Lecture 2 - Cancer standard agents Flashcards by Brendan Knapp

busulfan, cyclophasphamide, and the nitrosureas are all ______. they act when during the cell cycle?

alkylating agents;
all times (cell cycle non specific)

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alkylating agents in general do what to DNA?

form cross links –> prevent DNA replication/transcription –> apoptosis

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name 3 nitrosureas

carmustine, lamustine, streptozocin

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the nitrosureas require bioactivation via liver _______. they are very _______ and are used to treat what kind of tumors?

hydroxylation;

lipophillic, brain tumors (ie cross BBB)

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main side effect of nitrosureas:

CNS toxicity –> convulsions, dizziness, etc

bone marrow suppression, hepatotoxic, and pulm toxic according to notes

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cyclophosphamide:
activated or degraded by CYP450?
crosslink DNA at what specific molecule?

activated;

guanine N7

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cyclophosphamide:

can cause _______ (heme thing), _____ ____ which is prevented by _____

myelosuppression, hemorrhagic cystitis, mesna (binds toxic metabolites)

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cyclophosphamide:
what is its toxic metabolite?
other side effects include ____ ( a cancer), _____ (an endocrine thing), and _____ (reproductive thing)

acrolein;
bladder cancer (TCC), SIADH, infertility

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_______ is a slow acting nitrogen mustard that is the drug of choice for _____ lymphocytic leukemia

chlorambucil, chronic

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busulfan:
mainly used to treat ____ and for bone marrow ablation. most important side effect = ____. also can cause pulm fibrosis and _____ changes

CML;
severe bm suppression;
skin (ie hyperpigmentation)

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name 3 anti-tumor antibiotics

bleomycin, dactinomycin (actinomycin D), doxorubicin

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doxorubicin:

mechanism of action = ______ and ______

generates free radicals;

intercalates DNA–>DNA strand breaks

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doxorubin:

causes dose dependent ______ (most important toxicity) and _____ (heme thing)

cardiotoxicity (dilated cardiomyopathy);

myelosuppression

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mitoxantrone:

_____ inhibitor that induces DNA double strand breaks. similar to doxorubicin

topoisomerase II

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bleomycin:
mechanism of action =
when does it act in the cell cycle?

free radical formation –> DNA strand breaks;

G2 (also M phase)

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bleomycin:
mainly used for what 2 cancers?
most imp side effect - _____ _____;
also causes _____ changes

testicular cancer, lymphomas;

pulmonary fibrosis, skin (ie hyperpigmentation, atrophic striae)

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actinomycin D:
mechanism of action -
main side effect -

intercalates DNA;

myelosuppression

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cisplatin, carboplatin, and oxaliplatin are all _____ derivatives. they work by _______

platinum;

cross-linking DNA

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cisplatin is especially effective in ____ and _____ cancers.

testicular, ovarian

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3 important toxicities for cisplatin:

nephrotoxic, neurotoxic, ototoxic

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how to prevent nephrotoxicity of cisplatin?

what does carboplatin cause?

adequate hydration/saline diuresis (also diuretics);

myelosuppression

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oxaliplatin is mainly used to treat _____

colorectal cancer

rade side effects

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what cell cycle phase do the antimetabolites act in?

Study These Flashcards

S-phase

methotrexate is a _____ analog that competitively inhibits _____ = decreased _____ synthesis and decreased DNA synthesis

Study These Flashcards

folic acid;
dihydrofolate reductase, dTMP

used to treat lots of things

MTX side effects: mucositis ie _____; _______ which is reversible with _____ rescue; ____ toxicity

mouth ulcers; myelosuppression, leucovorin (folinic acid); hepato

MTX side effects: pulmonary ______; _____ anemia

fibrosis; | megaloblastic

6 mercaptopurine is a _____ analog. it is the active metabolite of _____

purine; | azathioprine;

6-mercaptopurine: activated by ______ (an enzyme); what other drug causes increased toxicity with 6-MP?

HGPRT; | allopurinol (inhibits XO)

6-MP: mainly used to treat what cancer? side effects = _____ (heme), _____ (a GI thing), and ____ toxicity

acute leukemia bm suppression/pancytopenia; pancreatitis; liver

clofarabine is a _____ analog that inhibits ______ and ribonucleotide reductase. used to treat ______

purine; DNA polymerase; acute leukemia

5-FU and cytarabine are _____ analogues

pyrimidine

5FU: | bioactivated to _____ which inhibits ______. _______ is a pro-drug with similar activity.

5-FdUMP; thymidylate synthase; | capecitabine

5-FU: | mainly used to treat _____ and _____ cancer and topically, _______

colon, pancreatic; | basal cell

5-FU: | side effects = _____ (heme thing). severe _____ (GI), and ______ (Skin)

bm suppression; diarrhea; palmar-plantar erythrodyesthesia also photosensitivity

cytarabine inhbibits ________. mainly used to treat _____ and ______.

DNA polymerase; | leukemia, lymphoma

cytarabine: | side effect = _____

bm suppression, pancytopenia

raltitrexexd and pemetrexed inhibit _____. can be used to treat malignant _______

thymidylate synthetase; | mesothelioma

gemcitabine: _______ analog that inhibits DNA polymerase and also ____ ____; main side effect is ______

pyrimidine; ribonucleotide reductase; myelosuppression

etoposide/teniposide: inhibit ______; active when during the cell cycle?

topoisomerase II; | S and G2

etoposide/teniposide: mainly used to treat _____ and _______ (Solid tumors) + heme tumors; 2 side effects

testicular, small cell lung cancer; | myelosuppression, alopecia

hydroxyurea: | inhibits _______. acts during what phase of the cell cycle?

ribonucleotide reductase; | s-phase

hydroxyurea: | used to treat ______ disorders, _____ _____ anemia, and melanoma

myeloproliferate (ie CML); sickle cell

hydroxyurea can cause severe ______

myelosuppression

microtubule inhibitors include what 2 drugs? | when are they active?

paclitaxel/other taxols; vincristine/vinblastine; M phase (mitosis)

vincristine and vinblastine bind _____ and effect polymerization how?

beta tubulin; | inhibit polymerization into microtubules

vinblastine is used to treat _____ cancer and _____ lymphoma

testicular; | hodgkin

vincristine is used to treat solid tumors, ____ lymphoma, and leukemias; main side effect =

non-hodgkin; neurotoxic--peripheral neuropathy, constipation

vinblastine is less neurotoxic but causes _____

bone marrow suppression

______ is used in advanced breast cancer and is first line treatment for advanced nonsmall cell lung cancer

vinorelbine

taxanes (taxol) mechanism of action?

hyperstabilize polymerized microtubules (ie prevent depolymerization)

taxols are used to treat what 2 types of cancer?

breast, ovarian

taxols can cause _____ and _____

myelosuppression, peripheral neuropathy

L-asparginase: | used to treat _____ mainly.

ALL

mitotane: | intereferes with synthesis of adrenocortical steroids and is used to treat tumors of the _____

adrenal cortex

irinotecan and topotecan are camptothecins that inhibit _____. they are active when during the cell cycle?

topoisomerase 1; | S phase and G2

irinotecan is mainly used to treat ____ cancer. topotecan treats _____ and _____ cancer

colon; | ovarian, small cell lung cancer

Lecture 2 - Cancer standard agents Flashcards

(56 cards)