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test 1 Flashcards

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1
Q

pyrimidine analogs

A

fluoruracil, floxuridine, capecitabine, cytarabine, gemcitabine

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2
Q

5-FU use

A

treatment for GI, pancreas, head & neck, colon, rectum, breast and ovarian cancers

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3
Q

5-FU toxicity

A

bone marrow suppression, mucosal damage, N/V, cardiac, hand and foot syndrome, alopecia, hyperpigmentation, neurologic deficits

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4
Q

arabinose nucleotides cannot form

A

phosphodiester bonds bc of the -OH at C2. -> DNA fragmentation

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5
Q

cytarabine (AraC) indication

A

acute leukemia

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6
Q

most specific antimetabolite for the S phase

A

cytarabine

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7
Q

cytarabine (AraC) MOA

A

activated by kinases to AraCTP which acts as an inhibitor of DNA polymerase

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8
Q

side effect of cytarabine

A

hand and foot syndrome. severe myelosuppression, mucosal membrane inflammation, etc

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9
Q

xeloda generic

A

capecitabine.

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10
Q

capecitabine indication

A

breast cancer. prodrug of 5-FU

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11
Q

gemcitabine is used to treat

A

locally advanced or metastatic pancreatic cancer

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12
Q

triphosphate-gemcitabine inhibits

A

DNA polymerases (termination of DNA chain elongation)

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13
Q

diphosphate- gemcitabine inhibits

A

ribonucleotide reductase

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14
Q

nucleotide analogue of the antiviral agent vidarabine

A

fludaraine

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15
Q

fludarabine MOA

A
  • phosphorylated (inhibition of DNA polymerases)

- incorporation into the DNA strands (chain termination)

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16
Q

purine analogs

A

6-MP, thioguanine, cladribine, pentostatin

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17
Q

6-mercaptopurine indication

A

childhood leukemia

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18
Q

both 6-MP and thioguanine are activated by

A

HGPRT to toxic nucleotides that inhibit several enzymes involved in purine metabolism

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19
Q

reistance to 6-MP and thioguanine

A

due to cancer cells have decreased HGPRT activity

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20
Q

6-MP is metabolized in the liver by

A

xanthine oxidase

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21
Q

drug interaction with 6-MP and

A

allopurinol. if used together, dose of 6-MP should be reduced by at least 75%

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22
Q

ribonucleotide reductase

A

catalyzes conversion of ribonucleotide diphosphates to deoxyribonucleotide diphosphates

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23
Q

hydroxyurea specifically inhibits

A

ribonucleotide reductase. inhibits DNA synthesis without affecting RNA synthesis. limited use in cancer

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24
Q

3 antimitotic agents

A

taxols, vinca alkaloids, colchicine

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25
vinca alkaloid MOA
bind with the already grown microtubule and help to depolymerize it-> break down microtubule
26
taxol MOA
binds to the microtubule and helps stabilize it, making it more rigid
27
vinca alkaloid drugs
vincristine, vinblastine, ajmalicine, vindesine
28
vinca alkaloids are
cell cycle specific. act in late G2 & M phases
29
vinblastine, vinorelbine and vincristine are both
vesicants
30
vincristine cannot be given
intrathecally- neurotoxicity
31
less neurotoxicity than all other vincas
vinorelbine
32
major mechanism of resistance
MDR-P glycoprotein efflux pump
33
taxols are
cell cycle specific. active in G2 and M phases
34
what is a requirement for biological activity of taxanes?
C13 side chain
35
taxol drugs are always administered after
premedication with antihistamines, corticosteroids, etc bc the vehicle can degrade tubing and cause histamine release. dexamethasone 20mg PO 12 and 6 hours prior, pepcid or tagamet, benedryl plus anti-emetic
36
when given with other chemo drugs, give taxol
first
37
is taxol an irritant?
yes
38
premedication with docetaxel
examethasone 8mg PO BID starting 1 day prior & continuing 4 days after
39
what is abraxane?
albumin-bound, cremophor- free formulation of paclitaxel (solvent free)
40
taxanes promote
microtubule formation!
41
adriyamycin
doxorubicin
42
type 1 topos
introduces a break in ONE strand to remove a supercoil
43
type 2 topos
introduce breaks in both chains
44
type 1 functions to remove
positive supercoils during transcription
45
type 2 performs a similar function during
DNA replication & decatanates & separates daughter chromosomes in mitosis
46
MOA of topo agents
cause accumulation of DNA cleavable complexes composed to protein-linked DNA strand breaks
47
epipodophyllotoxins
etoposide & teniposide | topo II inhibitors. cause DS breaks
48
etoposide/ teniposide toxicities
neutropenia, myelosuppression & secondary leukemias
49
topo I inhibitor drugs
camptothecin, irinotecan, topotecan
50
SN-38 aka
irinotecan
51
major side effect of irinotecan
major diarrhea
52
antitumor antibiotics- anthracyclines
daunorubicin, doxorubicin, idarubicin
53
antitumor antibiotics- others
bleomycin, dactinomycin, mitomycin, mitoxantrone
54
anthracycline structure
tetracycline ring with a daunasamine sugar. quinone moieties that allow electron-accepting & donating functions
55
anthracyclines act as
intercalators
56
doxorubicin can also bind
iron and produce free radicals
57
is doxorubicin cell cycle specific?
no- active in all phases, most cytotoxic in S phase
58
barbituattes & dox
dox metabolism increased
59
CCBs & dox
additive cardiotoxicity
60
what is the most cardiotoxic drug?
doxorubicin
61
most intercalating antitumor antibiotics mediate their effects through
topo II inhibition
62
cummulative anthracycline dose associated with 48% risk
700mg/m^2
63
at what dose must therapy be stopped
500mg/m^2
64
semiquinone an hydroxyquionone are
free radicals
65
dexrazoxane
cardioprotective chelating agent. EDTA- derivative that can be given before dox to prevent iron-mediated free radical damage
66
liposomal products prolong
plasma concentration time and result in increased tumor concentration
67
dactinomycin MOA
intercalates between G-C. inhibits RNA polymerase & mRNA production
68
is dactinomycin and mitoxantrone vesicants?
yes
69
mitoxantrone structure
3 rings
70
mitroxantrone lacks the ability to
produce free radicals (less cardiotoxic)
71
mitomycin
bifunctional alkylating antitunor antibiotic. cell cycle non-specific
72
bleomycin can associate with
iron like dox & cause free radicals and DNA strand breaks
73
what is the most pulmonary toxic drug?
bleomycin
74
what drug has meolytic uremic syndrome?
mitomycin
75
what can be used to determine cardiotoxicity risk with dox?
BNP levels
76
is non-hodgkin;s lymphoma curable?
yes
77
aromatase converts
androgens to estrogens
78
where does most estrogen come from in premenopausal?
ovary
79
where does most estrogen come from in postmenopausal
adrenal glands
80
estrogen deprivation in premenopausal women
tamoxifen +/- ovariectomy
81
estrogen deprivation in postmenopausal women
aromatase inhibitors
82
SERMs
tamoxifen, toremifene
83
steroidal aromatase inhibitors
exemestane, testolactone
84
pure anti-estrogens
fulvestrant
85
Non-steroidl aromatase inhibitors
anastrazole, letrozole,
86
LHRH agonists
leuprolide, gpserelin, buserelin, and nafarelin
87
chronic administration of LHRH agonists leads to
receptor desensitization and their loss in the pituitary
88
LHRH agonists initially
make more LH and testosterone and then depletes it | "Tumor flares"
89
anti-androgens
flutamide, icalutamide, nilutamide, enzalutamide
90
what drug has a disulfiram-like reaction with alcohol?
nilutamide
91
LHRH MOA
bind to GnRH receptors & decrease LH & FSH production through receptor desensitization
92
corticosteroid MOA
induce marked lymphopenia & are cytotoxic to leukemic lymphoblasts by binding to glucocorticoid receptors in the nucleus
93
solu-medrol generic
methylprednisolone
94
DOC for pancreatic cancer
gemcetabine

oncology (6 decks)

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