Antiplatelets, Anticoagulants & Thrombolysis Flashcards
What is the difference between a venous thrombus and an arterial thrombus.
Venous - ‘red’ - RBC and fibrin rich, platelet low.
Arterial - ‘white’ - platelet rich, fibrin low.
How does treatment differ for arterial and venous thrombosis?
Arterial - use antiplatelets and fibrinolytic drugs.
Venous - use anticoagulants.
Describe the production of prostaglandins and thromboxanes.
Tissue damage during the inflammatory process produces phospholipase A2, which converts phospholipids in the membrane into arachidonic acid. Oxidation of arachidonic acid by COX enzymes produces eicosanoids such as thromboxanes, prostaglandins and leukotrienes.
What is the rate limiting enzyme in the eicosanoid generation?
Phospholipase A2.
How is thromboxane A2 formed and what are its effects?
Formed by COX-1
Causes vasoconstriction and promotes platelet aggregation
How is PGI-2 produced and what are its effects?
Produced by COX-2
Causes vasodilation and inhibits platelet aggregation
Name 3 COX-1 selective inhibitors.
Aspirin
Ibuprofen
Naproxen
What is the MOA of COX-1 inhibitors.
Inhibit COX-1 enzyme, reducing TXA2 synthesis, therefore inhibits platelet aggregation.
What is the MOA of COX-2 inhibitors?
Inhibit COX-2 enzymes, reducing PGI2 synthesis, which promotes platelet aggregation.
Name a COX-2 selective inhibitor.
Celecoxib
Name a non-selective COX inhibitor.
Diclofenac
State a side effect of aspirin.
Prolonged bleeding time due to reduced TXA 2 synthesis and reduced platelet aggregation.
What are P2Y12 inhibitors used for? What is their MOA?
Antiplatelet agents
Inhibit binding of ADP to P2Y12 receptors, inhibits activation of GPIIb/IIIa receptors.
What drug class are clopidogrel and ticagrelor?
P2Y12 receptor antagonists, both are prodrugs.
What are Glycoprotein IIb/IIIa inhibitors used for? What is their MOA?
Antiplatelet agents
Antibody irreversibly blocks receptor, preventing fibrinogen binding to IIb/IIIa receptors on platelets, reduces platelet aggregation.
Name a GIIb/IIIa inhibitor.
Abciximab.