B3-042 Anti Cancer Drugs Flashcards

(118 cards)

1
Q

CCNS alkylating agents

A

cyclophosphamide
mechlorethamine
cis-platin

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2
Q

Mechanism: transfering an alkyl group over to DNA. Blocks access to DNA by cross linking.

A

CCNS alkylating agents

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3
Q

can lead to secondary malignancy due to DNA damage induced

A

CCNS alkylating agents

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4
Q

adds alkyl group to guanine
prodrug, metabolized by CYP450

A

cyclophosphamide

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5
Q

clinical use for multiple myeloma, lymphoma, leukemia, ovarian/breast cancer, small cell lung cancer, neuroblastoma, sarcoma

A

cyclophosphamide

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6
Q

delayed adverse effect is sterile hemorrhagic cystitis (hematuria/excessive voiding)

A

cyclophosphamide

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7
Q

produces acrolein-toxic metabolite

A

cyclophosphamide

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8
Q

mechanism of resistance for CCNS alkylating agents

A

impermeable to drug
pump drug out
alternate targets for drug (GSH)
increased DNA repair
no apoptosis

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9
Q

first ever alkylating agent, Hodgkins lymphoma

A

mechlorethamine

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10
Q

cross links DNA with platinum

A

cis-platin

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11
Q

cisplatin with less toxicity but more myelosuppression

A

carboplatin

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12
Q

cisplatin with less renal but more neurotoxicity

A

oxaliplatin

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13
Q

aromatase inhibitors that decreases estrogen synthesis [2]

A

anastrozole, letrozole

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14
Q

hormonal agents

A

anastrozole
letrozole
flutamide
hydrocortisone
prednisone
tamoxifen

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15
Q

androgen receptor antagonist

A

flutamide

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16
Q

adrenocorticosteroids [2]
suppress proliferation of immune cells

A

hydrocortisone
prednisone

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17
Q

selective estrogen receptor anatagonist

A

tomoxifen

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18
Q

used for breast cancer in post menopausal women
ER+ primary and metastatic cancers [2]

A

anastrozole
letrozole

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19
Q

used for metastatic prostate cancer

A

flutamide

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20
Q

hormonal agents [2] used for leukema/lymphoma

A

hydrocortisone
prednisone

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21
Q

hormonal agent used for breast cancer

A

tamoxifen

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22
Q

adverse effects: anastrozole

A

nausea, headache, hot flashes

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23
Q

adverse effects: flutamide

A

hepatic effects

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24
Q

adverse effects: hydrocortisone/prednisone

A

elevated fasting glucose
fluid retention
immunosuppression
diabetes

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25
hormonal agents: CYP2D6 activation
tamoxifen
26
CCS Topoisomerase inhibitors
etoposide irinotecan
27
inhibits DNA topoisomerase II
etoposide
28
inhibits DNA Topoisomerase I, pro-drug
irinotecan
29
topoisomerase inhibitor for colon cancer
irinotecan
30
topoisomerase inhibitor for testicular, small cell lung, leukemia, lymphoma
etoposide
31
irinotecan is metabolized by UGT1A1. A deficiency can cause
increased toxicity, leading to Crigler-Najjar, Gilbert's, hyperbilirubinemia
32
checkpoint inhibitors
ipilimumab nivolumab atezolimumab
33
mAb against CTLA-4
ipilimumab
34
mAb against PD-1
nivolumab
35
mAb against PD-L1
atezolimumab
36
checkpoint inhibitor used for unresectable or metastatic melanoma
ipilimumab
37
checkpoint inhibitor used for melanoma, colon, HENT, hepatocellular, hodgkins, non-small cell lung, urothelial
nivolumab
38
adverse effects: ipilimumab
immune inflammatory response
39
Antimetabolites CCS
cytarabine 5-flurouracil gemcitabine 6-thioguanine 6-mecaptopurine methotrexate
40
inhibits thymidylase synthase
5-FU
41
cytosine analog, chain terminator
cytarabine
42
cytosine analog, inhibits polymerase and chain terminator
gemcitabine
43
more toxic than purines, cause BM and GI toxicity
cytarabine 5-FU gemcitabine
44
purine analong blocks DNA and RNA synthesis inhibits AMP and GMP synthesis
6-mercaptopurine
45
purine analog incorporated into RNA and DNA, alters function
6-thioguanine
46
inactivated and cleared by TPMT thiopurine methyltransferase
6-thioguanine 6-mercaptopurine **test genotype for TPMT
47
folic acid analog inhibits DHFR by adding a hydrogen to reduce it
methotrexate
48
adverse effect: methotrexate
myelosuppression
49
CCS microtubule poisons
docetaxel paclitaxel vinblastine vincristine
50
stabilize microtubules in M phase, prevents progression to anaphase [2]
docetaxel paclitaxel
51
bind beta tubulin, inhibit formation of mitotic spindle causing metaphase arrest [2]
vinblastine vincristine
52
used for ovarian, breast, and pancreatic solid tumors [2]
docetaxel paclitaxel
53
adverse effects of docetaxel/paclitaxel
meyolesuppression neuropathy
54
adverse effects: vinblastine
nausea, vomiting, alopecia, myelosuppression
55
adverse effects: vincritstine
peripheral neuropathy
56
tyrosine kinase inhibitors [2]
gefitinib imatinib
57
TK inhibitor of EGFR
gefitinib
58
TK inhibitor of BCR-ABL
imatinib
59
TK used for non-small cell lung cancers
gefitinib **less effective for asian, non-smoker
60
TK used for CML, Ph+ALLm GI stromal tumors
imatinib
61
antitumor antibiotics CCNS [3]
bleomycin daunorubicin doxorubicin
62
binds to DNA and induces ROS production causing strand breaks
bleomycin
63
block topoisomerase II, generates ROS [2]
daunorubicin doxorubicin
64
adverse effect: bleomycin
pulmonary fibrosis
65
adverse effect: daunorubicin, doxorubicin
cardiotoxicity
66
decreases vascularization, increases capillary permeability, inhibits angiogenesis
bevacizumab
67
inhibits 26S proteosome, disrupts signaling cascades leading to apoptosis
bortezomib
68
mTOR inhibitor inhibits cell cycle progression, angiogenesis, promotes apoptosis
sirolimus
69
adverse effects: bevacizumab
arterial thromboembolism
70
adverse effects: bortezomib
thrombocytopenia, peripheral neuropathy
71
half life 60 hrs, CYP3A substrate
sirolimus
72
biologics [2]
interferon a trastuzamab
73
cytokine inhibitor of cell growth alters gene expression, antiviral immunomodulator
INF-a
74
Her-2/ErbB-2 onogene antogonist
trastuzamab
75
biologic used for hematologic malignancies, metastatic melanoma, renal cell carcinoma
INF-a
76
biologic used for HER-2 breast cancer
trastuzamab
77
adverse effects: trastuzamab
infusion reactions hypersensitivity cardiomyopathy
78
ancillary drugs
EPO GM-CSF Mesna Ondansetron
79
inactivates acrolein in kidneys
mesna
80
serotonin antagonist
ondansetron
81
used to stimulate erythroid precursor maturation in anemia
EPO
82
used to treat myelosuppression stimulates granulocytes/macrophage precursor development
GM-CSF
83
used for iatrogenic nausea and vomiting
ondansetron
84
used for prevention of hemorrhagic cystitis
mesna
85
dosing regimen is determined by
the time for recovery from adverse effects
86
chemotherapeutic administration is limited by
toxicity to other rapidly growing cell populations | bone marrow, GI, epitehlium
86
chemotherapeutic administration is limited by
toxicity to other rapidly growing cell populations | bone marrow, GI, epitehlium
87
most cancer drugs target
processess essential for cell proliferation
88
stimulates the production of WBCs
GM-CSF | WBCs are most sensitive to effects of decreased cell production
89
activated by salvage pathway for nucleotide synthesis
purine analogs
90
activated by hprt
purine analogs
91
bone marrow suppression only observed at very high doses
purine analogs
92
inhibits human dihydrofolate reductase
methotrexate
93
prevents denovo synthesis of purines and the conversion of uracil to thymidine
methotrexate
94
rescue methotrexate with
folinic acid (levocorine)
95
cytarabine gemcitabine methotrexate are all
cell cycle specific
96
cis platin is administered
IV
97
mechlorethamine is administered
IV
98
very short half life marked bone marrow suppression
mechlorethamine
99
particularly associated with secondary malignancy
alkylating agents and anti-tumor antibiotics
100
drug related cancers are caused by
DNA damage caused by the drugs in the normal cells producing oncogenic mutations
101
secondary malignancies develop ..... years after treatment
5-20
102
resistant cells are a
continuation of the same malignancy
103
blocks normal hormonal stimulation of the prostate
flutamide
104
alkylating agent associated with nephrotoxicity
cisplatin
105
microtubule poison associated with myelosuppresion
vinblastine
106
anti-tumor antibiotic that is cell cycle specific
bleomycin
107
SN-38 is the active metabolite for
irinotecan
108
SN-38 is inactivated by
glucuronidation of UGT1A1
109
FDA recommends genotyping for patients for UGT1A1 related to decreasing toxicity of
irinotecan
110
does not cross BBB
trastuzumab
111
targets VEGF-A receptro
bevacizumab
112
monotherapy for glioblastoma
bevacizumab
113
targets CTLA-4
ipilimumab
114
modulates T cell activation
CTLA-4
115
enhances T cell activations
ipilimumab
116
targets unique kinase found only in CML
imatinib | very selective in toxicity
117
signature adverse effect of bleomycin
irreversible pulmonary fibrosis