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CRP > Anticoagulants, Thrombolytic, Coagulant Agents > Flashcards

Anticoagulants, Thrombolytic, Coagulant Agents Flashcards

1
Q

What are the oral antiplatelet agents?

A

Aspirin, NSAIDs, Ticlopidine (Ticlid), Clopidogrel (Plavix), Prasugrel (Effient), Ticagrelor (Brilinta)

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2
Q

What is the MOA of Aspirin?

A

Irreversible COX inhibitor; reduces prostaglandin synthesis (and TXA2) > less platelet aggregation

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3
Q

When would you use Aspirin?

A

Preventing subsequent heart attack/stroke, coronary artery disease, history of coronary bypass operation or coronary angioplasty

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4
Q

What is the MOA of NSAIDs?

A

Reversible COX inhibitor; reduces prostaglandin synthesis > less platelet aggregation

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5
Q

When would you use NSAIDs?

A

Preventing subsequent heart attack/stroke, coronary artery disease, history of coronary bypass operation or coronary angioplasty

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6
Q

What are the contraindications of NSAIDs?

A

Aspirin is preferred due to irreversibility

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7
Q

What is the MOA of Ticlopidine (Ticlid)?

A

Inhibits platelet function (via induction of thrombasthenia-like state); irreversibly inhibits ADP-induced platelet fibrinogen binding and platelet-platelet interactions

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8
Q

When would you use Ticlopidine (Ticlid)?

A

Prevents stroke in patients with history of TIA or thrombotic stroke (if intolerant of or if aspirin fails); combo with aspirin to prevent coronary stent thrombosis

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9
Q

What are the ADRs of Ticlopidine (Ticlid)?

A

Nausea, dyspepsia, diarrhea (20%), hemorrhage (5%), leukopenia (1%), and TTP

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10
Q

What is the MOA of Clopidogrel (Plavix)?

A

Irreversible block/covalent binding of the ADP receptor on platelets; irreversibly inhibits platelet-fibrinogen and platelet-platelet interactions

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11
Q

When would you use Clopidogrel (Plavix)?

A

Unstable angina or non-ST-elevation acute MI (NSTEMI) in combo with aspirin; STEMI; recent MI, stroke, peripheral artery disease; cardiovascular conditions prone to clot formation

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12
Q

What are the ADRs of Clopidogrel (Plavix)?

A

TTP, rare neutropenia (preferred over ticlopidine)

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13
Q

What are the contraindications of Clopidogrel (Plavix)?

A

When using drugs that impair CYP2C19 function (CYP450 isoform needed for activation of drug)

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14
Q

What is the MOA of Prasugrel (Effient)?

A

Inhibits platelet activation and aggregation mediated by ADP receptor

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15
Q

When would you use Prasugrel (Effient)?

A

Unstable angina or non-ST-elevation acute MI (NSTEMI) in combo with aspirin; STEMI; recent MI, stroke, peripheral artery disease; cardiovascular conditions prone to clot formation

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16
Q

What are the ADRs of Prasugrel (Effient)?

A

Major and minor bleeding risk increased over clopidogrel

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17
Q

What are the contraindications of Prasugrel (Effient)?

A

Patients with TIA history or stroke due to increased bleeding risk

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18
Q

What is the MOA of Ticagrelor (Brilinta)?

A

Reversible antagonist of ADP receptor; does not require bioactivation > faster onset

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19
Q

When would you use Ticagrelor (Brilinta)?

A

Acute coronary synderomes in combo with low-dose aspirin

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20
Q

What are the ADRs of Ticagrelor (Brilinta)?

A

Increased non-cardiac surgical bleeding, shortness of breath at rest or after small exercise; chest pain; fast, slow, pounding, or irregular heartbeat

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21
Q

What are the injectable antiplatelet agents?

A

Abciximab (Reopro), Eptifibatide (Integrilin), Tirofiban (Aggrastat)

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22
Q

What is the MOA of Abciximab (Reopro)?

A

GpIIb/IIIa antagonist (chimeric monoclonal antibody against GpIIb/IIIa complex)

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23
Q

When would you use Abciximab (Reopro)?

A

Percutaneous coronary intervention and acute coronary syndromes

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24
Q

What are the ADRs of Abciximab (Reopro)?

A

Bleeding

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25
Q

What is the MOA of Eptifibatide (Integrilin)?

A

GpIIb/IIIa antagonist (cyclic peptide derived from rattlesnake venom); variant RGD motif; competes with fibrinogen for binding to GpIIb/IIIa; short half life

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26
Q

When would you use Eptifibatide (Integrilin)?

A

Percutaneous coronary intervention and acute coronary syndromes

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27
Q

What are the ADRs of Eptifibatide (Integrilin)?

A

Bleeding

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28
Q

What is the MOA of Tirofiban (Aggrastat)?

A

GpIIb/IIIa antagonist (peptidomimetic inhibitor with the RGD sequence motif)

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29
Q

When would you use Tirofiban (Aggrastat)?

A

Non-ST elevation acute coronary syndrome (NSTE-ACS); short half life (continuous infusion)

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30
Q

What are the ADRs of Tirofiban (Aggrastat)?

A

Minor bleeding

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31
Q

What are the combined antiplatelet agents?

A

Dipyridamole (Persantine), Cilostazol (Pletal)

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32
Q

What is the MOA of Dipyridamole (Persantine)?

A

Inhibits adenosine uptake and inhibits cGMP phosphodiesterase (cGMP/cAMP inhibitory to platelet adhesion/aggregation) > vasodilation that also inhibits platelet function

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33
Q

When would you use Dipyridamole (Persantine)?

A

Little or no effect when alone; with aspirin > prevent cerebral ischemia; with warfarin > prophylaxis of thromboemboli for prosthetic heart valves

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34
Q

What are the ADRs for Dipyridamole (Persantine)?

A

Chest pain, angina exascerbation (IV), abnormal ECG, headache (IV), dizziness, ST-T changes; abdominal discomfort (oral); extrasystole

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35
Q

What is the MOA of Cilostazol (Pletal)?

A

Phosphodiesterase inhibitor; promotes vasodilation and inhibits platelet aggregation

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36
Q

When would you use Cilostazol (Pletal)?

A

Claudication (cramping pain in leg due to exercise bc of peripheral vascular disease)

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37
Q

What are the ADRs of Cilostazol (Pletal)?

A

Headache, diarrhea, abnormal stools, infection, rhinitis, pharyngitis, dizziness, palpitations, peripheral edema, back pain, dyspepsia

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38
Q

What are the contraindications for Cilostazol (Pletal)?

A

CHF of any severity

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39
Q

What are the injectable indirect thrombin inhibitors?

A

Heparin, Fondaparinux (Arixtra)

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40
Q

What is the MOA of Heparin?

A

IV/SQ; Enhances the activity of anti-thrombin III (AT-III) > inhibition of thrombin (IIa), IXa, Xa, XIa, and XIIa; high molecular weight heparin has high affinity for AT-III and IIa, IXa, Xa (mainly IIa/Xa); low molecular weight inhibits Xa (enoxaparin, dalteparin, tinzaparin) with less frequent dosing needed

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41
Q

When would you use Heparin?

A

In vivo: prevention and treatment of deep vein thrombosis, pulmonary embolism, arterial thrombosis; in vitro: hemodialysis, indwelling vascular catheters, lab blood samples

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42
Q

What are the ADRs of Heparin?

A

Unwanted bleeding (mucous membranes, open wounds, intracranial, GI), allergic rxns, hair loss; induced thrombocytopenia (HIT) in 1-4% > skin necrosis; long term use > osteoporosis and fractures (mineralocorticoid deficit)

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43
Q

What is the antidote for heparin?

A

Protamine sulfate (complexes with heparin) given as SC or IV; close monitoring needed; unfractionated heparin = PTT, or LMW heparin by anti-factor Xa assay

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44
Q

What is the MOA of Fondaparinux (Arixtra)?

A

IV/SQ; synthetic pentasaccharide of heparin; enhances the activity of AT-III; mimics active site of heparin that binds AT-III (only enhances AT-III inactivation of Xa > less thrombin formed)

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45
Q

When would you use Fondaparinux (Arixtra)?

A

DVT/acute PE (treatment and prophylactic) and acute coronary syndrome; predictable pharmacokinetics therefore no monitoring

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46
Q

What are the ADRs of Fondaparinux (Arixtra)?

A

Some cross-reactivity with heparin antibodies, some cases of HIT; anemia, fever, nausea, rash, constipation, edema headache, insomnia, vomiting

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47
Q

What are the injectable direct thrombin inhibitors?

A

Bivalirudin (Angiomax), Argatroban (Acova)

48
Q

What is the MOA of Bivalirudin (Angiomax)?

A

IV; specific and reversible bivalent direct thrombin inhibitor; rapid on/off (25 min half life); inhibits platelet activation

49
Q

When would you use Bivalirudin (Angiomax)?

A

With aspirin: unstable angina with patients undergoing percutaneous transluminal coronary angioplasty (PTCA), percutaneous coronary intervention (PCI) with provisional use of GpIIb/IIIa inhibitor, with or at risk of HIT/heparin-induced TTP and thrombosis syndrome (HITTS) undergoing PCI

50
Q

What are the ADRs of Bivalirudin (Angiomax)?

A

Back, general pain; nausea, hemorrhage (minor), headache, hypotension, injection site pain, insomnia, pelvic pain, hypertension, anxiety, vomiting, bradycardia, dyspepsia, abdominal pain, fever, nervousness

51
Q

What is the MOA of Argatroban (Acova)?

A

IV (via infusion with short half life); thrombin inhibitor monitored with aPTT

52
Q

When would you use Argatroban (Acova)?

A

HIT (with or without thrombosis), coronary angioplasty with HIT, monitored by aPTT (argatroban increases INR > difficult transition to warfarin)

53
Q

What are the ADRs with Argatroban (Acova)?

A

GI bleeding, hematuria, chest pain, hemoglobin and hematocrit decrease, hypotension, dyspnea, fever, sepsis, cardiac arrest, diarrhea, nausea, groin hemorrhage, pain, urinary tract infection, ventricular tachycardia

54
Q

What are the oral direct thrombin inhibitor?

A

Dabigatran Etexilate (Pradaxa)

55
Q

What is the MOA of Dabigatran Etexilate (Pradaxa)?

A

Binds to and inhibits thrombin

56
Q

When would you use Dabigatran Etexilate (Pradaxa)?

A

Prevent venous thromboembolic events in adults following total hip/knee replacement; non-valvular atrial fibrillation (over warfarin)

57
Q

What is the antidote for Dabigatran Etexilate (Pradaxa)?

A

Idarucizumab (Praxbind): binds to dabigatran and its metabolites with higher affinity than dabigatran to thrombin > neutralization of anticoagulant effect

58
Q

What are the oral anti-clotting factor agents?

A

Warfarin (Coumadin), Rivaroxaban (Xarelto), Apixaban (Eliquis), Edoxaban (Savaysa)

59
Q

What is the MOA of Warfarin (Coumadin)?

A

Antagonist of vitamin K (decarboxylates to activate II, VII, IX, X, protein S and C); prevents reduction to allow for recycling

60
Q

When would you use warfarin (Coumadin)?

A

Prevent or treat DVT or PE; for blood clots that may be caused by certain heart conditions, open-heart surgery, or after MI; monitoring needed via prothrombin time (PT)/INR

61
Q

What are the ADRs of Warfarin (Coumadin)?

A

Unwanted bleeding (like heparin)

62
Q

What are the contraindications of Warfarin (Coumadin)?

A

Pregnancy > teratogen (birth defects in bone)

63
Q

What is the antidote for Warfarin (Coumadin)?

A

Vitamin K1 (Aquamephyton/Konakion 1)

64
Q

What is the MOA of Rivaroxaban (Xarelto)?

A

Inhibits free Xa and clot-bound Xa prothrombinase activity; directly inhibits platelet aggregation induced by thrombin (bc reduces thrombin formation)

65
Q

When would you use Rivaroxaban (Xarelto)?

A

Thromboembolism prevention after ortho surgeries; non-valvular atrial fibrillation (NVAF) prevention; treat and prevent DCT and PE

66
Q

What is the MOA of Apixaban (Eliquis)?

A

Direct inhibitor of free and clot-bound Xa

67
Q

When would you use Apixaban (Eliquis)?

A

Prevention of thromboembolism: to reduce risk of stroke, non-valvular atrial fibrillation, hip/knee replacement surgery; treatment of DVT or PE

68
Q

What is the MOA of Edoxaban (Savaysa)?

A

Selective (direct) Xa-inhibitor

69
Q

When would you use Edoxaban (Savaysa)?

A

Prevention of thromboembolism: ortho surgeries, patients with NVAF; treatment of DVT or PE: for patients initially treated with parenteral anticoagulant for 5-10 days

70
Q

What are the specific thromboembolytic agents?

A

Streptokinase (Streptase), Urokinase (Abbokinase)

71
Q

What is the MOA of Streptokinase (Streptase)?

A

Complexes with plasminogen > conformational change; activates free plasminogen > plasmin (systemic and not clot specific)

72
Q

When would you use Streptokinase (Streptase)?

A

IV: PE with hemodynamic instability, severe DVT (superior vena caval syndrome), and ascending thrombophlebitis of iliofemoral vein with severe lower extremity edema; intra-arterially: peripheral vascular disease; within 6 hrs post symptomatic onset of acute MI; t-PAs also for acute ischemic stroke within 3 hrs symptom onset

73
Q

What are the ADRs for Streptokinase (Streptase)?

A

Blurred vision, confusion, dizziness, faintness when getting up from lying or sitting position, fever sweating, unusual tiredness or weakness

74
Q

What are the contraindications of Streptokinase (Streptase)?

A

Patients with antistreptococcal antibodies > fever, allergic rxns, resistance

75
Q

What is the antidote for Streptokinase (Streptase)?

A

Aminocaproic Acid (Amicar)

76
Q

What is the MOA of Urokinase (Abbokinase)?

A

Cleaves arg-arg 560-561 peptide bond in plasminogen > active plasmin (systemic)

77
Q

When would you use Urokinase (Abbokinase)?

A

IV: PE with hemodynamic instability, severe DVT (superior vena caval syndrome), and ascending thrombophlebitis of iliofemoral vein with severe lower extremity edema; intra-arterially: peripheral vascular disease; within 6 hrs post symptomatic onset of acute MI; t-PAs also for acute ischemic stroke within 3 hrs symptom onset

78
Q

What are the ADRs for Urokinase (Abbokinase)?

A

Bleeding, dizziness, headache, paralysis, difficulty breathing or swallowing

79
Q

What is the antidote for Urokinase (Abbokinase)?

A

Aminocaproic Acid (Amicar)

80
Q

What are the Tissue Plasminogen Activators (t-PAs)?

A

Alteplase (Activase), Reteplase (Retavase), Tenecteplase (TNKase)

81
Q

What is the MOA of Alteplase (Activase)?

A

Binds to fibrin and activates bound plasminogen; cleaves arg-arg 560-561 bond of fibrin-bound plasminogen; inefficient at activating free systemic plasminogen (clot-specific)

82
Q

When would you use Alteplase (Activase)?

A

IV: PE with hemodynamic instability, severe DVT (superior vena caval syndrome), and ascending thrombophlebitis of iliofemoral vein with severe lower extremity edema; intra-arterially: peripheral vascular disease; within 6 hrs post symptomatic onset of acute MI; t-PAs also for acute ischemic stroke within 3 hrs symptom onset

83
Q

What are the ADRs of Alteplase (Activase)?

A

Similar to urokinase

84
Q

What is the antidote for Alteplase (Activase)?

A

Aminocaproic Acid (Amicar)

85
Q

What is the MOA of Reteplase (Retavase)?

A

Binds to fibrin and activates bound plasminogen; cleaves arg-arg 560-561 bond of fibrin-bound plasminogen; inefficient at activating free systemic plasminogen (clot-specific)

86
Q

When would you use Reteplase (Retavase)?

A

IV: PE with hemodynamic instability, severe DVT (superior vena caval syndrome), and ascending thrombophlebitis of iliofemoral vein with severe lower extremity edema; intra-arterially: peripheral vascular disease; within 6 hrs post symptomatic onset of acute MI; t-PAs also for acute ischemic stroke within 3 hrs symptom onset

87
Q

What are the ADRs for Reteplase (Retavase)?

A

Similar to Urokinase

88
Q

What is the antidote for Reteplase (Retavase)?

A

Aminocaproic Acid (Amicar)

89
Q

What is the MOA of Tenecteplase (TNKase)?

A

Binds to fibrin and activates bound plasminogen; cleaves arg-arg 560-561 bond of fibrin-bound plasminogen; inefficient at activating free systemic plasminogen (clot-specific)

90
Q

When would you use Tenecteplase (TNKase)?

A

IV: PE with hemodynamic instability, severe DVT (superior vena caval syndrome), and ascending thrombophlebitis of iliofemoral vein with severe lower extremity edema; intra-arterially: peripheral vascular disease; within 6 hrs post symptomatic onset of acute MI; t-PAs also for acute ischemic stroke within 3 hrs symptom onset

91
Q

What are the ADRs for Tenecteplase (TNKase)?

A

Similar to urokinase

92
Q

What is the antidote for Tenecteplase (TNKase)?

A

Aminocaproic Acid (Amicar)

93
Q

What is the anti-fibrinolytic agent?

A

Aminocaproic Acid (Amicar)

94
Q

What is the MOA of Aminocaproic Acid (Amicar)?

A

Oral/IV; binds to lysine binding sites on plasminogen and plasmin; blocks the binding of plasmin to target fibrin; potent inhibitor of fibrinolysis

95
Q

When would you use Aminocaproic Acid (Amicar)?

A

Antidote for steptokinase, urokinase, t-PA; to reverse excessive fibrinolysis states

96
Q

What are the ADRs for Aminocaproic Acid (Amicar)?

A

Myopathy, muscle weakness, others undefined

97
Q

What are the Specific coagulating agents?

A

Factors: VIII, IX, IX complex, VIIa, X, Vitamin K, Thrombin, Gelfoam, vWF (Vonvendi)

98
Q

What is the MOA of Factor VIII?

A

Plasma precipitate (fresh/frozen) with 8-12 hr half life; human (Alphanate, Hemofil M, Koate-DVI, Monoclate-P); recombinant DNA (adynovate)

99
Q

When would you use Factor VIII?

A

To treat hemophilia A

100
Q

What is the MOA of Factor IX?

A

Purified human factor (heat treated from plasma): Alphanine SD, Mononine; recombinant: Benefix, Alprolix, Rixubis, Ixinity, Idelvion

101
Q

When would you use Factor IX?

A

To treat hemophilia B

102
Q

What are the ADRs of Factor IX?

A

Formation of circulating antibodies against factor IX

103
Q

What is the MOA of Factor IX complex?

A

Recombinant DNA: Bebulin VH, Profilnine SD, Proplex T

104
Q

When would you use Factor IX complex?

A

To treat hemophilia B

105
Q

What are the ADRs of Factor IX complex?

A

Formation of circulating antibodies against factor IX

106
Q

What is the MOA of Factor VIIa?

A

IV; activates factor X to Xa and factor IX to IXa; recombinant DNA (Novoseven, AryoSeven)

107
Q

When would you use Factor VIIa?

A

To treat hemophilia A or B

108
Q

What are the ADRs for Factor VIIa?

A

Fever, hemorrhage, hemarthrosis, decreased fibrinogen, hypertension; Black box warning: serious arterial/venous thrombotic and thromboembolic events post admin

109
Q

What is the MOA of Factor X?

A

Human (Coagadex); IV

110
Q

When would you use Factor X?

A

Factor X deficiency/Stuart-Prower Factor Deficiency

111
Q

What are the ADRs for Factor X?

A

Infusion site erythema, back pain, infusion site pain

112
Q

What is the MOA of Vitamin K?

A

Dependent factors: II, VII, IX, X

113
Q

What is the MOA of Thrombin?

A

Bovine plasma, topical, powder

114
Q

When would you use Thrombin?

A

To arrest minor bleeding/oozing

115
Q

What is the MOA of Gelfoam?

A

Absorbable gelatin; senatured collagen, sponge/powder, nonantigenic

116
Q

When would you use Gelfoam?

A

Surgery

117
Q

When would you use von willebrand factor?

A

Von Willebrand Disease

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