major cause of SHC? Prophylactic tx? Major use of busulfan? Adverse effects? |
cyclophosphamide
acrolein accumulation - tx with hydration, Mesna, bladder irrigation palliative tx of CML bone marrow hypoplasia, Hepatic Veno-Occlusive disease, skin pigmentation, pulmonary fibrosis |
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Which drugs are used to tx brain tumors because they cross the BBB?
Drug used for colon cancer and is associated with peripheral neuropathy and cold exposure dysesthesia: Major toxicity of cisplatin? DNA agent used to treat Hodgkin's: |
nitrosureas - carmustine, lomustine, semustine
oxaliplatin ototoxic, neurotoxic dacarbazine (DTIC) |
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Most common anti-metabolite drug against folate:
Higher doses require what? Major purine antagonist drugs used: Which inhibits AMP/GMP synthesis, and has a DI with allopurinol? Which alters RNA/DNA function? |
MTX
leucovorin rescue, urine alkalinization 6-Mercaptopurine, 6 thioguanine 6-MCP - xanthine oxidase breaks down 6-MCP, so allopurinol may cause toxicity 6-TG |
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Major pyrimidine antagonist drugs?
Major toxicity of 5-FU, continuous infusion and bolus? Major toxicities of cytarabine? Explain how 5-FU causes cell death: |
5-FU, capecitabine (oral 5-FU), cytarabine - used for AML
continuous - GI; bolus - myelosuppression myelosuppression, cerebellar toxicity (ataxia, speech changes) inhibits DNA synthesis via thymineless death |
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Drug class that inhibits/reverses tubulin polymerization, causes Metaphase arrest, cumulative neurotoxicity:
Vinca alkaloid with less toxic to bone marrow, no N/V, limited because of peripheral neuropathy: Topoisomerase II inhibitors: Topo I inhibitors: |
Vinca alkaloids (Vin-)
Vincristine etoposide, tenoposide camptothecins (topotecan, irinotecan) |
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Stabilizes microtubules, non-functional, given IV:
Taxane with toxicity of fluid retention: Premedication with taxanes should include what drug, and why? Dose limiting toxicity for taxanes? |
Taxanes (Paclitaxel, Doxetaxel)
Docetaxel diphenhydramine - hypersensitivity rxn bone marrow suppression |
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Bacterial enzyme, used for ALL:
MOA of anthracyclines? Signature toxicity? What can you give to reduce free radical damage? Major toxicity of bleomycin? Particularly effective against solid tumors, very toxic: |
asparaginase
block DNA Topo II - cardiotoxicity dexrazoxane pulmonary toxicity, fibrosis; little myelosuppression mitomycin C |
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Hormonal therapy is particularly effective for which cancers?
Anti-estrogen drugs? Androgen receptor antagonists for tx of prostate cancer? Used to treat melanoma, CML, dose limiting toxicity is myelosuppression: Used to differentiate APL (AML M3): |
breast, prostate, endometrial, adrenal cortex
tamoxifen, fulvestrant, toremifene fultamide, bicalutamide, nilutamide hydroxyurea ATRA |
