Anti-Metabolites Flashcards
What enzyme does methotrexate bind?
Dihydrofolate reductase
What product is not formed when dihydrofolate reductase is inhibited?
Tetrahydrofolate
DHFR is an enzyme necessary in the production of what precursor molecule required for the S phase of DNA replication?
Purines
What must occur for methotrexate to be eliminated?
Polyglutamation
What is leucovorin used for?
Leucovorin can rescue the cell from the cytotoxicity of methotrexate
What is the MOA of pemetrexed?
Inhibition of thymidylate synthase
How can you reduce the extent of myelosuppression with pemetrexed?
Pre-treatment with B12 and folate
What is the MOA of cytosine arabinoside?
S-phase pyrimidine analog- undergoes sequential phosphorylation until it is a triphosphate and then is incorporated into the DNA.
Inhibits DNA polymerase and therefore chain elongation
How is cytosine arabinoside administered?
Approved for intrathecal administration
Which anti-metabolite causes photosensitivity and hyperpigmentation of the palms?
5-FU
5-FU can be replaced with which drug?
Capecitabine
Which drug must be reduced when administered with allopurinol?
6-mercaptopurine