Cell Cycle Specific Drug Tables - Fitz Flashcards

1
Q

5-Fluorouracil…active metabolites and their actions

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Cytarabine (Ara-C)…conversion and action

A

Kinases convert to Ara-CTP, which inhibits DNA synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Gemcitabine…conversion and action

A

Kinases convert it to nucleotide analogs, which inhibit DNA synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

5-FU uses

A
  • Solid tumors (colorectal, breast, ovarian)

- Topical - basal cell carcinoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Capecitabine uses

A

Colorectal, metastatic/resistant breast

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Gemcitabine use

A

Pancreatic cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Cytarabine use

A

AML (w/ 6-thioguanine, daunorubicin)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

5-FU toxicities

A

GI intolerance, mucositis, myelosuppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Capecitabine toxicities

A

Same as 5-FU, + hand-foot syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Gemcitabine toxicity

A

Neutropenia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Cytarabine toxicity

A

Granulocytopenia (severe)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

MTX function

MTX(glu)n function

A
MTX = blocks DHFR, blocking thymidine, methionine and serine synthesis
MTX(glu)n = blocks GAR and AICAR transformylase, blocking purine synthesis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Pemetrexed function

Specialty vs. MTX?

A

Thymidylate synthase and GAR transformylase inhibitor

Does NOT inhibit DHFR, circumvents MTX resistance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Pemetrexed uses

A

Mesothelioma (w/ cisplatin), refractory NSCLC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

High dose MTX uses

Requires what?

A

CNS prophylaxis for leukemia and high-risk lymphoma

Leucovorin rescue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Intermediate dose MTX use

A

Gestational trophoblastic disease (choriocarcinoma)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Low dose MTX uses

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

MTX toxicities

A

BM suppression, mucositis, renal failure (high dose)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Pemetrexed toxicities

A

BM suppression, renal failure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

6-Mercaptopurine function

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

6-Thioguanine function

A

Same as 6-Mercaptopurine

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Fludarabine conversion and function

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Cladribine conversion and functions

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

6-Mercaptopurine use

A

ALL remission maintenance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

6-Thioguanine use

A

AML (w/ daunorubicin and cytarabine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Fludarabine use

A

CLL (or hairy cell leukemia)

27
Q

Cladribine use

A

Hairy cell leukemia (or CLL)

28
Q

6-Mercaptopurine toxicities

A

Myelosuppression; toxicity w/ allopurinol or febuxostat; hepatotoxicity

29
Q

6-Thioguanine toxicities

A

Myelosuppression, hepatotoxicity (long use)

30
Q

Fludarabine toxicities

Why give IV?

A

Myelosuppression, opportunistic infections

IV = avoid GI bacteria generating toxic fluroradenine

31
Q

Cladribine toxicities

A

Myelosuppression, drug fever

32
Q

Vinca alkaloid function

A

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

33
Q

Taxane function

A

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

34
Q

Vinblastine uses

A

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

35
Q

Vincristine uses

A

ALL, lymphoma, neuroblastoma, Wilms, Ewings

36
Q

Vinorelbine use

A

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

37
Q

Paclitaxel uses

A

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

38
Q

Docetaxel uses

A

Solid tumors - Advanced breast, ovarian recurrence

39
Q

Vinblastine toxicities

A

BM suppression, blisters

40
Q

Vincristine toxicities

A

Neurotoxicity, peripheral neuropathy, ileus, blisters

41
Q

Vinorelbine toxicities

A

BM suppression, blisters

42
Q

Paclitaxel toxicities

Requires what?

A

Neutropenia, thrombocytopenia, peripheral neuropathy, hypersensitivity during infusion

Needs anti-histamine and corticosteroid pretreatment

43
Q

Docetaxel toxicities

A

Neutropenia, peripheral neuropathy

44
Q

Etoposine and Teniposide - function

A

Topoisomerase 2 inhibitors, causing DNA double strand breaks

45
Q

Irinotecan and Topotecan - function

A

Topoisomerase 1 inhibitors, causing DNA single strand breaks

46
Q

Etoposide uses

A

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

47
Q

Teniposide uses

A

Glioma, neuroblastoma

48
Q

Irinotecan use

A

Metastatic colorectal cancer

49
Q

Topotecan use

A

2nd line treatments for various failed 1st treatments

50
Q

Etoposide toxicities

A

Leukopenia, secondary leukemia (DNA repair error)

51
Q

Teniposide toxicity

A

Leukopenia

52
Q

Irinotecan toxicities

Requires what?

A

Severe diarrhea (life-threatening), myelosuppression

Loperamide co-treatment (for diarrhea)

53
Q

Topotecan toxicities

A

Neutropenia, mucositis

54
Q

Bleomycin function

A

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

55
Q

Dactinomycin function

A

DNA intercalating agents

56
Q

Doxorubicin, Daunorubicin, Epirubicin - functions

A
  • Inhibit topoisomerase 2
  • DNA intercalating agents
  • Free radical generation –> DNA strand breaks
57
Q

Mitoxantrone function

A

Inhibit topoisomerase 2

58
Q

Bleomycin use

A

Testicular (w/ Vinblastine, cisplatin/etoposide)

59
Q

Doxorubicin and Epirubicin - uses

A

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

60
Q

Daunorubicin uses

A

AML, ALL

61
Q

Idarubicin uses

A

AML, ALL, CML blast crisis

62
Q

Mitoxantrone uses

A

Breast, prostate, NHL

63
Q

Bleomycin toxicity

A

Pulmonary fibrosis

64
Q

‘rubicins and Mitoxantrone - toxicities

A

Cardiotoxicity, dilated cardiomyopathy, CHF (cumulative)