Anticoagulants & Thrombolytics: Antiplatelet Agents Flashcards
Damaged vascular epithelium exposes
collagen and von Willebrand factor
Binding of von Willebrand factor to GP1b receptors activates
platelets
Activated platelet degranulation releases
- ADP
- 5-HT
- TXA2
Platelet degranulation releases ADP, 5-HT, and TXA2, stimulating
platelet aggregation
Adenosine diphosphate (ADP) binds to
the P2-Y12 receptor on platelets causing aggregation
Platelet degranulation releases serotonin, causing
platelet aggregation and vasoconstriction
Platelet degranulation releases TXA2, causing
platelet aggregation and activation as well as vasoconstriction
COX-1 synthesizes
prostanoids (e.g.prostaglandins, TXA2) within platelets
COX-2 expression is induced by
inflammation
COX-1 synthesizes TXA2 from
the precursor molecule arachidonic acid (AA)
Aspirin
- irreversibly acetylates COX-1 and COX2
2. irreversibly inhibits COX-1 and COX-2
Thienopyridines suffix
“-grel”
Thienopyridines are
ADP receptor inhibitors
Thienopyridines include
- Clopidogrel
- Trcagrelor
- Prasugrel
Thienopyridines
irreversibly bind to the P2Y12 ADP receptor preventing platelet aggregation
Aspirin pseudo allergy is due to
excess leukotriene synthesis (use clopidogrel instead)
Antiplatelet agents
reduce cardiovascular events in patients with peripheral artery disease
Antiplatelet agents include
- aspirin
- ADP receptor inhibitors
- Phosphodiesterase inhibitors
Use antiplatelet therapy (e.g. aspirin, ADP receptor inhibitors) in the setting of
MI and other acute coronary syndromes
Give chewable aspirin in setting of
acute MI
Dual antiplatelet therapy (i.e. aspirin and ADP receptor inhibitors) prevents
coronary stent thrombosis
Antiplatelet therapy (i.e. aspirin and ADP receptor inhibitors) prevents
ischemic stroke in patients with atherosclerosis and known cerebrovascular disease
Ticlopidine is an
ADP receptor inhibitor
Ticlopidine can cause
granulocytopenia
Platelet surface receptor GP IIb/IIIa binds
fibrinogen
platelet surface receptor GP IIb/IIIa binds fibrinogen to promote
platelet aggregation
Abciximab function
Abciximab blocks the GP IIb/IIIa receptor preventing platelet aggregation
Abciximab is a
monoclonal IgG antibody
Eptifibatide and Tirofiban block
the GP IIb/IIIa receptor to prevent platelet aggregation
GP IIb/IIIa inhibitors can cause
thrombocytopneia
Antiplatelet therapy increases
bleeding time (measure of platelet function)
GP IIb/IIIa inhibitors include
- abciximab
- eptifibatide
- tirofiban
Phosphodiesterase inhibitors include
- Dipyridamole
2. Cilostazol
Phosphodiesterase inhibitors increase
cAMP
Phosphodiesterase inhibitors increase cAMP impairing
platelet function
Dipyridamole is an
antiplatelet phosphodiesterase inhibitor
Cilostazol is an
antiplatelet phosphodiesterase inhibitor
Cilostazol causes
arterial vasodilation
Cilostazol treats symptoms of
claudication due to peripheral artery disease
Dipyridamole can cause
coronary steal
Cilostazol and dipyridamole can cause
coronary artery vasodilation