31 & 32 - Common Cancer Drugs Flashcards
alkylating agents - general what are they
strong electrophiles that form pos charged intermediates w/ target molecules and cause DNA damage
alkylating agents - mechanism
inhibit DNA synth / cell division by covalent attachment at 2 points
crosslinks DNA > cytotoxicity
example class and drug of alkylating agents
nitrogen mustards > cyclophosphamide
cyclophosphamide - category
alkylating agent > nitrogen mustard
cyclophosphamide uses
lymphoma regimens, breast cancer, ovarian cancer, some kinds of lung cancer
cyclophosphamide - AEs
myelosuppression (dose limiting)
alopecia, immunosuppression, cystitis
anitmetabolites - what are they
structurally related to natural compounds, compete for normal metabolites
folate antagonist mechanism
block biosynth of fully reduced tetrahydrofolic acid
example of folate antagonist
methotrexate
methotrexate mech
competitively inhibits folic acid binding to dihydrofolate reductase > death due to thymidylate and purine blockage; s-phase specific agent
uses of methotrexate
curative regimen for ALL, trophoblastic choriocarcinoma, Burkitt’s
methotrexate AEs
myelosuppression - dose limiting
renal insufficiency - c/i in pts w/ renal impairment
rescue drug for myelosuppression due to methotrexate
leucovorin
purine analogue mechanism
prevent biosynth of purine precursors
get incorporated into RNA/DNA > fraudulent nucleic acids made
require activation - “lethal synthesis”
ex of purine analogue
thioguanine (a thiolated purine analogue)
use of thioguanine
AML, ALL, CML
AEs of thioguanine
myelosuppression
ex of pyrimidine analogue
5-fluorouracil (halogenated pyrimidine)
uses of 5FU
CA of breast, stomach, COLON, rectum, pancreas, liver, ovary
short story: lots of solid tumors
major AE of 5FU
myelosuppression
hydroxyurea - mech
inhibits ribonucleoside diphosphate reductase
hydroxyurea - use
myeloprolif syndromes
CML
AEs of hydroxyurea
myelosuppression
anticancer abx - general mechanism
inhibit nucleic acid synth by blocking DNA replication or transcription either by direct binding to nucleic acid or polymerizing enzyme