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Concepts in Pathology and Tissue Morphology > Antineoplastic pharmacology > Flashcards

Antineoplastic pharmacology Flashcards

1
Q

Mechanism of action of 5-FU

A

Inhibit thymidylate synthetase

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2
Q

Drug that causes acute hemorrhagic cystitis

A

Cyclophosphamide

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3
Q

Drug that is cell cycle specific, acting specifically in mitotic phase

A

Paclitaxel

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4
Q

Cardiotoxicity limits total administration of

A

Adriamycin

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5
Q

Drug that doesn’t suppress bone marrow

A

Bleomycin

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6
Q

Kinase inhibitors

A

Imatinib (gleevec)
Nilotinib
Dasatinib

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7
Q

Antibody against EGFR-HER2 receptor

A

Trastuzuma (herceptin)

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8
Q

Antibody against VEGF

A

Bevacizumab (avastin)

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9
Q

Checkpoint inhibitors

A

Ipilimumab (yervoy)

Nivolumab (opdivo)

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10
Q

Inhibit angiogenesis by blockin VEGF and bFGF

A

Thalidomide

Lenalidomid

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11
Q

Proteosome inhibitors

A

Bortezamib (velcade)

Carfilzomib

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12
Q

Alkylating agents

A 
Mechlorethamine
Cyclophosphamide
Busulfan
Carmustin
Cisplatin
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13
Q

Binds dsDNA containing guanosine, intercalates, and generates free radicals

A

Actinomycin D

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14
Q

Intercalated quinone redox center that binds Fe++ and oxidized to Fe+++ ->superoxides

A

Adriamycin

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15
Q

Glycopeptide that intercalates and generates free radicals

A

Bleomycin

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16
Q

Inhibitors of topoisomerase II

A

Etoposide

Teniposide

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17
Q

Inhibitor of topoisomerase I

A

Irinotecan

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18
Q

Imatinib (gleevec) is used frequently for

A

Ph+ CML and AML

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19
Q

Metabolism of imatinib (gleevec)

A

CYP3A4

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20
Q

Drugs that Compete with imatinib for CYP3A4 metabolism

A

Warfarin

Grapefruit juice

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21
Q

Drugs that induce CYP3A4 metabolism and affect imatinib administration

A

Phenytoin

St. John’s wort

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22
Q

Side effects of imatinib

A 
Nvd
Skin rxns
Hepatotoxicity
Htn
Myelosuppression
Edema
CHF
Musculoskeletal pain
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23
Q

Side effects of trastuzumab (herceptin)

A 
Nvd
Rigors
Infusion rxns
Cardiac dysfunction
CHF
Hypotension
Edema
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24
Q

Uses for bevacizumab (avastin)

A

Colon cancer, vasculopathy

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25
Q

Checkpoint inhibitor that is an MAB against CTLA4 on T cells

A

Ipilimumab (yervoy)

*CTLA4 = cyctotoxic t lymphocyte associated protein 4

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26
Q

Uses for ipilimumab (yervoy)

A

Melanoma
NSCLC
Hodgkins lymphoma

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27
Q

Checkpoint inhibitor that is an MAB against PD-1 on some NK cells

A

Nivolumab (opdivo)

PD-1=programmed death receptor

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28
Q

Drug that can cause significant incidence of secondary leukemias

A

Etoposide and teniposide

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29
Q

Toxicity from checkpoint inhibitors prominently includes

A

Autoimmunity

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30
Q

Chimeric antigen receptor (CAR) T cell can be used for

A

Cancer and autoimmune

Subsets of treatment resistand cancers

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31
Q

Uses for angiogenesis inhibitors - thalidomide and lanalidomide

A

Causes direct growth arrest in multiple myeloma cells

32
Q

Side effects of thalidomide

A

Teratogenic

Peripheral neuropathy

33
Q

Side effects of lanalidomide

A

Teratogenic
Peripheral neuropathy
Neutropenia
Thromboembolism

34
Q

Boron containing 26S proteasome inhibitor

A

Boretezamib

35
Q

Bortezamib mechanism

A

Disregulates turnover of proteins mediating cell cycle (cyclins, p53)
ER stress -> apoptosis

36
Q

Metabolism of bortezamib

A

CYP3A4

37
Q

Uses of bortezamib (velcade)

A

Mutliple myeloma and mantle cell lymphoma

38
Q

What is dose limiting toxicity of bortezamib (velcade)

A

Peripheral neuropathy

39
Q

Drug that has extremely low therapeutic index ~1

A

Bortezamib (velcade)

40
Q

Mechlorethamine mechanism

A

Alkylating agent

Form covalent adducts across DNA strands

41
Q

Administration of mechlorethamine (alkylating agent)

A

Iv infusion near tumor site

42
Q

Administration of cyclophosphamide (alkylating agent)

A

Oral -> wide distribution

43
Q

Elimination of cyclophosphamide (alkylating agent)

A

Urine (active alkylator and metabolites)

44
Q

Toxicities of cyclophosphamide

A

Classical toxicities + myocarditis and hemorrhagic cystitis

45
Q

Use of cyclophosphamide (alkylating agent)

A

Hematogenous tumors

46
Q

Administration of actinomycin d

A

IV

47
Q

Elimination of actinomycin d

A

Bile and urine - unchanged

48
Q

Uses of actinomycin d

A

Choriocarcinoma, wilms tumor, testicular tumors, karposis sarcoma

49
Q

Administration and distribution of adriamycin

A

IV; wide except CNS

50
Q

Elimination of adriamycin

A

Bile

51
Q

Metabolism of adriamycin

A

Liver

52
Q

Toxicities of adriamycin

A

Classical toxicities + adriamycin cardiotoxicity

53
Q

Administration of bleomycin

A

Iv or IM

54
Q

Use of bleomycin

A

Lymphoma, germ cell cancers, head/neck cancer

55
Q

Folic acid analog

A

Methotrexate

56
Q

Inhibits dihydrofolate reductase

A

Methotrexate

57
Q

What cant be synthesiaed due to methotrexate

A

Thymidine

Tetrahydrofolate

58
Q

Dose limiting toxicity of purine analogs (ie 6-MP)

A

Myelosuppression

59
Q

6-MP blocks synthesis of

A

ATP and GTP

60
Q

Metabolism of 6-MP (purine analog)

A

Tissue xanthine oxidase and thiopurine methyltransferase

61
Q

6-MP has a reaction with

A

Allopurinol

62
Q

5-FU inhibits

A

Thymidylate synthetase

63
Q

Effects of 5-FU enhanced by

A

Leukovorin

64
Q

Drug that can be used topically for basal cell carcinoma

A

5-FU

65
Q

Toxicities of 5-FU

A

Classical toxicities + CNS (ataxia, confusion)

66
Q

Drugs that bind to tubulin and disaggregate mitotic spindles -> metaphase arrest

A

Vinca alkaloids: vincristine, vinblastine

67
Q

Drug that binds tubulin and stabilized microtubules -> metaphase arrest

A

Taxol (paclitaxel)

68
Q

Estrogen agonist

A

Estradiol

69
Q

Estrogen antagonist

A

Tamoxifen

70
Q

Androgen agonist

A

Danazol

71
Q

Androgen antagonist

A

Flutamide

72
Q

GnRH agonist

A

Leuprolide

73
Q

GnRH antagonist

A

Degarelix

74
Q

Drugs that can be used for reversible chemical orchiectomy or oophorectomy

A

Leuprolide (GnRH agonist)

Degarelix (antagonist)

75
Q

Aromatase inhibitors

A

Anastrazole, letrozole, vorozole

76
Q

Mechanism of aromatase inhibitors

A

Prevent generation of estrogens from androgens

More effective than tamoxifen

Concepts in Pathology and Tissue Morphology (10 decks)

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