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Pharm > Coagulation drugs > Flashcards

Coagulation drugs Flashcards

1
Q

Unfractionated heparin: routes of administration?

A

Mainly IV, also subQ.

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2
Q

Unfractionated heparin: MoA?

A

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

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

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3
Q

Unfractionated heparin: indications?

A

Surgical anticoagulation

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4
Q

Unfractionated heparin: adverse effects?

A

Bleeding, HIT, osteoporosis, alopecia

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5
Q

How is unfractionated heparin monitored?

A

Monitored by APTT (2-2.5x baseline therapeutic)

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6
Q

LMW heparins: routes of administration?

A

SubQ

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7
Q

LMW heparins: MoA?

A

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

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8
Q

LMW heparins: indications?

A

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

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9
Q

LMW heparins: adverse effects?

A

Bleeding

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10
Q

How is LMW heparin monitored?

A

Monitored by anti-Xa.

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11
Q

Fondaparinux (pentasaccharide): route of administration?

A

SubQ

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12
Q

Fondaparinux (pentasaccharide): MoA?

What class of drugs does it fall under?

A

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

“Heparin anticoagulants”

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13
Q

Indications for fondaparinux?

A

Mgmt of DVT

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14
Q

Toxic/adverse effects of Fondaparinux?

A

Bleeding

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15
Q

Argatroban: route of administration?

A

IV

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16
Q

Argatroban: MoA?

What drug category does it fall under?

A

Direct IIa inhibitor

“Heparin anticoagulants”

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17
Q

Argatroban: indications?

A

Anticoagulant mgmt of HIT pts

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18
Q

Argatroban: adverse effects?

A

Bleeding

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19
Q

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

A

Bivalrudin & hirudin

(“Heparin anticoagulants.”

MoA: direct IIa inhibitor.

Indications: mgmt of HIT pts.

Adverse effects: bleeding)

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20
Q

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

Is there T1/2 longer or shorter?

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

All short T1/2

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21
Q

How is antithrombin concentrate administered?

A

IV

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22
Q

Antithrombin concentrate: MoA?

A

Direct IIa inhibitor

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23
Q

Antithrombin concentrate: indications?

A

DIC, sepsis, thrombophilia, hypercoagulable state

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24
Q

Antithrombin concentrate: toxicity?

A

None!

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25
Q

What is protamine sulfate? What is it used for?

A
  • Heparin antagonist
  • Reverses the effects of heparin
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26
Q

Protamine sulfate: adverse effects/toxicity?

A

Bradycardia, hypotension

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27
Q

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

A

10

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28
Q

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

A
  1. Unfactionated heparin
  2. LMW heparin (branded + generic)
  3. Fondaparinux (pentasaccharide)
  4. Argatroban
  5. Bivalirudin
  6. Hirudin
  7. Antithrombin concentrate
  8. Protamine sulfate
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29
Q

What is the brand name of warfarin?

How is it administered?

A

Coumadin

PO (“oral anticoagulant”)

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30
Q

Warfarin: MoA?

A

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

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31
Q

Warfarin: indications?

A

Prolonged tx of a-fib and DVT

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32
Q

*Warfarin: toxic/adverse effects?

A

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.

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33
Q

How are warfarin levels monitored?

A

Monitored via PT/INR.

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34
Q

How is vitamin K administered?

A

PO

(“oral anticoagulants”)

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35
Q

Vitamin K: MoA?

A

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

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36
Q

Vitamin K: indications?

A
  • Hypoprothrombinemia
  • Intestinal disorders
  • Gastrectomy
  • Reverses the effects of warfarin
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37
Q

Vitamin K: adverse effects?

A

Hemolysis

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38
Q

How is vitamin K monitored?

A

Trick: monitoring not required

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39
Q

*Name the 3 oral anti-Xa anticoagulant drugs.

A
  • Rivaroxaban
  • Apixaban
  • Edoxaban

(EAR)

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40
Q

Edoxaban, apixaban, rivaroxaban (ear): MoA?

Route of administration?

A

Xa inhibitor

PO

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41
Q

Edoxaban, apixaban, rivaroxaban (ear): indications?

  • Which are approved for prophylaxis and tx of DVT?
  • Which are approved for tx of ACS?
A

Stroke prevention in patients with a-fib.

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

R approved for ACS.

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42
Q

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

A

Bleeding; liver toxicity

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43
Q

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

A

Monitoring not required

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44
Q

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

A
  • Oral antithrombin
  • Dabigatran
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45
Q

What is the MoA of both oral antithrombin and dabigatran?

Routes of administration?

A

Inhibits IIa

PO

46
Q

What are the indications for oral antithrombin and dabigatran?

A

Stroke prevention for pts w/a-fib

47
Q

Oral antithrombin and dabigatran: toxic effects?

A

Bleeding; liver toxicity

48
Q

What organ clears oral antithrombin and dabigatran?

A

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

49
Q

How are oral antithrombin and dabigatran monitored?

A

Trick: they do not need monitoring

50
Q

Try to name the 7 oral anticoagulants discussed in class.

A
  1. Warfarin
  2. Vitamin K
  3. Edoxaban
  4. Apixaban
  5. Rivaroxaban
  6. Oral antithrombin
  7. Dabigatran
51
Q
  1. Name 3 cyclooxigenase inhibitors that affect platelets.
    1. Which affect which COX enzymes?
    2. How are they administered?
A
  1. ASA, NSAIDs, celecoxib
    1. ASA/NSAIDs: inhibit COX-1 and 2. Celecoxib only inhibits COX-2
    2. PO
52
Q

How does a platelet aggregation assay work?

A
  1. Prepare platelet-rich plasma
  2. Activate platelets (ADP, TRAP, epi, 5-HT, collagen, ristocetin, AA)
  3. Measure light transmittence
53
Q

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

A

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

54
Q

What condition is ASA resistance a/w?

A

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

55
Q

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

A

Aspirin

(can do double or triple inhibitor therapy)

56
Q

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

A
  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
Q

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

A

Prostaglandins

Leukotrienes

58
Q

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

A
  • PGI2
    • Vasodilation
    • Inhibits
  • TXA2
    • Vasoconstriction
    • Promotes
59
Q

ASA: indications?

A

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

60
Q

NSAIDs (propionic acid derivatives): indications?

A

Pain, inflammation, pyrexia (fever)

61
Q

Celecoxib: indications?

A

RA, OA

62
Q

Aspirin: adverse effects?

A

Bleeding, gastric irritation

63
Q

NSAIDs/celecoxib: which has more adverse effects?

A

NSAIDs (bleeding)

64
Q

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

A

Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor

65
Q

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

What is their MoA?

A

PO

ADP-receptor inhibitors (anti-platelet)

66
Q

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

A

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

67
Q

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

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

A

Bleeding

Clopidogrel also causes TTP

(Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor)

68
Q

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

A

P2Y12 receptor

69
Q

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

A

Anti-platelet drugs

70
Q

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

A

Anti-platelet drugs

(“grel”s)

71
Q

Name the 2 drugs that are phosphodiesterase inhibitors?

What does inhibiting phosphodiesterase do?

A

Dipyridamole and cilostazole

They are anti-platelet drugs

72
Q

Dipyridamole and cilostazole: MoA?

A

Phosphodiesterase inhibitors (^cAMP)

73
Q

Dipyridamole and cilostazole: routes of administration?

A

PO

74
Q

Dipyridamole: indications?

Cilostazol: indications?

A
  • Dipyridamole: Arterial thrombosis, CVA
  • Cilostazol: *Intermittent claudication

(both phosphodiesterase inhibitors)

75
Q

Dipyridamole: toxicity?

Cilostazol: toxicity?

A
  • Dipyridamole: Bleeding
  • Cilostazol: Hypotension (due to vasodilation)
76
Q

Name 2 leukotriene receptor inhibitor drugs.

What overall class of drugs do these belong in?

A

Monteleukast and zafirleukast

Anti-platelet drugs

77
Q

Monteleukast and zafirleukast: MoA?

A

Leukotriene receptor inhibitor (anti-platelet)

78
Q

Monteleukast and zafirleukast: route of administration?

A

PO

79
Q

Indications:

  • Monteleukast
  • Zafirleukast
A
  • Monteleukast: Allergies (allergic rxns)
  • Zafirleukast: Asthma
80
Q

Adverse effects:

  • Monteleukast
  • Zafirleukast
A
  • Monteleukast: Hypotension; behavioral changes
  • Zafirleukast: Hypotension
81
Q

Name 3 GP IIb/IIIa inhibitors.

A

“II/III TEA”

Abciximab, eptifibatide, tirofiban

82
Q

Abciximab, eptifibatide, tirofiban: MoA?

What class of drugs do they belong in?

A

Inhibit gp IIb/IIIa receptor on platelets

Antiplatelet

83
Q

*Abciximab, eptifibatide, tirofiban: indications?

A

ACS/PCI (percutaneous coronary intervention)

84
Q

Abciximab, eptifibatide, tirofiban: toxicity?

A

Bleeding

85
Q

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

A

Thromboxane receptor antagonist

86
Q

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

A

Omega-3 fatty acids

87
Q

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

Indications?

A
  • Membrane effects; TXA3 (?)
  • Prevention of heart dz (?)
88
Q

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

A

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

89
Q

What class of drug is zileuton?

What’s its MoA?

A

Antiplatelet

Lipooxygenase inhibitor

90
Q

Zileuton: indications?

A

Asthma

91
Q

Zileuton: toxicity?

A

Hypotension

92
Q

Name 4 thrombolytic agents.

Name 3 anti-thrombolytic agents.

A

Streptokinase, urokinase, tPA, ancrod

Epsilon amino caproic acid, aprotinin, tranexamic acid

93
Q

What type of drug is streptokinase?

How is it adminsitered?

A

Thrombolytic

IV

94
Q

What type of drug is urokinase?

How is it adminsitered?

A

Thrombolytic

IV

95
Q

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

How is it adminsitered?

A

Thrombolytic

IV

96
Q

What type of drug is ancrod?

How is it adminsitered?

A

Fibrinolytic

IV

97
Q

What are the indications for streptokinase and urokinase?

A

Thrombolysis: CVA, MI, PE

98
Q

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

A

Fibrinolysis (convert plasminogen to plasmin)

99
Q

What are the indications for tPA?

A

Thrombolysis: CVA, MI

100
Q

What are the indications for ancrod?

Under what conditions would it be used?

A

CVA

*Used when pts allergic to heparin

101
Q

Where does ancrod come from?

A

Snake venom

102
Q

What are the adverse effects of all thrombolytic agents?

Which have additional adverse effects?

A

Bleeding, as well as re-occlusion and CVA

Steptokinase: mild allergic rxns

Ancrod: allergic rxns

103
Q

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

A

Antiplatelet drugs, dextrans, heparin

104
Q

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

A
  • Head trauma
  • Recent intracranial surgery
  • Severe HTN
  • Cerebral hemorrhage (white on CT)
105
Q

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

A

Anti-thrombolytic (blocks plasminogen to plasmin)

106
Q

What type of drug is aprotinin? (MoA?)

A

Anti-fibrinolytic (inhibits kallikrein to decrease factor XII)

107
Q

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

A

Anti-fibrinolytic: blocks plasminogen to plasmin

108
Q

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

A

Reversal of bleeding

109
Q

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

A

Hypotension

110
Q

What toxic effects are a/w aprotinin?

A

Graft thrombosis

111
Q

What toxic effects are a/w tranexamic acid?

A

Retinopathy

112
Q
A

Pharm (32 decks)

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