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
S
DNA synthesase
26
G2
synthesis of components for division
27
M
mitosis | divides into 2 cells which can enter G1 or G0
28
intermittent high dose therapy
most common | better for phase non-specific
29
continuous effusion
drugs that are rapidly metabolised and/or excreted | better for cell cycle specific
30
resistance pathways
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
31
multidrug resistance
MDR1 gene -> P-glycoprotein -> pumps (ATP dependent) drug out of tumor cells may be inhibited by CaCh blocers (verapamil)
32
highly dividing cells at high risk for toxicity
``` bone marrow FI tract hair folicles buccal mucosa sperm forming cells ```
33
nadir
blood count low point due to cehmo | usually 10-14 days after Tx and recover in 21-28 days
34
sargramostim
GM-CSF to stimulate WBC proliferation
35
filgrastim and pegfilgrastim
G-CSF to stimulate WBC proliferation
36
oprelvekin
counteract thrombocytopenia | IL11
37
erythropoietin and darbpoetin
RBC proliferation
38
anti-emetics
``` serotonin antagonists- ondansetron promethiazine cannabionoids benxos corticosteroids ```
39
stomatis
inflammation of oral mucosa that may cause painful ulcers | good oral hygiene and topical anesthetics
40
skeletal complications
fractures and pain | bisphosphonates
41
Alkylating agents MOA
covalent bonds in DNA -> strand corssing -> cannot unwind and stand breakage non cell cycle specific (but most effective in S)
42
alkylating adverse effects
nausea, vomiting, tissue damage at site of injection, meylosupression, secondary malignancies (AML)
43
Cyclophosphamide adverse effects
hemorrhagic cystits | prevented by Mesna
44
cisplatin adverse effects
nephrotoxic- routine hydration and diureiss | ototoxic- more in kids
45
Bulsulfan adverse effects
hyperpigmentation pulmonary fibrosis adrenal insufficiency
46
methotrexate MOA
folic acid analog inhibits dihyrofolate reductase and blocks voncersion of folic acid to tetrahydrofolic acid cannot synthesize thymidylate, purines, serine, and methionine
47
low doses methotrexate
used to Tx other conditons such as RA, colitis, psoriasis
48
leucovorin
rescues healthy cells from methotrexate toxicity
49
methotrexate adverse effects
``` mucosistis diarrhea myelosupression (thrombocytopenia and neutropenia) nuasea, vomiting immunosupression hepatotoxic fatigue ```
50
Fluorouracil MOA
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
5-FU uses
most widely used agent for colorectal CA
52
5-FU adverse effects
anorexia, nausea, stomatitis, diarrhea
53
Mercaptopurine (6-MP) MOA
purine analog inhibits purine synthesis and DNA and RNA synthesis S phase
54
Mercaptopurine metabolism
first pass large effect | when given PO with allopurinol dose must be decreased by 50-75%
55
vinca alkaloids MOA
bind beta tubulin and inhibit microtubule assembly | M phase
56
vinca alkaloid drug resistance
efflux pump P-glycoprotein
57
vinca alkaloids adverse rxns
hair loss and local cellulits vinblastine- myelosupression vincristine- neurologic
58
paclitaxel MOA
taxane | bind to beta-tubulin and promotre microtubule formation and stabalization
59
paclitaxel adverse effects
bone marrow depression peripheral fluid sensory neuropathy fluid retention neutropenia
60
epipodophyllotoxins MOA
etoposide and teniposide inhibit topoisomerase II -> DNA damage thru strand breakage late S-G2 phase
61
epipodophyllotoxins adverse effects
common chemo side affects
62
anthracyclines MOA
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
anthracyclines Adverse effects
``` nausea, red urine alopencia myelosupression stomatitis cadiotoxic (due to ROS) ```
64
Bleomycin MOA
binds DNA -> single and double stranded breaks and inhibits synthesis G2 specific
65
bleomycin adverse effects
``` pulmonary toxicity: pneumonia, cough, dyspnea, crackes, infiltrates allergic rxns fever hypotension skin toxicity mucosisits alopecia ```
66
asparaginase MOA
hydrolyzes circulting l-asparagine into aspartic acid and ammonia blocking protein synthesis G1 ALL
67
asparaginase adverse effects
acute hypersensitivity rxn increased risk of clotting and bleeding pancreatitis CNS
68
imatinib
inhibits tyrosine kinase domain of Bcr-Abl onocprotein preventing phosphorylation of kinase substrate inhibits the kinase PDGFR, stem cell factor, and c-kit
69
uses of imatinib
CML with Philadelphia chrom (9;22) | GI stomal tumors expressing c-kit
70
imatinib adverse effects
myelosupression fluid retention diarrhea myalgias
71
trastuzumab MOA
bind to HER2/neuR (ErbB-3) | expressed in breast CA blocking proliferation
72
trastuzumab adverse effects
cardiotoxic | must monitor ventricular fnx and be discontinued if damage occurs
73
what metabolite of what drug causes hemorrhagic cystitis and
acrolein | cyclophosphamide
74
cytarabine
aka ara-C | pyrimidine analog
75
cytarabine MOA
competitively inhibits DNA polymerase alpha and beta blocking synthesis and repair S-phase only works in hematological tumors
76
cytarabine adverse reactions
myelosupression, mucositis, nausea, vomiting, and neurotoxic at high doses
77
why does allopurinol increase 6-MP
because it is a xanthine oxidase inhibitor
78
other inhibitors of Bcr-Abl
dasatinib | nilotinib
79
TK inhibitor that blocks EGFR
erotinib geftinib used for Tx of non-small cell lung CA
80
TK inhibitor that blocks HER2
lapatinib | less cardiotoxic then trastuzumab
81
rituximab
CD20 (proliferation and differentiation)
82
Alemtuzumab
CD52
83
Gemtuzumab
CD33
84
Cetuximab
EGFR (TK)
85
Bevacizumab
VEGF
86
ibritumomab
CD20 (proliferation and differentiation)
87
tositumomab
CD20 (proliferation and differentiation)