Anticoagulants and Antiplatelet Agents Chapter 21

1. Definitions
   1. Hemostasis
   2. Thrombosis
   3. Thrombus
   4. Embolus
   5. Bleeding disorders
2. Blood clotting
   1. Blood vessel anatomy
      1. endothelium
      2. smooth muscle
      3. collagen fibers
   2. Three steps of hemostasis
      1. vasospasm
      2. platelet plug formation
      3. coagulation
3. Platelet plug formation and inhibition
   1. Platelet background
      1. thrombopoietin
      2. resting
   2. Platelet plug formation
      1. activated by 2 means
      2. collagen binding
      3. platelet activation
      4. platelet secretions
         1. ADP
         2. thromboxane A2
         3. serotonin
   3. Mechanisms to block platelet activation
      1. block ADP binding
         1. ADP cell surface receptor = P2Y12
         1. drugs
            1. clopidogrel - (Plavix)
            2. prasugrel - (Effient)
            3. ticagrelor - (Brilinta)
            4. ticlopidine - (Ticlid)
      2. Increase cAMP levels
         1. dipyridamole - (Persantine)
         2. cilostazol - (Pletal)
      3. block production of thromboxane A2 - Aspirin
         1. mechanism of action
            1. cyclooxygenase
      4. block fibrinogen receptor
         1. abciximab - (Reopro)
         2. eptifibatide - (Integrilin)
         3. tirofiban - (Aggrastat)Coagulation and Inhibitors
   4. Blood clotting
      1. clotting factors
      2. pathway(s)
         1. Phase 1
            1. contact activation pathway
            2. tissue factor pathway
         2. Phase 2 - prothrombin -> thrombin
         3. Phase 3 - fibrinogen -> fibrin
4. Blood Coagulation Inhibitors
   1. Inhibit Xa
      1. fondaparinux - (Arixtra)
      2. rivaroxaban - (Xarelto)
      3. apixaban - (Eliquis)
   2. Inhibit thrombin (IIa)
      1. argatroban - (Argatroban)
      2. dabigatran - (Pradaxa)
   3. Warfarin (Coumadin)
5. Activate Normal Anticoagulation Pathways
   1. Antithrombin
   2. Heparin
      1. LMWHs
         1. enoxaparin - (Lovenox)
         2. dalteparin - (Fragmin)
6. Thrombolytic Drugs
   1. Background
      1. plasminogen
      2. plasmin
      3. two step activation
         1. tissue plasminogen activator (tPA)
         2. urokinase plasminogen activator (uPA)
   2. Recombinant drugs
      1. alteplase - (Activase)
      2. reteplase - (Retavase)
      3. tenecteplase - (Tnkase)
      4. streptokinase
      5. urokinase (Kinlytic)
7. Drugs Used to Treat / block Bleeding
   1. Stop conversion of plasminogen to plasmin
      1. aminocaproic acid - (Amicar)
      2. tranexamic acid - (Cyklokapron, Lysteda)
   2. Antagonize heparin
      1. protamine sulfate
   3. Block warfarin
      1. vitamin K