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Flashcards in Coagulation drugs Deck (112):
1

Unfractionated heparin: routes of administration?

Mainly IV, also subQ.

2

Unfractionated heparin: MoA?

Complexes w/AT III and mainly inhibits factors Xa and IIa. (also XIa, XIIa).

Increases AT-III's binding affinity by 1000x.

3

Unfractionated heparin: indications?

Surgical anticoagulation

4

Unfractionated heparin: adverse effects?

Bleeding, HIT, osteoporosis, alopecia

5

How is unfractionated heparin monitored?

Monitored by APTT (2-2.5x baseline therapeutic)

6

LMW heparins: routes of administration?

SubQ

7

LMW heparins: MoA?

Complexes w/AT and mainly inhibits factors Xa and IIa.

8

LMW heparins: indications?

Prophylaxis and tx of DVT and ACS. (Alt. tx for HIT)

9

LMW heparins: adverse effects?

Bleeding

10

How is LMW heparin monitored?

Monitored by anti-Xa.

11

Fondaparinux (pentasaccharide): route of administration?

SubQ

12

Fondaparinux (pentasaccharide): MoA?

What class of drugs does it fall under?

Complexes w/AT to inhibit factor Xa (not IIa)

"Heparin anticoagulants"

13

Indications for fondaparinux?

Mgmt of DVT

14

Toxic/adverse effects of Fondaparinux?

Bleeding

15

Argatroban: route of administration?

IV

16

Argatroban: MoA?

What drug category does it fall under?

Direct IIa inhibitor

"Heparin anticoagulants"

17

Argatroban: indications?

Anticoagulant mgmt of HIT pts

18

Argatroban: adverse effects?

Bleeding

19

*Besides argatroban, name 2 other drugs with the same MoA, indications, and toxic effects?

Bivalrudin & hirudin

 

("Heparin anticoagulants." 

MoA: direct IIa inhibitor.

Indications: mgmt of HIT pts.

Adverse effects: bleeding)

20

Argatroban, bivalrudin, and hirudin are all direct IIa inhibitors. How are each of them excreted?

Is there T1/2 longer or shorter?

  • Argatroban: Liver
  • Bivalrudin: Renal
  • Hirudin: Renal

All short T1/2

21

How is antithrombin concentrate administered?

IV

22

Antithrombin concentrate: MoA?

Direct IIa inhibitor

23

Antithrombin concentrate: indications?

DIC, sepsis, thrombophilia, hypercoagulable state

24

Antithrombin concentrate: toxicity?

None!

25

What is protamine sulfate? What is it used for?

  • Heparin antagonist
  • Reverses the effects of heparin

26

Protamine sulfate: adverse effects/toxicity?

Bradycardia, hypotension

27

One USP unit of heparin is neutralized by ___ ug of protamine sulfate.

10

28

Try to name all all 8 types of "heparin anticoagulants," including the inhibitor.

  1. Unfactionated heparin

  2. LMW heparin (branded + generic)

  3. Fondaparinux (pentasaccharide)

  4. Argatroban

  5. Bivalirudin

  6. Hirudin

  7. Antithrombin concentrate

  8. Protamine sulfate

29

What is the brand name of warfarin?

How is it administered?

Coumadin

PO ("oral anticoagulant")

30

Warfarin: MoA?

Competitive antagonist of vitamin K. Suppresses the synthesis of functional forms of factors II, VII, IX and X by blocking enzyme epoxide reductase in liver

31

Warfarin: indications?

Prolonged tx of a-fib and DVT

32

*Warfarin: toxic/adverse effects?

Bleeding, coumadin induced necrosis. Has interaction with several medications which can either potentiate the effects or inhibit the effects. Crosses placental barrier causing birth defects.

33

How are warfarin levels monitored?

Monitored via PT/INR.

34

How is vitamin K administered?

PO

("oral anticoagulants")

35

Vitamin K: MoA?

Cofactor in the synthesis of functional forms of factors II, VII, IX and X.

36

Vitamin K: indications?

  • Hypoprothrombinemia
  • Intestinal disorders
  • Gastrectomy
  • Reverses the effects of warfarin

37

Vitamin K: adverse effects?

Hemolysis

38

How is vitamin K monitored?

Trick: monitoring not required

39

*Name the 3 oral anti-Xa anticoagulant drugs.

  • Rivaroxaban
  • Apixaban
  • Edoxaban

(EAR)

40

Edoxaban, apixaban, rivaroxaban (ear): MoA?

Route of administration?

Xa inhibitor

PO

41

Edoxaban, apixaban, rivaroxaban (ear): indications?

- Which are approved for prophylaxis and tx of DVT?

- Which are approved for tx of ACS?

Stroke prevention in patients with a-fib.

R & A also approved for prophylaxis and treatment of DVT.

R approved for ACS.

42

Edoxaban, apixaban, rivaroxaban (ear): toxic effects?

Bleeding; liver toxicity

43

How are Edoxaban, apixaban, rivaroxaban (ear) monitored?

Monitoring not required

44

What are the names of the 2 oral anticoagulants that inhibit thrombin?

  • Oral antithrombin
  • Dabigatran

45

What is the MoA of both oral antithrombin and dabigatran?

Routes of administration?

Inhibits IIa

PO

46

What are the indications for oral antithrombin and dabigatran?

Stroke prevention for pts w/a-fib

47

Oral antithrombin and dabigatran: toxic effects?

Bleeding; liver toxicity

48

What organ clears oral antithrombin and dabigatran?

The kidney (could be problems for pts w/renal failure. Also, don't confuse it since it can also cause liver toxicity)

49

How are oral antithrombin and dabigatran monitored?

Trick: they do not need monitoring

50

Try to name the 7 oral anticoagulants discussed in class.

  1. Warfarin
  2. Vitamin K
  3. Edoxaban
  4. Apixaban
  5. Rivaroxaban
  6. Oral antithrombin
  7. Dabigatran

51

  1. Name 3 cyclooxigenase inhibitors that affect platelets.
    1. Which affect which COX enzymes?
    2. How are they administered?

 

  1. ASA, NSAIDs, celecoxib
    1. ASA/NSAIDs: inhibit COX-1 and 2. Celecoxib only inhibits COX-2
    2. PO

52

How does a platelet aggregation assay work?

  1. Prepare platelet-rich plasma
  2. Activate platelets (ADP, TRAP, epi, 5-HT, collagen, ristocetin, AA)
  3. Measure light transmittence

53

Genearlly, why might one prefer an anti-platelet drug to an oral anticoagulants or heparin?

Anti-platelet drugs are effective in the arterial circulation, where anticoagulants such as heparin and oral anticoagulants have relatively little effect.

54

What condition is ASA resistance a/w?

May be a cause of recurrent ischemic vascular events in patients taking aspirin.

55

Dual anti-platelet therapies usually combine ___________ with another anti-platelet drug such as ADP receptor inhibitors, gp IIb/IIIa inhibitors, or phosphodiesterase inhibitors.

Aspirin

(can do double or triple inhibitor therapy)

56

Name some drugs that can interact w/anti-platelet drugs.

1.  Thrombolytic agents (urokinase, streptokinase and tPA)

2.  Heparin/LMW Heparin/oral anticoagulants

3.  Warfarin and other oral anticoagulant drugs

4.  Antithrombin agents (hirudin, bivalirudin and argatroban)

57

The cyclooxygenase pw produces ______________, while the lipooxygenase pw produces _______________.

Prostaglandins

Leukotrienes

58

Prostacyclin (PGI2) causes vaso-__________ and __________ platelet aggregation, while TXA2 causes vaso-__________ and __________ platelet aggregation.

  • PGI2
    • Vasodilation
    • Inhibits
  • TXA2
    • Vasoconstriction
    • Promotes

59

ASA: indications?

ACS, CVA, aterial thrombosis (long-term vascular events)

60

NSAIDs (propionic acid derivatives): indications?

Pain, inflammation, pyrexia (fever)

61

Celecoxib: indications?

RA, OA

62

Aspirin: adverse effects?

Bleeding, gastric irritation

63

NSAIDs/celecoxib: which has more adverse effects?

NSAIDs (bleeding)

64

*Name the 5 ADP-receptor inhibitor anti-platelet drugs.

Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor

65

How are clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor adminsitered?

What is their MoA?

PO

ADP-receptor inhibitors (anti-platelet)

66

Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor: indications?

ACS, CVA, in stent thrombosis (long-term vascular events)

67

What are the adverse effects of the ADP-receptor inhibitors?

Which of them has 1 additional side effect and what is it?

Bleeding

Clopidogrel also causes TTP

 

(Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor)

68

What is the name of the receptor on platelets that bind ADP?

P2Y12 receptor

69

If aspirin is intollerable, what would be a good class of drugs to consider giving?

Anti-platelet drugs

70

What drug class is recommended as duel-antiplatelet therapy w/ASA in conditions including STEMI, stent placement, and cerebrovascular dz?

Anti-platelet drugs

("grel"s)

71

Name the 2 drugs that are phosphodiesterase inhibitors?

What does inhibiting phosphodiesterase do?

Dipyridamole and cilostazole

They are anti-platelet drugs

 

A image thumb
72

Dipyridamole and cilostazole: MoA?

Phosphodiesterase inhibitors (^cAMP)

73

Dipyridamole and cilostazole: routes of administration?

PO

74

Dipyridamole: indications?

Cilostazol: indications?

  • Dipyridamole: Arterial thrombosis, CVA

  • Cilostazol: *Intermittent claudication

(both phosphodiesterase inhibitors)

75

Dipyridamole: toxicity?

Cilostazol: toxicity?

  • Dipyridamole: Bleeding
  • Cilostazol: Hypotension (due to vasodilation)

76

Name 2 leukotriene receptor inhibitor drugs.

What overall class of drugs do these belong in?

Monteleukast and zafirleukast

Anti-platelet drugs

77

Monteleukast and zafirleukast: MoA?

Leukotriene receptor inhibitor (anti-platelet)

78

Monteleukast and zafirleukast: route of administration?

PO

79

Indications:

  • Monteleukast
  • Zafirleukast

  • Monteleukast: Allergies (allergic rxns)
  • Zafirleukast: Asthma

80

Adverse effects:

  • Monteleukast
  • Zafirleukast

  • Monteleukast: Hypotension; behavioral changes
  • Zafirleukast: Hypotension

81

Name 3 GP IIb/IIIa inhibitors.

"II/III TEA"

Abciximab, eptifibatide, tirofiban

82

Abciximab, eptifibatide, tirofiban: MoA?

What class of drugs do they belong in?

Inhibit gp IIb/IIIa receptor on platelets

Antiplatelet

83

*Abciximab, eptifibatide, tirofiban: indications?

ACS/PCI (percutaneous coronary intervention)

84

Abciximab, eptifibatide, tirofiban: toxicity?

Bleeding

85

What is the MoA of iloprost? (not on chart)

Thromboxane receptor antagonist

86

What is the active anti-platelet agent of fish oil?

Omega-3 fatty acids

87

What is the MoA of omega-3 fatty acids (in fish oil)?

Indications?

  • Membrane effects; TXA3 (?)
  • Prevention of heart dz (?)

88

*What is the route of administration for the gp IIb/IIIa inhibitors?

IV (pretty sure all others we looked at were PO)

89

What class of drug is zileuton?

What's its MoA?

Antiplatelet

Lipooxygenase inhibitor

90

Zileuton: indications?

Asthma

91

Zileuton: toxicity?

Hypotension

92

Name 4 thrombolytic agents.

Name 3 anti-thrombolytic agents.

Streptokinase, urokinase, tPA, ancrod

 

Epsilon amino caproic acid, aprotinin, tranexamic acid

93

What type of drug is streptokinase?

How is it adminsitered?

Thrombolytic

IV

94

What type of drug is urokinase?

How is it adminsitered?

Thrombolytic

IV

95

What type of drug is tissue plasminogen activator (tPA)?

How is it adminsitered?

Thrombolytic

IV

96

What type of drug is ancrod?

How is it adminsitered?

Fibrinolytic

IV

97

What are the indications for streptokinase and urokinase?

Thrombolysis: CVA, MI, PE

98

What is the MoA for the thrombolytic agents urokinase, streptokinase, ancrod, and tPA?

Fibrinolysis (convert plasminogen to plasmin)

99

What are the indications for tPA?

Thrombolysis: CVA, MI

100

What are the indications for ancrod?

Under what conditions would it be used?

CVA

*Used when pts allergic to heparin

101

Where does ancrod come from?

Snake venom

102

What are the adverse effects of all thrombolytic agents?

Which have additional adverse effects?

Bleeding, as well as re-occlusion and CVA

Steptokinase: mild allergic rxns

Ancrod: allergic rxns

103

What are 3 drugs/drug classes that thrombolytics interact w/?

Antiplatelet drugs, dextrans, heparin

104

*What are the absolute contraindications of thrombolytics? (4)

  • Head trauma
  • Recent intracranial surgery
  • Severe HTN
  • Cerebral hemorrhage (white on CT)

105

What type of drug is epsilon amino caproic acid, EACA (MoA)?

Anti-thrombolytic (blocks plasminogen to plasmin)

106

What type of drug is aprotinin? (MoA?)

Anti-fibrinolytic (inhibits kallikrein to decrease factor XII)

107

What type of drug is tranexamic acid? (MoA?)

Anti-fibrinolytic: blocks plasminogen to plasmin

108

What are the indications for EACA, aprotinin, and tranexamic acid?

Reversal of bleeding

109

What toxic effects are a/w epsilon amino caproic acid?

Hypotension

110

What toxic effects are a/w aprotinin?

Graft thrombosis

111

What toxic effects are a/w tranexamic acid?

Retinopathy

112