Cell Cycle Specific Drug Tables - Fitz Flashcards Preview

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Flashcards in Cell Cycle Specific Drug Tables - Fitz Deck (64):
1

5-Fluorouracil...active metabolites and their actions

FdUMP - inhibits thymidylate synthase (no dTMP)
FdUTP - insert and damage DNA
FUTP - insert and damage RNA

2

Cytarabine (Ara-C)...conversion and action

Kinases convert to Ara-CTP, which inhibits DNA synthesis

3

Gemcitabine...conversion and action

Kinases convert it to nucleotide analogs, which inhibit DNA synthesis

4

5-FU uses

- Solid tumors (colorectal, breast, ovarian)
- Topical - basal cell carcinoma

5

Capecitabine uses

Colorectal, metastatic/resistant breast

6

Gemcitabine use

Pancreatic cancer

7

Cytarabine use

AML (w/ 6-thioguanine, daunorubicin)

8

5-FU toxicities

GI intolerance, mucositis, myelosuppression

9

Capecitabine toxicities

Same as 5-FU, + hand-foot syndrome

10

Gemcitabine toxicity

Neutropenia

11

Cytarabine toxicity

Granulocytopenia (severe)

12

MTX function

MTX(glu)n function

MTX = blocks DHFR, blocking thymidine, methionine and serine synthesis
MTX(glu)n = blocks GAR and AICAR transformylase, blocking purine synthesis

13

Pemetrexed function

Specialty vs. MTX?

Thymidylate synthase and GAR transformylase inhibitor

Does NOT inhibit DHFR, circumvents MTX resistance

14

Pemetrexed uses

Mesothelioma (w/ cisplatin), refractory NSCLC

15

High dose MTX uses

Requires what?

CNS prophylaxis for leukemia and high-risk lymphoma

Leucovorin rescue

16

Intermediate dose MTX use

Gestational trophoblastic disease (choriocarcinoma)

17

Low dose MTX uses

CNS prophylaxis (intrathecal), bladder and desmoid (IV), ALL and APL (oral)

18

MTX toxicities

BM suppression, mucositis, renal failure (high dose)

19

Pemetrexed toxicities

BM suppression, renal failure

20

6-Mercaptopurine function

Inhibits purine ring biosynthesis and nucleotide interconversion, disrupting DNA and RNA

21

6-Thioguanine function

Same as 6-Mercaptopurine

Inhibits purine ring biosynthesis and nucleotide interconversion, disrupting DNA and RNA

22

Fludarabine conversion and function

Tumor kinases convert it to nucleotide triphosphates, which insert and disrupt DNA and RNA

23

Cladribine conversion and functions

Tumor kinases convert it to nucleotide analogs, which inhibit DNA synthesis; also inhibits ribonucleotide reductase

24

6-Mercaptopurine use

ALL remission maintenance

25

6-Thioguanine use

AML (w/ daunorubicin and cytarabine)

26

Fludarabine use

CLL (or hairy cell leukemia)

27

Cladribine use

Hairy cell leukemia (or CLL)

28

6-Mercaptopurine toxicities

Myelosuppression; toxicity w/ allopurinol or febuxostat; hepatotoxicity

29

6-Thioguanine toxicities

Myelosuppression, hepatotoxicity (long use)

30

Fludarabine toxicities

Why give IV?

Myelosuppression, opportunistic infections

IV = avoid GI bacteria generating toxic fluroradenine

31

Cladribine toxicities

Myelosuppression, drug fever

32

Vinca alkaloid function

Inhibit tubulin polymerization, causing microtubule shortening and M-phase disruption

33

Taxane function

Inhibit tubulin fraying, causing microtubule lengthening and M-phase disruption

34

Vinblastine uses

Testicular (w/ bleomycin and cisplatin), lymphomas, neuroblastoma

35

Vincristine uses

ALL, lymphoma, neuroblastoma, Wilms, Ewings

36

Vinorelbine use

Advanced non-small cell lung cancer (alone or w/ cisplatin)

37

Paclitaxel uses

Solid tumors - Advanced breast and ovarian (w/ cisplatin)

38

Docetaxel uses

Solid tumors - Advanced breast, ovarian recurrence

39

Vinblastine toxicities

BM suppression, blisters

40

Vincristine toxicities

Neurotoxicity, peripheral neuropathy, ileus, blisters

41

Vinorelbine toxicities

BM suppression, blisters

42

Paclitaxel toxicities

Requires what?

Neutropenia, thrombocytopenia, peripheral neuropathy, hypersensitivity during infusion

Needs anti-histamine and corticosteroid pretreatment

43

Docetaxel toxicities

Neutropenia, peripheral neuropathy

44

Etoposine and Teniposide - function

Topoisomerase 2 inhibitors, causing DNA double strand breaks

45

Irinotecan and Topotecan - function

Topoisomerase 1 inhibitors, causing DNA single strand breaks

46

Etoposide uses

Oat cell carcinoma of lung, testicular cancer (w/ cisplatin and bleomycin)

47

Teniposide uses

Glioma, neuroblastoma

48

Irinotecan use

Metastatic colorectal cancer

49

Topotecan use

2nd line treatments for various failed 1st treatments

50

Etoposide toxicities

Leukopenia, secondary leukemia (DNA repair error)

51

Teniposide toxicity

Leukopenia

52

Irinotecan toxicities

Requires what?

Severe diarrhea (life-threatening), myelosuppression

Loperamide co-treatment (for diarrhea)

53

Topotecan toxicities

Neutropenia, mucositis

54

Bleomycin function

Fe(3+)-mediated free radical damage to DNA

55

Dactinomycin function

DNA intercalating agents

56

Doxorubicin, Daunorubicin, Epirubicin - functions

- Inhibit topoisomerase 2
- DNA intercalating agents
- Free radical generation --> DNA strand breaks

57

Mitoxantrone function

Inhibit topoisomerase 2

58

Bleomycin use

Testicular (w/ Vinblastine, cisplatin/etoposide)

59

Doxorubicin and Epirubicin - uses

Breast, ovarian, lung, thyroid, lymphoma, sarcoma, etc.

60

Daunorubicin uses

AML, ALL

61

Idarubicin uses

AML, ALL, CML blast crisis

62

Mitoxantrone uses

Breast, prostate, NHL

63

Bleomycin toxicity

Pulmonary fibrosis

64

'rubicins and Mitoxantrone - toxicities

Cardiotoxicity, dilated cardiomyopathy, CHF (cumulative)