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Pharm > Antineoplastic agents II > Flashcards

Antineoplastic agents II Flashcards

1
Q

What are the three major ways in which tumors become resistant to cytarabine?

A
  1. Downregulate transporter
  2. Downregulate deoxycyidine
  3. Upregulate cytidine deaminase
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2
Q

What is the MOA of gemcitabine?

A

difluorodeoxycytidine is converted by deoxycitidine kinase, and is incoroprated into DNA, and inhibits ribonucleotide reductase

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3
Q

What are the two MOA of resistance to gemcitabine?

A

Reduced deoxycytidine kinase

Increased production of deoxycytidine

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4
Q

What is the MOA of 6-mercaptopurine and 6-thioguanine?

A

HGPRT enzyme converts them to thio IMP or thioGMP, inhibiting RNA/DNA synthesis

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5
Q

What is the enzyme that degrades 6MP and 6TG? What is significant about this enzyme?

A

Thiopurine methyltransferase (TPMT)

Some in the population do not have this, thus have much higher toxicity levels

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6
Q

What are the cancers that 6MP and 6TP treat?

A

Acute myelogenous leukemia

Acute lymphocytic leukemia

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7
Q

What are the adverse effects of 6MP and 6TP?

A

Bone marrow suppression

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8
Q

What is the MOA of resistance to 6MP and 6TP?

A

Deficiency in HGPRT

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9
Q

What is the MOA of fludarabine?

A

Deoxycitidine kinase activates it in cells, and it is incorporated into DNA/RNA, and inhibiting DNA polymerase and ribonucleotide reductase

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10
Q

What are the cancers the fludarabine is used to treat?

A

chronic lymphocytic leukemia

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11
Q

What is the MOA of resistance to fludarabine and cladribine?

A

Decreased deoxycitidine kinase

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12
Q

What is the MOA of cladribine?

A

Deoxycitidine kinase activates it in cells, and it is incorporated into DNA/RNA, and inhibiting DNA polymerase and ribonucleotide reductase

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13
Q

What is the enzyme that activates fludarabine and cladribine?

A

deoxycitidine kinase

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14
Q

Why do we have to give purine/pyrimidine analogs in an inactive form?

A

Otherwise will not enter the cell

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15
Q

What is the cancer that cladribine?

A

Hair cell leukemia

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16
Q

What is the general MOA of alkylating agents?

A

intrastrand linking and cross linking

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17
Q

When in the cell cycle are alkylating agents effective?

A

All stages

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18
Q

What are the two nitrogen mustards that are used as alkylating agents?

A

Mechlorethamine

Cyclophosphamide

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19
Q

What cancer is mechlorethamine used to treat?

A

Hodgkin’s lymphoma

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20
Q

What are the unique adverse effects of cyclophosphamide? MOA?

A

Hemorrhagic cystitis

converted to acrolein, which is toxic to the baldder cells

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21
Q

What is the drug that you coadminister with cyclophosphamide to reduce the chances of developing hemorrhagic cystitis? MOA?

A

Mesna

Inactivates acrolein

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22
Q

What is the MOA of carmustine?

A

Alkylating agent

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23
Q

What is carmustine used to treat?

A

Brain ca

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24
Q

What are the adverse effects of alkylating agents?

A

Mutagenic, teratogenic, and myelosuppressive

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25
Q

What cancer develops with the use of alkylating agents?

A

Leukemia

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26
Q

Besides the usual routes of resistance to drugs, how do tumor resist alkylating agents?

A

Inactivation by glutathione

Increased expression of 06-methylguanine-DNA methyltransferase (MGMT)

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27
Q

What is the MOA of 06-methylguanine-DNA methyltransferase (MGMT)?

A

Removes the alkyl groups on DNA that were added by alkylating agents

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28
Q

What is the MOA of the platinum compunds?

A

Cause cross-linking of DNA

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29
Q

What are the three platinum compounds that act like alkylating agents?

A

Cisplatin
Carboplatin
Oxaliplatin

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30
Q

Platinum compounds increase the risk for what cancer?

A

Leukemia

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31
Q

Which causes less n/v: cisplatin or carboplatin?

A

Carboplatin

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32
Q

What are the adverse effects of cisplatin?

A

tinnitus
Nephrotoxicity
peripheral neuropathy

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33
Q

What is the MOA of procarbazine? What is it used to treat?

board

A

Non-classical alkylating agent

Hodgkins

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34
Q

What is the MOA of dacarbazine?

board

A

Non-classical alkylating agent

melanoima/sarcoma

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35
Q

What is the MOA of temozolomide?

board

A

Non-classical alkylating agent

Glioblastomas

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36
Q

What is the dynamic instability of microtubules?

A

Constant breakdown and restructuring

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37
Q

What is the MOA of vinblasine and vincristine?

A

Causes mitotic arrest by preventing formation of microtubules

38
Q

Which drug has neurotoxicity: vinblastine or vincristine?

A

Vincristine

39
Q

What is the MOA of paclitaxel?

A

Binds to beta tubulin of microtubules, and prevent the disassembly

40
Q

What is the MOA of docetaxel?

A

Binds to beta tubulin of microtubules, and prevent the disassembly

41
Q

What are the adverse effects of paclitaxel?

A

Myelosuppression and peripheral neuropathy

42
Q

What are the adverse effects of docetaxel?

A

Periperhal neuropathy

43
Q

What is the drug that is used with paclitaxel, to reduce myelosuppression?

A

Filgrastim

44
Q

What do topoisomerases do in DNA replication?

A

Cut DNA, unwind, and repair the cut

45
Q

What are the two topoisomerase inhibitors?

A

Irinotecan

Topotecan

46
Q

What is the MOA of etoposide?

A

Class IITopoisomerase inhibitor

47
Q

What is the MOA of doxorubin?

A

Abx that intercalates with DNA, leading to inhibition of DNA polymerase

48
Q

What is the significant adverse effect of doxorubin?

A

cardiomyopathy via free radical formation

49
Q

What is the drug that is administered with doxorubicin that mitigates the cardiotoxicity?

A

Dexrazoxane (Fe chelator)

50
Q

What is the MOA of bleomycin?

A

Small glycopeptide antibiotic that chelates iron and copper and binds to DNA and causes
single and double strand breaks.

51
Q

What are the adverse effects of bleomycin?

A

Pulmonary toxicity

52
Q

Which of the antineoplastic are minimally myelosuppressive (3)?

A

Bleomycin
Vincritine
Methotrexate

53
Q

What is the MOA of glucocorticoids in the treatment of cancer?

A

Inhibit lymphocyte proliferation

54
Q

What is the MOA of dexamethasone?

A

Glucocorticoid

55
Q

What is the MOA of tamoxifen?

A

Selective estrogen receptor modulator (competes for estrogen receptor)

56
Q

What are the adverse effects of tamoxifen?

A

Increased risk of endometrial CA

Increased risk of thromboembolism

57
Q

What are the resistance mechanisms of tamoxifen?

A

Estrogen receptor changes cause a reduced affinity with tamoxifen.

58
Q

What is the MOA of anastrozole?

A

Aromatase inhibitor (recall that aromatase synthesizes estrogen from androgens in peripheral tissue)

59
Q

What is anastrozole used for?

A

Treatment of breast cancers

60
Q

What are the two androgen receptor inhibitors? What are thy used to treat?

A

Flutamide
Bicalutamide

Prostate CA

61
Q

What is the MOA of flutamide?

A

androgen receptor inhibitor

62
Q

What is the MOA of bicalutamide?

A

androgen receptor inhibitor

63
Q

What is the MOA of leuprolide?

A

GnRH agonist

64
Q

What is the MOA of goserelin?

A

GnRH agonist

65
Q

How do the GnRH agonists work?

A

Cause a desensitization of the GnRH receptors, which reduces the secretion of both LH
and FSH from the anterior pituitary

66
Q

What is the MOA of degarelix

A

GnRH antagonist, which decreases LH and FSH production

67
Q

What is the MOA of trastuzumab?

A

Binds to estrogen growth signal receptor (HER2), and inhibits it

68
Q

What is the MOA of cetuximab?

A

Monoclonal antibody against EGFR

69
Q

What are the adverse effects of trastuzumab?

A

Cardiac toxicity if combined

70
Q

What cancer does cetuximab treat?

A

EGRF expressing Colorectal cancers

71
Q

What is the mechanism of resistance to cetuximab?

A

Acquiring activating mutations in RAS

72
Q

What is the general MOA of monoclonal antibodies in treating CA?

A

Inhibit growth signals

Cause immune mediated destruction

73
Q

What is the MOA of bevacizumab?

A

Ab against VEGF, inhibiting angiogenesis

74
Q

What is the cancer that bevacizumab is used to treat?

A

clear cell renal cancer

75
Q

What are the adverse effects of bevacizumab?

A

significant blood vessel injury and reduces wound healing

76
Q

What is the MOA of lapatinib?

A

Inhibits EGFR and HER-2 kinase activity

77
Q

What is the MOA of erlotinib?

A

EGRF inhibitor

ATP competitive inhibitor

78
Q

How does the EGRF molecule work?

A

Y kinase that is activated extracellularly, when epidermal growth factor binds, and activates the MAP kinase cascade

79
Q

What is the therapeutic use of erlotinib?

A

Nonsmall cell lung carcinoma if pts have mutation in gene

80
Q

How does resistance come about with erlotinib?

A

Secondary mutation in EGRF or amplification of MET oncogene

81
Q

What is the MOA of imantinib (gleevec)?

A

Binds to ABL portion of the philidelphia chromosome, and prevents kinase from binding its substrate/phosphate donor

82
Q

What is imantinib used to treat?

A

Chronic myelogenous leukemia

83
Q

What is the mechanism of resistance to imantinib?

A

Point mutation BCR-ABL protein to not bind imantinib anymore

84
Q

What is the MOA of asparaginase?

A

Lowers blood [asparagine], which kills tumor cells since they cannot synthesize sufficient asparagine

85
Q

What is asparaginase used to treat?

A

acute lymphoblastic leukemia

86
Q

What are the adverse effects of aparaginase?

A

anaphylaxis

87
Q

What is the MOA of bortezomib? (2)

A

Inhibits proteasome, which increases p53

88
Q

What cancer does bortezomib treat?

A

multiple myeloma

89
Q

What is the main adverse effect with bortezomib?

A

Peripheral neuropathy

90
Q

What is the MOA of temsirolimus?

A

inhibition of mTOR complex, which promotes cell cycle

91
Q

What cancer is temsirolimus used to treat?

A

renal cell carcinoma

92
Q

What is the mechanism of resistance against temsirolimus?

A

mTOR 2 increased

Pharm (73 decks)

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