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

mech: heparin

A

cofactor for antithrombin activation

2
Q

PT or PTT elevated with heparin?

A

Only PTT

3
Q

heparin side effects

A
  1. thrombocytopenia (HIT)

2. osteoporosis

4
Q

benefit of low molecular weight heparins?

A

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

5
Q

pathophys: hepariin induced thrombocytopenia

A

development of IgG antibodies against heparin bound to platelet factor 4

6
Q

Lepirudin, bivalirudin: derived from?

A

derivative of hirudin, from leeches

7
Q

mech: lepirudin, bivalirudin?

A

inhibit thrombin

8
Q

when would you use lepirudin/bivalirudin?

A

If a pt cannot use heparin because of HIT

9
Q

warfarin metabolized by

A

cytochrome P450

10
Q

warfarin affects PT or PTT?

A

PT. affects extrinsic pathway.

11
Q

clinical use of warfarin

A

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

12
Q

warfarin contraindicated in

A

pregnancy. Unlike heparin, which does NOT cross the placenta

13
Q

Tox: warfarin

A

skin/tissue necrosis
drug/drug interactions
-teratogenic

14
Q

which inhibits coagulation in vitro, heparin or warfarin?

A

heparin

15
Q

alteplace, reteplace, tenecteplase

tPA, rPA, TNK-tPA

A

thrombolytics

16
Q

tPA mechanism

A

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

17
Q

tPA: PT or PTT change?

A

Increases both

18
Q

reversal of tPA overdose with

A

aminocaproic acid

19
Q

tPA contraindicated in

A

active bleed
history of intracranial bleed
bleeding diathesis
severe hypertension

20
Q

aspirin effect on PT or PTT

A

none

21
Q

aspirin decreases plasma levels of

A

TXA2 and prostaglandins

22
Q

tox: ticlopidine

A

neutropenia

23
Q

clopidogrel
ticlopidine
prasugrel
ticagrelor

A

ADP receptor inhibitors

24
Q

ADP receptor inhibitor: usage

A

acute coronary syndrome
coronary stenting
decreased incidence of thrombotic stroke

25
Q

cilostazol mechanism

A

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

26
Q

indications: cilostazol

A

intermittent claudication, prevention of stroke

angina prophylaxis

27
Q

dipyridamole class

A

phosphodiesterase II inhibitor like cilostazol.

28
Q

tox: cilostazol

A

nausea, headache, facial flushing, hypotension

29
Q

eptifibatide

A

GpIIb/IIIa inhibitor

30
Q

tirofiban

A

GpIIb/IIIa inhibitor

31
Q

toxicity of GpIIb/IIIa inhibitors

A

bleeding, thrombocytopenia

32
Q

which cancer drugs work on the M phase

A

vinca alkaloids

taxols

33
Q

which cancer drugs work on the G2 phase

A

bleomycin and etoposide

34
Q

which cancer drugs work on the S phase

A

etoposide and antimetabolites

35
Q

Methotrexate: mechanism

A

decreases dTMP

decreases dNA

36
Q

methomtrexate for which cancers?

A

leukemia
lymphoma
choriocarcinoma
sarcoma

37
Q

methotrexate use: nonneoplastic

A

abortion
ectopic pregnancy
RA
psoriasis

38
Q

tox: methotrexate

A

myelosuppression
macrovesicular fatty change in liver
mucositosis
teratogen

39
Q

tx of methotrexate myelosuppression

A

folinic acid

leucovorin

40
Q

5-FU: indication

A

colon cancer

basal cell carcinoma, topical

41
Q

tox: FU

A

myelosuppression.

photosensitivity

42
Q

tx for FU myelosuppression?

A

thymidine.

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

43
Q

mechanism: cytarabine

A

inhibition of DNA polymerase. A pyrimidine analog

44
Q

Use: cytarabine

A

leukemia and lymphoma

45
Q

tox: cytarabine

A

leukopenia
thrombocytopenia
megaloblastic anemia

46
Q

azathioprine, 6mercaptopurine, and 6thioguanine mech

A

purine analog decrease purine synthesis

47
Q

activation of azathioprine/6MP requires

A

HGPRT

48
Q

tox of azathioprine

A

bone marrow, GI, liver

49
Q

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

A

allopurinol. Because it’s metabolized by xanthine oxidase!

50
Q

mechanism: dactinomycin

A

intercalates DNA

51
Q

tox: dactinomycin

A

myelosuppression

52
Q

clinical use of dactinomycin

A

wilms’ tumor
ewing’s sarcoma
rhabdomyosarcoma
CHILDHOOD tumors

53
Q

doxo/daunorubicin mechanism

A

generates free radicals

–INTERCALATES into DNA, causing breaks

54
Q

Clinical use of doxorubicin

A

solid tumors, leukemias, lymphomas

55
Q

toxicity of doxo/dauno

A

dilated cardiomyopathy
myelosuppression
alopecia

56
Q

prevention of doxo/dauno cardiotoxicity

A

dexrazoxane

57
Q

Bleomycin mechanism

A

free radicals

-breaks DNA

58
Q

use: bleomycin

A

testicular cancer

hodgkins

59
Q

toxicity of bleomycin

A

pulmonary fibrosis

skin changes

60
Q

which cancer agents are alkylating

A

cyclophosphamide, ifosfamide
busulfan
nitrosoureas

61
Q

cyclophosphamide, ifosfamide mech

A

covalently X links DNA at guanine N7

62
Q

cyclophosphamide requires activation by

A

liver

63
Q

Side effects of cyclophosphamide

A

myelosuppression

hemorrhagic cystitis

64
Q

how to prevent cyclophosphamide hemorrhagic cystitis

A

mesna, binds toxic metabolite

65
Q

use: cyclophosphamide

A

solid tumors, brain cancers

leuk, lymph

66
Q

carmustine, lomustine, semustine, stretpzocin

A

nitrosureas

67
Q

carmustine and friends mechanism

A

bioactivation then crosses blood brain barrier

68
Q

use: nitrosureas (carmustine)

A

brain tumors like GBM

69
Q

tox of nitrosureas

A

CNS dizziness and ataxia

70
Q

busulfan mechanism

A

alkylates DNA

71
Q

use: busulfan

A

CML

–also bone marrow ablation

72
Q

tox: busulfan

A

pulmonary fibrosis

hyperpigmentation

73
Q

Mech: vincrinstine, vinblastine

A

Bind tubulin and block microtubule polymerization

74
Q

vincristine tox

A

neurotox (areflexia, peripheral neuritis, ileus)

75
Q

vinblastine tox

A

bone marrow suppression

76
Q

paclitaxel mechanism

A

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

77
Q

indications of paclitaxel

A

ovarian/breast

78
Q

tox of paclitaxel

A

myelosuppression

hypersensitivity

79
Q

cisplatin/carboplatin tox

A

nephrotoxicity and acoustic nerve damage

80
Q

prevent cisplastin nephrotoxicity with

A

amifostine, a free radical scavenger and chloride diuresis

81
Q

indications of cisplatin

A

testicular, bladder, ovary, lung cancer

82
Q

etoposide, teniposide mechanism:

A

inhibit topoisomerase II=DNA degradation

83
Q

tox of etoposide

A

myelosuppression
GI
alopecia

84
Q

hydroxyurea affects which phase of cell cycle

A

S phase

–inhibits ribonucleotide reductase

85
Q

prednisone cancer use?

A

CLL

non-hodgkins. triggers apoptosis

86
Q

tamoxifen/raloxifene mechanism

A

blocks estrogen binding to receptor

87
Q

SERM indication

A

breast cancer and osteoporosis

88
Q

tamoxifen tox

A

increased endometrial cancer and hot flashes. partial endometrial agonist

89
Q

raloxifen tox

A

NO increase in endometrial carcinoma. complete antagonist

90
Q

trastuzumab mechanism

A

antibody against HER2, a tyrosine kinase

91
Q

trastuzumab tox

A

cardiotoxicity

92
Q

imatinib toxicity

A

fluid retention

93
Q

rituximab indications

A

NHL, rheumatoid arthritis

94
Q

vemurafenib mechanism

A

inhibits B-Raf kinase with V600E mutation

95
Q

use: vemurafenib

A

metastatic melanoma

96
Q

bevacizumab use:

A

Solid tumors

97
Q

mechanism bevacizumab

A

monoclonal antibody against VEGF