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

Exam 6 - Anticoagulant, Antiplatelet, and Fibrinolytic Drugs Flashcards

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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
Fondaparinux pharmacokinetics
contraindicated in sever renal impairment
26
Fondaparinux adverse effects
bleeding - lack of antidote
27
Rivaroxaban
oral anticoagulant
28
Rivaroxaban MOA
oral direct Xa inhibitor
29
Rivaroxaban indications
- 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
30
Rivaroxaban adverse effects
spinal/epidural hematomas | - neuraxial anesthesia or spinal puncture
31
Rivaroxaban drug interactions
- drugs that inhibit 3A4 and P-gp (erythromycin and clarithromycin) - drugs that induce 3A4 and P-gp (rifampin and phenytoin)
32
Dabigatran
oral anticoagulant
33
Dabigatran MOA
direct thrombin inhibitor
34
Dabigatran indication
reduce the risk of stroke and systemic embolism in patients w/ nonvalvular atrial fibrillation
35
Dabigatran pharmacokinetics
must be adjusted for renal function
36
Dabigatran adverse effects
bleeding and gastritis
37
Apixaban
oral anticoagulant
38
Apixaban MOA
oral factor Xa (thrombin) inhibitor
39
Apixaban indication
reduce the risk of stroke and systemic embolism in patients w/ nonvalvular atrial fibrillation
40
Lepirudin
parenteral anticoagulant; hirudin analogue
41
Bivalridin
parenteral anticoagulant; hirudin analogue
42
Hirudin analogue MOA
direct thrombin inhibitors - does not cause HIT - administered IV
43
Aspirin effects
- antipyretic - analgesic - anti-inflammatory - antiplatelet
44
Aspirin MOA
inhibits thromboxane A2 (TXA2); IRRIVERSIBLY inhibits platelet aggregation for life of platelet
45
Aspirin indications
prevent thrombosis in - coronary artery disease - stroke/TIA (transient ischemic attack) - peripheral arterial disease
46
Aspirin adverse effects
- GI bleeding - tinnitus - Reyes syndrome
47
Aspirin interactions
- warfarin - anticoagulants - NSAIDs * these drugs interact w/ all antiplatelets
48
Dipyridamole
antiplatelet
49
Dipyridamole MOA
inhibits platelet aggregation
50
Dipyridamole indications
used in combination w/ ASA (Aggrenox); indicated for TIAs and stroke
51
Clopidogrel
antiplatelet
52
Clopidogrel MOA
irreversibly binds to platelet receptors
53
Clopidogrel pharmacokinetics
prodrug (metabolized to active drug by 2C19); inhibiting 2C19 may decrease effectiveness
54
Clopidogrel indications
- 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
Clopidogrel adverse effects
- bleeding | - thrombotic thrombocytopenic purpura
56
What should be used if a patient is allergic to aspirin?
Clopidogrel
57
Prasugrel
antiplatelet
58
Prasugrel MOA
irreversibly binds to platelet receptors
59
Prasugrel indications
- 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
Prasugrel adverse effects
bleeding
61
Prasugrel contraindications
prior transient ischemic attack or stroke; generally not recommended for patients or are 75 years or older
62
Ticagrelor
antiplatelet
63
Ticagrelor MOA
REVERSIBLY bind to platelet receptor
64
Ticagrelor indications
- 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
Ticargrelor contraindications
- history of intracranial hemorrhage | - active pathological bleeding
66
Ticagrelor warnings and precautions
- avoid maintenance doses of aspirin above 100 mg | - dyspnea
67
Ticagrelor adverse effects
- bleeding (12%) | - dyspnea (14%)
68
Ticagrelor drug interactions
avoid strong 3A4 inhibitors and inducers
69
Abciximab
antiplatelet; glycoprotein IIb/IIIa antagonist
70
Abciximab MOA
prevents aggregation by binding to GP IIb/IIIa receptor; prevents fibrinogen binding and cross-linking of platelets
71
Abciximab indications
percutaneous coronary interventions
72
Abciximab adverse effects
- bleeding - hypotension - bradycardia - thrombocytopenia
73
Tirofiban
antiplatelet; glycoprotein IIb/IIIa antagonist
74
Eptifibatide
antiplatelet; glycoprotein IIb/IIIa antagonist
75
Tirofiban and Eptifibatide MOA
prevents aggregation by binding to GP IIb/IIIa receptor; prevents fibrinogen binding and cross-linking of platelets
76
Tirofiban and Eptifibatide indications
- percutaneous coronary interventions | - ACS (acute coronary syndrome)
77
Tirofiban and Eptifibatide adverse effects
bleeding
78
Alteplase
fibrinolytic/thrombolytic
79
Reteplase
fibrinolytic/thrombolytic
80
Tenecteplace
fibrinolytic/thrombolytic
81
How are fibrinolytic drugs given?
given IV
82
Fibrinolytic/thrombolytic MOA
- thrombolytics are enzymes that convert plasminogen to plasmin - plasmin degrades fibrin and fibrinogen causing clot dissolution
83
Fibrinolytic/thrombolytic drugs adverse effects
hemorrhage
84
Fibrinolytic/thrombolytic drugs interaction
increase bleeding associated w/ anticoagulants and antiplatelets

Pharmacology (19 decks)

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