chemo drugs Flashcards

1
Q

alkylating agents

A
nitrogen mustards
mehtyhydrazine derivative
alkyl sulfonate
nitrosoureas
triazenes
platinum coordination complexes
not cell cycle specific
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2
Q

nitrogen mustards

A

cyclophosphamide

ifosfamide

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3
Q

alkyl suflonate

A

busulfan

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4
Q

platinum coordination complexes

A

cisplatin

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5
Q

antimetabolites

A

Folic acid analogs
pyrimidine analogs
purine analogs
cell cycle specific (S)

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6
Q

folic acid analogs

A

methotrexate (MTX)

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7
Q

pyrimidine analogs

A

fluorouracil (5-FU)

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8
Q

purine analogs

A

mercaptopurine (6-MP_

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9
Q

natural products

A
vinca alkaloids
taxanes
epipofophyllotoxins
camptothecins
antibiotics
echionocandins
anthracenedione
enzymes
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10
Q

vinca alkaloids

A

vineblastine

vincristine

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11
Q

taxanes

A

paclitaxel

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12
Q

epipodophyollotoxins

A

etopodise

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13
Q

antibiotics

A

doxorubicin

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14
Q

anthracenedione

A

bleomycin

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15
Q

enzymes

A

L-asparaginase

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16
Q

proteins tyrosine kinase inhibitos

A

Imatinib

all end in tinib

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17
Q

monoclonal Abs

A

trastuxumab

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18
Q

rescue agents

A

leucovorin

Mesna

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19
Q

agents to minimize adverse effects

A

filgrastim and pegfilgrastin
erythopoietin
ondansetron (serotonin antagonist)

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20
Q

primary induction chemo

A

Tx for advanced stage with no other alternative

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21
Q

Neoadjuvant chemotherapy

A

localized cancer for which surgery or radiation are not effective

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22
Q

adjuvant chemo

A

reduce incidence of both local and systemic recurrence and increase overall survival

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23
Q

Cell cycle

A

G0 -> G1 -> S -> G2 -> M

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24
Q

G1

A

preceded DNA synthesis

synthesis of DNA componenets

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25
Q

S

A

DNA synthesase

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26
Q

G2

A

synthesis of components for division

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27
Q

M

A

mitosis

divides into 2 cells which can enter G1 or G0

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28
Q

intermittent high dose therapy

A

most common

better for phase non-specific

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29
Q

continuous effusion

A

drugs that are rapidly metabolised and/or excreted

better for cell cycle specific

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30
Q

resistance pathways

A

decreased drug transport into cells
reduced drug affinity due to mutations of drug target
increased expression of enzymes that inactivate drug
increased expression of DNA repair enzymes

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31
Q

multidrug resistance

A

MDR1 gene -> P-glycoprotein -> pumps (ATP dependent) drug out of tumor cells
may be inhibited by CaCh blocers (verapamil)

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32
Q

highly dividing cells at high risk for toxicity

A
bone marrow
FI tract
hair folicles
buccal mucosa
sperm forming cells
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33
Q

nadir

A

blood count low point due to cehmo

usually 10-14 days after Tx and recover in 21-28 days

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34
Q

sargramostim

A

GM-CSF to stimulate WBC proliferation

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35
Q

filgrastim and pegfilgrastim

A

G-CSF to stimulate WBC proliferation

36
Q

oprelvekin

A

counteract thrombocytopenia

IL11

37
Q

erythropoietin and darbpoetin

A

RBC proliferation

38
Q

anti-emetics

A
serotonin antagonists- ondansetron
promethiazine
cannabionoids
benxos
corticosteroids
39
Q

stomatis

A

inflammation of oral mucosa that may cause painful ulcers

good oral hygiene and topical anesthetics

40
Q

skeletal complications

A

fractures and pain

bisphosphonates

41
Q

Alkylating agents MOA

A

covalent bonds in DNA -> strand corssing -> cannot unwind and stand breakage
non cell cycle specific (but most effective in S)

42
Q

alkylating adverse effects

A

nausea, vomiting, tissue damage at site of injection, meylosupression, secondary malignancies (AML)

43
Q

Cyclophosphamide adverse effects

A

hemorrhagic cystits

prevented by Mesna

44
Q

cisplatin adverse effects

A

nephrotoxic- routine hydration and diureiss

ototoxic- more in kids

45
Q

Bulsulfan adverse effects

A

hyperpigmentation
pulmonary fibrosis
adrenal insufficiency

46
Q

methotrexate MOA

A

folic acid analog
inhibits dihyrofolate reductase and blocks voncersion of folic acid to tetrahydrofolic acid
cannot synthesize thymidylate, purines, serine, and methionine

47
Q

low doses methotrexate

A

used to Tx other conditons such as RA, colitis, psoriasis

48
Q

leucovorin

A

rescues healthy cells from methotrexate toxicity

49
Q

methotrexate adverse effects

A
mucosistis
diarrhea
myelosupression (thrombocytopenia and neutropenia)
nuasea, vomiting
immunosupression
hepatotoxic
fatigue
50
Q

Fluorouracil MOA

A

purine analog prodrug
covalently binds thymidylate synthetase and blocks synthesis of thymidylate
interferes with DNA synthesis, DNA fnx, RNA processing, mRNA translation
S phase specific

51
Q

5-FU uses

A

most widely used agent for colorectal CA

52
Q

5-FU adverse effects

A

anorexia, nausea, stomatitis, diarrhea

53
Q

Mercaptopurine (6-MP) MOA

A

purine analog
inhibits purine synthesis and DNA and RNA synthesis
S phase

54
Q

Mercaptopurine metabolism

A

first pass large effect

when given PO with allopurinol dose must be decreased by 50-75%

55
Q

vinca alkaloids MOA

A

bind beta tubulin and inhibit microtubule assembly

M phase

56
Q

vinca alkaloid drug resistance

A

efflux pump P-glycoprotein

57
Q

vinca alkaloids adverse rxns

A

hair loss and local cellulits
vinblastine- myelosupression
vincristine- neurologic

58
Q

paclitaxel MOA

A

taxane

bind to beta-tubulin and promotre microtubule formation and stabalization

59
Q

paclitaxel adverse effects

A

bone marrow depression
peripheral fluid sensory neuropathy
fluid retention
neutropenia

60
Q

epipodophyllotoxins MOA

A

etoposide and teniposide
inhibit topoisomerase II -> DNA damage thru strand breakage
late S-G2 phase

61
Q

epipodophyllotoxins adverse effects

A

common chemo side affects

62
Q

anthracyclines MOA

A

doxorubicin
-inhibits topoisomerase II
-intercalates DNA and blocks synthesis of DNA and RNA synthesis
-generates semiquinone and oxygen free radicals
-binds to cellular membranes changing fluidity and transport
not specific to cell cycle phase

63
Q

anthracyclines Adverse effects

A
nausea, 
red urine
alopencia
myelosupression
stomatitis
cadiotoxic (due to ROS)
64
Q

Bleomycin MOA

A

binds DNA -> single and double stranded breaks and inhibits synthesis
G2 specific

65
Q

bleomycin adverse effects

A
pulmonary toxicity: pneumonia, cough, dyspnea, crackes, infiltrates
allergic rxns
fever
hypotension
skin toxicity
mucosisits
alopecia
66
Q

asparaginase MOA

A

hydrolyzes circulting l-asparagine into aspartic acid and ammonia blocking protein synthesis
G1
ALL

67
Q

asparaginase adverse effects

A

acute hypersensitivity rxn
increased risk of clotting and bleeding
pancreatitis
CNS

68
Q

imatinib

A

inhibits tyrosine kinase domain of Bcr-Abl onocprotein preventing phosphorylation of kinase substrate
inhibits the kinase PDGFR, stem cell factor, and c-kit

69
Q

uses of imatinib

A

CML with Philadelphia chrom (9;22)

GI stomal tumors expressing c-kit

70
Q

imatinib adverse effects

A

myelosupression
fluid retention
diarrhea
myalgias

71
Q

trastuzumab MOA

A

bind to HER2/neuR (ErbB-3)

expressed in breast CA blocking proliferation

72
Q

trastuzumab adverse effects

A

cardiotoxic

must monitor ventricular fnx and be discontinued if damage occurs

73
Q

what metabolite of what drug causes hemorrhagic cystitis and

A

acrolein

cyclophosphamide

74
Q

cytarabine

A

aka ara-C

pyrimidine analog

75
Q

cytarabine MOA

A

competitively inhibits DNA polymerase alpha and beta
blocking synthesis and repair
S-phase
only works in hematological tumors

76
Q

cytarabine adverse reactions

A

myelosupression, mucositis, nausea, vomiting, and neurotoxic at high doses

77
Q

why does allopurinol increase 6-MP

A

because it is a xanthine oxidase inhibitor

78
Q

other inhibitors of Bcr-Abl

A

dasatinib

nilotinib

79
Q

TK inhibitor that blocks EGFR

A

erotinib
geftinib
used for Tx of non-small cell lung CA

80
Q

TK inhibitor that blocks HER2

A

lapatinib

less cardiotoxic then trastuzumab

81
Q

rituximab

A

CD20 (proliferation and differentiation)

82
Q

Alemtuzumab

A

CD52

83
Q

Gemtuzumab

A

CD33

84
Q

Cetuximab

A

EGFR (TK)

85
Q

Bevacizumab

A

VEGF

86
Q

ibritumomab

A

CD20 (proliferation and differentiation)

87
Q

tositumomab

A

CD20 (proliferation and differentiation)