Anti-Neoplastics Flashcards

(79 cards)

1
Q

cell cycle nonspecific alkylating agents

A

mechlorethamine, carmustine

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2
Q

cell cycle specific phase nonspecific alkylating agents

A

cyclophosphamide

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3
Q

least selective of the anti-neoplastics

A

alkylating agents

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4
Q

typical side effects of anti-neoplastics

A

myelosuppression, GI effects (nausea/vomiting), alopecia

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5
Q

nitrogen mustards

A

mechlorethamine, cyclophosphamide

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6
Q

nitrosoureas

A

carmustine

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7
Q

non-Hodgkins lymphoma drug

A

mechlorethamine

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8
Q

cyclophosphamide: mechanism, cell cycle specificity, side effects, uses

A

prodrug activated by liver cytochrome P450s, cell cycle specific phase nonspecific, bladder toxicity, broad uses

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9
Q

carmustine: cell cycle specificity, uses

A

cycle-nonspecific, brain tumors (crosses blood-brain barrier)

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10
Q

treats brain tumors

A

carmustine

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11
Q

methotrexate: mechanism

A

binds to dihydrofolate reductase and prevents formation of tetrahydrofolate

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12
Q

followed by “rescue” of host cells by leucovorin

A

methotrexate

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13
Q

methotrexate: side effects and uses

A

myelosuppression, GI damage, renal tubular necrosis, displaces other drugs from serum albumin; acute lymphocytic leukemia (ALL)

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14
Q

pyrimidine analogs

A

5-FU, cytarabine

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15
Q

5-FU: mechanism, uses

A

pyrimidine analog that inhibits RNA and DNA synthesis; broad spectrum of uses but mostly for GI cancers

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16
Q

cytarabine: mechanism, side effects, uses

A

pyrimidine analog that causes chain termination of DNA, myelosuppression and neurotoxicity, acute myelocytic leukemia (AML)

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17
Q

has neurotoxicity and myelosuppression as side effects

A

cytarabine

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18
Q

pyrimidine analog that causes chain termination of DNA

A

cytarabine

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19
Q

treats acute myelocytic leukemia (AML)

A

cytarabine, 6-MP, etoposide

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20
Q

6-mercaptopurine: mechanism, metabolism, use

A

purine analog, inhibits RNA and DNA synthesis; metabolized by TPMT; acute leukemias

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21
Q

patients with no functional TPMT cannot tolerate what drug?

A

6-mercaptopurine

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22
Q

hydroxyurea: mechanism

A

inhibits ribonucleotide reductase, prevents DNA synthesis, arrests cells at G1-S interface

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23
Q

hydroxyurea: use

A

granulocytic leukemia

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24
Q

inhibits ribonucleotide reductase

A

hydroxyurea

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25
treats granulocytic anemia
hydroxyurea
26
binds to tubulin, inhibiting proper formation of microtubules and mitotic spindle
vincristine, vinblastine
27
major differences between vincristine and vinblastine
vinblastine is strongly myelosuppressive and treats breast cancer, vincristine treats acute lymphocytic leukemia (ALL)
28
vinca alkaloids: mechanism
binds to tubulin, inhibiting proper formation of microtubules and mitotic spindle
29
enhances assembly and stability of microtubules
taxanes (paclitaxel)
30
paclitaxel mechanism
enhances assembly and stability of microtubules, interferes with DNA repair
31
paclitaxel: use, side effect
refractory ovarian cancer; peripheral neuropathy
32
treats refractory ovarian cancer
paclitaxel
33
antitumor antibiotic
doxorubicin
34
only drug with some anti-angiogenic properties
doxorubicin
35
doxorubicin: cell cycle specificity
cycle-specific phase non-specific
36
multi-faceted mechanism of doxorubicin
1. intercalates in DNA, distorting DNA helix 2. causes lipid peroxidation and free radical generation 3. binds to DNA + topoisomerase II
37
doxorubicin: unique side effect
cardiomyopathy (cardiotoxicity)
38
cardiomyopathy (cardiotoxicity) as a side effect
doxorubicin
39
pulmonary toxicity as a side effect
bleomycin
40
bleomycin: mechanism
iron-containing glycopeptides that bind to DNA, makes site-specific DNA breaks, phase-specific for G2
41
bleomycin: unique side effect
pulmonary toxicity
42
etoposide: mechanism
stabilizes DNA-topoisomerase II complexes, results in dsDNA breaks that cannot be repaired
43
goal is to limit chemotherapy-induced neutropenia
filgrastim (G-CSF)
44
filgrastim (G-CSF): unique side effect
bone pain
45
filgrastim (G-CSF): mechanism
promotes progenitor of neutrophils
46
treats breast cancers that overexpress HER2
trastuzumab
47
trastuzumab: mechanism
monoclonal antibody that binds HER2 receptor and blocks proliferation of cells
48
has nephrotoxicity as a side effect
cisplatin
49
cisplatin: mechanism; cycle specificity
platinum coordination complex, causes DNA crosslinks; cycle-specific phase-nonspecific
50
cisplatin: unique side effect
nephrotoxicity
51
revolutionized treatment of testicular cancer
cisplatin
52
procarbazine: mechanism
activated in vivo by liver enzymes to methylating agent which causes chromosomal damage
53
procarbazine: use
Hodgkin's lymphoma
54
treats Hodgkin's lymphoma
procarbazine
55
prednisone: mechanism
binds to steroid receptors, depress expression of many growth related genes, induce nucleases which may modulate cell lysis
56
prednisone: uses, palliative effects
lymphoma, leukemia, breast cancer; anti-emetic, anti-inflammatory, stimulates appetite
57
estrogen receptor antagonist
tamoxifen
58
tamoxifen: mechanism, uses
estrogen receptor antagonist that competitively blocks estrogen receptors in breast tissue, cytostatic (stops cell growth without killing the cells); pre-menopausal metastatic breast cancer and advanced post-menopausal breast cancer, breast cancer prophylaxis for those at higher risk
59
breast cancer prophylaxis for those at higher risk
tamoxifen
60
tamoxifen: metabolism
activated by CYP2D6
61
tamoxifen: unique side effects
bone and other musculoskeletal pain, may increase rates of uterine/endometrial cancer
62
may increase rates of uterine/endometrial cancer
tamoxifen
63
blocks conversion of angdrogens to estrogens by inhibiting aromatase
letrozole
64
letrozole: mechanism, use
blocks conversion of angdrogens to estrogens by inhibiting aromatase; first line treatment of post-menopausal advanced or metastatic breast cancer
65
analog of GnRH
leuprolide
66
leuprolide: mechanism, use, side effects
analog of GnRH, desensitizes GnRH signaling and decreases testosterone; advanced hormonally responsive prostate cancer; hot flashes and impotence
67
treats advanced hormonally responsive prostate cancer
leuprolide
68
has side effects of hot flashes and impotence
leuprolide
69
antiandrogen that blocks androgen receptors
flutamide
70
flutamide: mechanism and use
antiandrogen that blocks androgen receptors; metastatic prostate cancer
71
3 drugs that lack significant bone marrow toxicity
vincristine, prednisone, bleomycin
72
treats metastatic prostate cancer
flutamide
73
define concurrent inhibition
inhibitors block two separate pathways that lead to the same end product
74
define complementary inhibition
one drug affects the function of an end product, the other drug affects the synthesis of that end product
75
define the synchronization strategy of antineoplastic therapy
synchronize cells so they are in one phase and then use a drug that is specific for that phase
76
define the recruitment strategy of antineoplastic therapy
bring cells out of G0 and back into cell cycle via therapy with cell cycle-nonspecific drugs and then hit them with cycle-specific drugs
77
which drug has bladder toxicity (cystitis) as a side effect and what drug prevents this?
cyclophosphamide; mesna
78
inhibits BCR-ABL tyrosine kinase in CML
imatinib mesylate (Gleevec)
79
imatinib mesylate (Gleevec): mechanism, net effect
inhibits BCR-ABL tyrosine kinase in CML, net effect blocks cell proliferation and increases apoptosis