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Flashcards in Oncology Drugs Deck (83)
1

Name the antimetabolites

Azathioprine, 6-mercaptopurine, 6-thioguanine, cladribine, cytarabine, 5-fluorouracil, methotrexate

2

Mechanism of azathioprine, 6-MP and 6-TG

purine (thiol) analogs --> decreased de novo purine synthesis
activated by HGPRT
azathioprine is prodrug to 6-MP

3

Use of azathioprine, 6-MP and 6-TG

preventing organ rejection
RA
IBD
SLE
to wean pts off steroids and to tx steroid-refractory chronic disease

4

Toxicity of azathioprine, 6-MP and 6-TG

MYELOSUPPRESSION
GI, liver

5

Metabolism of azathioprine and 6-MP

metabolized via xanthine oxidase
increased toxicity if used with allopurinol or febuxostat (used to treat gout)

6

Mechanism of cladribine

purine analog --> multiple mechanism (e.g. inhibition of DNA polymerase, DNA strand breaks)

7

Use of cladribine

hairy cell leukemia

8

Toxicity of cladribine

myelosuppression, nephrotoxicity, and neurotoxicity

9

Mechanism of cytarabine

pyrimidine analong --> inhibition of DNA polymerase

10

Use of cytarabine

leukemias (AML), lymphomas

11

Toxicity of cytarabine

leukopenia, thrombocytopenia, megaloblastic anemia

CYTarabine causes panCYTopenia

12

Mechanism of 5-fluorouracil

pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes with folic acid
complex inhibits thymidylate synthase --> decreased dTMP --> decreased DNA synthesis

13

Use of 5-FU

colon cancer, pancreatic cancer, basal cell carcinoma (topical)

14

Toxicity of 5-FU

myelosuppression, which is NOT reversible with leucovorin (folinic acid)

15

Mechanism of methotrexate

folic acid analog that competitively inhibits dihydrofolate reductase --> decreased dTMP --> decreased DNA synthesis

16

Use of methotrexate

cancers: leukemia (ALL), lymphoma, choriocarcinoma, sarcomas

Non-neoplastic: ectopic pregnancy, medical abortion (with misoprostol), RA, psoriasis, IBD, vasculitis

17

Toxicity of methotrexate

myelosuppression (reversible with leucovorin)
hepatotoxicity
mucostitis (e.g. mout ulcers)
pulmonary fibrosis

18

Name the antitumor antibiotics

bleomycin, dactinomycin, doxorubicin, daunorubicin

19

Mechanism of bleomycin

induces free radical formation --> breaks in DNA strands

20

Use of bleomycin

testicular cancer, Hodgkin lymphoma

21

Toxicity of bleomycin

pulmonary fibrosis
skin hyperpigmentation
mucositis

22

Mechanism of dactinomycin (actinomycin D)

intercalates in DNA

23

Use of dactinomycin

Wilms tumor
Ewing sarcoma
Rhabdomyosarcoma

CHILDHOOD TUMORS - Kids ACT out

24

Toxicity of dactinomycin

myelosuppression

25

Mechanism of doxorubicin/daunorubicin

generate free radicals
intercalate in DNA --> breaks in DNA --> decreased replication

26

Use of doxorubicin/daunorubicin

solid tumors
leukemias
lymphomas

27

Toxicity of doxorubicin/daunorubicin

CARDIOTOXICITY (dilated cardiomyopathy)
myelosuppression
alopecia
toxic to tissues following extravasation

28

Agent given with doxorubicin/daunorubicin to prevent cardiotoxicity

Dexrazoxane - iron chelating agent

29

Name the alkylating agents

busulfan, cyclophosphamide, ifosfamide, nitrosureas (carmustine, lomustine, semustine, streptozocin)

30

Mechanism of busulfan

cross-links DNA

31

Use of busulfan

CML
used to ablate bone marrow before transplant

32

Toxicity of busulfan

SEVERE MYELOSUPPRESSION
pulmonary fibrosis
hyperpigmentation

33

Mechanism of cyclophosphamide/ifosfamide

cross-link DNA at guanine N-7
require bioactivation by liver

34

Use of cyclophosphamide/ifosfamide

solid tumors
leukemia
lymphoma

35

Toxicity of cyclophosphamide/ifosfamide

myelosuppression
HEMORRHAGIC CYSTITIS (partially prevented with MESNA and hydration)

36

Mechanism of nitrosureas

require bioactivation
cross BBB --> CNS
cross link DNA

37

Use of nitrosureas

brain tumors (including glioblastoma multiforme)

38

Toxicity of nitrosureas

CNS toxicirty (convulsions, dizziness, ataxia)

39

Name the microtubule inhibitors

paclitaxel (other taxols), vincristine, vinblastine

40

Mechanism of paclitaxel/taxols

hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)

41

Use of paclitaxel/taxol

ovarian and breast carcinomas

42

Toxicity of paclitaxel/taxol

myelosuppression
alopecia
hypersensitivity

43

Mechanism of vincristine/vinblastine

vinea alkaloids that bind beta-tubulin and inhibit its polymerization into MTs --> prevent mitotic spindle formation (M-phase arrest)

44

Use of vincristine/vinblastine

solid tumors
leukemias
Hodgkin (vinblastine) lymphoma
Non-Hodgkin (vincristine) lymphoma

45

Toxicity of vincristine

neurotoxicity (areflexia, peripheral neuritis)
paralytic ileus

46

Toxicity of vinblastine

bone marrow supression

47

Mechanism of cisplatin/carboplatin

cross-link DNA

48

Use of cisplatin/carboplatin

testicular
bladder
ovary
lung carcinomas

49

Toxicity of cisplatin/carboplatin

nephrotoxicity, ototoxicity

50

How can prevent nephrotoxicity of cisplatin/carboplatin

use with amifostine (free radical scavenger) and chloride (saline) diuresis

51

Mechanism of etoposide/teniposide

etoposide inhibits topoisomerase II --> increased DNA degradation

52

Use of etoposide/teniposide

solid tumors (testicular and small cell lung)
leukemia
lmyphoma

53

Toxicity of etoposide/teniposide

myelosuppression, GI upset, alopecia

54

Mechanism of irinotecan, topotecan

inhibit topoisomerase I and prevent DNA unwinding and replication

55

Use of irinotecan, topotecan

colon cancer (irinotecan)
ovarian and small cell lung (topotecan)

56

Toxicity of irinotecan, topotecan

severe myelosuppression
diarrhea

57

Mechanism of hydroxyurea

inhibits ribonucleotide reductase --> decreased DNA synthesis (S-phase specific)

58

Use of hydroxyurea

melanoma, CML, sickle cell disease (increase HbF)

59

Toxicity of hydroxyurea

severe myelosupression
GI upset

60

Mechanism of prednisone/prednisolone

various; bind intracytoplasmic receptor; alter gene transcription

61

Use of prednisone/prednisolone

CLL
non-Hodgkin lymphoma (part of combo)
immunosuppressants (autoimmune diseases)

62

Toxicity of prednisone/prednisolone

Cushing like symptoms

63

Mechanism of bevacizumab

monoclonal antibody against VEGF inhibiting angiogenesis

64

Use of bevacizumab

colon cancer and renal cell carcinoma
age related macular degeneration

65

Toxicity of bevacizumab

hemorrhage
blood clots
impaired wound healing

66

Mechanism of erlotinib

EGFR tyrosine kinase inhibitor

67

Use of erlotinib

non small cell lung carcinoma (adenocarcinoma if EGF positive)

68

Toxicity of erlotinib

rash

69

Mechanism of imatinib

tyrosine kinase inhibitor of BCR-ABL (philadelphia chromosome fusion gene) and c-kit (GI stromal tumors)

70

Use of imatinib

CML, GI stromal tumors

71

Toxicity of imatinib

fluid retention

72

Mechanism of rituximab

Ab against CD20 on B cells

73

Use of rituximab

Non-Hodgkin lymphoma
CLL
IBD
RA

74

Toxicity of rituximab

increased risk of progressive multifocal leukoencephalopathy (PML) from JC virus

75

Mechanism of tamoxifen/raloxifene

selective estrogen receptor modulators
- antagonists in breast and agonists in bone
- block binding of estrogen to ER + cells in breast

76

Use of tamoxifen/raloxifene

breast cancer treatment (tamoxifen only) and prevention
osteoporosis for raloxifene

77

Toxicity of tamoxifen

partial agonist in endometrium --> increased risk of endometrial hyperplasia and cancer
increased risk for hot flashes

78

Toxicity of raloxifene

no increase in endometrial cancer because antagonist in endometrial tissue

79

Mechanism of trastuzumab

Ab against Her-2, a tyrosine kinase receptor (through interrupted cellular signaling and antibody-dependent cytotoxicity)

80

Use of trastuzumab

HER2 + breast cancer and gastric cancer

81

Toxicity of trastuzumab

cardiotoxicity

82

Mechanism of vemurafenib

small molecule inhibitor of BRAF oncogene + melanoma

83

Use of vemurafenib

metastatic melanoma