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Pharmacology > Thrombotics > Flashcards

Thrombotics Flashcards

1
Q

Indirect thrombin inhibitors?

A

Unfractioned heparin, Dalteparin, Enoxaparin, Tinzaparin, Fondaparinux

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2
Q

Unfractionated heparin class and mxn?

A

Indirect thrombin inhibitor; Bind antithrombin and potentiate formation of antithrombin-coagulation factor complex (Xa, IIa)

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3
Q

Unfractionated for?

A

Prevention and tx of venous thromboembolism

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4
Q

Unfractionated heparin side effects?

A

Heparin-induced thrombocytopenia, bleeding, osteoporosis

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5
Q

How is unfractionated heparin monitored?

A

PTT: wasnt 2-2.5 normal value

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6
Q

How is unfractionated heparin given?

A

Parenterally

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7
Q

Reversal of unfractionated heparin effects?

A

Protamine

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8
Q

Protamine is an antidote for?

A

Unfractionated heparin, Dalteparin, Enoxaparin, Tinzaparin

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9
Q

Dalteparin class and mxn?

A

LMWH that inhibits thrombin less effectively than Xa

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10
Q

Dalteparin for?

A

Prevent thrombosis and embolism from clots

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11
Q

Dalteparin side effect?

A

Bleeding

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12
Q

How is dalteparin monitored?

A

Heparin assay (anti-factor Xa)

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13
Q

Dalteparin half-life?

A

Longer than heparin (1-2/day)

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14
Q

Reversal of dalteparin effects?

A

Protamine

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15
Q

Enoxaparin class and mxn?

A

LMWH that inhibits thrombin less effectively than Xa

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16
Q

Tinzaparin class and mxn?

A

LMWH that inhibits thrombin less effectively than Xa

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17
Q

Enoxaparin for?

A

Drug of choice in pregnancy for prevention and tx of venous thromboembolism

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18
Q

Side effects of enoxaparin?

A

HIT, bleeding. Osteoporosis and thrombocytopenia are uncommon

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19
Q

Enoxapain half-life?

A

Longer than heparin (1-2/day)

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20
Q

Tinzaparin half-life?

A

Longer than heparin (1-2/day)

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21
Q

How is enoxaparin monitored?

A

Heparin assay (anti-factor Xa)

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22
Q

How is tinzaparin monitored?

A

Heparin assay (anti-factor Xa)

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23
Q

Tinzaparin side effects?

A

HIT, bleeding. Osteoporosis and thrombocytopenia are uncommon

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24
Q

Fondaparinux class and mxn?

A

Indirect thrombin inhibitor; Synthetic polysaccharide that binds active site of antithrombin and inhibits Xa

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25
Q

Indirect thrombin inhibitor without an antidote?

A

Fondaparinux

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26
Q

Reversal of fondararinux effects?

A

No antidote

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27
Q

Fondaparinux for?

A

HIT

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28
Q

Fondaparinux side effect?

A

Bleeding

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29
Q

Warfarin class and mxn?

A

Vitamin K antagonist; Blocks Vit K-dependent gamma-carboxylaton of factors II, VII, IX, X, Protein C and S (does not affect already synthesized factors)

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30
Q

Warfarin for?

A

Long term anticoagulation

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31
Q

Warfarin side effects?

A

Thrombosis and warfarin skin necrosis (Relative Protein C depression); Bleeding

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32
Q

How is warfarin monitored?

A

PT/INR

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33
Q

Monitor ___ with PTT?

A

Heparin, Bivalirudin, Argatroban

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34
Q

Monitor ___ with PT/INR?

A

Warfarin

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35
Q

Warfarin contraindicate in who?

A

Pregnancy (teratogen)

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36
Q

Warfarin can be reversed how?

A

Vitamin K, factor concentrates

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37
Q

Special note about warfarin metabolism?

A

Enhanced by drugs that induce P450 activity (barbiturates)

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38
Q

Direct thrombin inhibitors?

A

Bivalirudin, Argatroban, Dabigatran

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39
Q

Bivalirudin class and mxn?

A

Direct thrombin inhibitor; Irreversibly inactivate fibrinogen-bound and unbound thrombin

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40
Q

Argatroban class and mxn?

A

Direct thrombin inhibitor; binds to catalytic site of thrombin and inactivates fibrinogen-bound and unbound thrombin

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41
Q

Dabigatran class and mxn?

A

Direct thrombin inhibitor; Reversibly (competitively) inactivate fibrinogen-bound and unbound thrombin

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42
Q

Reversible (Competitive) direct thrombin inhibitor?

A

Dabigatran

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43
Q

Irreversible direct thrombin inhibitors?

A

Bivalirudin, Argatroban

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44
Q

Bivalirudin for?

A

Percutaneous coronary intervention

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45
Q

Argatroban for?

A

Percutaneous coronary intervention + HIT

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46
Q

Dabigatran for?

A

DVT, PE, AFib

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47
Q

Bivalirudin side effect?

A

Bleeding

48
Q

Argatroban side effect?

A

Bleeding

49
Q

Dabigatran side effect?

A

Bleeding

50
Q

Reversal of direct thrombin inhibitors?

A

No antidote

51
Q

How is bivalirudin administered?

A

Parenterally

52
Q

How is argatroban administered?

A

Parenterally

53
Q

How is dabigatran administered?

A

Orally

54
Q

Note about dabigatran clearance?

A

Renal fixed dose clearance

55
Q

How is bivalirudin monitored?

A

PTT

56
Q

How is argatroban monitored?

A

PTT

57
Q

Direct Xa inhibitors?

A

Rivaroxaban, Apixaban

58
Q

Rivaroxaban class and mxn?

A

Direct Xa inhibitor; reversibly bind active site of Xa

59
Q

Apixaban class and mxn?

A

Direct Xa inhibitor; reversibly bind active site of Xa

60
Q

Rivaroxaban for?

A

DVT PE prophylaxis

61
Q

Apixaban for?

A

DVT PE prophylaxis

62
Q

How are direct xa inhibitors administered?

A

Rivaroxaban and apixaban: Orally

63
Q

Reversal of rivaroxaban and apixaban effects?

A

No antidote

64
Q

Note on direct xa inhibitor clearance?

A

Rivaroxaban and apixaban: Renal fixed dose clearance

65
Q

Fibrinolytic drugs?

A

Alteplase, Reteplase, Tenecteplase

66
Q

Alteplase class and mxn?

A

Fibrinolytic, Lyse already formed clots by activating circulating plasminogen

67
Q

Reteplase class and mxn?

A

Fibrinolytic, Lyse already formed clots by activating circulating plasminogen

68
Q

Tenecteplase class and mxn?

A

Fibrinolytic, Lyse already formed clots by activating circulating plasminogen

69
Q

Alteplase, reteplase, tenecteplase for?

A

Acute MI, acute stroke, central DVT, multiple PE

70
Q

Antiplatelet drugs?

A

Aspirin, Dipyridamidole, Cloidogrel, Abciximab, Eptifibatide, Tirofiban

71
Q

Remind me of aspirin class and mxn.

A

Antiplately; Irreversible inhibitor of platelets and prevent thromboxane A2 formation

72
Q

Aspirin for?

A

Often as “baby” to prevent and treat MI and strok

73
Q

Dipyridamole class and mxn?

A

Antiplatelet; PDE inhibitor –> Increase platelet cAMP

74
Q

Dipyridamole for?

A

Weak antiplatelet effect

75
Q

How is dipyridamole administered?

A

Parenterally

76
Q

Clopidogrel class and mxn?

A

Antiplatelet; Inhibit platelet ADP receptor

77
Q

Clopidogrel for?

A

Prevent and treat ACS, stroke, peripheral vascular disease, angina, stent

78
Q

Reversal of clopidogrel?

A

Platelet transufion

79
Q

Clopidogrel side effects?

A

Bleeding, TTP

80
Q

Abciximab class and mxn?

A

Antiplatelet; mab against GPIIb/IIIa

81
Q

How is abciximab given?

A

Parenterally

82
Q

How is eptifibatide given?

A

Parenterally

83
Q

How is tirofiban given?

A

Parenterally for an immediate effect

84
Q

Abciximab side effect?

A

Immune response

85
Q

Eptifibatide class and mxn?

A

antiplatelet; fibrinogen analog which competes with endogenous fibrinogen for IIb/IIIa

86
Q

Tirofiban class and mxn?

A

antiplatelet; fibrinogen analog which competes with endogenous fibrinogen for IIb/IIIa

87
Q

Eptifibatide side effect?

A

Bleeding, ACS, PCI, thrombocytopenia

88
Q

Tirofiban side effects?

A

Bleeding, NSTE-ACS

89
Q

Fibrinogen analogs?

A

Eptifibatide, Tirofiban

90
Q

PDE inhibitor?

A

Dipyridamole

91
Q

Monoclonal antiplatelet antibody?

A

Abciximab

92
Q

Inhibits plately ADP receptors?

A

Clopidogrel

93
Q

LMWH reversal with protamine is ______?

A

Less-effective

94
Q

The risk of HIT with LMWH is _____?

A

Less than with unfractionated heparin

95
Q

Is there a need for monitoring with LMWH?

A

No, there is a predictable dose response.

96
Q

Similar to Fondaparinux but with 5-6 day half-life?

A

Idraparinux

97
Q

Half-life of Fondaparinux?

A

17-21 hours

98
Q

Why is warfarin dosing difficult?

A

Competes with VitK, >99% bound to albumin, hepatic metabolism, fluctuation of the cascade, has a very narrow therapeutic index

99
Q

Are direct thrombin inhibitors active in clots?

A

yes!

100
Q

Bivalirudin half-life?

A

Very short

101
Q

Argatroban clearance?

A

Hepatic

102
Q

Dabigatran clearance?

A

Renal

103
Q

Dabigatran is?

A

Serine-protease inhibitor

104
Q

Dabigatran a predrug?

A

Yes

105
Q

Need for monitoring with dabigatran?

A

No, safe over a large range of doses

106
Q

2 generalizations of oral direct inhibitors of Xa and IIa (thrombin)?

A

No antidote, no methods to assess levels

107
Q

Fibrinolytic timing?

A

Effective if within 3-12 hours; Given for 1-2 days

108
Q

Is alteplase clot specific?

A

No

109
Q

Is tenecteplase clot specific?

A

Yes

110
Q

Is reteplase clot specific?

A

Somewhat

111
Q

Does a high or low dose of aspirin provide greater antiplatelet effect?

A

Low dose! High dose will increasingly affect endothelial cell COX1 which can be re-made

112
Q

PDE inhibitors aside from dipyramidole?

A

Cilostazol, Pentoxifylline

113
Q

Is clopidogrel reversible

A

NO

114
Q

Onset of clopidogrel?

A

Slow, and offset is slow as well and can last up to 10 days

115
Q

Other ADP receptor blockers?

A

Prasugrel, Ticagrelor

116
Q

Abciximab lasts?

A

24-48 hours

117
Q

Eptifibatide timing?

A

Rapid onset, short half-life

Pharmacology (46 decks)

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