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Step 1 Hematology/Oncology-First Aid 2017 > Pharmacology-Cancer drugs > Flashcards

Pharmacology-Cancer drugs Flashcards

1
Q

What is azathioprine metabolized into?

A

6-MP

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2
Q

What is azathioprine activated by?

A

HGPRT

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3
Q

What is the mechanism of 6-MP/Azathioprine?

A

Decreases de novo purine synthesis

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4
Q

Indications for azathioprine/6-MP

A

Prevent organ rejection

RA, IBD, SLE

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5
Q

What enzyme metabolizes azathioprine/6-MP

A

Xanthine oxidase

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6
Q

What drugs increase toxicity of azathioprine/6-MP

A

Allopurinol and febuxostat

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7
Q

What are side effects of azathioprine/6-MP?

A

Myelosuppression, GI, liver

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8
Q

Drug that is a purine analog which inhibits DNA polymerase and causes DNA strand breaks

A

Cladribine

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9
Q

What is the indication for the purine analog Cladribine?

A

Hairy cell leukemia

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10
Q

What are the side effects of purine analog Cladribine?

A

Myelosuppression, nephrotoxicity, and neurotoxicity

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11
Q

Pyrimidine analog that inhibits DNA polymerase and indicated for AML and lymphomas

A

Cytarabine

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12
Q

Side effects of Cytarabine

A

Myelosuppression with megaloblastic anemia and pancytopenia

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13
Q

Antimetabolite used topically for treatment of basal cell carcinoma; also used for colon cancer and pancreatic cancer

A

5-FU

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14
Q

What is the mechanism of 5-FU

A

Converted to 5-FdUMP which inhibits thymidylate synthase

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15
Q

What is the effect of 5-FU converting to 5-FdUMP and inhibiting thymidylate synthase?

A

Decreases dTMP causing decreased DNA synthesis

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16
Q

What drug is used to enhance the effects of 5-FU?

A

Leucovorin

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17
Q

What is the mechanism of methotrexate?

A

Folic acid analog that inhibits dihydrofolate reductase

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18
Q

What is the effect of methotrexate inhibiting dihydrofolate reductase?

A

Decreases dTMP causing decreased DNA synthesis

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19
Q

What are side effects of 5-FU?

A

Myelosuppression and redness, swelling and desquamation of soles and palms

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20
Q

Non-neoplastic indications for methotrexate

A

Ectopic pregnancy, medical abortion, RA, psoriasis, IBD, vasculitis

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21
Q

What drug is used with methotrexate to induce abortions?

A

Misoprostol

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22
Q

Myelosuppression caused by methotrexate can be reversed with what drug?

A

Leucovorin

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23
Q

Side effects of methotrexate

A

Myelosuppression, hepatotoxicity, mouth ulcers, and pulmonary fibrosis

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24
Q

What are the antitumor medications?

A

Bleomycin, Dactinomycin, and doxorubicin

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25
Q

What antitumor drug induces free radical formation causing DNA strand breaks?

A

Bleomycin

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26
Q

Which antitumor drug is indicated for testicular cancer and Hodgkin lymphoma?

A

Bleomycin

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27
Q

What are the side effects of Bleomycin?

A

Pulmonary fibrosis and skin hyperpigmentation

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28
Q

Antitumor agent indicated for testicular agent that causes minimal myelosuppression

A

Bleomycin

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29
Q

Antitumor drug that intercalates DNA and causes myelosuppression

A

Dactinomycin

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30
Q

Antitumor drug indicated for Wilms tumor, Ewing sarcoma, rhabdomyosarcoma and used in childhood tumors

A

Dactinomycin

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31
Q

Antitumor drug that generates free radicals and intercalates into DNA causing double stranded breaks

A

Doxorubicin and Daunorubicin

32
Q

Antitumor drug indicated for solid tumors, leukemias and lymphomas

A

Doxorubicin and Daunorubicin

33
Q

Antitumor drug that causes dilate cardiomyopathy

A

Doxorubicin

34
Q

Iron chelating agent that is used to prevent cardiotoxicity when using doxorubicin

A

Dexrazoxane

35
Q

What are the alkylating agents?

A

Busulfan, Cyclophosphamide, Nitrosoureas

36
Q

Alkylating agent used to treat CML and bone marrow ablation which cross-links DNA

A

Busulfan

37
Q

Alkylating agent that almost always causes severe myelosuppression, pulmonary fibrosis, and hyperpigmentation

A

Busulfan

38
Q

Alkylating agent used for solid tumors, leukemias and lymphomas that cross-links DNA at guanine N-7

A

Cyclophosphamide

39
Q

What is used to prevent hemorrhagic cystitis when using cyclophosphamide?

A

Mesna or N-acetylcysteine

40
Q

What does cyclophosphamide need before it can have an effect?

A

Bioactivation by the liver

41
Q

Side effects of cyclophosphamide

A

Myelosuppression and hemorrhagic cystitis

42
Q

Alkylating agent used for brain tumors since the are able to cross the BBB

A

Nitrosoureas

43
Q

CNS toxicity resulting in seizures, dizziness and ataxia is seen with which alkylating agent?

A

Nitrosoureas

44
Q

What are the microtubule inhibitors?

A

Paclitaxel, Vincristine and Vinblastine

45
Q

Microtubule inhibitor used for ovarian and breast carcinomas?

A

Paclitaxel

46
Q

What phase in mitosis is stopped by paclitaxel?

A

Anaphase - stabilizes microtubules so mitotic spindle cannot break down

47
Q

Side effects of paclitaxel

A

Myelosuppression, neuropathy, hypersensitivities

48
Q

Anticancer drug that binds B-tubulin and inhibits polymerization of microtubules preventing mitotic spindle formation

A

Vincristine or Vinblastine

49
Q

Anticancer drug indicated for solid tumors and leukemias that binds B-tubulin

A

Vincristine or Vinblastine

50
Q

Anticancer drug with neurotoxicity and used for treatment of non-Hodgkin lymphoma that binds B-tubulin

A

Vincristine

51
Q

Anticancer drug with used for treatment of Hodgkin lymphoma that binds B-tubulin

A

Vinblastine

52
Q

Used to prevent nephrotoxicity when using cisplatin

A

Amifostine and chloride

53
Q

Anticancer drug for treatment of testicular, bladder, ovary and lung carcinomas that cross-links DNA

A

Cisplatin or carboplatin

54
Q

Cisplatin or carboplatin side effects

A

Nephrotoxicity, peripheral neuropathy, ototoxicity

55
Q

Anticancer drug that inhibits topoisomerase II causing DNA degradation

A

Etoposide and Teniposide

56
Q

Etoposide and Teniposide side effects

A

Myelosuppression and alopecia

57
Q

Anticancer drug that inhibits topoisomerase I preventing unwinding and replication of DNA

A

Irinotecan, Topotecan

58
Q

Topoisomerase I inhibitor used for colon cancer

A

Irinotecan

59
Q

Topoisomerase I inhibitor used for ovarian and small cell cancers

A

Topotecan

60
Q

Anticancer drug that inhibits ribonucleotide reductase decreasing DNA synthesis and is S-phase specific

A

Hydroxyurea

61
Q

Anticancer drug that causes severe myelosuppression and used fro myeloproliferative disorders, sickle cell, and melanoma that is S-phase specific

A

Hydroxyurea

62
Q

Monoclonal antibody against VEGF which inhibits angiogenesis used for solid tumors

A

Bevacizumab

63
Q

Monoclonal antibody used for treatment of colorectal cancer and renal cell carcinoma that causes hemorrhage, blood clots and impaired wound healing

A

Bevacizumab

64
Q

EGFR tyrosine kinase inhibitor used for non-small cell lung carcinoma that causes a rash

A

Erlotinib

65
Q

Monoclonal antibody against EGFR used for stage IV colorectal cancer and head and neck cancer that causes rash, elevated LFTs and diarrhea

A

Cetuximab

66
Q

Tyrosine kinase inhibitor of Bcr-Abl and c-kit use for treatment of CML and GI stromal tumors that cause fluid retention

A

Imatinib

67
Q

Monoclonal antibody against CD20 used for non-Hodgkin lymphoma, CLL, TIP, and RA that increases risk of progressive multifocal leukoencephalopathy

A

Rituximab

68
Q

Proteosome inhibitors that induce arrest at G2-M phase and apoptosis used in MM and mantle cell lymphoma that cause peripheral neuropathy and herpes zoster reactivation

A

Bortezomib and Carfilzomib

69
Q

Selective estrogen receptor blocker used in the treatment of breast cancer that block binding of estrogen to ER positive cells

A

Tamoxifen

70
Q

Selective estrogen receptor modulator used for treatment of osteoporosis

A

Raloxifene

71
Q

Selective estrogen receptor blocker that is a partial agonist in endometrium which increases the risk of endometrial cancer

A

Tamoxifen

72
Q

Estrogen receptor antagonist that is safe to use since it does not increase risk of endometrial cancer and used for treatment of osteoporosis

A

Raloxifene

73
Q

What drug is a monoclonal antibody against HER-2 used for the treatment of breast and gastric cancer that causes cardiotoxicity?

A

Trastuzumab

74
Q

Small molecule inhibitor of BRAF oncogene positive melanoma used for V600E metastatic melanoma

A

Vemurafenib

75
Q

Oncologic emergency triggered by massive tumor lysis

A

Tumor lysis syndrome

76
Q

Treatment for Tumor lysis syndrome

A

Aggressive hydration, allopurinol and rasburicase

77
Q

Recombinant uricase that catalyzes metabolism of uric acid and used for prevention and treatment of tumor lysis syndrome

A

Rasburicase

Step 1 Hematology/Oncology-First Aid 2017 (5 decks)

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