Chemo drugs Flashcards
What are the folate antagonists?
methotrexate and pemetrexed
What is the MOA of methotrexate?
inhibits dihydrofolate reductase which results in blockage of thymidylate and purine synthesis
What is the MOA of pemetrexed?
multi-targeted antifolate
What are the ADRs of the folate antagonists?
- myelosuppression
- mucositis
- renal tubular necrosis with high dose MTX
- Hematologic toxicity - neutropenic sepsis
What other disease states are the folate antagonists used for?
rheumatoid arthritis
What should be supplemented with the folate antagonists?
folic acid and vitamin B12
What is the rescue medicine for MTX?
leucovorin
What are the pyrimidine antagonists?
fluorouracil, capecitabine, cytarabine, and gemcitabine
What is the MOA of 5-FU?
inhibits thymidylate synthase, which inhibits formation of thymidine (affects DNA and RNA)
What is the MOA of cytarabine?
pyrimidine analog incorporated into DNA, but primary action is inhibition of DNA polymerase resulting in decreased DNA synthesis and repair
What is the MOA of gemcitabine?
pyrimidine antimetabolite that inhibits DNA synthesis by inhibition of DNA polymerase and ribonucleotide reductase
What are the major ADRs of the pyrimidine antagonists?
- myelosuppression
- mucositis, stomatitis
- diarrhea
- hand-foot syndrome
- cytarabine cerebellar toxicity
- cytarabine rash and conjunctivitis
What is the only oral pyrimidine antagonist?
capecitabine
What is the reversal agent for 5-FU
uridine triacetate
How do you treat cytarabine conjunctivitis?
steroid eye drops
What is the major drug interaction with pyrimidine antagonists?
warfarin
What are the purine antagonists?
fludarabine, thioguanine, and mercaptopurine
What is the MOA of the purine antagonists?
analogues of purines which get incorporated into DNA to prevent functional DNA synthesis
What are the ADRs of purine antagonists?
myelosuppression and liver toxicity
What is the most immunosuppressive purine antagonist?
fludarabine
What prophylaxis is required with fludarabine?
antiviral and bactrim
What drug classes are the antimetabolites?
purine antagonists, pyrimidine antagonists, and folate antagonists
What drug classes are the alkylating agents?
nitrogen mustard derivatives, platinum analogs, alkyl sulfonates
What are the nitrogen mustard derivatives?
cyclophosphamide, ifosfamide, bendamustine, and mechlorethamine
What is the MOA of the nitrogen mustard derivatives?
form DNA cross-links resulting in inhibition of DNA synthesis and function
What are the ADRs of the nitrogen mustard derivatives?
- myelosuppression
- N/V
- alopecia
- infertility
- hemorrhagic cystitis (acrolein)
- infections (bendamustine)
What is the antidote for bladder toxicity associated with the cyclophosphamide or ifosfamide?
hydration or mesna
What other type of cancer can alkylating agents cause?
leukemia