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Pharm 2014 Unit 1 > Cancer 3 > Flashcards

Cancer 3 Flashcards

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1
Q

What are names of DNA intercalating agents?

A
  1. Dactinomycin
  2. Daunorubicin, Doxorubicin
  3. Bleomycin
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2
Q

DNA intercalating agents are also called

A

anti-tumor antibiotics, which are derived from various strains of the soil microbe Streptomyces

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3
Q

what is the mech of DNA intercalating agents?

A

bind to DNA through intercalation between specific bases and block synthesis of DNA, RNA, or both, cause DNA strands break, and interfere with cell replication

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4
Q

Dactinomycin is also known as

A

Actinomycin D

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5
Q

what is the mech of Dactinomycin (Actinomycin D)?

A

intercalates between G-C base pairs of DNA, forming stable dactinomycin-DNA complex. The complex interferes with DNA-dependent RNA polymerase causing inhibition of transcription of DNA

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6
Q

what is the main therapeutic uses of Dactinomycin?

A

to treat pediatric umors such as Wilms’ tumor, rhabdomyosarcoma and Ewing’s sracoma

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7
Q

what are antrhacycline antibiotics derived from Streptomyces that have a broad spectrum of clinical usefulness in hematologic and solid tumors?

A

Daunorubicin, Doxorubicin, Epirubicin, and Idarubicin

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8
Q

daunorubicin and idarubicin are mainly used for

A

AML treatment

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9
Q

what are the toxicity of - rubicin drugs?

A

irreversible does-limiting cardiotoxicity (cardiomyopathy)

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10
Q

what is a mixture of two copper-chelating peptides obtained from Streptomyces?

A

bleomycin

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11
Q

what is the mech of bleomycin?

A

in the presence of Fe and O2, it forms free radical and induce

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12
Q

what is the therapeutic usage of bleomycin?

A

testicular tumors (usually in combination with vinblastine or etoposide)

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13
Q

toxicity of bleomycin?

A 
pulmonary toxicity (pulmonary fibrosis)
cutaenous toxicity (hyperpigmentation)
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14
Q

what are the three monoclonal antibodies?

A
  1. Rituximab
  2. Trastuzumab (Herceptin)
  3. Cetuximab
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15
Q

what is useful for treating Non-Hodgkin’s lymphomas?

A

Rituximab

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16
Q

what is a monoclonal antibody that targets the CD20?

A

Rituximab

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17
Q

what are two tyrosine kinase inhibitors?

A
  1. Imatinib (Gleevac)

2. Gefitinib

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18
Q

what is an inhibitor of Abl kinase?

A

Imatinib

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19
Q

Imatinib also inhibits

A

PDGFR and c-kit and effective treating CML

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20
Q

Imatinib is approved for CML, but also approved for

A

gastrointestinal tumor

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21
Q

what are the miscellaneous agents used to treat cancer?

A
  1. Hydroxyurea
  2. Retinoids
  3. Arsenic Trioxide
  4. Thalidomide
  5. Interferons
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22
Q

what is the mech of hydroxyurea?

A

inhibits the enzyme ribonucleoside diphosphate reductase, which catalyze the conversion of ribonucleotides to deoxyribonucleotides (a critical rate limiting step in the biosynthesis of DNA)

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23
Q

what are the two therapeutic usage of hydroxyurea?

A
  1. sickle cell diz

2. myeloproliferative neoplasms polycythemia vera and thrombocythemia

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24
Q

what is all-trans retinoic acid (ATRA) what is useful for treating acute promyelocytic leukemia (APL)?

A

Retinoids

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25
what is used for relapsed APL?
arsenic trioxide
26
what is used for treating multiple myeloma and myelodysplastic syndromes?
thalidomide
27
what is used for treating of hairy-cell leukemia, CML, and AIDS-related Kaposi's sarcoma?
Interferons
28
what are the hormone therapies for prostate cancer?
1. Leuprolide, Goserelin | 2. Flutamide, Bicalutamide
29
what are gonadotropin-releasing hormone (GnRH) analogs?
Leuprolide, Goserelin
30
what is the mech for leuprolide?
GnRH analogs, they bind to GnRH receptor and inhibit the release of FSH and LH
31
as a result of leuprolide what happens?
reduced testicular production of testosterone
32
what are nonsteroidal androgen-receptor (AR) blockers?
flutamide, bicalutamide
33
what is the mech of AR blocker (flutamide)
compete with the natural hormone for binding to the androgen receptor and prevent its translocation to the nucleus
34
what is complete androgen ablation therapy?
it involves combination of GnRH analogs and AR blockers
35
what is aromatase enzyme?
conversion of androstenedione and testosterone to the estrogen, estrone and estradiol.
36
in breast cancer pts, there is increased
aromatase activity
37
what is the 1st generation AI?
aminoglutathamide
38
paclitaxel can cause what kind of toxicity?
peripheral neuropathy
39
what is a 3rd generation AI?
Anastrozole
40
what are selective estrogen-receptor downregulator?
pure anti-estrogens (they are devoid of estrogen agonist activity)
41
what is the name of SERDs drug?
Fulvestrant
42
what is Fulvestrant?
the 1st FDA approved SERDs, it binds to ER with much higher affinity (more than 100 fold) than tamoxifen
43
how is Fulvestrant diff from tamoxifen?
tamoxifen stabilizes or even increase ER expression, fulvestrant reduces the number of ER molecules in cells
44
what is therapeutic uses of Fulvestrant?
approved for postmenopausal women with ER-positive metastatic breast cancer
45
dactinomycin is also known as
Actinomycine
46
the main therapetuic uses of Dactinoomycin is
Wilm's tumor, Ewing's sarcoma in children
47
what are anthracyclines?
daunorubicin, doxorubicin, epirubicin, idarubicin
48
mech of action of anthracyclines (doxorubicin)?
intercalate between DNA base pairs, donate electrons to make superoxide
49
sarcomas treatment?
Doxorubicine
50
what is important about the side effect of anthracycline?
dose-limiting cardiotoxicity,
51
Dexrazoxone is an
iron-chelating agent that blocks the fomration of free radical
52
bleomycin is
a mixture of two peptides obtained from Streptomyces, G2 phase specific
53
therapeutic usage of bleomycin?
1. squamous cell caricnomas, ABVD
54
toxicity of bleomycin?
1. minimally myelosuppressive | 2. dose-related pulmonary toxicity (pulmonary fibrosis)
55
microtubule inhibitos
vinca alkaloids, taxanes
56
mech of vinca?
prevent polymerization of tubulin into microtubules
57
what is the therapeutic usage of vinca alkaloids?
Vinblastine --> ABVD | Vincristine --> MOPP, used with glucocorticoids in the treatment of childhood ALL
58
what is the resistance mech of vinca?
P-glycoprotein, mutation in tubulin
59
what are taxanes?
paclitaxel, docetaxel
60
where are taxanes from?
alkaloids dervied from the ye tress
61
the mech of taxanes?
prevent the depolymerization of microtubules
62
docetaxel is useful against
hormone refractory prostate cancer
63
what are the toxicity of taxanes?
perepheral neuropathy
64
topoisomerase inhibitors?
1. epipodophyllotoxins: etoposide, teniposide (top II) | 2. camptothecin analgos: irinotecan, topotecan (top I)
65
epidophyllotoxins
inhibit topoisomerase II --> apoptosis
66
camptothecin analogs
inhibitn topoisomerase I --> apoptosis
67
hormone therapy is suefull in
lymphomas and leukemia, breast, prostate
68
glucocorticoids (prednisone, dexamethasone) are used for
lymphomas and leukemia
69
prednisone is used for
ALL, both Hodkin and non-Hodgkin
70
breast cancer is usually
estrogen dependent, so it can be suppressed by estrogen antagonist
71
SERMs
selective estrogen receptor modulators: Tamoxifen
72
tamoxifen is
a weak agonist in endometrium --> increase risk for endometrial cancer and thromboembolism
73
SERDs
selective estrogen-receptor downregulators: Fulvestrant
74
SERD, Fulvestrant
bins to ER with a much higher affinity (more than 100 fold) than tamoxifen
75
hydroxyurea inhibit
ribonucleotide reductase, for sickle cells
76
all trans-retinoic acid is for
APL = AML M3 --> promotes differentiation of promyelocyte
77
inteferone alpha
hairy cell leukemia, Kaposi's sarcoma
78
Gefitinib
EGFR inhibitor
79
Cetuximab is a
mAb against ErbB1 for treatment of metastatic colon cancer
80
multi-drug resistance
P-glycoprotines --> drug efflux
81
what is verapamil?
Ca2+ channel antagonist, which inhibits these drug transporters
82
P-glyoprotein forms
a central channel for the ATP dependent pumping of drugs from the cell
83
what are the 3 toxicities of cisplatin?
1. nephrotoxicity 2. ototoxicity 3. peripheral neuropathy
84
what are the 3 toxicities of methotrexate?
1. renal toxicity 2. hepatotoxicity 3. bone marrow toxicity
85
toxicity of paclitaxel?
perepheral neuropathy
86
toxicity of vincristine?
neurotoxicity (peripheral neuropahty)
87
resistance to which anticancer drug is associated with decreased expression of hypoxanthine-guanine phosphoribosyl transferase (HGPRT)?
6-MP

Pharm 2014 Unit 1 (13 decks)

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