Antineoplastic Agents II

Question 1

primary resistance

Answer 1

absence of response on first exposure

Question 2

acquired resitance

Answer 2

develops in response to eposure to give chemo drug

Question 3

multidrug resistance

Answer 3

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

Question 4

toxicity

Answer 4

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

also - mutagenic - so may cause cancer

Question 5

nadir

Answer 5

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

Question 6

most regimens

Answer 6

given in cycles of 21-28 days

Question 7

nitroureas

Answer 7

longer period of recovery - given every 6 weeks

Question 8

GM-CSF

Answer 8

sargramostim

given to minimize neutropenia

Question 9

G-CSF

Answer 9

filgrastim and pegfilgrastim

given to minimize neutropenia

Question 10

oprelvekin

Answer 10

platelet growth factor

-given to counteract thrombocytopenia

Question 11

tx of anemia side effect

Answer 11

erythropoietin and darbepoetin

Question 12

control of vomiting

Answer 12

two medullary centers
-vomiting center and chemoreceptor trigger zone

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

Question 13

emesis

Answer 13

vomiting

Question 14

ondansetron

Answer 14

serotonin antagonist

-to treat and minimize nausea and vomiting

Question 15

stomatitis

Answer 15

inflammation of oral mucosa

adverse effect of chemo drugs

Question 16

bisphosphonates

Answer 16

inhibit osteoclast action and bone resorption

delay time to first skeletal complication with chemo drug use

Question 17

MOA alkylating agents

Answer 17

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

Question 18

alkylating agents

Answer 18

CCNS

-although cells in G1 and S more susceptible

Question 19

alkylating agents types

Answer 19

nitrogen mustards
methylhydrazines
alkyl sulfonates
nitrosoureas
triazenes

Question 20

hemorrhagic cystitis

Answer 20

with cyclophosphamide

accumulation of metabolite acrolein

prevented with parenteral mesna

Question 21

mesna

Answer 21

reacts and neutrolizes acrolein in cyclophosphamide induced hemorrhagic cystitis

Question 22

nephrotoxicity and ototoxicity

Answer 22

cisplatin

ototoxicity - tinnitus and hearing loss in high frequency range

nephrotoxicity - overcome with hydration and diuresis

Question 23

hyperpigmentation, pulmonary fibrosis, adrenal insufficiency

Answer 23

busulfan

Question 24

antimetabolites

Answer 24

folic acid analogs, pyrimidine analogs, purine analogs

CCS agents

Question 25

methotrexate

Answer 25

folic acid analog - antimetabolite

Question 26

MOA methotrexate

Answer 26

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

Question 27

high dose methotrexate

Answer 27

causes injury to health tissues | -enters health cells by diffusion

Question 28

low dose methotrexate

Answer 28

actie transported into cell | -less harmful to healthy tissues

Question 29

rescue for methotrexate

Answer 29

leucovorin

Question 30

leucovorin

Answer 30

rescue for methotrexate | -enters thymidylate synthesis pathway in healthy cells and allows thymidine synthesis to proceed

Question 31

methotrexate

Answer 31

CCS

Question 32

mucositis

Answer 32

with methotrexate

Question 33

5-FU

Answer 33

pyrimidine analog - antimetabolite

Question 34

MOA of 5-FU

Answer 34

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

Question 35

6-MP

Answer 35

purine analog CCS - S phase

Question 36

MOA of 6-MP

Answer 36

inhibits de novo purine nucleotide synthesis due to triphosphate incorporation

Question 37

biotransformation of 6-MP

Answer 37

to inactive metabolite 6-thiouric acid by xanthine oxidase | -first pass metabolism

Question 38

allopurinol

Answer 38

xanthine oxidase inhibitor -used as supportive care in tx of acute leukemias to prevent development of hyperuricemia with 6-MP - causes increased levels - toxic

Question 39

reduce dose of 6-MP

Answer 39

if given with allopurinol

Question 40

vinblastine

Answer 40

vinca alkaloid CCS - M phase

Question 41

vincristine

Answer 41

vinca alkaloid CCS - M phase

Question 42

MOA of vinblastine and vincristine

Answer 42

bind beta-tubulin and inhibit microtubule assembly**

Question 43

drug resistance vinca alkaloids

Answer 43

membrane efflux pump P-glycoprotein

Question 44

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

Answer 44

vinca alkaloids

Question 45

paclitaxel

Answer 45

taxane - CCS - M phase

Question 46

MOA of paclitaxel

Answer 46

bind to beta-tubulin and promote microtubule formation and stabilization

Question 47

peripheral sensory neuropathy

Answer 47

paclitaxel

Question 48

etoposide

Answer 48

epipodophyllotoxin - anti-mitotic drug | -CCS - late S-G2

Question 49

etoposide MOA

Answer 49

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

Question 50

doxorubicin

Answer 50

anthracycline - antitumor antibiotic

Question 51

MOA of doxorubicin

Answer 51

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

Question 52

nausea, red urine, alopecia, stomatitis, cardiotoxicity

Answer 52

doxorubicin

Question 53

bleomycin

Answer 53

CCS - G2 antitumor antibiotic

Question 54

MOA bleomycin

Answer 54

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

Question 55

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

Answer 55

bleomycin

Question 56

asparaginase

Answer 56

enzyme - natural agent CCS - G1

Question 57

MOA of asparaginase

Answer 57

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

Question 58

ALL tx

Answer 58

asparaginase cannot synthesize L-asparagine

Question 59

acute hypersensitivity rxn

Answer 59

asparaginase