Antithrombotics Flashcards
Aspirin MOA
COX inhibitor, inhibits thromboxane synthesis
Aspirin indication
primary/secondary prevention
and acute coronary syndromes, PCI, recurrent stroke
ADP Receptor Blocker MOA
prevent platelet aggregation; these are PRODRUGS
ADP examples
irreversible=grel: clopidogrel, prasugrel
Reversible: Ticagrelor +aspirin
ADP Use
Irreversibles:
Clopidigril :w aspirin during/after PCI or alone if aspirin isn’t tolerated
Prasugrel: PCI related thrombosis
Reversible: Ticagrelor w Aspirin for thombotic events with ACS or MI/ST elevation
G2b3a inhibitors MOA
Bind GP IIb/IIIa – prevent fibrinogen binding and subsequent crosslinking of platelets
G2b3a inhibitors examples
A: abciximab (irreversible)
T: tirofiban
E: eptifibatide
G2b3a inhibitors indication
efficacious antiplatelets
G2b3a inhibitors warnings
Thrombocytopenia
Heparin MOA
heparin/enoxaparin
enhances antithrombin 3
Heparin adverse effects
bleeding
HIT
Thombocytopenia
Heparin indication
• Prophylaxis: DVTs and PE
• Thromboembolic events. related to unstable angina, MI, AF
• Acute DVT & PE
Acute Coronary Syndrome (+ antiplatelet)
F10a inhibitors examples
rivaroxABAN (xarelto)
apixABAN
F10a indication
-ABAN
Prophylaxis: DVT, PE
Stroke prevention with non-valvular A-fib
F10a MOA
-ABAN
Inhibits free & clot-bound Xa
**no antidote to bleeding
F10a interactions
CYP3A4, PGP
Renal elimination
Parenteral direct thrombin inhibitors MOA
Inhibit Thrombin(IIa) (thus preventing fibrinogenfibrin)
Parenteral direct thrombin inhibitors examples
BivallRUDIN
agatroban
lepiRUDIN
Parenteral direct thrombin inhibitors INDICATION
Lepirudin & Argatroban: Thrombosis due to heparin induced thrombocytopenia (HIT)
Bivalirudin: combine with antiplatelet having PCI
Direct thrombin inhibitor MOA
Dabigantran
Prodrughydrolyzed to dabigatran and conjugated to acyl glucoronides (both are active)
DIrect Thrombin inhibitor INDICATION
Dabigatran
Non-valvular A-fib assoc. stroke and embolism
Warfarin MOA
Thrombin synthesis inhibitor
Inhibits Vit. K Reductase
Factors II, VII, IX, X & Proteins C & S aren’t regenerated
Warfarin indication
Primary Prevention: DVT & PE
Only approved drug in patients with prosthetic valves
Secondary: Acute DVT & PE. Combine with heparin for fast onset, warfarin kicks in later
Warfarin metabolism
40 hr half-life, binds plasma albumin
Metabolized by 3 enzymes:
CYP2C9, 3A4, 1A2
Many potential interactions leading to bleeding
Slow onset of action, often combined with faster-acting heparin
warfarin side effects
bleeding, birth defects, do not use in pregnancy!
Fibrinolytics- examples
-PLASE
alteplase
reteplase
tenectplase
streptokinase
Fibrinolytics indication
-PLASE
activates plasminogen
opens clotted vessels
- Acute MI, especially if PCI unavailable
- PE, DVT
- Stroke
Fibrinolytics AE
renal failure
-PLASE
fibrinolytics
-ABAN
F10a inhibitors
-GREL
ADP receptor blockers
Heparin antidote
protamine sulfate
Partially reverses LMWH effects but has no effect on fondaparinux
warfarin antidote
vitamin K,
fresh frozen plasma,
prothrombin complex concentrates,
rFVIIa