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SS- CMOD Block 2 > Anticancer Drugs > Flashcards

Anticancer Drugs Flashcards

1
Q

methotrexate

A

S phase
DHFR inhibitor: no THF to provide carbon for DNA and DNA
inhibit thymidylate synthase (decrease DNA syn.)
inhibits GRAFT, AICARFT: accumulation of adenosine (anti-inflamm.)
polyglutamation: traps in cell
hepatotoxicity, GI toxicity (mucositis and esophagitis), pulmonary fibrosis
renal excretion

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2
Q

flurouracil

A

S phase
req. activation
pyrimidine analog that complexes with folic acid that irreversible inhibits thymidylate synthase (decrease DNA syn.)
genetic differences in dihydropyrmidine dehydrogenase: major pathway of detoxification in tumor cells (converts 5-FU to dihydrofluorouracil): significant differences in toxicity
myelosuppresion, hand-foot syndrome, GI toxicity

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3
Q

capecitabine

A

S phase
oral prodrug for fluoruracil
CNS toxicity, more hand-foot syndrome

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4
Q

cytarabine

A

S phase
other names: arabinoside and Ara-C
req. activation to Ara-CTP
ITH, SC, IV
pyrimidine analog: selective inhibition of DNA pol
myleosuppresion, stomatitis, hand-foot syndrome

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5
Q

gemcitiabine

A

S phase
req. activation
deoxycytidine analog: decrease DNA syn.
myelosupression, pulmonary toxicity

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6
Q

6-mercaptopurine

A 
S phase
Purine analog
req. activation by HGPRT
patient: TPMT genotype (deficient: normal dose will kill patient)
allopurinol increases toxicity
myelosuppresion and hepatic dysfunction
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7
Q

thioguanine

A 
oral
S phase
Purine analog
req. activation by HGPRT
patient: TPMT genotype (deficient: normal dose will kill patient)
myelosuppresion and hepatic dysfunction
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8
Q

fludarabine

A

S phase

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9
Q

cyclophosphamide

A

oral or IV
cross-linking of dsDNA: N7 guanine
req. activation: microsomal enzymes-> aldophosphamide-> nonenzymatic cleavage-> phosphoramide mustard and acrolein
acrolein: hemorrhagic cystitis
lung fibrosis, nephrotoxicity, CHF (temporary)

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10
Q

ifosfamide

A

cross-link DNA at N7 guanine
requires liver bioactivation
acroelin: hemorrhagic cystitis
CNS toxicity, renal/urotoxic

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11
Q

mechlorethamine

A 
cross-link DNA at N7 guanine
spontaneous rearrangement (NO metabolic activation needed)
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12
Q

melphalan

A

cross-link DNA at N7
spontaneous rearrangement (NO metabolic activation)
lung fibrosis

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13
Q

busulfan

A

oral or IV
cross-links DNA
hepatic veno-occlusive, lung fibrosis, Addison-like adrenal insufficiency (hyperpigmentation)

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14
Q

BCNU

A 
carmustine: paranteral
cross-link DNA
carbamoylate: no cross-resistance with other alkylating agents
cross BBB
req. bioactivation
hepatic "veno-occlusive"
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15
Q

CCNU

A 
lomustine: oral
cross-link DNA
cross BBB
req. bioactivation
CNS toxicity: seizures, dementia
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16
Q

dacarbazine

A

methylating agent

req. metabolic activation

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17
Q

procarbazine

A

methylating agent
req. activation
disulfarim-like effect, weak MAO inhibition, male infertility

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18
Q

cisplatin

A

Intrastrand DNA links
spontaneous activation in aqueous
nephrotoxicity, ototoxicity, peripheral neuropathy
CNS toxicity

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19
Q

carboplatin

A

Intrastrand DNA links
spontaneous activation in aqueous
peripheral neuropathy, thrombocytopenia

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20
Q

allopurinol

A

Tx: tumor lysis syndrome
inhibit xanthine oxidase: hypoxanthine to uric acid
prophylaxis of hyperuricemia
increases toxicity of mercaptopurine

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21
Q

rasburicase

A

Tx: tumor lysis syndrome

catalyzes urate oxidase: uric acid to allantoin

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22
Q

doxorubicin

A

intercalate with DNA: inhibition of DNA-dependent RNA synthesis,
stabilize DNA-topo-II complex: topo-II inhibition, generate free radicals from semiquinone
cardiotoxicity
extravasional necrosis
red urine
more active in solid tumors than daunorubicin

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23
Q

MESNA

A

protect against acreolein: prevent hemorrhagic cystitis adjuvant: cyclophosphamide, ifosfomide

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24
Q

vincristine

A 
M phase
binds B-tubulin and blocks polymerization into microtubules (+ end)
cumulative neurotoxicity (peripheral neuropathy), paralytic ileus
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25
vinblastine
M phase binds B-tubulin and blocks polymerization into microtubules (+ end) myelosuppresion: leukopenia, less peripheral neuropathy
26
topotecan
stabilizes DNA-topo I complex: inhibition of of topoisomerase I renal elimination
27
irinotecan
stabilizes DNA-topo I complex: inhibition of of topoisomerase I longer t1/2 than topotecan hepatic elimination avoid in Gilbert: UGT polymorphisms (defective) diarrhea (loperamide), AchE inhibtion (atropine)
28
etoposide
oral S and G2 phase topoisomerase II inhibitor
29
paclitaxel
M phase binds B-tubulin and antagonizes disassembly of microtubules (B-subunit) hand foot syndrome, more peripheral neuropathy than docataxel, hypersensitivity admin with: cremaphor
30
docataxel
M phase Binds a B-tubulin and antagonizes disassembly of microtubules (B-subunit) edema-fluid retention, peripheral neuropathy, hand-foot syndrome Greater potency than paclitaxel admin with: polysorbate 80 or cremaphor
31
daunorubicin
intercalate with DNA: inhibition of DNA-dependent RNA synthesis, stabilize DNA-topo-II complex: topo-II inhibition, generate free radicals from semiquinone cardiotoxicity extravasational necrosis red urine
32
idarubicin
intercalate with DNA: inhibition of DNA-dependent RNA synthesis, stabilize DNA-topo-II complex: topo-II inhibition, generate free radicals from semiquinone cardiotoxicity extravasional necrosis red urine
33
bleomycin
G2 phase free radical formation: oxidizes deoxyribose of thymidylate and other nucleotides single and double DNA strand breaks pulmonary fibrosis, hyperpigmentation
34
pegaspargase
degrades asparagine: starve protein synthesis | pancreatitis
35
lanalidomide
thalidomide derivative inhibits tumor cell proliferation, cell adhesion to stroma, and angiogenesis enhances NK cell activity peripheral neuropathy
36
dexrazoxane
inhibitor of iron-mediated free radical generation; iron chlelator protect against cardiotoxicity of doxirubicin and daunorubicin
37
leucovorin
folinic acid that converts to THF without DHFR adjuvant: methotrexate to protect from myelosuppresion adjuvant: enhance response to 5-FU by increasing TS complex
38
liposomal doxorubicin
less cardiotoxicity | hand foot syndrome instead
39
bevacizumab
VEGF inhibitor: esp. important in large solid tumors that are outgrowing their blood supply HTN, CHF, pulmonary hemorrhage, GI perforation Tx: colorectal cancer and non-small cell lung cancer
40
cetuximab
EGFR infusion rxn, skin rash with sun Tx: colorectal cancer, head and neck cancer
41
panitumumab
EFGR infusion rxn, skin rash with sun Tx: colorectal cancer
42
rituximab
CD20 inhibitor: depletion of B cells Tx: chronic lymphocytic leukemia and non-hodgkin's lymphoma +ve B cell depletion, lymphopenia, progressive multifocal leukoencephalopathy
43
trastuzumab
bind Her-2 and down regulate: CdK inhibitor p27 accumulates: cell cycle arrest cardiomyopathy, infusion reaction Tx: breast cancer cardiotoxicity
44
ipilimumab
CTLA-4 inhibitor: T cell activation and proliferation | Tx: melanoma
45
ofatumumab
CD20 Tx: chronic lymphocytic leukemia infection, progressive leukoencephalopathy, neutropenia
46
boretezomib
IV 26-S proteosome inhibitor: prevents IkB-alpha degredation: keeps NFkB inhibited Tx: multiple myeloma cardiotoxicity, peripheral neuropathy, hepatotoxicity, hypotension
47
vismodegib
oral SMO inhibitor hedgehog pathway inhibitor Tx: basal cell carcinoma
48
T-DM1
Her-2 inhibitor and delivery of cytotoxic agent
49
pertuzumab
block heterodimerization of Her-2 and Her-3
50
Mab administration
IgG NOT orally active drugs: large MW protein; IV or SC potential poor penetration of solid tumors infusion reactions: anaphylaxis, angiodema, pulmonary toxicity; HTN; pancytopenia
51
Tyrosine kinase inhibitor
-nib oral: vary bioavailability with food or CYP3A4 binds ATP binding domain: resistance diminishes therapeutic window SE: disrupt endocrine function, blood dycrasias, QT prolongation TK (EGFR)-> RAS-> BRAF->MEK-> ERK/MAPK
52
temsirolimus
mTOR inhibitor: decrease angiogenesis, cell proliferation and metabolism Tx: renal cancer
53
sirolimus
mTOR inhibitor:decrease angiogenesis, cell proliferation and metabolism
54
everolimus
mTOR inhibitor | Tx: renal cancer
55
resistance to alkylating agents
increased repair
56
stimuli for N/V
1. chemotrigger zone 2. GI tract 3. psychological
57
adjuvant therapy
chemotherapy used after surgery or radiation
58
neo-adjuvant therapy
chemotherapy used before surgery or radiation
59
Amifostine
adjuvant: cisplatin to prevent nephrotoxicity | free radical scavenger
60
drug cocktail for prophylaxis of N/V
serotonin antagonist, NK-1 antagonist, corticosteroid
61
azathioprine
metabolized into 6-MP
62
hydroxyurea
S phase free radical scavenger: inhibits ribonucleotide reductase: inhibits DNA syn. NO conversion of ribonucleotides to deoxyribonucleotides desquamative interstitial penumonitis, skin toxicities
63
efflux pump names
1. P-gp 2. BCRP 3. MRP
64
crempahor
surfactant that makes taxes more soluble | hypersensitivity reaction
65
polysorbate 80
surfactant that makes docataxel more soluble | less hypersensitivity than cremaphor
66
topotecan
stabilizes DNA-topo I complex: inhibition of of topoisomerase I
67
atropine
M receptor antagonist | adjuvant: irinotecan if <24hrs
68
loperamide
anti-diarrheal | adjuvant: irinotecan if >24hrs
69
tretinoin
ATRA: all-trans retinoic acid oral chimeric TF that interferes with RARalpha retinoid acid syndrome: fever, dyspnea, weight gain, pulmonary infiltrates, and pleural or pericardial effusions cheilitis, hyperlipidemia, dry skin, bone tenderness
70
26S proteasome complex
normal-> HIF-1-> degraded by 26S proteasome | low oxygen-> HIF-1 ->VEGF
71
erlotinib
TKI: EGFR Tx: non-small cell lung cancer, pancreatic cancer photo-sensitivity rash
72
imatinib
TKI: BCR-ABL, c-KIT, PDGFR Tx: chronic myeloid leukemia, chronic eosinophilic leukemia, acute lymphoblastic leukemia, GIST (GI stromal tumors) fluid retention, thyroid dysfunction
73
getfitnib
TKI: EGFR Tx: non-small cell lung carcinoma skin rash with sun
74
vemurafenib
TKI: BRAF Tx: metastatic melanoma hand-foot syndrome
75
crizotinib
TKI: ALK, HGFR Tx: Non-small cell lung carcinoma
76
dasatinib
TKI: SRC, BCR-ABL, c-KIT, PDGFR Tx: chronic myeloid leukemia, acute lymphoblastic leukemia
77
lapatinib
TKI: EGFR, HER2 Tx: breast cancer skin rash with sun
78
nilotinib
TKI: BCR-ABL, c-KIT, PDGFR Tx: chronic myeloid leukemia
79
pazopanib
TKI: VEGFR, PRGFR, c-KIT Tx: soft tissue sarcoma, renal cell carcinoma hand-foot syndrome
80
sorafenib
TKI: BRAF, VEGFR, PDGFR Tx: renal cell carcinoma, hepatocellular carcinoma hand-foot syndrome, thyroid dysfunction
81
sunitinib
TKI: VEGFR, PDGFR, c-KIT Tx: GIST, renal cell carcinoma, pancreatic neuroendocrine tumor hand-foot syndrome, thyroid dysfunction
82
photo-sensitivity
cetuximab, panitumumab, erlotinib, getfitinib, lapatinib
83
hand foot syndrome
capecitabine, fluorouracil, cytarabine, docetaxel, paclitaxel, liposomal doxorubicin, doxorubicin, sunitinib, sorafenib, pazopanib, vemurafenib
84
lung fibrosis
cyclophosphomide, mephalan, busulfan, bleomycin, MTX
85
peripheral neuropathy
cisplatin, carboplatin, vincristine, lanalidomide, paclitaxel
86
renal toxicity
cyclophosphamide, ifosfamide, cisplatin, (less) carboplatin
87
encephalopathy 1. with seizures 2. no seizures
1. ifosfamide, cisplatin | 2. capecitabine
88
transient aseptic meningitis
IT MTX
89
chronic leukoencephalopathy
characterized by headache, confusion, seizures, visual loss | caused by MTX
90
stroke
cisplatin
91
hepatic veno-occlusive
BCNU, busulfan
92
ototoxic
cisplatin
93
hepatic dysfunction
thioguanine, 6-MP

SS- CMOD Block 2 (16 decks)

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