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cisplatin was discovered by applying an electrical field to- |
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cisplatin is curative for- |
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cisplatin prolongs survival in? also used in-4 |
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Definition
ovarian cancer head, neck, baldde,r lung |
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what is the most freq used anticancer agent |
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cisplatin has what toxicites- |
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what other drugs have similar effiacy but less ADEs- |
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how are platinum agents similar to alkylating |
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Definition
they are displaced by nucelophillic attacks to form covalent bonds |
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what is the target of cisplatin |
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what platinum drug is used with 5-FU for colon cancer |
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why are trans-platinums inactive? |
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Definition
inability of the isomers to form DNA cross links |
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Cisplatin formed more intra/interstrand cross links |
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Definition
90% intrastrand (the trans-cis does inter) |
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carboplatin has less _ than cisplt? 3 has more?3 |
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Definition
nephrotox (subst Cl), neurotox, N/V stability and Pk predictability, marrow tox |
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the majority of adducts formed by cisplt and carboplat? what is 2nd? |
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Definition
G-G intrastrand XL 60% A-G intrastrand XL |
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what crosslinks account for cytotoxicity of platinum drugs? |
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diff in oxiplatin adducts from the tohers-2 what does it look like? |
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Definition
hydrophobic bulkier DNA-protein XL (not strnad) |
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consequences of DNA adduct-2 |
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Definition
preoteins that participate in DNA rxns may become abnormal processes controlled by proteins that recognize damaged DNA may be activated |
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cisplatin: high/low prot bound? half life? eliminated thru? |
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look at slide 13 for a quick overview of cisplatin before test |
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the diff in pk for cicplt and carboplt is |
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slower conversion of carboplatin to reactive subst |
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disspaereance of platinum after carboplatin IVs is biphasic- occurs in _ min |
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the clearence of carboplatin is closely related to? |
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dosing of carboplatin is done by? |
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carboplatin might have _ cleaving it to beocme more active in cells than IV |
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half life of inital and terminal phases for oxiplatin |
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oxiplatin has prolonged retention where |
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unlike cisplaitin, oxalpplatin doesnt accum after courses, this means: |
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oxiplatin is excreted mianly by |
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toxicites for oxiplatin are when its added to flurouricil : 3 |
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myleosuppre, stomatitis, neuropathy |
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can prevent nephrotox of cisplatin with |
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look at slide 18 for table overview of toxicite sof the agents! |
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tumor resistance pathways-3 |
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Definition
glutathione conjugation (by adenosine triphosphates) metallothioneins and other sulfahydryls inactivate it increase platinum-DNA adduct repair/ damage tolerance |
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what are the sufahydrl groups used to prevetn platinum ADes-3 |
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Definition
MESNA sodium thiosulfate amifostine |
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