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Kaplan: Anticancer Drugs, Immunopharmacology, and Toxicology > Anticancer Drugs > Flashcards

Anticancer Drugs Flashcards

1
Q

What is the Log kill hypothesis.

A

Theory that cytotoxic drugs kill fixed percentage of tumor cells not a fixed number. Follow 1st order kinetics.

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2
Q

What is growth fraction meaning.

A

tumors with high turn over

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3
Q

Name a few cytotoxic agents that are S phase specific.

A
  • cytarabine
  • 6-mercaptopurine
  • 6-thioguanine
  • 5-FU
  • methotrexate
  • hydroxyurea
  • irinotecan (blocks topoisomerase I)
  • etoposide (blocks topoisomerase II)
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4
Q

Name some cytotoxic agents that are non-cell cycle specific.

A
  • alkylating agents (cyclophosphamide, cisplatin, procarbazine)
  • antitumor antibiotic (doxorubicin, daunorubicin)
  • nitrosoureas (lomustine, carmustine)
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5
Q

What are the cytotoxic agents that inhibit the M phase of the cell cycle?

A

vinblastine
vincristine
* blocks tubular polymerization

Paclitaxel
(blocks depolymerization of microtubules)

colchicine and griseofulvin also act via this mechanism

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6
Q

What are the cytotoxic agents that act by inhibiting the G2 phase of the cell cycle?

A

Bleomycin (antibiotic)

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7
Q

What is the MOA of cyclophosphamide?

A

alkylating agent basically alkylates DNA by attacking guanine N7 - dysfunctional DNA

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8
Q

S/E of cyclophosphamide?

A

BMS, hemorrhagic cystitis

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9
Q

Antidote cyclophosphamide toxicity? How does it work?

A

mesna which traps the toxic metabolite acrolein and is protective

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10
Q

Uses for cyclophosphamide?

A

really it is used for many conditions including but not limited to non hodgkin lymphoma, ovarian, breast cancer, neuroblastoma

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11
Q

MOA cisplatin?

A

alkylating agent- cross-links DNA strands

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12
Q

Indications for cisplatin?

A

testicular, ovarian, bladder, lung cancer

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13
Q

S/E of using cisplatin?

A

nephrotoxicity; neurotoxicity (deafness)

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14
Q

What drug would you use to protect the kidneys for the nephrotoxic side effects of using cisplatin?

A

amifostine

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15
Q

What is the MOA procarbazine?

A

alkylating agent

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16
Q

Indication procarbazine?

A

Hodgkin

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17
Q

S/E of procarbazine?

A

BMS, leukemogenic

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18
Q

MOA Doxorubicin?

A

Intercalator (meaning it can insert mini grooves in DNA and cause DNA strand breaks), forms free radicals, inhibits topoisomerase

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19
Q

Indications Doxorubicin?

A

Hodgkin, breast, endometrial, lung, and ovarian cancers

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20
Q

S/E doxorubicin?

A

BMS - delayed CHF

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21
Q

Antidote to cardio toxicity caused by doxorubicin?

A

dexrazoxane which is an iron-chelating agent that prevents the formation of free radicals; it is not a free radical “trapper”

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22
Q

Methotrexate MOA?

A

antimetabolite- inhibits DHF reductase (S phase)

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23
Q

Indications for methotrexate?

A

leukemias, lymphomas, breast cancer; rheumatoid arthritis, psoriasis

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24
Q

S/E methotrexate use?

A

BMS

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25
Q

Antidote for methotrexate?

A

folinic acid (leucovorin rescue)

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26
Q

What is the S/E of 5-FU?

A

BMS

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27
Q

MOA Capecitabine?

A

pyrimidine antimetabolite (S phase) bio activated to inhibit thymidilate synthetase

28
Q

S/E capecitabine?

A

BMS

29
Q

Indications capecitabine?

A

breast, ovarian, head and neck cancer, topical for basal cell cancer and keratoses; colorectal cancer

30
Q

6-mercaptopurine MOA.

A

purine antimetabolite bio activated by HGPR transferase.

31
Q

Indications for 6-mercaptorpurine.

A

acute lymphocytic leukemia; immunosuppression

32
Q

S/E 6 mercaptopurine.

A

BMS

33
Q

Bleomycin MOA?

A

complexes with Fe and O2 > DNA strand scission

34
Q

Indications bleomycin?

A

Hodgkin, testicular, head, neck, skin cancer

35
Q

S/E bleomycin

A

pneumonitis, pulmonary fibrosis

36
Q

VInblastine MOA.

A

dec micro tubular polymerization (spindle poison)

37
Q

Vincristine MOA.

A

dec micro tubular polymerization (spindle poison)

38
Q

Indication vinblastine.

A

Hodgkin, testicular cancer, Kaposi

39
Q

Indication Vincristine.

A

Hodkin, leukemias, Wilms

40
Q

VInblastine S/E?

A

BMS

41
Q

Vincristine S/E?

A

neurotoxicity

42
Q

MOA All-trans retinoid acid (ATRA)

A

differentiating agent, promotes differentiation of promyelocytes

43
Q

Indication for ATRA?

A

acute myelogenous leukemia (AML) M3

44
Q

S/E of ATRA?

A

differentiation syndrome with respiratory distress, pleural and pericardial effusions, CNS symptoms

45
Q

Target of Imatinib

A

BCR-ABL (treats CML, GI stromal tumors GIST)

46
Q

Cetuximab target?

A

ErbB1 (head and neck and colon cancer)

47
Q

Trastuzumab target?

A

ErbB2 (HER2/neu) (breast cancer)

48
Q

Bevacizumab target?

A

VEGF-A

49
Q

Sorafenib target?

A

RAF kinase

50
Q

What are the more marrow sparing cytotoxic medications?

A

cisplatin, bleomycin, vincristine

51
Q

Popular nephrotoxic medications cytotoxic?

A

cisplatin, methotrexate

52
Q

Popular cytotoxic medications implicated in pulmonary toxicity?

A

bleomycin, busulfan, procarbazine

53
Q

Popular cardiotoxic cytotoxic meds?

A

Doxorubicin, daunorubicin

54
Q

Popular neurotoxic cytotoxic meds?

A

Vincristine, cisplatin

55
Q

Popular immunosuppressive cytotoxic meds?

A

cyclophosphamide, methotrexate

56
Q

What asparaginase causes what notable side effect?

A

pancreatitis

57
Q

CSF, erythropoietin and thrombopoietin therapy can be supportive in care for cancer in what way?

A

helps to reduce infections and need for antibiotics

58
Q

Aldesleukin MOA

A

IL-2 analog; inc. lymphocyte differential and inc. NKs

59
Q

Indication aldesleukin?

A

used in renal cell cancer and metastatic melanoma

60
Q

Interleukin 11 indications.

A

inc. platelet formation used in thrombocytopenia

61
Q

Filgrastim MOA

A

G-CSF inc. granulocytes

62
Q

Filgrastim indications?

A

marrow recovery

63
Q

Sargramostim indications.

A

inc. granulocytes and macrophages - used for marrow recovery

64
Q

MOA Sargramostim?

A

GM-CSF

65
Q

Erythropoeitin indications.

A

anemia, especially associated with renal failure

66
Q

Thrombopoietin indications.

A

thrombocytopenia

Kaplan: Anticancer Drugs, Immunopharmacology, and Toxicology (2 decks)

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