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Pharmacology > Exam 6 - Anticoagulant, Antiplatelet, and Fibrinolytic Drugs > Flashcards

Exam 6 - Anticoagulant, Antiplatelet, and Fibrinolytic Drugs Flashcards

1
Q

Warfarin

A

oral antigocagulant

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2
Q

Warfarin MOA

A
  • inhibits synthesis of clotting factors II, VII, IX, X (2, 7, 9, 10)
  • inhibits anticoagulant proteins C and S
  • blocks vitamin K
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3
Q

Warfarin indications

A
  • deep vein thrombosis (DVT)
  • atrial fibrillation
  • artificial heart valves
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4
Q

Warfarin goal

A

International normalized ratio (INR) 2-3

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5
Q

Warfarin pharmacokinetics

A
  • metabolized by 2C9 (S), 2C19 (R), 1A2 (R), 3A4 (R)

- maximal effects not seen for 3 to 5 days

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6
Q

Warfarin adverse effects

A

Bleeding

  • reversed by vitamin K
  • Kcentra (Prothrombin Complex - factors II (prothrombin) VII, IX, X) - used w/ administration of vitamin K to reverse the anticoagulation effect and stop bleeding
  • contraindicated in pregnancy
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7
Q

Polymorphism of 2C9 and VKORC1 (poor metabolizers)

A

will need lower dose

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8
Q

Warfarin interactions CYP 450 inducers

A

serum levels decreased by CYP 450 inducers (rifampin, carbamazepine, phenobarbital)

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9
Q

Warfarin interactions CYP 450 inhibitors

A

serum levels increased by CYP 450 inhibitors (amiodarone, azole antifungals, metronidazole, TMP/SMX

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10
Q

Warfarin (other) interactions

A
  • aspirin, antiplatelets, NSAIDs, increase bleeding

- food containing vitamin K (can inhibit the action of warfarin)

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11
Q

Heparin MOA

A
  • forms complex w/ antithrombin III
  • irreversibly inactivates thrombin (factor IIa) and Xa
  • HELPS PREVENT GROWTH AND EXTENSION OF THE CLOT BUT DOES NOT LYSE THE CLOT
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12
Q

Heparin indications

A

treatment and prevention DVT

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13
Q

Heparin adverse effects

A
  • bleeding (reversed by protamine)
  • Heparin Induced Thrombocytopenia (Type I HIT, Type II HIT; Type II HIT discontinue heparin)
  • hyperkalemia (decreased aldosterone secretion)
  • osteoporosis (long term use)
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14
Q

Heparin-induced thrombocytopenia (HIT-II)

A
  • immune-mediated reaction
  • platelets drop >50% or <100,000cells/mm3
  • usually begins within 5-14 days but can begin immediately
  • this is a HYPERCOAGULABLE STATE
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15
Q

Heparin

A

Parenteral anticoagulant

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16
Q

Enoxaparin MOA

A

inactivates clotting factors

  • binds to antithrombin III (AT-III)
  • LMWH-ATIII complex less affinity for thrombin
  • primarily inactivates factor X
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17
Q

Enoxaparin

A

low molecular weight heparin (LMWH)

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18
Q

Enoxaparin is indicated for everything on the chart except

A

extended treatment for symptomatic VTE (venous thromboembolism) in cancer patients to reduce recurrence

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19
Q

Enoxaparin adverse effects

A
  • spinal/epidural hematomoas

- DO NOT USE IN PATIENTS W/ TYPE II HIT (use a direct thrombin inhibitor such as Lepirudin or Bivalridin)

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20
Q

What is the comparison of UFH w/ LMWHs in regards to efficacy of antidote (protamine sulfate)

A

efficacy is only partial

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21
Q

Fondaparinux

A

parenteral anticoagulant

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22
Q

Fondaparinux MOA

A

indirect Xa inhibitor

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23
Q

Fondaparinux indications

A

prophylaxis of DVT in patients undergoing

  • hip fracture and replacement surgery
  • knee replacement surgery
  • abdominal surgery

treatment of DVT and PE

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24
Q

Main difference between UFH, LMWH and Fondaparinux

A

Fondaparinux = no inactivation of thrombin

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25
Q

Fondaparinux pharmacokinetics

A

contraindicated in sever renal impairment

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26
Q

Fondaparinux adverse effects

A

bleeding - lack of antidote

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27
Q

Rivaroxaban

A

oral anticoagulant

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28
Q

Rivaroxaban MOA

A

oral direct Xa inhibitor

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29
Q

Rivaroxaban indications

A
  • prophylaxis of DVT which may lead to pulmonary embolism in patients undergoing knee or hip replacement surgery
  • treatment of DVT or PE and to reduce risk for recurrences after initial treatment
  • prevention of stroke in AF w/ nonvalvular atrial fibrillation
  • must be adjusted for renal function
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30
Q

Rivaroxaban adverse effects

A

spinal/epidural hematomas

- neuraxial anesthesia or spinal puncture

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31
Q

Rivaroxaban drug interactions

A
  • drugs that inhibit 3A4 and P-gp (erythromycin and clarithromycin)
  • drugs that induce 3A4 and P-gp (rifampin and phenytoin)
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32
Q

Dabigatran

A

oral anticoagulant

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33
Q

Dabigatran MOA

A

direct thrombin inhibitor

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34
Q

Dabigatran indication

A

reduce the risk of stroke and systemic embolism in patients w/ nonvalvular atrial fibrillation

35
Q

Dabigatran pharmacokinetics

A

must be adjusted for renal function

36
Q

Dabigatran adverse effects

A

bleeding and gastritis

37
Q

Apixaban

A

oral anticoagulant

38
Q

Apixaban MOA

A

oral factor Xa (thrombin) inhibitor

39
Q

Apixaban indication

A

reduce the risk of stroke and systemic embolism in patients w/ nonvalvular atrial fibrillation

40
Q

Lepirudin

A

parenteral anticoagulant; hirudin analogue

41
Q

Bivalridin

A

parenteral anticoagulant; hirudin analogue

42
Q

Hirudin analogue MOA

A

direct thrombin inhibitors

  • does not cause HIT
  • administered IV
43
Q

Aspirin effects

A
  • antipyretic
  • analgesic
  • anti-inflammatory
  • antiplatelet
44
Q

Aspirin MOA

A

inhibits thromboxane A2 (TXA2); IRRIVERSIBLY inhibits platelet aggregation for life of platelet

45
Q

Aspirin indications

A

prevent thrombosis in

  • coronary artery disease
  • stroke/TIA (transient ischemic attack)
  • peripheral arterial disease
46
Q

Aspirin adverse effects

A
  • GI bleeding
  • tinnitus
  • Reyes syndrome
47
Q

Aspirin interactions

A
  • warfarin
  • anticoagulants
  • NSAIDs
  • these drugs interact w/ all antiplatelets
48
Q

Dipyridamole

A

antiplatelet

49
Q

Dipyridamole MOA

A

inhibits platelet aggregation

50
Q

Dipyridamole indications

A

used in combination w/ ASA (Aggrenox); indicated for TIAs and stroke

51
Q

Clopidogrel

A

antiplatelet

52
Q

Clopidogrel MOA

A

irreversibly binds to platelet receptors

53
Q

Clopidogrel pharmacokinetics

A

prodrug (metabolized to active drug by 2C19); inhibiting 2C19 may decrease effectiveness

54
Q

Clopidogrel indications

A
  • prevention of MI, strokes/TIA, peripheral arterial disease

- used alone or w/ ASA in ACS (acute coronary syndrome which can be STEMI or NSTEMI)

55
Q

Clopidogrel adverse effects

A
  • bleeding

- thrombotic thrombocytopenic purpura

56
Q

What should be used if a patient is allergic to aspirin?

A

Clopidogrel

57
Q

Prasugrel

A

antiplatelet

58
Q

Prasugrel MOA

A

irreversibly binds to platelet receptors

59
Q

Prasugrel indications

A
  • reduction of thrombotic cardiovascular events (including stent thrombosis) IN PATIENTS W/ ACUTE CORONARY SYNDROME WHO ARE TO BE MANAGED W/ PCI AS FOLLOWS:
  • patients w/ unstable angina or non-ST-elevation myocardial infarction (NSTEMI)
  • patients w/ ST-elevation myocardial infarction (STEMI) when managed w/ either primary or delayed PCI
60
Q

Prasugrel adverse effects

A

bleeding

61
Q

Prasugrel contraindications

A

prior transient ischemic attack or stroke; generally not recommended for patients or are 75 years or older

62
Q

Ticagrelor

A

antiplatelet

63
Q

Ticagrelor MOA

A

REVERSIBLY bind to platelet receptor

64
Q

Ticagrelor indications

A
  • reduce the rate of thrombotic cardiovascular events in patients w/ acute coronary syndrome (ACS) (unstable angina, non-ST elevation myocardial infarction, or ST-elevation myocardial infarction)
  • always used w/ aspirin
65
Q

Ticargrelor contraindications

A
  • history of intracranial hemorrhage

- active pathological bleeding

66
Q

Ticagrelor warnings and precautions

A
  • avoid maintenance doses of aspirin above 100 mg

- dyspnea

67
Q

Ticagrelor adverse effects

A
  • bleeding (12%)

- dyspnea (14%)

68
Q

Ticagrelor drug interactions

A

avoid strong 3A4 inhibitors and inducers

69
Q

Abciximab

A

antiplatelet; glycoprotein IIb/IIIa antagonist

70
Q

Abciximab MOA

A

prevents aggregation by binding to GP IIb/IIIa receptor; prevents fibrinogen binding and cross-linking of platelets

71
Q

Abciximab indications

A

percutaneous coronary interventions

72
Q

Abciximab adverse effects

A
  • bleeding
  • hypotension
  • bradycardia
  • thrombocytopenia
73
Q

Tirofiban

A

antiplatelet; glycoprotein IIb/IIIa antagonist

74
Q

Eptifibatide

A

antiplatelet; glycoprotein IIb/IIIa antagonist

75
Q

Tirofiban and Eptifibatide MOA

A

prevents aggregation by binding to GP IIb/IIIa receptor; prevents fibrinogen binding and cross-linking of platelets

76
Q

Tirofiban and Eptifibatide indications

A
  • percutaneous coronary interventions

- ACS (acute coronary syndrome)

77
Q

Tirofiban and Eptifibatide adverse effects

A

bleeding

78
Q

Alteplase

A

fibrinolytic/thrombolytic

79
Q

Reteplase

A

fibrinolytic/thrombolytic

80
Q

Tenecteplace

A

fibrinolytic/thrombolytic

81
Q

How are fibrinolytic drugs given?

A

given IV

82
Q

Fibrinolytic/thrombolytic MOA

A
  • thrombolytics are enzymes that convert plasminogen to plasmin
  • plasmin degrades fibrin and fibrinogen causing clot dissolution
83
Q

Fibrinolytic/thrombolytic drugs adverse effects

A

hemorrhage

84
Q

Fibrinolytic/thrombolytic drugs interaction

A

increase bleeding associated w/ anticoagulants and antiplatelets

Pharmacology (19 decks)

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