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What are the prototype anticoagulant drugs?
- Warfarin Sodium (coumadin)
- Heparin (unfractionated)
- Enoxaparin (lovenox)
- Direct Thrombin inhibitors
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What are the prototype Thrombolytic drugs?
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What are the prototype Antiplatelet drugs?
- Aspirin
- Clopidogrel (plavex)
- Abeiximab (ReoPro)
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Describe how ANTICOAGS work:
Block caog cascade, prevent formation of venous thrombosis
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Describe how ANTIPLATELETS work:
block platelet aggregation, prevent formation of arterial thrombus
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Describe how THROMBOLYTICS work:
dissolution of existing thrombus
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Warfarin inhibits Vit ___ dependent __ _________, leading to a ______ in circulating levels of mature, active clotting factors.
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What inhibits active clotting factors, specifically Xa and thrombin (IIa)?
- heparin (Low MW- enoxaparin- less active against thrombin than Xa)
- antithrombin III (endogenous)
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What drugs act to directly target active, catalytic or substrate-binding site of active thrombin?
Lepirudin, argatroban, ximelagatran.
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Aspirin inihibits _________ irreversibly. This also blocks synthesis of TXA2 and _________.
- cyclo-oxygenase
- prostacyclin (PGT)
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Aspirin has greater effect on platelets than ___________, lowering the ration to inihbit __________ _____________.
- endothelium
- platelet aggregation
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How does Clopidogrel work? Is this a pro-drug?
- Irreversibly modifies platelet ADP receptor and impairs ADP-mediated activation of glycoproetin II/III receptor expression.
- YES
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Abeiximab (IV) mode of action?
PRevents fibrinogen binding to glycoprotein II/III receptors.
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What are the Therapeutic uses of antiplatelet drugs in art thromboembolitic disorders?
- prevent transient ischemic attacks and cerebral vasc thrombosis
- tx angina pectoris
- prophylaxis of myocardial infarctions
- prevention of acute arterial re-occlusion after vasc surgery
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Adverse effects of antiplt drugs
prolonged bleeding time, risk of hemorrhage.
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Adverse fx of ABEIXIMAB
allergic response
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adverse fx of CLOPIDOGREL
thrombotic thrombocytopenic purpura
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What is the mech of action of thrombolytic drugs?
Convert plasminogen ot plasmin, leading to clot dissolution
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streptokinase is a _________ drug. It is a non-________ plasminogen activator, forms autocatalytic proactivator with plasminogen. ______ clot selective. Can cause _______ response. relatively __________.
- thrombolytic
- enzymatic
- NOT
- allergic
- inexpensive
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Alteplase is a __________ drug. it is a _________ human tissue plasminogen activator. binds to fibrin, kinetcially activating nearby plasminogen. clot _________. ____________.
- thrombolytic
- recombinant
- selective
- EXPENSIVE
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Theraputic uses of thrombolytics
- emergency MI- heparin
- emergency DVT or PE
- emergenc AIS
- reverse occlusion of cannulas/ catheters
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adverse fx of thrombolytics
hemorrhage- used only in hospital settings.
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contraindications of thromboembolytics
- healing wounds or internal bleeding
- history of CA
- clotting disorders
- severe HTN
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how to treat an overdose of thromboembolytics
aminocaproic acid- competitive inhibitor that prevents plasminogen and t-PA from binding fibrin and inhibits thrombolysis.
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