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Flashcards in Heme/oncology drugs Deck (97):
1

mech: heparin

cofactor for antithrombin activation

2

PT or PTT elevated with heparin?

Only PTT

3

heparin side effects

1. thrombocytopenia (HIT)
2. osteoporosis

4

benefit of low molecular weight heparins?

act more on factor Xa, better bioavailability and a longer half life
--no lab monitoring needed

5

pathophys: hepariin induced thrombocytopenia

development of IgG antibodies against heparin bound to platelet factor 4

6

Lepirudin, bivalirudin: derived from?

derivative of hirudin, from leeches

7

mech: lepirudin, bivalirudin?

inhibit thrombin

8

when would you use lepirudin/bivalirudin?

If a pt cannot use heparin because of HIT

9

warfarin metabolized by

cytochrome P450

10

warfarin affects PT or PTT?

PT. affects extrinsic pathway.

11

clinical use of warfarin

chronic anticoagulation after STEMI, DVT, prevention of stroke in Afib

12

warfarin contraindicated in

pregnancy. Unlike heparin, which does NOT cross the placenta

13

Tox: warfarin

skin/tissue necrosis
drug/drug interactions
-teratogenic

14

which inhibits coagulation in vitro, heparin or warfarin?

heparin

15

alteplace, reteplace, tenecteplase
tPA, rPA, TNK-tPA

thrombolytics

16

tPA mechanism

aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin

17

tPA: PT or PTT change?

Increases both

18

reversal of tPA overdose with

aminocaproic acid

19

tPA contraindicated in

active bleed
history of intracranial bleed
bleeding diathesis
severe hypertension

20

aspirin effect on PT or PTT

none

21

aspirin decreases plasma levels of

TXA2 and prostaglandins

22

tox: ticlopidine

neutropenia

23

clopidogrel
ticlopidine
prasugrel
ticagrelor

ADP receptor inhibitors

24

ADP receptor inhibitor: usage

acute coronary syndrome
coronary stenting
decreased incidence of thrombotic stroke

25

cilostazol mechanism

phosphodiesterase III inhibitor. Increases cAMP in platelets, inhibiting aggregation
--also a vasodilator

26

indications: cilostazol

intermittent claudication, prevention of stroke
angina prophylaxis

27

dipyridamole class

phosphodiesterase II inhibitor like cilostazol.

28

tox: cilostazol

nausea, headache, facial flushing, hypotension

29

eptifibatide

GpIIb/IIIa inhibitor

30

tirofiban

GpIIb/IIIa inhibitor

31

toxicity of GpIIb/IIIa inhibitors

bleeding, thrombocytopenia

32

which cancer drugs work on the M phase

vinca alkaloids
taxols

33

which cancer drugs work on the G2 phase

bleomycin and etoposide

34

which cancer drugs work on the S phase

etoposide and antimetabolites

35

Methotrexate: mechanism

decreases dTMP
decreases dNA

36

methomtrexate for which cancers?

leukemia
lymphoma
choriocarcinoma
sarcoma

37

methotrexate use: nonneoplastic

abortion
ectopic pregnancy
RA
psoriasis

38

tox: methotrexate

myelosuppression
macrovesicular fatty change in liver
mucositosis
teratogen

39

tx of methotrexate myelosuppression

folinic acid
leucovorin

40

5-FU: indication

colon cancer
basal cell carcinoma, topical

41

tox: FU

myelosuppression.
photosensitivity

42

tx for FU myelosuppression?

thymidine.

Note: leucovorin does NOT help! Because even if sufficient amount of N5, N10 THF, the enzyme thymidylate synthase doesn't work

43

mechanism: cytarabine

inhibition of DNA polymerase. A pyrimidine analog

44

Use: cytarabine

leukemia and lymphoma

45

tox: cytarabine

leukopenia
thrombocytopenia
megaloblastic anemia

46

azathioprine, 6mercaptopurine, and 6thioguanine mech

purine analog decrease purine synthesis

47

activation of azathioprine/6MP requires

HGPRT

48

tox of azathioprine

bone marrow, GI, liver

49

what drug should you NOT give with azathioprine and 6MP?

allopurinol. Because it's metabolized by xanthine oxidase!

50

mechanism: dactinomycin

intercalates DNA

51

tox: dactinomycin

myelosuppression

52

clinical use of dactinomycin

wilms' tumor
ewing's sarcoma
rhabdomyosarcoma
CHILDHOOD tumors

53

doxo/daunorubicin mechanism

generates free radicals
--INTERCALATES into DNA, causing breaks

54

Clinical use of doxorubicin

solid tumors, leukemias, lymphomas

55

toxicity of doxo/dauno

dilated cardiomyopathy
myelosuppression
alopecia

56

prevention of doxo/dauno cardiotoxicity

dexrazoxane

57

Bleomycin mechanism

free radicals
-breaks DNA

58

use: bleomycin

testicular cancer
hodgkins

59

toxicity of bleomycin

pulmonary fibrosis
skin changes

60

which cancer agents are alkylating

cyclophosphamide, ifosfamide
busulfan
nitrosoureas

61

cyclophosphamide, ifosfamide mech

covalently X links DNA at guanine N7

62

cyclophosphamide requires activation by

liver

63

Side effects of cyclophosphamide

myelosuppression
hemorrhagic cystitis

64

how to prevent cyclophosphamide hemorrhagic cystitis

mesna, binds toxic metabolite

65

use: cyclophosphamide

solid tumors, brain cancers
leuk, lymph

66

carmustine, lomustine, semustine, stretpzocin

nitrosureas

67

carmustine and friends mechanism

bioactivation then crosses blood brain barrier

68

use: nitrosureas (carmustine)

brain tumors like GBM

69

tox of nitrosureas

CNS dizziness and ataxia

70

busulfan mechanism

alkylates DNA

71

use: busulfan

CML
--also bone marrow ablation

72

tox: busulfan

pulmonary fibrosis
hyperpigmentation

73

Mech: vincrinstine, vinblastine

Bind tubulin and block microtubule polymerization

74

vincristine tox

neurotox (areflexia, peripheral neuritis, ileus)

75

vinblastine tox

bone marrow suppression

76

paclitaxel mechanism

stabilizes polymerized microtubules in M phase. mitotic spindles can't break down-->no anaphase

77

indications of paclitaxel

ovarian/breast

78

tox of paclitaxel

myelosuppression
hypersensitivity

79

cisplatin/carboplatin tox

nephrotoxicity and acoustic nerve damage

80

prevent cisplastin nephrotoxicity with

amifostine, a free radical scavenger and chloride diuresis

81

indications of cisplatin

testicular, bladder, ovary, lung cancer

82

etoposide, teniposide mechanism:

inhibit topoisomerase II=DNA degradation

83

tox of etoposide

myelosuppression
GI
alopecia

84

hydroxyurea affects which phase of cell cycle

S phase
--inhibits ribonucleotide reductase

85

prednisone cancer use?

CLL
non-hodgkins. triggers apoptosis

86

tamoxifen/raloxifene mechanism

blocks estrogen binding to receptor

87

SERM indication

breast cancer and osteoporosis

88

tamoxifen tox

increased endometrial cancer and hot flashes. partial endometrial agonist

89

raloxifen tox

NO increase in endometrial carcinoma. complete antagonist

90

trastuzumab mechanism

antibody against HER2, a tyrosine kinase

91

trastuzumab tox

cardiotoxicity

92

imatinib toxicity

fluid retention

93

rituximab indications

NHL, rheumatoid arthritis

94

vemurafenib mechanism

inhibits B-Raf kinase with V600E mutation

95

use: vemurafenib

metastatic melanoma

96

bevacizumab use:

Solid tumors

97

mechanism bevacizumab

monoclonal antibody against VEGF