Chemotherapeutics: Antimetabolites Flashcards
irreversibly and competitively binds DHF reductase
methotrexate
brings folate cycle to halt
methotrexate
builds up DHF
methotrexate
what phase is methotrexate most effective in
S phase
what does methotrexate treat
RA and cancer therapy drugs
Adverse effects of methotrexate
megaloblastic anemia, myelosuppression, pulmonary fibrosis, hepatotoxicity, alopecia, mucositis
what reduces the toxic affects of methotrexate
Leucovorin (called leucovorin rescue)
Leucovorin is also called
Folinic acid
how does Leucovorin work
restores active folate stores
inhibits thymidylate synthase
5-Flourouracil (5-FU)
block thymidine production
5-Flourouracil
causes increased dUMP
5-Flurouracil
what does 5-Flurouracil treat
colon cancer
leucovorin rescue works for 5-FU toxicity true/false
false
5-Flourouracil side effects
severe diarrhea, photosensitivity, myelosuppression, hyper pigmentation
blocks synthesis of IMP
Azathioprine and 6-MP
prodrug of 6MP
Azathioprine
Azathioprine converted to 6MP by what enzyme
Hypoxanthine-Guanine Phosphoribosyl Transferase (HGPRT)
What phase does Azathioprine arrest cells in
S Phase
Side effects of Azathioprine
myelosuppression