Antithrombotics Flashcards

1
Q

what are the 3 categories of antithrombotic drugs?

A
  • antiplatelets
  • anticoagulants
  • fibrinolytics
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2
Q

what do antiplatelets do?

A

prevent thrombus

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3
Q

what do anticoagulants do?

A

Prevent initial thrombus and prevent extension of current thrombus

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4
Q

what do fibrinolytics do?

A

Lyse active thrombus

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5
Q

all antithrombotics have a risk of ____

A

bleeding

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6
Q

antiplatelet drug names to be familiar with

A
  • Aspirin

- clopidogrel (Plavix)

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7
Q

Aspirin MOA

A
  • inhibits COX-1 and COX-2
  • reduces production of thromboxane A2
  • inhibits platelet aggregation
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8
Q

At low doses (81 mg), Aspirin primarily inhibits COX-1 for _____

A

cardiovascular protection

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9
Q

clopidogrel (Plavix) is an ADP receptor inhibitor, also known as ____ or ____

A

thienopyridines; P2Y12 inhibitors

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10
Q

clopidogrel (Plavix) MOA

A
  • prevents ADP from binding to platelet by irreversibly blocking PY12 receptor
  • prevents platelet aggregation for lifespan of platelet (7-10 days)
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11
Q

clopidogrel (Plavix) AEs

A
  • generally well tolerated

- biggest concern is bleeding (monitor symptoms and lab values for Hgb/Hct)

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12
Q

T/F: clopidogrel (Plavix) is a prodrug

A
  • true

- CYP2C19 to active metabolite

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13
Q

boxed warnings for clopidogrel (Plavix)

A

↓ efficacy in some genetic variants that make them CYP2C19 poor metabolizers (present in 50% of Asians, 30% African-Americans, 25% Caucasians)

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14
Q

heparin MOA

A

prevents conversion of fibrinogen to fibrin

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15
Q

heparin tx doses require monitoring of ____ levels

A
  • aPTT

- these levels indicate how long it takes your blood to form a clot

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16
Q

what is the reversal agent for heparin?

A
  • protamine sulfate

- binds heparin so it is inactivated

17
Q

Heparin induced thrombocytopenia (HIT)

A
  • Body creates antibodies which bind to heparin when it is in a complex platelet factor IX
  • this activates platelets
  • clotting and ↓ platelet levels
  • Treat with direct thrombin inhibitors or Factor Xa inhibitors
18
Q

Low-molecular weight heparin (LMWH) MOA

A

prevents conversion of fibrinogen to fibrin

19
Q

why is LMWH preferred over regular heparin?

A

more simple dosing, no monitoring required, ↓ risk HIT

20
Q

LMWH drug to be familiar with

“we love not being hit”

A

enoxaparin (Lovenox)

21
Q

warfarin (Coumadin) MOA

A
  • vitamin K antagonist (VKA)

- depletes vitamin K stores and inhibits synthesis of factors VII, IX, X and II, and protein C and S

22
Q

warfarin reversal agent

23
Q

warfarin usually takes ____ days for full effect

A
  • 3-5

- takes even longer to stabilize dose

24
Q

warfarin is an NTI drug and requires frequent monitoring of ____

A

INR (international normalized ratio)

25
low INR = risk of ____
clot
26
high INR = risk of ____
bleeding
27
PO Direct Thrombin Inhibitor MOA
- binds directly and reversibly to thrombin with high selectivity - inhibits conversion of fibrinogen to fibrin
28
PO Direct Thrombin Inhibitor risks
- Less intracranial bleeding than warfarin but more GI bleeding - Beers List: ↑ risk of GI bleeding in >75 years
29
other AE for PO Direct Thrombin Inhibitor
- dyspepsia (aka indigestion) | - 10%, take with food, improves with time
30
Factor XA Inhibitors MOA
- selectively and reversibly binds FXa | - stops further coagulation cascade
31
Factor XA Inhibitor drug names to know (end in "xaban")
- apixaban (Eliquis) | - rivaroxaban (Xarelto)
32
rivaroxaban is on the Beers List because it has more risk of ____
GI bleed
33
which factor XA inhibitor has lowest bleed risk?
apixaban (Eliquis)
34
All factor XA inhibitors have less ____ than warfarin
- risk of intracranial bleed | - drug interactions
35
andexanet alfa (Andexxa) is a reversal agent for which drugs?
- LMWH | - Factor XA Inhibitors
36
T/F: rivaroxaban must be taken with food
true
37
fibrinolytics MOA
- mimic endogenous tissue plasminogen activator (TPA) which converts plasminogen to plasmin - plasmin breaks fibrin links in the thrombus
38
when are fibrinolytics used?
immediately after stroke, MI, PE