Anticoagulants and Antiplatelet agents

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anhpham
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227545
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Anticoagulants and Antiplatelet agents
Updated:
2013-07-27 18:23:04
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Anticoagulants Antiplatelet agents
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Brand names, generic names, Class, mechanism, and indications
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  1. Heparin
    Heparin

    IV

    Unfractionated heparin

    Binds antithrombin III with pentasaccharide chain. Antitrombin III bnds thrombin and Factor Xa (slowly), inhiboiting clotting.


    Initial treatment of:

    • Venous thrombosis
    • Pulmonary embolism
    • Unstable angina
    • Acute MI

    • During and after coronary angioplasty or stent replacement
    • During surgery requiring cardiopulmonary bypass
    • Disseminated intravascular coagulation (DIC)
    • Prevention of venous thromboembolism






    —
  2. —Normiflo

    Ardeparin

    SQ

    • Low-Molecular weight heparin
    • Similar to heparin
    • Less activity on thrombin

    • Prophylaxis and treatment of DVT
    • ACS (Unstable angina, non-ST-segment MI, ST-elevation MI)

  3. Fragmin
    Dalteparin

    SQ

    • Low-Molecular weight heparin
    • Similar to heparin
    • Less activity on thrombin
    • Prophylaxis and treatment of DVT
    • ACS (Unstable angina, non-ST-segment MI, ST-elevation MI)
  4. Lovenox
    Enoxaparin

    SQ

    • Low-Molecular weight heparin
    • Similar to heparin
    • Less activity on thrombin
    • Prophylaxis and treatment of DVT
    • ACS (Unstable angina, non-ST-segment MI, ST-elevation MI)
  5. Orgaran
    Danaparoid

    SQ

    • Low-Molecular weight heparin
    • Similar to heparin
    • Less activity on thrombin
    • Prophylaxis and treatment of DVT
    • ACS (Unstable angina, non-ST-segment MI, ST-elevation MI)
  6. Coumadin, Jantoven
    Warfarin

    Oral

    Class: Coumarin

    • Mechanism:
    • Vitamin K is used in the synthesis of clotting factors VII, IX, X, and prothrombin.  The structure of warfarin is very similar to the structure of Vitamin K.  When the liver tries to use warfarin instead of Vitamin K to produce clotting factors, abnormal clotting factors are formed

    • Indication:
    • Prophylaxis and treatment of thromboembolic disorders and embolic complications from atrial fibrillation or heart valve replacement
    • To reduce the risk of stroke or subsequent MI after MI.


  7. Pradaxa
    Dabigtran

    • Class:
    • Direct thrombin inhibitor

    Oral


    • Mechanism:
    • Reversible thrombin inhibitor that prevents platelet aggregation and clot formation.

    • Indication:
    • Prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation.

  8. Arixtra
    Fondaparinux

    IV

    Class: Factor Xa Inhibitors

    Mechanism:

    • Inhibits platelet activation and fibrin clot formation via inhibition of factor Xa.  These drugs prevent the conversion of prothrombin to thrombin and thus
    • prevent clot formation

    • Indication:
    • Prevention of DVT in patients undergoing hip or knee replacement surgery or abdominal surgery.
    • Treatment of acute pulmonary embolism

  9. Xarelto
    Rivaroxaban

    Oral

    Class: Factor Xa Inhibitors

    Mechanism:

    • Inhibits platelet activation and fibrin clot formation via inhibition of factor Xa.  These drugs prevent the conversion of prothrombin to thrombin and thus
    • prevent clot formation

    • Indication:
    • Prevention of DVT in patients undergoing hip or knee replacement surgery or abdominal surgery.
    • Treatment of acute pulmonary embolism
  10. Normiflo
    Ardeparin

    SQ

    • Low-Molecular weight heparin
    • Similar to heparin
    • Less activity on thrombin
    • Prophylaxis and treatment of DVT
    • ACS (Unstable angina, non-ST-segment MI, ST-elevation MI)

  11. Anticoagulants
    • Indirect Thrombin Inhibitors
    • Unfractionated Heparin (UFH)
    • Low-molecular-weight Heparin (LMWH)
    • Fondaparinux
    • Danaparoid
    • Direct Thrombin Inhibitors
    • Lepirudin
    • Bivalirudin
    • Argatroban
    • Warfarin
  12. Innohep
    Tinzaparin

    Low Molecular weight heparin

    Concern with this drug in patients with renal insufficiency
  13. Antidote for Heparin overdose
    Protamine sulfate


    • —Antagonist of heparin activity: binds free heparin prevents binding with thrombin
    • —Protein high in arginines (Protamine Sulfate is positively charged while Heparin is negative)
  14. Lepirudin
    Refludan

    Direct thrombin inhibitors

    Product is discontinued after May 31, 2012
  15. Angiomax
    Bivalirudin

    IV

    Direct thrombin inhibitor

    Percutaneous coronary intervention- thrombosis; prophylaxis

    Percutaneous transluminal coronary angioplasty- Thromboembolic disorder; Prophylaxis-Unstable angina
  16. Argatroban
    Argatroban

    IV

    Direct thrombin inhibitor

    • Indications:
    • Coronary artery thrombosis, in patients with or at risk for heparin-induced thrombocyopenia
    • Prophylaxis- Percutaneous coronary intervention
  17. Warfarin toxicity
    • Bleeding
    • Less than 5% if INR is 2-3
    • Risk of intracranial hemorrhage increases dramatically with INR >4
    • Patient education
    • Laboratory monitoring
    • In cases INR 5 or above – vitamin K1 can be given
    • In cases of severe bleeding or overdose (INR >20) – concentrated clotting factors can be given (FFP)
    • Administration during pregnancy can lead to birth defects and abortion
    • Do not use oral anticoagulants – use heparin if anticoagulation is needed during pregnancy
    • Skin necrosis – rare
    • Skin lesions appear 3-5 days after initiation of treatment
    • Reversible, painful, blue-tinge discoloration of bottoms and sides of toes – due to cholesterol emboli released from plaques
    • Precipitates instances of venous limb gangrene and multicentric skin necrosis in HIT patients
  18. Clinical uses of warfarin
    • Prevent the progression or reoccurrence of acute DVT or pulmonary embolism
    • The oral anticoagulants follow an initial course of heparin
    • Prevention of venous thromboembolism in patients undergoing orthopedic or gynecological surgery
    • Prevention of systemic embolization in patients with acute MI, prosthetic heart valves, or chronic atrial fibrillation
  19. Fibrinolytics/Thrombolytics
    • Tissue plasminogen activators (t-PAs)
    • Streptokinase
    • Urokinase
    • Alteplase
    • Reteplase
    • Tenecteplase
  20. Streptase
    Streptokinase

    First generation

    tPA (Rissue Plasminogen Activator)

    • Mechanism:
    • Binding to plasminogen, then producing a complex that possesses activator properties and accelerates the further transforomation of plasminogen into the proteolytic and fibrinolytic plasmin

    • Indication:
    • Acute myocardial infarctioon
    • Arterial thrombosis
    • Arteriovenous cannulation, clearance
    • Deep venous thrombosis
    • Pulmonary embolism
  21. Abbokinase, kinlytic
    Urokinase

    First generation
  22. Activas, Cathflo Activase
    Alteplase, recombinant

    tPA

    Second generation
  23. Plavix
    Clopidogrel

    Antiplatelet

    • Irreversible antagoniost of platelet P2Y12 purinergic receptors.
    • Antagonism of receptor prevent initation of aggregation

    • Indication:
    • - Acute ST segment elevation myocardial infarction-Thrombosis; Prophylaxis
    • - Cerbrovascular accident, Recent-Thrombosis; Prophylaxis
    • - Myocardial infarction, Recent-Thrombosis; Prophlaxis
    • - Non-ST segment elevation myoocardial infarction, acute-opercutaneous coronary intervention-thrombosis; Prophylaxis
    • - Non-ST segment elevation myocardial infarction, acute-Thrombosis; POrophylaxis
    • - Percutaneous coronary intervention-Thrombosis; Prophylaxis- Unstable angina
    • - Peripheral arterial occlusive disease-Thrombosis; Prophylaxis
  24. Ticlid
    Ticlopidine


    Antiplatelet

    • Irreversible antagoniost of platelet P2Y12 purinergic receptors.
    • Antagonism of receptor prevent initation of aggregation

    • Indication:
    • Placement of stent in coronary artery;Adjunct
    • Thromboembolic stroke
  25. Brilinta
    Ticagrelor

    • Irreversible antagoniost of platelet P2Y12 purinergic receptors.
    • Antagonism of receptor prevent initation of aggregation

    • Indication:
    • Used alone or together with aspirin to help prevent stroke, heart attack, and other heart and blood vessel problems.
  26. Effient
    Prasugrel

    • Antiplatelet
    • Irreversible antagoniost of platelet P2Y12 purinergic receptors.
    • Antagonism of receptor prevent initation of aggregation

    • Indication:
    • Prevents strokes and heart attacks in patients who need to have a heart procedure called percutaneous coronary intervention (PCI)
  27. Reopro
    Abciximab

    Antiplatelets

    • Glycoprotein IIb/IIIa receptor antagonist
    • Prevents fibrinogen cross-linking between platelets.

    • Indication:
    • Prevents blood clots from forming during a procedure to open blocked blood vessels
  28. Integrillin
    Epitifibatide

    Antiplatelets

    • Glycoprotein IIb/IIIa receptor antagonist
    • Prevents fibrinogen cross-linking between

    • Indication:
    • Used during a heart attack or angioplasty to keep blood clots from forming.
  29. Aggrastat
    Tirofiban

    Antiplatelet

    • Glycoprotein IIb/IIIa receptor antagonist
    • Prevents fibrinogen cross-linking between

    • Indication:
    • Treats chest pain and certain heart conditions, and is used during medical procedures involving the heart or arteries.
  30. Pletal
    Cilostazol

    Antiplatelets

    Phosphodiesterase inhibitor

    • Indication:
    • Treats a circulation problem in which too little blood flows into your leg muscles (intermittent claudication). Helps you walk longer distances with less pain.
  31. Persantine
    Dipyridamole

    Antiplatelets

    Phosphodiesterase inhibitor

    • Indication:
    • Keeps blood clots from forming after some types of heart surgery. Also used to prevent strokes and heart attacks. Used in combination with other medicines.
  32. Ecotrin, Fasprin
    Aspirin

    Irreversible antiplatelates

    • Non sterooidal anti-inflammatory drugs (NSAIDs)
    • Acetylation prevents formation of sown stream activator of aggregation.

    • Indication:
    • Treats pain, fever, arthritis, and inflammation. It may also be used to reduce the risk of heart attack.

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