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10 Cards in this Set

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Antimetabolties are CCS or CCNS?
CCS - target S phase
Methotrexate mechanism of action?
dihydrofolate reducatase inhibitor leads to decreased synthesis of thymidylate synthesis, purine nucleotides and amino acids.
Mercaptopurine and thioguanine mechanism of action?
Purine antagonists - prodrugs needs HPGRT to activate to cytotoxic form. inhibit denovo purine and pyrimdine synthesis
5-FU mechanism?
Pyrimidine antagonist - gets converted to FdUMP which inhibits thymidylate synthase (suicide inhibition)
methotrexate toxicity?
Myelosuppression, skin adn GI mucosa toxic reduced by folinic acid (leucovorin rescue). Pulmonary infiltrates.
leucovarin rescue with mtx?
Rescue with mtx - leucovorin needs to be actively tranported into cells to reduce mtx cytotoxicity. normal cells can transport it and cancer cells cannot.
Resistance to mercaptopurine?
Loss of HGPRT
Mercaptopurine toxicity?
Myelosuppression, cholestasis, pancreatitis, oral/GI ulcers. Allopurinol decreses tox. mostly well tolerated.
methotrexate resistance/
DHFR mutations and decreased polyglutamate formation
leucovorin and 5-FU/
enhances formation of ternary complex and thus efficacy of 5-FU. leads to increased toxicity in non-cancerous tissue.