Chemo drugs Flashcards by Tyler Boyd

What are the folate antagonists?

methotrexate and pemetrexed

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What is the MOA of methotrexate?

inhibits dihydrofolate reductase which results in blockage of thymidylate and purine synthesis

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What is the MOA of pemetrexed?

multi-targeted antifolate

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What are the ADRs of the folate antagonists?

myelosuppression
mucositis
renal tubular necrosis with high dose MTX
Hematologic toxicity - neutropenic sepsis

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What other disease states are the folate antagonists used for?

rheumatoid arthritis

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What should be supplemented with the folate antagonists?

folic acid and vitamin B12

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What is the rescue medicine for MTX?

leucovorin

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What are the pyrimidine antagonists?

fluorouracil, capecitabine, cytarabine, and gemcitabine

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What is the MOA of 5-FU?

inhibits thymidylate synthase, which inhibits formation of thymidine (affects DNA and RNA)

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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

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What is the MOA of gemcitabine?

pyrimidine antimetabolite that inhibits DNA synthesis by inhibition of DNA polymerase and ribonucleotide reductase

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What are the major ADRs of the pyrimidine antagonists?

myelosuppression
mucositis, stomatitis
diarrhea
hand-foot syndrome
cytarabine cerebellar toxicity
cytarabine rash and conjunctivitis

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What is the only oral pyrimidine antagonist?

capecitabine

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What is the reversal agent for 5-FU

uridine triacetate

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How do you treat cytarabine conjunctivitis?

steroid eye drops

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What is the major drug interaction with pyrimidine antagonists?

warfarin

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What are the purine antagonists?

fludarabine, thioguanine, and mercaptopurine

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What is the MOA of the purine antagonists?

analogues of purines which get incorporated into DNA to prevent functional DNA synthesis

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What are the ADRs of purine antagonists?

myelosuppression and liver toxicity

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What is the most immunosuppressive purine antagonist?

fludarabine

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What prophylaxis is required with fludarabine?

antiviral and bactrim

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What drug classes are the antimetabolites?

purine antagonists, pyrimidine antagonists, and folate antagonists

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What drug classes are the alkylating agents?

nitrogen mustard derivatives, platinum analogs, alkyl sulfonates

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What are the nitrogen mustard derivatives?

cyclophosphamide, ifosfamide, bendamustine, and mechlorethamine

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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?

1. myelosuppression 2. N/V 3. alopecia 4. infertility 5. hemorrhagic cystitis (acrolein) 6. 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

What are the platinum analogs?

Cisplatin, carboplatin, and oxaliplatin

What is the MOA of the platinum analogs?

form intrastrand and interstrand DNA cross-links; binds to nuclear and cytoplasmic proteins

What are the ADRs of cisplatin?

nephrotoxicity, ototoxicity, severe N/V, neuropathy, and electrolyte depression

What are the ADRs of carboplatin?

myelosuppression, moderate-severe N/V, and hypersensitivity

What are the ADRs of oxaliplatin?

Neuropathy, moderate-severe N/V, myelosuppression, and hypersensitivity

What is the antidote for cisplatin nephrotoxicity?

amifostine

When should cisplatin be avoided?

CrCl < 50

What can be used to treat platinum analog induced neuropathy?

duloxetine

What can be done to reduce ADRs associated with platinum analogs?

reduce the dose

What is the one alkylsulfonate?

busulfan

What is the MOA of busulfan?

cleavage of alkyl-oxygen bond and formation of a butyl compound that forms crosslinks with DNA

What are the ADRs of busulfan?

myelosuppression, pulmonary toxicity, and skin pigmentation

What is the MOA of bleomycin and dacarbazine?

binds to DNA, breaks single strand and double stand, leads to free radical formation and inhibits DNA synthesis

What are the ADRs of bleomycin?

pulmonary toxicity, hyperpigmentation, and febrile reactions

What are the ADRs of dacarbazine?

myelosuppression and N/V

What baseline test must be performed before initiating bleomycin?

pulmonary function test

What drug classes are enzyme inhibitors?

anthracyclines, epipodophyllotoxins, and camptothecans

What are the anthracyclines?

daunorubicin, doxorubicin, idarubicin, and epirubicin

What is the MOA of the anthracyclines?

1. topoisomerase II inhibition 2. Intercalation of DNA 3. Formation of free radicals

What is the MOA of cardiotoxicity in the anthracyclines?

generation of semiquinone free radicals and oxygen free radicals

What are the ADRs of the anthracyclines?

myelosuppression, cardiomyopathy, N/V, extravasation, red urine (daunorubicin and idarubicin)

What tests should be monitored with anthracyclines?

EKG, BNP, and EF

What is the antidote for doxorubicin for cardiotoxicity?

dexrazoxane

What type of cancer can the anthracyclines cause?

leukemia

What are the epipodophyllotoxins?

etoposide and tenoposide

What is the MOA of the epipdodphyllotoxins?

topoisomerase II inhibition

What are the ADRs of the epipodophyllotoxins?

myelosuppression, hypotension, and alopecia

What is the for oral etoposide?

2 x IV dose (poor bioavailability)

What other cancer can epipodophyllotoxins cause?

leukemia

What are the camptothecans?

ironotecan and topotecan

What is the MOA of camptothecans?

topoisomerase I inhibition which is responsible for cutting single DNA strands

What are the ADRs of camptothecans?

myelosuppression, alopecia, and diarrhea

What is the treatment for early onset diarrhea secondary to camptothecans?

atropine within 2-6 hours

What is the treatment for late onset diarrhea secondary to camptothecans?

high dose loperamide

What are the microtubule targeting drug classes?

taxanes and vinca alkaloids

What are the taxanes?

paclitaxel, docetaxel, and cabazitaxel

What are the vinca alkaloids?

vincristine, vinblastine, and vinorelbine

What is the MOA of the taxanes?

bind to tubulin and stabilize microtubules. This prevents depolymerization (freezes cell in anaphase/telophase)

What is the MOA of the vinca alkaloids?

binds to tubulin and interferes with microtubule assembly. Prevents spindle formation

What are the ADRs of the taxanes?

myelosuppression, hypersensitivity, alopecia, and peripheral neuropathy

What are the ADRs of the vinca alkaloids

myelosuppression, constipation, and extravasation

What are the ADRs associated with vincristine?

less myelosuppression but dose-dependent neurotoxicity

Which drug can not be given intrathecally?

vincristine