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Pharm term 2 module 1 > Antiplatelets & anticoagulants > Flashcards

Antiplatelets & anticoagulants Flashcards

1
Q

What is Aspirin used for

A

Primary prevention of ischemic stroke, TIA, angina, coronary stenting, MI

Clot risk reduction in TKA/THA

DAPT w/ clopidogrel after CABG, PCI, TIA, stroke

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2
Q

What is the mechanism of action for Aspirin

A

Irreversible inhibition of COX-1-> an enzyme required by platelets to synthesize TXA2

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3
Q

What are the pharmacokinetics of Aspirin

A

Oral admin

Rapidly hydrolyzed by liver, excreted by kidneys

effects last for lifetime of platelets

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4
Q

What are the contraindications of Aspirin

A

GI bleeding
Hemorrhagic stroke
Tinnitus
*consider using PPI w/ ASA for GI bleeding

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5
Q

When is Clopidogrel used

A

First line anti platelet therapy

Prevents further atherosclerotic events in MI, ACS, PAD, coronary angioplasty, unstable angina

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6
Q

What is the MOA for clopidogrel

A

Irreversibly blocks P2Y12 ADP receptor on platelet surface

Decrease ADP-stimulated aggregation

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7
Q

What are the pharmacokinetics of Clopidogrel

A

Oral admin
Prodrug that undergoes hepatic CYP metabolism for active form

Reduced effectiveness in patients who are poor metabolizers

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8
Q

What are the contraindications / side effects of clopidogrel

A

Abdominal pain
dyspepsia
Diarrhea
Rash
Thrombotic thrombocytopenia purpura
*use with caution in drugs like omeprazole

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9
Q

What is Ticagrelor used for

A

Secondary prevention of atherothrombotic events in patients with ACS

*used instead of clopidogrel in patients who are poor metabolizers

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10
Q

What is the MOA of Ticagrelor

A

Reversibly blocks P2Y12 ADP receptors on platelet surface

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11
Q

What is the pharmacokinetics for ticagrelor

A

Oral admin
rapid onset (1-3 hours)
Has loading dose

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12
Q

What are the side effects. / contraindications of ticagrelor

A

Bleeding
abdominal pain
dyspepsia
diarrhea
rash

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13
Q

What is prasugrel used for

A

ACS
Secondary prevention of MI
Use with aspirin
*not routinely used

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14
Q

What is the MOA of pasugrel

A

Irreversibly blocks P2Y12 ADP receptors on platelet surface
*decrease platelet aggregation

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15
Q

What are the pharmacokinetics of Pasugrel

A

Oral admin
Effects last for lifetime of platelets

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16
Q

What are the side effects of pasugrel

A

Bleeding
abdominal pain
dyspepsia
diarrhea
rash

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17
Q

What is ticlopidine used for

A

TIA
Pts. with hx of stroke
*DISCONTINUED IN 2015

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18
Q

What is the MOA of ticlopidine

A

Blocks P2Y12 ADP receptors on platelet surface-> decrease aggregation

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19
Q

What are the side effects of Ticlopidine

A

Thrombocytopenia
agranulocytosis
TTP

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20
Q

How often does a CBC need to be done while on Ticlopidine

A

Every 2 weeks for 4 months

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21
Q

What is the primary indication for antiplatelet agents

A

Prevention of thrombosis in arteries

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22
Q

What is DAPT

A

Dual anti platelet therapy

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23
Q

What is ACS

A

Acute coronary syndrome
*blood supplied to the heart is suddenly blocked (MI)

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24
Q

What is Virchow’s Triad

A

Stasis
Defects in hemostatic mechanism
Endothelial injury

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25
Q

What forms the basis of clot formation

A

Fibrin

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26
Q

What is the simplified explanation of the clotting cascade

A

Conversion of prothrombin to thrombin which converts fibrinogen to fibrin

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27
Q

What fibrinolyzes the clot once the area of injury has stabilized

A

Plasmin (tPa)

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28
Q

What drugs are fibrinolytic

A

tPa
Anistreplase
Urokinase
Reteplase
Alteplase

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29
Q

What are P2Y12 ADP receptor inhibitors

A

Clopidogrel
Prasugrel
Ticlopidine
Ticagrelor

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30
Q

GP2B/3A receptor inhibitors

A

Abcixamab
Tirofiban
Eptifbatide

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31
Q

What are phosphodiesterase inhibitors

A

Dipyridamole
Cilostezol

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32
Q

What operations do you discontinue ASA 81typically

A

Intracranial
Intramedullary
Posterior eye surgery

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33
Q

What is a PPI

A

proton pump inhibitor
-Omeprazole

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34
Q

What are the anticoagulation antidotes

A

Protamine Sulfate
Vitamin K
Idarucizumab

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35
Q

What are direct oral anticoagulant drugs

A

Thrombin inhibitors
-Dabigatran
-Argatroban

Factor Xa inhibitors
-Rivaroxaban
-Apixaban
-Fonduparinux

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36
Q

What is the most significant side effect of unfractionated heparin

A

HIT
Heparin induced thrombocytopenia

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37
Q

What are examples of low molecular weight heparin

A

Enoxaparin
Dalteparin
Tinzaparin

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38
Q

What drugs increase the activity of Warfarin

A

ASA
Heparin
Antibiotics

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39
Q

What drugs decrease Warfarin activity

A

Vitamin K: Promote clotting factor synthesis

Cholestyramine: reduced absorption

Barbituates / phenytoin : Induction of metabolic enzymes

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40
Q

What does DOAC stand for

A

Direct
Oral
Anti-
Coagulants

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41
Q

What is Dipyramidole used for

A

Secondary stroke prevention

always combined with ASA

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42
Q

What is the MOA of Dipyramidole

A

Inhibits platelet adenosine deaminase phosphodiesterase which inhibits platelet aggregation and causes vasodilation

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43
Q

What are the side effects of Dipyramidole

A

Bleeding
dizziness
GI upset
rash
orthostatic hypotension

44
Q

What is cilostazol used for

A

Intermittent claudication in legs in PVD

45
Q

What is the MOA of Cilostazol

A

Binds to phosphodiesterase so cAMP cannot be broken down.

cAMP levels increase which inhibits platelet aggregation and causes vasodilation.

Increase HDL cholesterol and decrease TG

46
Q

What is the pharmacokinetics of cilostazol

A

Oral admin

takes up to 12 weeks to develop but will reverse quickly in 48hours after drug withdrawal.

Metabolized by CYP3A4

47
Q

What are the side effects of cilostazol

A

HA
GI upset
*contraindicated in heart failure

48
Q

What is Abciximab used for

A

Humanized monoclonal antibody

preferred GP antagonist

used short term to prevent ischemic events in patients with ACS and those undergoing PCI

49
Q

What is the MOA of Abciximab

A

Binds to platelets around GP 2b/3a receptors and prevents the receptors from binding to fibrinogen

50
Q

What is the pharmacokinetics of Abciximab

A

IV bolus and then IV infusion

peak effect in 30min, persists for 24 hours

51
Q

What are the side effects of Abciximab

A

bleeding

52
Q

What is eptifibatide and Tirofiban used for

A

Short term to prevent thrombotic CV events

NSTEMI w PCI

interchangeable with Tirofiban

53
Q

What is the MOA of eptifibatide and Tirofiban

A

Selective and reversible inhibition of GP 2b/3a receptors

54
Q

What is unfractioned heparin used for

A

prevention of thromboembolism esp. when rapid anticoagulant is needed

does NOT cross placenta (preferred use in pregnancy)

adjunct therapy in acute MI

55
Q

What is the MOA of unfractioned heparin

A

Binds to and activates antithrombin which inactivates thrombin, factor 9 and factor 10

increases antithrombin activity 1000 fold

56
Q

What is the pharmacokinetics of unfractioned heparin

A

IV / Sub Q
Anticoagulant effects develop w/in a min

Dosing adjustment made based on PTT

57
Q

What are side effects for unfractioned heparin

A

Bleeding
hyperkalemia*
HIT
Osteoporosis

58
Q

What are the contraindications of unfractioned heparin

A

Pts. with uncontrolled bleeding
Thrombocytopenia
Surgery of Eye, brain, or spinal cord
Avoid with NSAID use

59
Q

When is enoxaparin used (Low molecular weight heparin)

A

DVT/PE treatment
DVT prophylaxis in TKA/THA & abd. surgery
safe in pregnancy

60
Q

What in the MOA for enoxaparin

A

Preferentially inactivate factor 10

61
Q

What are the pharmacokinetics of enoxaparin

A

Sub Q
1/2t= 4.5-7hours
dosing is weight based
*also adjust for low creatinine clearance (<30)

62
Q

What are the side effects of enoxaparin

A

Bleeding (less than heparin)
Thrombocytopenia

63
Q

What is the antidote for Enoxaparin

A

protamine sulfate

64
Q

What is Dalteparin used for

A

DVT/PE treatment
DVT prophylaxis in TKA/THA/abd surgery
*used primarily in patients with malignancy

65
Q

What is the MOA of Dalteparin

A

Preferentially inactivates factor 10

66
Q

What are the pharmacokinetics of Dalteparin

A

Sub Q
1/2t = 3-5 hours
Adjust for low creatinine clearance (<30)

67
Q

What are the side effects of Dalteparin

A

Bleeding
Thrombocytopenia
peripheral edema

68
Q

When is Tinzaparin used

A

DISCONTINUED IN 2011

69
Q

When is Warfarin used

A

To prevent thrombosis but is inappropriate in emergencies (use for long term prophylaxis)

Standard prevention in strokes

*INR needs to be higher in those with a mechanical valve

70
Q

What is Warfarin being replaced by as the standard for stroke prevention

A

DOACs

71
Q

What is the MOA of Warfarin

A

Inhibits reactivation of vitamin K, which prevents activation of factors 2, 9,10, VII which prevents fibrin clot formation

72
Q

What are the pharmacokinetics of warfarin

A

Takes 5 days to reach therapeutic level

can cross placenta

metabolized by CYP

Narrow TI

INR must be monitored

73
Q

What are the side effects of Warfarin

A

Bleeding

74
Q

What are the contraindications with warfarin

A

Pregnancy
breastfeeding
Thrombocytopenia
severe bleeding
Vit K deficiency
Liver disease
alcoholism

75
Q

What is the antidote for Warfarin

A

Vitamin K

76
Q

What are the DOAC drugs

A

Dabigatran
Argatroban (not actually oral)
Apixaban
Rivaroxaban

77
Q

When is Dabigatran used

A

Prevention of stroke and systemic embolism in patients with nonvalvular afib

TKA/THA DVT and PE

78
Q

What is the MOA of Dabigatran

A

Binds to thrombin and inhibits conversion of fibrinogen to fibrin

79
Q

What are the pharmacokinetics of Dabigatran

A

Oral admin

Not highly protein bound, eliminated via kidneys

80
Q

What are the side effects of Dabigatran

A

Bleeding
GI upset
D/c can cause rebound thromboses

81
Q

What is the antidote for Dabigatran

A

Idarucizumab

82
Q

When is Argatroban used

A

Prophylaxis of thromboses and and treatment of HIT

Can be used in PCI

83
Q

What is the MOA of argatroban

A

Binds to thrombin and inhibits conversion of fibrinogen to fibrin

84
Q

What are the pharmacokinetics of Argatroban

A

Continuous IV infusion (inpatient only)

Treatment monitored by measuring PTT

Dose adjust in patients with hepatic impairment

85
Q

What are the side effects of argatroban

A

Hemorrhage
allergic reaction

86
Q

When is apixaban used

A

DVT/PE prevention after TKA/THA

Stroke prevention in non-valvular afib

87
Q

What is the MOA of apixaban

A

Binds to factor 10 and inhibits the production of thrombin

88
Q

What are the pharmacokinetics of apixaban

A

Primarily metabolized by CYP3A4

2x/daily

89
Q

What are the side effects of apixaban

A

Bleeding

90
Q

When is Rivaroxaban used

A

DVT/PE prevention in non-valvular afib

91
Q

What is the MOA of Rivaroxaban

A

Binds to factor 10 to inhibit the production of thrombin

92
Q

What are the pharmacokinetics of Rivaroxaban

A

Rapid onset
fixed dose, 1x/daily
No INR monitoring

93
Q

What are the side effects of Rivaroxaban

A

Bleeding (lower than warfarin)
Highest bleeding risk of the factor 10 inhibitors

Avoid in patients with severe renal impairment

unsafe in pregnancy

94
Q

When is fonduparinux used

A

Prevention of DVT after orthopedic surgery

Treatment of DVT/PE

Slightly more effective that enoxaprin

95
Q

What is the MOA of fonduparinux

A

Binds to antithrombin 3 and inhibits factor 10

96
Q

What are the pharmacokinetics of Fonduparinux

A

Sub Q, fixed dose
No lab monitoring
Anticoagulation may persist 2-4 days after the last dose

97
Q

What are the side effects of fonduparinux

A

Slightly higher bleeding risk than enoxaprin

Bleeding risk increases with age, renal impairment, and low body weight

98
Q

When is protamine sulfate used

A

Antidote for heparin and low molecular weight heparin overdose

99
Q

When is Vitamin K used

A

Antidote for warfarin overdose

100
Q

When is Idarucizumab used

A

dabigatran OD

101
Q

What is the MOA of protamine sulfate

A

Multiple positively charged groups bond ionically with negative groups on heparin to devoid anticoagulant activity

102
Q

What are the pharmacokinetics of protamine sulfate

A

Admin by slow IV

Neutralization of heparin happens immediately and will last 2 hours

103
Q

What is the MOA of vitamin K

A

Antagonizes warfarins actions and can thereby reverse the warfarin induced inhibition of clotting synthesis

104
Q

What is the MOA of Idarucizumab

A

Monoclonal antibody fragment that binds to dabigatran

105
Q

What is the pharmacokinetics of Vitamin K

A

Small oral doses

106
Q

What is the pharmacokinetics of Idarucizumab

A

IV admin

Pharm term 2 module 1 (3 decks)

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