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Flashcards in Cancer Chemotherapy Drugs Deck (82):
0

Mention some main alkylating agents.

1. Cyclophosphamide
2. Mechlorethamine
3. Procarbazine
4. Busulfan carmustine
5. Lomustine
6. Dacarbazine

1

What is the mechanism of action of cyclophosphamide?

Forms DNA cross links, resulting in inhibition of DNA synthesis and function.

2

What are the clinical applications of cyclophosphamide?

1. Breast cancer
2. Ovarian cancer
3. NHLs
4. CLL
5. Neuroblastoma

3

What are the acute toxicities of cyclophosphamide?

Nause and vomiting

4

What are the chronic toxicities of cyclophosphamide?

1. Myelosuppression
2. Alopecia
3. Hemorrhagic cystitis

5

Mention 5 main antimetabolites.

1. Methotrexate
2. 6-mercaptopurine
3. 5-fluorouracil
4. Cytarabine
5. Gemcitabine

6

What is the mechanism of action of methotrexate?

Inhibits dihydrofolate reductase, resulting in inhibition of synthesis of thymidylate, purine nucleotides, serine, and methionine.

7

What are the clinical applications of methotrexate?

1. Breast cancer
2. Head and neck cancer
3. Primary CNS lymphoma
4. NHL
5. Bladder cancer
6. Choriocarcinoma

8

What are the acute side effects of methotrexate?

Mucositis and diarrhea.

9

What are the late side effects of methotrexate?

Myelosuppression

10

What is the mechanism of action of 6-mercaptopurine?

Inhibits de novo purine synthesis.

11

What are the clinical applications of 6-mercaptopurine?

AML

12

What are the acute side effects of 6-mercaptopurine?

Nausea and vomiting.

13

What are the late side effects of 6-mercaptopurine?

1. Myelosuppression
2. Immunosuppression
3. Hepatotoxicity

14

What is the mechanism of action of 5-fluorouracil?

Inhibits thymidylate synthase, and its metabolites are incorporated into DNA and RNA, all resulting in inhibition of DNA synthesis and function and in RNA processing.

15

What is the clinical use of 5-fluorouracil?

1. GI cancers
2. Breast cancers
3. Head and neck cancer
4. HCC

16

What are the acute side effects of 5-fluorouracil?

1. Nausea
2. Mucositis
3. Diarrhea

17

What are the late side effects of 5-fluoracil?

Myelosuppression and neurotoxicity.

18

Mention 3 major vinca alkaloids.

1. Vincristine
2. Vinblastine
3. Vinorelbine

19

What is the mechanism of action of vincristine?

Interferes with microtubule function, resulting in impaired mitosis.

20

What is the clinical use of vincristine?

1. ALL
2. NHL and HL
3. Wilms' tumor
4. Neuroblastoma

21

What are the acute side effects of vincristine?

None.

22

What are the chronic side effects of vincristine?

1. Neurotoxicity with peripheral neuropathy.
2. Paralytic ileus
3. Myelosuppression
4. Alopecia
5. Inappropriate ADH secretion

23

Mention 2 major podophyllotoxins.

1. Etoposide
2. Teniposide

24

What is the mechanism of etoposide?

Inhibits topoisomerase II, resulting in DNA damage.

25

What are the clinical applications of etoposide?

1. Lung cancer
2. NHL
3. Gastric cancer

26

What are the acute side effects of etoposide?

Nausea and vomiting.

27

What are the chronic side effects of etoposide?

Alopecia and myelosuppression.

28

Mention 2 major camptothecins.

1. Topotecan
2. Irinotecan

29

What is the mechanism of topotecan?

Inhibits topoisomerase I, resulting in DNA damage.

30

What is the clinical use of topotecan?

1. Small cell lung cancer.
2. Ovarian cancer.

31

What are the acute side effects of topotecan?

Nausea - vomiting - diarrhea.

32

What are the late side effects of topotecan?

Myelosuppression

33

Mention 2 major taxanes.

1. Paclitaxel
2. Docetaxel

34

What is the mechanism of action of paclitaxel?

Interferes with microtubule function, resulting in impaired mitosis.

35

What is the clinical use of paclitaxel?

1. Breast
2. Lung
3. Ovarian
4. Gastroesophageal
5. Prostate
6. Bladder
7. Head and neck
Cancers.

36

What are the acute effects of paclitaxel?

1. Nausea
2. Vomiting
3. Hypotension
4. Arrhythmias
5. Hypersensitivity

37

What are the chronic effects of paclitaxel?

1. Myelosuppression
2. Peripheral sensory neuropathy

38

Mention 5 main anthracyclines.

1. Doxorubicin
2. Daunorubicin
3. Idarubicin
4. Epirubicin
5. Mitoxantrone

39

What is the mechanism of action of doxorubicin?

1. Oxygen free radicals bind to DNA causing strand to breakage.
2. Inhibits topoisomerase II
3. Intercalates into DNA.

40

What is the clinical use of doxorubicin?

1. Lymphomas
2. Myelomas
3. Sarcomas
4. Breast - lung - ovarian - thyroid cancers.

41

What are the acute side effects of doxorubicin?

Nausea and arrhythmias.

42

What are the chronic side effects of doxorubicin?

1. Alopecia
2. Myelosuppression
3. Cardiomyopathy
4. Myelosuppression

43

Mention 2 antitumor antibiotics.

1. Bleomycin
2. Mitomycin

44

Mention 6 tyrosine kinase inhibitors.

1. Imatinib
2. Dasatinib
3. Nilotinib
4. Sorafenib
5. Sunitinib
6. Pazopanib

45

What is the mechanism of imatinib?

Inhibits bcr-abl tyrosine kinase and other receptor tyrosine kinases.

46

What is the clinical use of imatinib?

1. CML
2. GIST

47

What are the acute side effects of imatinib?

Nausea and vomiting.

48

What are the chronic side effects of imatinib?

1. Fluid retention with ankle and periorbital edema.
2. Diarrhea
3. Myalgias
4. CHF

49

Mention 5 major growth factor receptor inhibitors.

1. Trastuzumab
2. Cetuximab
3. Panitumumab
4. Gefitinib
5. Erlotinib

50

What is the mechanism of trastuzumab?

Inhibits the binding of EGF to HER-2/neu growth receptor.

51

What is the clinical use of trastuzumab?

HER-2/neu receptor (+) breast cancer.

52

What are the acute side effects of trastuzumab?

1. Nausea
2. Vomiting
3. Chills
4. Fever
5. Headache

53

What are the chronic side effects of trastuzumab?

Cardiac dysfunction.

54

What is the mechanism of action of bevacizumab?

Inhibits binding of VEGF to its receptor, resulting in inhibition of tumor vascularization.

55

What is the clinical use of bevacizumab?

1. Colorectal
2. Breast
3. Non-small cell lung
4. Renal
cancers.

56

What are the acute side effects of bevacizumab?

1. HTN
2. Infusion reaction

57

What are the chronic side effects of bevacizumab?

1. Arterial thromboembolic events
2. GI perforations
3. Wound healing complications
4. Proteinuria

58

What is the mechanism of action of bortezomib?

Reversibly inhibits chymotrypsin-like activity of the 26S proteasome.

59

What is the clinical use of bortezomib?

Multiple myeloma.

60

What are the acute side effects of bortezomib?

1. HTN
2. Edema
3. GI upset

61

What are the chronic side effects of bortezomib?

1. Peripheral neuropathy
2. Cardiac dysfunction

62

Mention 6 mechanisms by which the tumor cells acquire resistance to anticancer drugs.

1. Increased DNA repair
2. Formation of trapping agents
3. Changes in target enzymes
4. Decreased activation of prodrugs
5. Inactivation of anticancer drugs
6. Decreased drug accumulation

63

For what anticancer drugs is increased DNA repair an important resistance mechanism?

1. Alkylating agents
2. Cisplatin

64

Where have we see formation of trapping agents as a mechanism of resistance?

1. Bleomycin
2. Cisplatin
3. Anthracyclines

65

What are the mechanisms of resistance to methotrexate?

1. Changes in the drugs sensitivity of a target enzyme (dihydrofolate reductase).
2. Increased synthesis of this enzyme.

66

What is the mechanism of resistance to the purine antimetabolites and the pyrimidine antimetabolites?

Decrease in the activity of the tumor cell enzymes needed to convert these prodrugs to their cytotoxic metabolites.

67

What is the main mechanism of resistance to purine and pyrimidine antimetabolites?

Increased activity of enzymes capable of inactivating anticancer drugs.

68

Mention a general anticancer drug resistance mechanism.

Decreased drug accumulation - multidrug resistance that involves the increased expression of a normal gene (MDR1) for a surface glycoprotein (P-glycoprotein).

69

Mention 4 general principles of cancer combined chemotherapy.

1. Each drug should be active when used alone against the particular cancer.
2. Drugs should have different mechanisms of action.
3. Cross-resistance between drugs should be minimal.
4. Drugs should have different cytotoxic effects.

70

What do we give in childhood ALL?

1. Prednisone
2. Vincristine
3. Asparaginase or an anthracycline
4. Intrathecal methotrexate

71

What do we give in AML?

Cytarabine and idarubicin or daunorubicin.

72

What do we give in breast carcinoma?

1. Cytotoxic agents
2. Hormonal therapy with tamoxifen or an aromatase inhibitor (anastrozole).
3. Trastuzumab

73

What do we give in CML?

Imatinib, newer tyrosine kinase inhibitors, interferon.

74

What do we give in colon carcinoma?

Fluorouracil + leucovorin + oxaliplatin.

75

What do we give in HL?

ABVD regimen
1. Doxorubicin (adriamycin)
2. Bleomycin
3. Vincristine
4. Dacarbazine

76

What do we give in NHL?

CHOP regimen
1. Cyclophosphamide
2. Doxorubicin
3. Vincristine
4. Prednisone
+ rituximab.

77

What do we give in ovarian cancer?

1. Paclitaxel
2. Carboplatin

78

What do we give in pancreatic cancer?

1. Gemcitabine
2. Erlotinib

79

What do we give in prostate cancer?

GnRH agonist (leuprolide) or blocker (abarelix) + androgen receptor blocker.

80

What do we give in lung cancer?

1. Carboplatin
2. Paclitaxel
3. Bevacizumab

81

What do we give in testicular cancer?

PEB regimen
1. Cisplatin (platinol)
2. Etoposide
3. Bleomycin

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