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Hem/Onc > 31 & 32 - Common Cancer Drugs > Flashcards

31 & 32 - Common Cancer Drugs Flashcards

(62 cards)

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1
Q

alkylating agents - general what are they

A

strong electrophiles that form pos charged intermediates w/ target molecules and cause DNA damage

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2
Q

alkylating agents - mechanism

A

inhibit DNA synth / cell division by covalent attachment at 2 points
crosslinks DNA > cytotoxicity

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3
Q

example class and drug of alkylating agents

A

nitrogen mustards > cyclophosphamide

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4
Q

cyclophosphamide - category

A

alkylating agent > nitrogen mustard

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5
Q

cyclophosphamide uses

A

lymphoma regimens, breast cancer, ovarian cancer, some kinds of lung cancer

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6
Q

cyclophosphamide - AEs

A

myelosuppression (dose limiting)

alopecia, immunosuppression, cystitis

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7
Q

anitmetabolites - what are they

A

structurally related to natural compounds, compete for normal metabolites

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8
Q

folate antagonist mechanism

A

block biosynth of fully reduced tetrahydrofolic acid

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9
Q

example of folate antagonist

A

methotrexate

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10
Q

methotrexate mech

A

competitively inhibits folic acid binding to dihydrofolate reductase > death due to thymidylate and purine blockage; s-phase specific agent

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11
Q

uses of methotrexate

A

curative regimen for ALL, trophoblastic choriocarcinoma, Burkitt’s

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12
Q

methotrexate AEs

A

myelosuppression - dose limiting

renal insufficiency - c/i in pts w/ renal impairment

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13
Q

rescue drug for myelosuppression due to methotrexate

A

leucovorin

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14
Q

purine analogue mechanism

A

prevent biosynth of purine precursors
get incorporated into RNA/DNA > fraudulent nucleic acids made

require activation - “lethal synthesis”

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15
Q

ex of purine analogue

A

thioguanine (a thiolated purine analogue)

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16
Q

use of thioguanine

A

AML, ALL, CML

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17
Q

AEs of thioguanine

A

myelosuppression

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18
Q

ex of pyrimidine analogue

A

5-fluorouracil (halogenated pyrimidine)

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19
Q

uses of 5FU

A

CA of breast, stomach, COLON, rectum, pancreas, liver, ovary

short story: lots of solid tumors

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20
Q

major AE of 5FU

A

myelosuppression

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21
Q

hydroxyurea - mech

A

inhibits ribonucleoside diphosphate reductase

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22
Q

hydroxyurea - use

A

myeloprolif syndromes

CML

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23
Q

AEs of hydroxyurea

A

myelosuppression

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24
Q

anticancer abx - general mechanism

A

inhibit nucleic acid synth by blocking DNA replication or transcription either by direct binding to nucleic acid or polymerizing enzyme

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25
ex of anthracycline (anticancer abx)
doxorubicin
26
doxorubicin mech
intercalating agent - insert btwn DNA base pairs, S-phase specific
27
use of doxorubicin
CA of breast, ovary, endometrium, bladder, thyroid, lung bottom line: solid tumors
28
AEs of doxorubicin
cardiotoxicity (unique) | myelosuppressive (major)
29
bleomycin mech
strand scission - cut phosphate backbone
30
use of bleomycin
potentially curative in combo for testicular CA; | Hodgkin's and non-Hodgkin's lymphoma
31
AEs of bleomycin
``` lung tox (fibrosis) skin toxic ```
32
mech of platinum coordination complexes
electrophile that forms strong coordination complexes w/ DNA (guanine)
33
use of cisplatin
curative for testicular cancer
34
AEs of cisplatin
renal tox
35
2 subcategories of plant derived cancer drugs
vinca alkaloids | taxanes
36
vincristine mech
binds to tubulin and blocks polymerization > M phase specific agent
37
use of vincristine
curative for ALL, hodgkins and NHL
38
AEs of vincristine
neuro toxicity (dose limiting)
39
ex of taxane
paclitaxel
40
mech of paclitaxel
binds to beta tubulin and antagonizes MT diasassembly
41
use of paclitaxel
cisplatin refractory metatstatic ovarian and breast CA
42
AEs of paclitaxel
myelosuppressive, myalgias, stocking/glove sensory neuropathy
43
topotecan mech and class
camptothecin analog | binds to topoisomerase I, ssDNA breaks
44
use of topotecan
ovarian and small cell lung CA
45
AEs of topotecan
neutropenia
46
etoposide mech
complex w/ topoisomerase II, dsDNA breaks
47
use of etoposide
testicular cancer
48
AEs of etoposide
causes leukemia w/ chromosomal translocation
49
uses of prednisone for cancer
*used to induce remission in ALL* used to treat both Hodgkin and NHL destroys lymphocytes
50
what did estrogens used to be used for in cancer?
prostate cancer
51
tamoxifen
``` estrogen agonist (SERM) - binds but not transcriptionally active first line therapy for ER+ breast cancer ```
52
use of GnRH agonists and antagonists
prostate cancer - leuprolide is equivalent to orchiectomy in terms of response
53
examples of GnRH agonists
leuprolide histerelin nafarelin goserelin
54
examples of GnRH antagonists
abarelix *(no testosterone flare) | triptorelin
55
aromatase inhibitors mech
stop extra-adrenal synth of estrogen in other tissues
56
ex of aromatase inhib
anastrozole
57
use of anastrozole
adv ER and PR pos breast cancers
58
aminoglutethimide
first aromatase inhib, largely replaced by newer ones that dont block hydrocortisone synth
59
exemestane
irreversible inhib of aromatase
60
imatinib (Gleevic)
tyrosine kinase inhib targeted to PDGF-R good for inhibiting Philadelphia chromosome product in CML and c-kit (in GI stromal tumors) lots of side effects - basically platelet like bleeding, fever/flu sx
61
bevacizumab (avastin)
ab against VEGF that inhibits angiogenesis | used in colorectal cancer, non-small cell lung cancer, some breast cancers
62
bortezomib
reversible inhibitor of proteasome (stop breakdown of cell cycle regulators) used in multiple myeloma and relapsed mantle cell lymphoma

Hem/Onc (29 decks)

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