17. Anti-Cancer Agents Flashcards

1
Q

Cyclophosphamide

A

alkylating agent. causes DNA damage in various ways (can cross link DNA strands, bind groups…)

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2
Q

Odansetron

A

Serotonin receptor blocker, anti-emetic that makes use of alkylating agents much more bearable.

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3
Q

methotrexate

A

antimetabolite, inhibits DHFR, blocks DNA synthesis, only works in S phase

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4
Q

general, side effects?

A

nausea, vomiting, alopecia

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5
Q

Leucovorin: with methotrexate?

A

rescue body cells, still kill cancer cells

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6
Q

5-fluorouracil (5-FU)

A

binds thymidylate synthase, prevents purine synthesis

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7
Q

Leucovorin with 5-FU?

A

stabilizes binding to thymidylate synthase, enhances effect

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8
Q

vincristine

A

binds to protein tubulin, prevents mT assembly, M phase specific. NOT toxic to BM, can be combined with drugs that are

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9
Q

vinblastine

A

binds to protein tubulin, prevents mT assembly, M phase specific. toxic to bone marrow.

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10
Q

toxicity: vincristine v vinblastine?

A

vinc: NOT toxic to BM,
vinb: TOXIC to BM

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11
Q

taxol

A

binds to mTs, prevents normal mitosis

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12
Q

Velcade

A

proteasome blockade! binds proteosome, abnl proteins build up, apoptosis

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13
Q

Lenolidimide

A

immunomodulatory in a way we don’t understand. SE = neuropathy
very effective in multiple myeloma

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14
Q

G-CSF, GM-CSF, EPO

A

hematopoietic growth factors. prevent blood counts from dropping w chemo

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15
Q

IL2

A

biologic response modifier. give to pts to incr immune response to cancer

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16
Q

rituximab

A

monoclonal antibody, targets CD20, B cell NHL. then macrophage destroys cell.

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17
Q

5-Azacytidine

A

DNA methylation can –> cancer. this prevents methylation. tumor suppressor genes that may have been silenced will be turned back on.

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18
Q

biggest class of chemo drugs?

A

DNA damaging agents

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19
Q

in general, how do these drugs all work?

A

by inducing apoptosis in various ways

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20
Q

alkylating agents: phase? response curve?

A

phase non-specific. linear dose response.

21
Q

alkylating agents associated with high incidence of what?

A

secondary cancers (esp leukemia, lymphoma, MDS)

22
Q

cyclophosphamide: has to be activated? by what?

A

yes by the hepatic p450 system

23
Q

side effect of cyclophosphamide?

A

hemorrhagic cystitis. caused by acrolein.

24
Q

how to prevent cyclophosphamide-induced hemorrhagic cystitis?

A

MESNA, binds acrolein

25
Q

secondary malignancies are mos common with what drugs, treatments?

A

alkylating agents, XRT

26
Q

what is an antiemetic that can be combined with 5-HT inhibitors like odansetron?

A

aprepitant. blocks Substance P binding

27
Q

antimetabolite drugs have to act on drugs in what phase?

A

S phase

28
Q

what are ways tumor cells can become resistant to methotrexate?

A

decreased transport, gene amplification, mutation of DHFR

29
Q

methotrexate is also used for what?

A

immunosuppression in other diseases like RA, lupus, to prevent GVHD

30
Q

Cytarbine (ara-C)

A

nucleoside analog. inhibit DNA polymerase.

31
Q

Ara-C: phase specific?

A

S phase specific

32
Q

Ara-C most commonly used to treat what?

A

AML

33
Q

Ara-C: part of what chemo regimen?

A

given continuously for 7 days as part of the 7+3 regimen, with daunarubicin.

34
Q

Ara-C: what side effects?

A

acute cerebellar toxicity.

35
Q

topo inhibitors: what do they do?

A

cause single or double strand breaks.

36
Q

anthracycline antibiotics: what are the classic drugs of this group?

A

doxorubicin and daunarubicin

37
Q

anthracyclines: what do they do?

A

get right into the DNA strand, inhibit repl and mRNA synth. Topo II inhibitor as well.

38
Q

anthracycline antibiotics: side effects?

A

damage to the heart, vesicants. problems with IV sites

39
Q

Etoposide: mechanism

A

Topo II inhibitor

40
Q

Camptotheca: mechanism?

A

Topo I inh

41
Q

what can happen if we drive EPO too high with exogenous growth factors?

A

HTN, stroke

42
Q

ESA stands for what?

A

erythropoietin stim agent

43
Q

benefit of G-CSF?

A

counts will recover earlier, increases the max dose a patient can tolerate

44
Q

Gemtuzumab: target, disease?

A

CD33 (immature myeloid), AML

45
Q

Rituximab: target, disease?

A

CD20 (B lymphs), lymphoma

46
Q

tiuxetan: target, disease?

A

CD20 (B lymphs), NHL

47
Q

cetuximab: target, disease?

A

EGFR, colorectal, head, neck

48
Q

bevacizumab: target, disease?

A

VEGF, several