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41 Cards in this Set
- Front
- Back
what does MDR stand for in tumor drug resistance?
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multiple drug resistance
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explain the MDR theory of chemotherapy drug resistance?
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P-glycoprotein, an ATP dependent glycoprotein that spits out drugs from cell thus cells with more P-glycoprotein survive chemotherapy and repopulate to make a chemotherapy resistant tumor
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which cell cycle does this drug effect?
Antimetabolites and folate pathway inhibitors |
S
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which cell cycle does this drug effect?
Topoisomerase inhibitors |
S and G2
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which cell cycle does this drug effect?
Antitumor Antibiotics |
G2
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which cell cycle does this drug effect?
Inhibitors of microtuble function |
M
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which cell cycle does this drug effect?
Alkylating agents and platinum complexes |
All phases
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which cell cycle does this drug effect?
Glucocorticoids |
G1
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a newly palpable tumor contains how many cells?
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10^9 and wieghs 1 gram
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how big does a tumor get when it kills someone?
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10^12 and wieghs 1 kilogram
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what does methotrexate inhibit?
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dihydrofolate reductase
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what does the body use folate for?
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1-carbon transfers such as methylation to produce certain amino acids for DNA synthesis
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what is the enzyme which facilitates the conversion of dUMP to dTMP?
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thymidylate synthase
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what reduces DHF to tetrahydrofolate?
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dihydrofolate reductase
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what does thymidylate synthase
use as a carbon source for iits methylation of dUMP? |
tetrahydrofolate
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what is the one drug which inhibits ribonucleotide reductase?
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hydryxuria
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what is the specific side effect seen with methotrexate that is not really seen with the other chemo drugs
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liver cirrhosis
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methotrexate closely resembles what vitamine?
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folic acid
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why is methotrexate used more often then most other chemo drugs?
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it is less mutagenic
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what is the rescue drug (antidote) for methotrexate?
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LEUKOVORIN (FOLINIC ACID)
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why does LEUKOVORIN (FOLINIC ACID) restore levels of dTMP?
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it replaces the depleted tetrahydrofolate that have been depleted by the inhibition of dyhrofolate reductase by methotrexate
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what is the drug that irreversibly blocks thymidylate synthase activity by acting like dUMP, but is incapable of being methylated into dTMP?
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5-FLUOROURACIL (5-FU) which is then metabolized to FdUMP
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what is the main toxicity associated with 5-FU?
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stem cell toxicity, thus it is only used in hard to treat cancers such as breast and colon
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what is the enzyme that converts thioguanine to its nucleotide form to block DNA sysnthesis?
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hypoxanthine-guanine phosphoribosyl transferase(HGPRT)
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what enzyme does allopurinal inhibit and why is this a problem?
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xanthine oxidase, it is the enzyme which metabolizes 6-MP, so if its inhibited 6-MP levels become toxic
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what is the drug that is recognized as adenosine, but isnt?
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pentostatin
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what does pentostatin inhibit?
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adenosine deaminase
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what does the increase in adenosine levels cause to happen in the body?
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it is very toxic to lymphocytes so people become severely immunocompromised
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what are CLADRIBINE and FLUDARABINE?
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Purine look-a-likes that stop DNA synthesis
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what is CLDRIBINE most useful for treating?
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hairy cell leukemia
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what is FLUDARABINE best for treating?
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lympho-proliferative disorders
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what are the two cytodine look-a-likes that block DNA synthesis?
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1. 5-AZACYTIDINE
2. CYTARABINE OR CYTOSINE ARABINOSIDE (ARA C) |
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what is ARA C best used to treat?
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Acute Myelogenous Leukemia (AML, very myelotoxic
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what are two examples of POLY-FUNCTIONAL BIS-ALKYLATING AGENTS?
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CYCLOPHOSPHAMIDE AND BCNU
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where does crosslinking occur mostly?
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N-7 on guanine
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given CYCLOPHOSPHAMIDES destructive nature in regards to DNA damage, why can it be given orally and not damage tissue on its way through the body and GI tract?
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it is a pro-drug which must first be turned on in the liver
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bladder damage (hemorrhagic cystitis) decreased with the use of CYCLOPHOSPHAMIDE by co-administration of ___ antidote which binds drug locally in bladder?
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Mesna
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what is the highly toxic metabolite of CYCLOPHOSPHAMIDE that Mesna binds in the bladder?
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Acrolein
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explain how resistance can be developed against ALKYLATORS?
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increased content of glutathione scavenger, increased repair enzyme, decreased drug uptake
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what is a major side-effect/toxicity of using ALKYLATORS?
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MUTAGENIC AND CARCINOGENIC
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how do CISPLATIN AND CARBOPLATIN disrupt DNA?
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they allow guanines on the same chain to bind with each other for intra-strand bonds
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