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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
What forms the basis of clot formation
Fibrin
26
What is the simplified explanation of the clotting cascade
Conversion of prothrombin to thrombin which converts fibrinogen to fibrin
27
What fibrinolyzes the clot once the area of injury has stabilized
Plasmin (tPa)
28
What drugs are fibrinolytic
tPa Anistreplase Urokinase Reteplase Alteplase
29
What are P2Y12 ADP receptor inhibitors
Clopidogrel Prasugrel Ticlopidine Ticagrelor
30
GP2B/3A receptor inhibitors
Abcixamab Tirofiban Eptifbatide
31
What are phosphodiesterase inhibitors
Dipyridamole Cilostezol
32
What operations do you discontinue ASA 81typically
Intracranial Intramedullary Posterior eye surgery
33
What is a PPI
proton pump inhibitor -Omeprazole
34
What are the anticoagulation antidotes
Protamine Sulfate Vitamin K Idarucizumab
35
What are direct oral anticoagulant drugs
Thrombin inhibitors -Dabigatran -Argatroban Factor Xa inhibitors -Rivaroxaban -Apixaban -Fonduparinux
36
What is the most significant side effect of unfractionated heparin
HIT Heparin induced thrombocytopenia
37
What are examples of low molecular weight heparin
Enoxaparin Dalteparin Tinzaparin
38
What drugs increase the activity of Warfarin
ASA Heparin Antibiotics
39
What drugs decrease Warfarin activity
Vitamin K: Promote clotting factor synthesis Cholestyramine: reduced absorption Barbituates / phenytoin : Induction of metabolic enzymes
40
What does DOAC stand for
Direct Oral Anti- Coagulants
41
What is Dipyramidole used for
Secondary stroke prevention always combined with ASA
42
What is the MOA of Dipyramidole
Inhibits platelet adenosine deaminase phosphodiesterase which inhibits platelet aggregation and causes vasodilation
43
What are the side effects of Dipyramidole
Bleeding dizziness GI upset rash orthostatic hypotension
44
What is cilostazol used for
Intermittent claudication in legs in PVD
45
What is the MOA of Cilostazol
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
What is the pharmacokinetics of cilostazol
Oral admin takes up to 12 weeks to develop but will reverse quickly in 48hours after drug withdrawal. Metabolized by CYP3A4
47
What are the side effects of cilostazol
HA GI upset *contraindicated in heart failure
48
What is Abciximab used for
Humanized monoclonal antibody preferred GP antagonist used short term to prevent ischemic events in patients with ACS and those undergoing PCI
49
What is the MOA of Abciximab
Binds to platelets around GP 2b/3a receptors and prevents the receptors from binding to fibrinogen
50
What is the pharmacokinetics of Abciximab
IV bolus and then IV infusion peak effect in 30min, persists for 24 hours
51
What are the side effects of Abciximab
bleeding
52
What is eptifibatide and Tirofiban used for
Short term to prevent thrombotic CV events NSTEMI w PCI interchangeable with Tirofiban
53
What is the MOA of eptifibatide and Tirofiban
Selective and reversible inhibition of GP 2b/3a receptors
54
What is unfractioned heparin used for
prevention of thromboembolism esp. when rapid anticoagulant is needed does NOT cross placenta (preferred use in pregnancy) adjunct therapy in acute MI
55
What is the MOA of unfractioned heparin
Binds to and activates antithrombin which inactivates thrombin, factor 9 and factor 10 increases antithrombin activity 1000 fold
56
What is the pharmacokinetics of unfractioned heparin
IV / Sub Q Anticoagulant effects develop w/in a min Dosing adjustment made based on PTT
57
What are side effects for unfractioned heparin
Bleeding hyperkalemia* HIT Osteoporosis
58
What are the contraindications of unfractioned heparin
Pts. with uncontrolled bleeding Thrombocytopenia Surgery of Eye, brain, or spinal cord Avoid with NSAID use
59
When is enoxaparin used (Low molecular weight heparin)
DVT/PE treatment DVT prophylaxis in TKA/THA & abd. surgery safe in pregnancy
60
What in the MOA for enoxaparin
Preferentially inactivate factor 10
61
What are the pharmacokinetics of enoxaparin
Sub Q 1/2t= 4.5-7hours dosing is weight based *also adjust for low creatinine clearance (<30)
62
What are the side effects of enoxaparin
Bleeding (less than heparin) Thrombocytopenia
63
What is the antidote for Enoxaparin
protamine sulfate
64
What is Dalteparin used for
DVT/PE treatment DVT prophylaxis in TKA/THA/abd surgery *used primarily in patients with malignancy
65
What is the MOA of Dalteparin
Preferentially inactivates factor 10
66
What are the pharmacokinetics of Dalteparin
Sub Q 1/2t = 3-5 hours Adjust for low creatinine clearance (<30)
67
What are the side effects of Dalteparin
Bleeding Thrombocytopenia peripheral edema
68
When is Tinzaparin used
DISCONTINUED IN 2011
69
When is Warfarin used
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
What is Warfarin being replaced by as the standard for stroke prevention
DOACs
71
What is the MOA of Warfarin
Inhibits reactivation of vitamin K, which prevents activation of factors 2, 9,10, VII which prevents fibrin clot formation
72
What are the pharmacokinetics of warfarin
Takes 5 days to reach therapeutic level can cross placenta metabolized by CYP Narrow TI INR must be monitored
73
What are the side effects of Warfarin
Bleeding
74
What are the contraindications with warfarin
Pregnancy breastfeeding Thrombocytopenia severe bleeding Vit K deficiency Liver disease alcoholism
75
What is the antidote for Warfarin
Vitamin K
76
What are the DOAC drugs
Dabigatran Argatroban (not actually oral) Apixaban Rivaroxaban
77
When is Dabigatran used
Prevention of stroke and systemic embolism in patients with nonvalvular afib TKA/THA DVT and PE
78
What is the MOA of Dabigatran
Binds to thrombin and inhibits conversion of fibrinogen to fibrin
79
What are the pharmacokinetics of Dabigatran
Oral admin Not highly protein bound, eliminated via kidneys
80
What are the side effects of Dabigatran
Bleeding GI upset D/c can cause rebound thromboses
81
What is the antidote for Dabigatran
Idarucizumab
82
When is Argatroban used
Prophylaxis of thromboses and and treatment of HIT Can be used in PCI
83
What is the MOA of argatroban
Binds to thrombin and inhibits conversion of fibrinogen to fibrin
84
What are the pharmacokinetics of Argatroban
Continuous IV infusion (inpatient only) Treatment monitored by measuring PTT Dose adjust in patients with hepatic impairment
85
What are the side effects of argatroban
Hemorrhage allergic reaction
86
When is apixaban used
DVT/PE prevention after TKA/THA Stroke prevention in non-valvular afib
87
What is the MOA of apixaban
Binds to factor 10 and inhibits the production of thrombin
88
What are the pharmacokinetics of apixaban
Primarily metabolized by CYP3A4 2x/daily
89
What are the side effects of apixaban
Bleeding
90
When is Rivaroxaban used
DVT/PE prevention in non-valvular afib
91
What is the MOA of Rivaroxaban
Binds to factor 10 to inhibit the production of thrombin
92
What are the pharmacokinetics of Rivaroxaban
Rapid onset fixed dose, 1x/daily No INR monitoring
93
What are the side effects of Rivaroxaban
Bleeding (lower than warfarin) Highest bleeding risk of the factor 10 inhibitors Avoid in patients with severe renal impairment unsafe in pregnancy
94
When is fonduparinux used
Prevention of DVT after orthopedic surgery Treatment of DVT/PE Slightly more effective that enoxaprin
95
What is the MOA of fonduparinux
Binds to antithrombin 3 and inhibits factor 10
96
What are the pharmacokinetics of Fonduparinux
Sub Q, fixed dose No lab monitoring Anticoagulation may persist 2-4 days after the last dose
97
What are the side effects of fonduparinux
Slightly higher bleeding risk than enoxaprin Bleeding risk increases with age, renal impairment, and low body weight
98
When is protamine sulfate used
Antidote for heparin and low molecular weight heparin overdose
99
When is Vitamin K used
Antidote for warfarin overdose
100
When is Idarucizumab used
dabigatran OD
101
What is the MOA of protamine sulfate
Multiple positively charged groups bond ionically with negative groups on heparin to devoid anticoagulant activity
102
What are the pharmacokinetics of protamine sulfate
Admin by slow IV Neutralization of heparin happens immediately and will last 2 hours
103
What is the MOA of vitamin K
Antagonizes warfarins actions and can thereby reverse the warfarin induced inhibition of clotting synthesis
104
What is the MOA of Idarucizumab
Monoclonal antibody fragment that binds to dabigatran
105
What is the pharmacokinetics of Vitamin K
Small oral doses
106
What is the pharmacokinetics of Idarucizumab
IV admin

Pharm term 2 module 1 (3 decks)

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