Cancer Pharm Flashcards
mechlorethamine - how is it broken down?
non-enzymatic hydrolysis
mechlorethamine SE
myelosupression = dose-limiting
high incidence of secondary cancers (leukemia, lymphoma, MDS)
mechlorethamine MOA
alkalating agent
damages DNA in 4 ways: cross-linking, abnormal pairing w/ T residues, ring cleavage, depurination
cyclophosphamide (MOA and PK)
alkalating agent
activated by CYP450
cyclophosphamide SE
hemorrhagic cystitis - b/c metabolite acrolein in urine
MESNA
used to tx hemorrhagic cystitis from cyclophosphamide
binds to and inactivates acrolein
cisplatin (MOA and indication)
bifunctional alkating agent
used widely for lung, breast, ovarian, head & neck cancers
cisplatin SE
renal insufficiency
neuropathy
ondansetron (zofran) MOA
blocks 5HT stem of vagal nerve (maybe CNS too) –> prevents nausea
aprepitant
neurokinin 1 agonist. blocks substance P binding –> antiemetic, can be combined w/ ondansetron
methotrexate MOA
analogue of folic acid, inhibits DHFR by competitive inhibition
methotrexate SEs
marrow suppression, GI tox, renal failure
prevent renal failure w/ alkalinized urine
what do you give concurrently w/ really high dose of MTX to prevent lethal side effects?
leucovorin rescue
5 Fluoroucil (MOA and indication)
inhibits thymidylate synthase by suicide mech
indications: breast and GI malignancy
leucovorin action w/ 5FU
potentiates action of 5FU