Antineoplastic Agents II Flashcards

1
Q

primary resistance

A

absence of response on first exposure

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2
Q

acquired resitance

A

develops in response to eposure to give chemo drug

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3
Q

multidrug resistance

A

increased MDR1 gene
-cell surface transporter glycoprotein

ATP dependent pump of anthracyclines, vinca alkyloids, etoposide, paclitaxel, dactinomycin

may be inhibited by CCBs such as verapamil

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4
Q

toxicity

A

major sites of toxicity - high growth fraction cells - BM, GI tract, hair follicles, buccal mucosa, sperm forming cells

also - mutagenic - so may cause cancer

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5
Q

nadir

A

low point blood counts reach this after 10-14 days after chemo treatment

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6
Q

most regimens

A

given in cycles of 21-28 days

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7
Q

nitroureas

A

longer period of recovery - given every 6 weeks

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8
Q

GM-CSF

A

sargramostim

given to minimize neutropenia

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9
Q

G-CSF

A

filgrastim and pegfilgrastim

given to minimize neutropenia

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10
Q

oprelvekin

A

platelet growth factor

-given to counteract thrombocytopenia

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11
Q

tx of anemia side effect

A

erythropoietin and darbepoetin

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12
Q

control of vomiting

A

two medullary centers
-vomiting center and chemoreceptor trigger zone

CTZ stimulated by various toxins or drugs - release dopamine - get N and V

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13
Q

emesis

A

vomiting

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14
Q

ondansetron

A

serotonin antagonist

-to treat and minimize nausea and vomiting

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15
Q

stomatitis

A

inflammation of oral mucosa

adverse effect of chemo drugs

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16
Q

bisphosphonates

A

inhibit osteoclast action and bone resorption

delay time to first skeletal complication with chemo drug use

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17
Q

MOA alkylating agents

A

strong electrophiles form covalent bonds with DNA

intra and inter strand cross linking

-revents tumor from unwinding DNA

also cross-linking of DNA is cytotoxic

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18
Q

alkylating agents

A

CCNS

-although cells in G1 and S more susceptible

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19
Q

alkylating agents types

A
nitrogen mustards
methylhydrazines
alkyl sulfonates
nitrosoureas
triazenes
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20
Q

hemorrhagic cystitis

A

with cyclophosphamide

accumulation of metabolite acrolein

prevented with parenteral mesna

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21
Q

mesna

A

reacts and neutrolizes acrolein in cyclophosphamide induced hemorrhagic cystitis

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22
Q

nephrotoxicity and ototoxicity

A

cisplatin

ototoxicity - tinnitus and hearing loss in high frequency range

nephrotoxicity - overcome with hydration and diuresis

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23
Q

hyperpigmentation, pulmonary fibrosis, adrenal insufficiency

A

busulfan

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24
Q

antimetabolites

A

folic acid analogs, pyrimidine analogs, purine analogs

CCS agents

25
Q

methotrexate

A

folic acid analog - antimetabolite

26
Q

MOA methotrexate

A

inhibits dihydrofolate reductase and blocks conversion of folic acid to tetrahydrofolic acid

27
Q

high dose methotrexate

A

causes injury to health tissues

-enters health cells by diffusion

28
Q

low dose methotrexate

A

actie transported into cell

-less harmful to healthy tissues

29
Q

rescue for methotrexate

A

leucovorin

30
Q

leucovorin

A

rescue for methotrexate

-enters thymidylate synthesis pathway in healthy cells and allows thymidine synthesis to proceed

31
Q

methotrexate

A

CCS

32
Q

mucositis

A

with methotrexate

33
Q

5-FU

A

pyrimidine analog - antimetabolite

34
Q

MOA of 5-FU

A

prodrug - active compound FdUMP covalently binds thymidilate synthetase

also - FdUTP incorporated to DNA and FUTP incorporated into RNA - interfere with DNA synthesis and mRNA translation

35
Q

6-MP

A

purine analog

CCS - S phase

36
Q

MOA of 6-MP

A

inhibits de novo purine nucleotide synthesis due to triphosphate incorporation

37
Q

biotransformation of 6-MP

A

to inactive metabolite 6-thiouric acid by xanthine oxidase

-first pass metabolism

38
Q

allopurinol

A

xanthine oxidase inhibitor
-used as supportive care in tx of acute leukemias to prevent development of hyperuricemia

with 6-MP - causes increased levels - toxic

39
Q

reduce dose of 6-MP

A

if given with allopurinol

40
Q

vinblastine

A

vinca alkaloid

CCS - M phase

41
Q

vincristine

A

vinca alkaloid

CCS - M phase

42
Q

MOA of vinblastine and vincristine

A

bind beta-tubulin and inhibit microtubule assembly**

43
Q

drug resistance vinca alkaloids

A

membrane efflux pump P-glycoprotein

44
Q

hair loss, local cellulitis, loss of DTR, motor weakness

A

vinca alkaloids

45
Q

paclitaxel

A

taxane - CCS - M phase

46
Q

MOA of paclitaxel

A

bind to beta-tubulin and promote microtubule formation and stabilization

47
Q

peripheral sensory neuropathy

A

paclitaxel

48
Q

etoposide

A

epipodophyllotoxin - anti-mitotic drug

-CCS - late S-G2

49
Q

etoposide MOA

A

inhibit topoisomerase II - lead to DNA damage through strand breakage induced by formation of ternary complex of drug, DNA, and enzyme

50
Q

doxorubicin

A

anthracycline - antitumor antibiotic

51
Q

MOA of doxorubicin

A

1 inhibit topoisomerase II
2 intercalate DNA and block synthesis of DNA and RNA and blocks DNA strand scission
3 generates semiquinone and oxygen free radicals
4 bind to membrane and alter fluid/ion transport

CCNS - intercalation of DNA

52
Q

nausea, red urine, alopecia, stomatitis, cardiotoxicity

A

doxorubicin

53
Q

bleomycin

A

CCS - G2

antitumor antibiotic

54
Q

MOA bleomycin

A

small peptide that binds to DNA resulting in single or double strand breaks and inhibits DNA biosynthesis

55
Q

pneumonitis with cough, dyspnea, dry inspiratory crackles, CXR infiltrates, allergic rxns, fever

A

bleomycin

56
Q

asparaginase

A

enzyme - natural agent

CCS - G1

57
Q

MOA of asparaginase

A

hydrolyzes circulating L-asparagine to aspartic acid and ammonia - inhibits protein synthesis

58
Q

ALL tx

A

asparaginase

cannot synthesize L-asparagine

59
Q

acute hypersensitivity rxn

A

asparaginase