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Flashcards in Heme & Onc Pharm Deck (160):
1

What is the MOA of heparin?

Cofactor for activation of antithrombin III
Decreases thrombin and factor Xa

2

What is the clinical use of heparin?

Immediate anticoagulant for PE, acute coronary syndrome, MI, DVT.
Can be used during pregnancy

3

What is the toxicity of heparin?

Bleeding, thrombocytopenia, osteoporosis, drug interactions.

4

What is the antidote for heparin toxicity?

Protamine sulfate

5

What's the MOA of protamine sulfate?

I is a positively charged molecule that binds negatively charged heparin

6

What are the advantages to using low MW heparins?

Longer half life
More effect on factor Xa
More bioavailability
Can be given subq

7

What is heparin induced thrombocytopenia?

Development of igG antibodies against heparin and platelet factor 4.
This complex of all 3 activates platelets causing thrombosis and thrombocytopenia

8

What is lepirudin, bivalirudin?

Anticoagulant used by leeches. Used as an alternative to heparin for patients with HIT

9

What is the MOA of lepirudin?

Inhibits thrombin

10

What is the MOA of warfarin?

Interferes with normal gamma carboxylation of vit-K dependent factors --> increased PT time
Metabolized by P450

11

What is the clinical use of warfarin?

Chronic anticoagulant after STEMI
venous TE prophylaxis
atrial fib
Chronic anticoagulant after a valve replacement or for anyone with a mechanical valve

12

What is the toxicity of warfarin?

Bleeding
Teratogenic
Skin/tissue necrosis
Drug interaction

13

What do you give to reverse the effects of warfarin?

Vit K
Or fresh frozen plasma

14

What is the route of admin of heparin?

IV, SC

15

Where does heparin work?

In the blood

16

What is the duration of action of heparin?

Rapid

17

What is the structure of heparin?

Large anionic, acidic polymer

18

What is the structure of warfarin?

Small lipid-soluble molecule

19

Where does warfarin act?

In the liver

20

What is the route of admin of warfarin?

Oral

21

What is the duration of action of warfarin?

Slow

22

What are the thrombolytics?

Alteplase (tPA), reteplase, tenecteplase

23

What is the MOA of thrombolytics?

Directly or indirectly convert plasminogen to plasmin --> cleaner thrombin and fibrin --> increased PT and PTT time

24

What are the clinical uses of thrombolytics?

Early MI, early ischemic stroke, direct thrombolysis of severe PE

25

What are the toxicities of thrombolytics?

Bleeding

26

What are the contraindications to thrombolytics?

Active bleeding
Intracranial bleeding
Recent surgery
Known bleeding diatheses
Severe HTN

27

What is given to treat thrombolytics toxicity?

Aminocaproic acid - inhibitor of fibrinolysis

28

What is urokinase used for?

For tx of MI or PE

29

What is the MOA of urokinase?

Converts plasminogen to plasmin

30

What are the ADP receptor inhibitors?

Clopidrogrel, ticlodipine, prausgrel, ticagrelor

31

What is the MOA of clopidogrel?

Irreversibly blocking ADP receptors thereby inhibiting GPIIB/IIIa from binding fibrinogen

32

What are the clinical uses of clopidogrel?

Acute coronary syndrome, coronary scenting, decreased incidence or recurrence of thrombotic stroke.

33

What is the toxicity of ADP receptor inhibitors?

Neutropenia

34

What is the MOA of cilostazol or dipyramidole?

Phosphodiesterase III inhibitor; increases camp in platelets to inhibit platelet aggregation

35

What is the clinical use of dipyramidole and cilostazol?

Intermittent claudication, coronary vasodilation, prevention of stroke or TIA, angina prophylaxis

36

What is the toxicity of cilostazol and dipyramidole?

Nausea
Headache
Facial flushing
Hypotension
Ab pain

37

What are the GPIIB/IIIa inhibitors?

Abciximab
Eptifibatide
Tirofiban

38

What is the MOA of abciximab?

Binds to GPIIB/IIIa receptors on platelets and inhibits aggregation.

39

What is the clinical use of abciximab?

Acute coronary syndrome, percutaneous transluminal coronary angioplasty

40

What is the toxicity of abciximab?

Bleeding
Thrombocytopenia

41

What phase of the cell cycle do vinca alkaloids and taxols work in?

M phase

42

What cell cycle phase do etoposides work in?

G2, S phase

43

What cell cycle phase does bleomycin work in?

g2

44

What cell cycle phase do anti metabolites work in?

S phase

45

What is the MOA of MTX?

Folic acid analog that inhibits dihydrofolate reductase so it decreases DNA and protein synthesis

46

What are the clinical uses of MTX?

Cancers, abortion, ectopic pregnancy, RA, psoriasis

47

What are the toxicities of MTX?

Myelosuppression
Macrovesicular fatty change in the liver
Mucositis
Teratogenic

48

What is the rescue drug for MTX toxicity?

Leucovorin - used to reverse myelosuppression

49

What is the MOA of 5-fluorouracil?

Pyrimidine analog that's converted to 5F-dUMP which complexes with folic acid thereby inhibiting thymidylate synthase decreasing DNA and protein synthesis

50

What are the used of 5-fluorouracil?

Colon cancer
BCC

51

What are the toxicities of 5-fluorouracil?

Myelosuppression
Photosensitivity

52

What can be used in an overdose of 5-fluorouracil?

Thymidine

53

What's th MOA of cytarabine?

Pyrimidine analog -- inhibitor of DNA synthesis

54

What is cytarabine used for?

Leukemia
Lymphoma

55

What are the toxicities of cytarabine?

Leukopenia
Thrombocytopenia
Megaloblastic anemia

56

What is the MOA of azathioprine,6-mercaptopurine, 6-thioguanine?

Purine analogs -- inhibit de novo purine synthesis
Activated by HGPRT
Toxic to proliferating lymphocytes

57

What are the purine analogs used for?

Leukemia and kidney transplants
Autoimmune hemolytic anemia and glomerulonephritis

58

What are the toxicities of the purine analogs?

BM, GI, liver (cholestasis/hepatitis)
Increases with allopurinol because metabolized by xanthine oxidase

59

What is the MOA of dactinomycin?

Intercalates in DNA

60

What is dactinomycin used for?

Wilms tumor, Ewing's sarcoma, rhabdomyosarcoma,

61

What is the toxicity of dactinomycin?

Myelosuppression

62

What is the MOA of doxorubicin?

Generate free radicals
Intercalates in DNA noncovalentky causing breaks

63

What is doxorubicin used for?

Solid tumors, leukemias, lymphomas

64

What is the toxicity of doxorubicin?

Dilated cardiomyopathy
Myelosuppression
Alopecia

65

What drug is used to prevent cardio toxicity of doxorubicin?

Dexrazoxane - iron cheating agent

66

What is the MOA of bleomycin?

Induces free radicals causing breaks in DNA

67

What are the clinical uses of bleomycin?

Hodgkin's lymphoma and testicular cancer

68

What are the toxicities of bleomycin?

Pulmonary fibrosis, skin changes, minimal myelosuppression

69

What are the alkylation agents?

Cyclophosphamide
Nitrosureas
Busulfan

70

What is the MOA of cyclophosphamide?

Covalently binds DNA at guanine N-7

Note: it is metabolized by P450

71

What is cyclophosphamide used for?

Solids tumors, leukemia, lymphoma, brain cancers

72

What is the toxicity of cyclophosphamide?

Myelosuppression
Hemorrhagic cystitis
Bladder cancer

73

What substance can help prevent hemorrhagic cystitis caused by cyclophosphamide?

Mesna - binds toxic metabolite

74

What do alkylating agents require?

Bioactivation

75

Which alkylating agent can cross the bb barrier?

Nitrosureas: carmustine, lomustine, semustine

76

What are nitrosureas used for?

Brain tumors

77

What is the toxicity of nitrosureas?

Dizziness
Ataxia

78

What is the toxicity of busulfan?

Pulmonary fibrosis
Hyper pigmentation

79

What is busulfan used for?

CML
Ablation of patients BM before transplant

80

What is the MOA of vincristine and vinblastine?

Binds to Tubulin in M phase and block polymerization of the micro tubules

81

What are alkaloids used for?

Cancers

82

What is the toxicity of vincristine?

Neurotoxicity - areflexia, paralytic ileus, peripheral neuritis

83

What is the toxicity of vinblastine?

BM suppression

84

What is the MOA of taxols?

Hyper stabilize polymerized micro tubules in M Phase so they can't break down (anaphase cannot occur)

85

What are taxols used for?

Breast and ovarian carcinoma

86

What are the toxicities of taxols?

Myelosuppression
Hypersensitivity

87

What is the MOA of cisplatin/carboplatin?

Cross-link DNA

88

What is cisplatin/carboplatin used for?

Testicukar, bladder, ovary and lung cancer

89

What are the toxicities of cisplatin and carboplatin?

Nephrotoxicity
Acoustic nerve damage

90

How can nephrotoxicity of cisplatin be prevented?

Amifostine - free radical scavenger
Chloride diuresis

91

What is the MOA of etoposide and teniposide?

Inhibit topoisomerase II - increases DNA degradation

92

What is the toxicity of etoposide?

GI
Myelosuppression
Alopecia

93

What is the MOA of hydroxurea?

Inhibits ribonucleotide reductase decreasing DNA synthesis in S phase

94

What is hydroxurea used for?

Melanoma
CML
Sickle cell

95

What is the tox of hydroxurea?

GI
BM suppression

96

How does prednisone work as a anti-neoplastic agent?

Triggers apoptosis

97

When is prednisone used in cancer?

CLL, non-Hodgkin's

98

What is the tox of prednisone?

Cushing's
Cataracts
Acne
Osteoporosis
HTN
Peptic ulcers
Hyperglycemia
Psychosis

99

What is the MOA of tamoxifen?

SERMs - receptor antagonists in breast and agonist in bone
Block binding if estrogen to ER positive cells

100

What is tamoxifen used for?

Breast cancer
Osteoporosis

101

What is the tox of tamoxifen?

Partial agonist in endometrium so increases the risk of endometrial cancer
Hot flashes

102

Which drug should be used for breast cancer in women who still have a uterus?

Raloxifene

103

What is the MOA of trastuzamab (herceptin)?

Monoclonal Ab against Her-2 -- kills cells over expressing her-2

104

What is trastuzamab used for?

Her-2 positive breast cancer

105

What is the tox of trastuzamab?

Cardiotoxicity

106

What is the MOA of imatinib?

Philadelphia chromosome bCR-abl tyrosine kinase inhibitor

107

What is imatinib used for?

CML
GI stromal tumors

108

What is the toxicity of imatinib?

Fluid retention

109

What is the MOA of rituximab?

Monoclonal Ab against CD20

110

What is rituximab used for?

Non-Hodgkin lymphoma, RA

111

What is the MOA of vemurafenib?

Inhibits forms of the b-raf kinase with the V600E mutation

112

What is vemurafenib used for?

Metastatic melanoma

113

What is the MOA of bevaxizumab?

Monoclonal Ab against VEGF. Inhibits angiogenesis!

114

What is bevaxizumab used for?

Solid tumors

115

What is the MOA of cyclosporine?

Binds to cyclophilins and this complex blocks the differentiation and activation of T cells by inhibiting calcineurin. Prevents production of IL-2 and its receptor

116

What is cyclosporine used for?

Suppresses organ rejection
Autoimmune diseases

117

What is the tox of cyclosporine?

Nephrotoxicity
HTN
Hyperlipidemia
Hyperglycemia
Tremor
Gingival hyperplasia
Hirsutism

118

What is the MOA of tacrolimus?

Binds FK-binding protein, inhibiting calcineurin and secretion of IL-2 and other cytokines

119

What is tacrolimus used for?

Suppression in organ transplant recipients

120

What is the tox of tacrolimus?

Same as cyclosporine but no gingival hyperplasia or hirsutism

121

What is the MOA of sirolimus (rapamycin)

Inhibits mTOR.
Inhibits T cell prolif in response to IL-2

122

What is sirolimus used for?

Immunosuppression after kidney transplant in combo with cyclosporine and corticosteroids

123

What is the toxicity of sirolimus?

Hyperlipidemia
Thrombocytopenia
Leukopenia

124

What is the MOA of muromonab?

Monoclonal Ab that binds to CD3 so T cells can't transduce

125

What is muromonab used for?

Immunosuppressive after kidney transplant

126

What is the toxicity of muromonab?

Cytokines release syndrome
Hypersensitivity

127

What is aldesleukin?

Recombinant IL-2

128

What is aldesleukin used for?

Renal cell carcinoma
Metastatic melanoma

129

What is alpha interferon used for?

Hep B,C, kaposi's, leukemia, malignant melanoma

130

What is beta INF used for?

Multiple sclerosis

131

What is gamma INF used for?

Chronic granulomatous disease

132

What is oprelvekin?

Recombinant IL-11 used for thrombocytopenia

133

What is infliximab and adalimumab?

Monoclonal Ab to TNF-a

134

What are TNF-a monoclonal abs used for?

Crohn's, anklyosing spondylitis, RA, psoriatic arthritis

135

What is abciximab?

Monoclonal Ab to GPIIB/IIIa for prevention of cardiac ischemia in unstable angina
Percutaneous coronary intervention

136

What is omalizumab?

Monoclonal Ab to IgE used for asthma

137

What is celecoxib used for?

Inflammatory conditions such as RA without risk of GI bleed

138

What is COX2?

An inducible enzyme formed by inflammatory stimuli

139

Which platelet aggregation inhibitor causes neutropenia?

Ticlodipine - manifests as fever and mouth ulcers

140

What is a potential side effect of infliximab, adalimumab, and etanercept?

TB activation because of blocking TNF-alpha

141

What should be done before prescribing TNF-alpha?

Do a PPD test to check for inactive TB

142

What are the direct factor X inhibitors?

Idraparinux
Rivaroxaban
Apixaban
Ultra low MW heparin

143

What do direct factor X inhibitors prolong?

PT and PTT time

144

What do factor X inhibitors not inhibit and therefore not prolong?

Don't inhibit thrombin so don't prolong TT time

145

What are direct factor X inhibitors used for?

DVT

146

What is rat poison?

It is a long acting 4-hydroxycoumarin derivative - basically warfarin so it will deprive you of your vit K dependent factors

147

What should be given in the setting of rat poison?

Fresh frozen plasma

148

What does cryoprecipitate contain?

Factor 8/9
vWF
Fibrinogen

149

What is enoxaparin?

A low MW heparin
Greater activity against Factor Xa than thrombin

150

Why is unfractionated heparin preferred over other anticoagulants in acute coronary syndrome?

Because it complexes with both antithrombin and thrombin to allow antithrombin to inactivate Factor Xa thereby also inhibiting thrombin

151

What is given in subarachnoid hemorrhage and why?

Nimodipine due to risk of vasospasm from blood breakdown

152

DOC to treat vonWillenbrands disease?

DDAVP (desmopressin)

153

What is the MOA of certolizumab?

It is a pegylated humanized monoclonal antibody that targets TNF-alpha. It lacks the Fc region and is used in treating autoimmune diseases

154

Uses for DDAVP?

VonWillenbrand's Disease
Central DI
sleep enuresis

156

What is the tx for primary myelofibrosis?

Ruxolitinib - JAK2 inhibitor

157

What is mercaptopurine inactivated by?

Xanthine oxidase

158

What is mercaptopurine activated by?

HGPRT

159

What is pentostatin?

An irreversible inhibitor of ADA

160

What is basiliximab?

Inhibitor of IL2 receptor

161

What is the MOA of desmopressin?

It stimulates release of factor XIII and vWF from endothelial cells