Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm Exam 2 > 16/17- Antineoplastic agents > Flashcards

16/17- Antineoplastic agents Flashcards

1
Q

folate is required for the synthesis of ..,

A

purines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

primary target of methotrexate

A

dihydrofolate reductase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

2 actions of methotrexate

A
  • reduces synthesis of purines
  • reduces synthesis of dTMP by inhibiting the necessary cofactor for thymidylate synthetase

—> reduces cellular proliferation and induces cellular death by preventing synthesis of RNA and DNA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

used to reduce methotrexate toxicity

A

leucovorin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

MOA 5-fluorouracil

A

metabolised to FdUMP which inhibits thymidylate synthase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

5-FU causes damage by..

A

decreasing levels of dTMP and by incorporating into DNA and RNA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

prodrug of 5-FU taken orally

A

capecitabine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

adverse effects 5-FU

A

oral and GI ulcers

bone marrow suppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

specific treatment uses for cytarabine

A

acute myelogenous leukemia

only used in treatment of hematologic malignancies

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

during what stage of the cell cycle is cytarabine active?

A

only active in s phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

MOA cytarabine

A

incorporation into DNA inhibits DNA polymerase thus halting elongation of DNA molecules

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

inactivates cytarabine

A

cytidine deaminase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

toxicity of cytarabine

A

cerebellar syndrome because CNS is exposed to higher levels than the rest of the body

-> dysarthria, nystagmus, ataxia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what does cytarabine need in order to become activated?

A

nucleoside transporter and deoxycytidine kinase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

cytotoxic effects of gemcitabine

A
  • incorporated into DNA -> inhibit synthesis and function

- ihibits ribonucleotide reductase (decrease dNTPS for DNA synthesis)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

what enzyme is necessary for 6TG and 6MP to act?

A

hypoxanthine-guanine phosphoribosyl transferase HGPRT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

MOA 6-TG and 6-MP

A

incorporation into DNA

stop purine synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

MOA fludarabine

A

incorporated into DNA and RNA

inhibits DNA pol and ribonucleotide reductase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

what enzyme is necessary to activate fludarabine?

A

deoxycytidine kinase

also necessary to activate cladribine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

standard therapy for hairy cell leukemia

A

cladribine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

MOA cladribine

A

incorporated into DNA

potent inhbitor of ribonucleotide reductase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

cytotoxic MOA methotrexate

A

inhbits dihydrofolate reductase –> reduces precursors for RNA and DNA synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

cytotoxic MOA 5-FU

A

incorporated into DNA and RNA –> inhibts synthesis and function

inhbits thymidylate synthetase which reduces DNA precursors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

cytotoxic MOA cytarabine

A

incorporated into DNA and RNa, which inhbits synthesis and function

inhibits DNA synthesis by inhibiting DNA polymerase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

cytotoxic MOA gemcitabine

A

incorporated into DNA, which inhibits synthesis and function

inhibits ribonucleotide reductase which reduces precursors for DNA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

cytotoxic MOA 6-MP and 6-TG

A

incorporated into DNA which inhibits synthesis and function

reduce precursors for RNA and DNA by inhibiting purine synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

cytotoxic MOA fludarabine

A

incorporated into DNA and RNA which inhibits synthesis and function

inhibits DNA polymerase and ribonucleotide reductase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

cytotoxic MOA cladribine

A

incorporated into DNA

causes strand breaks

potent inhibitor of ribonucleotide reductase which reduces DNA precursors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

most common binding site for alkylating agents

A

seven nitrogen group of guanine –> causes DNA crosslinking and strand breakage

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

are alkylating agents specific to a certain stage of the cell cycle?

A

nope - toxic in all stages

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

most common adverse affect of cyclophosphamide

A

hemorrhagic cystits

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

what drug is used to combat hemorrhagic cystitis of cyclophosphamide?

A

mesna

33
Q

why is carmustine commonly used to treat brain tumors?

A

lipophilic and can cross BBB

34
Q

3 common adverse effects of alkylating agents

A

can cause leukemia (4 yrs later peak incidence)

blistering properties that damage veins

bone marrow suppresion and damage to intestinal mucosa

35
Q

increased expression of MGMT stops what drugs?

A

alkylating agents

prevents permanent DNA damage by removing alkyl groups from guanin before cross-links form

36
Q

what can inactivate alkylating agents

A

glutathione

37
Q

what transports non-classical alkylating agents into cells?

A

Cu2+ transporter

38
Q

would you rather use cisplatin or carboplatin with another drug that cause a lot of myelosuppresion?

A

cisplatin

carboplatin causes more myelosuppression but less nausea, neurotoxicity, ototoxicity and nephrotoxicity than cisplatin

39
Q

unique adverse effects of cisplatin

A

peripheral neuropathy

tinnitus

nephrotoxicity

hypomagnesia

40
Q

antimicrotubule agents

A

vinblastine and vincristine

prevent formation of microtubules and kill in mitosis

41
Q

which is more neurotoxic: vincristine or vinblastine?

A

vincristine has more neurological side effects but vinblastine has more significant myelosuppression

42
Q

antimicrotubule agent

A

paclitaxel

kills in mitosis by preventing the de-polymerization of microtubules

43
Q

major adverse effect of paclitaxel

A

peripheral neuropathy and bone marrow toxiicity

44
Q

what drug is used with paclitaxel to reduce myelosuppression

A

filgrastim

45
Q

inhibitors of topoisomerase I

A

irinotecan

topotecan

46
Q

class II topoisomerase inhibitor

A

Etoposide

47
Q

fuction of topoisomerases

A

cut DNA, unwind it, and repair the cut during DNA replication

48
Q

cytotoxic antibiotics

A

doxorubicin

bleomycin

49
Q

cytotoxic MOA of doxorubicin

A

intercalates with DNA –> inhibition of DNA polymerase

also inhibits topoisomerase II –> double strand breaks

50
Q

unique adverse effect of doxorubicin and solution

A

irreversible cardiomyopathy due to free radical formation

dexrazoxane an iron chelator can reduce cardiotoxicity

51
Q

MOA bleomycin

A

small peptide that binds to DNA and causes single and double strand breaks

52
Q

what stage of the cell cycle does bleomycin affect>

A

causes cells to arrest in G2 pahse

53
Q

what is the unique side effect for bleomycin?

A

pulmonary toxicity that is cumulative and irreversible BUT good news it is minimally myelosuppressive

54
Q

MOA of the glucocorticoids prednisone and dexamethasone

A

inhbit lymphocyte proliferation

reduce intracranial pressure with brain tumors

reduce adverse effects such as nausea and vomiting

55
Q

partial estrogen receptor antagonist

A

tamoxifen

56
Q

aromatase inhbitor

A

anatrozole

57
Q

androgen receptor antagonist useful for treatment of prostate cancer

A

flutamide

prevents dihydrotestosterone from binding to androgen receptors

58
Q

GnRH receptor agonist

A

leuuprolide and goserelin

cause desensitizationof GnRH receptor on pituitary

used to treat prostate cancer

59
Q

GnRh receptor antagonist

A

degarelix

used to treat prostate cancer

60
Q

risk of tamoxifen

A

increase risk for endometrial cancer

61
Q

what does aromatase do?

A

converts testosterone into estrogen

62
Q

used to treat estrogen-sensitive breast tumors in post-menopausal women

A

anastrozole

63
Q

used to treat breast cancer with Her-2 amplified

A

trastuzumab

blocks her-2 mediated signaling and can induce antibody dependent cytotoxicity

64
Q

toxicity of trastuzumab

A

cardiotoxicity

65
Q

used to treat EGFR expressing colorectal tumors in combination with other drugs

A

cetuximab

66
Q

what causes tumors to be resistance to cetuximab

A

activating mutations in RAS

routine tests of RAS mutational status need to be preformed

67
Q

binds to VEGF which prevents VEGF binding to VEGFR to promote angiogenesis

A

bevacizumab

used to treat colorectal and breast cancer

68
Q

adverse effects bevacizumab

A

HTN
increased thrombosis or bleeding
increased risk GI perforation
decreased wound healing

69
Q

inhibits both EGFR and HER2 kinase activity

A

lapatinib

70
Q

use of lapatinib

A

used in combination with capecitabine to treat Her2, trastuzumab refractory breast cancer

71
Q

first line treatment for metastatic nonsmall cell lung carcinoma

A

erlotinib

72
Q

MOA erlotinib

A

EGFR inhibitor and ATP competitive inhibitor

73
Q

treatment for chronic myelogenous leukemia caused by philadelphia chromosome

A

imatinib

inhibits the consitiutively active AL

74
Q

used to treat acute lymphoblastic leukemia

A

asparaginase

75
Q

MOA asparaginase

A

starve tumor cells of L-asparagine

76
Q

proteasome inhibitor

A

bortezomib

by inhibiting the proteasome, it elevates levels of p53

77
Q

adverse effects of bortezomib

A

thrombocytopenia, peripheral neuropathy, anemia

78
Q

used to treat renal cell carcinoma

A

temsirolimus

79
Q

MOA temsirolimus

A

inhibition of mTOR complex 1 reduces prtn translation, promotes cell cycle inhibition, and promotes apoptosis

NOT mTORC2 (resistant)

Pharm Exam 2 (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions