Chemotherapy 2 Flashcards
____________ include methotrexate, 5-fluorouracil, and 6-mercaptopurine
Antimetabolites
Methotrexate mimics _______ and inhibits ________
folic acid
dihydrofolate reductase
5-fluorouracil mimics _________
pyrimidines
6-mercaptopurine mimics _________
purines
Methotrexate, trimetrexate, and pemetrexed are _________
Folic acid analogs
Trimetrexate is _________
lipid soluble
__________ directly inhibits thymidylate synthase
Pemetrexed
Folic acid analogs are cell cycle specific targeting _______ phase
S
When methotrexate is in cell there will be _______ amounts of dihydrofolate and tetrahydrofolate in cell
small
Methotrexate combined with dactinomycin has great cure rate for __________
Choriocarcinoma
Used for maintenance in ALL children, less active in adult leukemias
Methotrexate and Pemetrexed
Minimizes toxic effects of folate depletion in cells. Bypasses metabolic block induced by methotrexate by administering cofactors and does not decrease anti-tumor activity of methotrexate
Leucovorin rescue
Cell cycle non specific, but mostly affects G1 and S phases.
Can cause Oral and GI ulcerations. Stop at earliest signs of stomatitis and diarrhea
Causes decreased DNA synthesis by inhibiting thymidylate synthase. Incorporated into RNA and DNA making it unstable with altered fns
5-Fluorouracil
Cell cycle specific at S phase.
Can cause oral ulceration (but less than 5-fluorouracil)
Inhibits DNA Pol alpha. Incorporated into DNA making it unstable, chain terminator
Cytarabine (cytostar)
Cell cycle non specific
Gemcitabine
5-fluorouracil gets metabolized into active agent ___________
fDUMP
FDUMP gets further broken down into ______ and ________
FUTP and FdUTP
FDUMP directly inhibits _______
Thymidylate synthase
Allopurinol inhibits ___________
Mercaptopurine