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Edit Comment Close Premium member Presentation Transcript Anticoagulant, Antiplatelet, and Thrombolytic Drugs : Anticoagulant, Antiplatelet, and Thrombolytic Drugs Objectives : Objectives Give a basic overview of the pathways involved in hemostasis, including platelet plug formation and reinforcement of platelet plugs, and mechanisms by which the body protects against widespread coagulation. Explain the differences between anticoagulant, antiplatelet, and thrombolytic drugs in terms of what coagulation processes they affect and their main clinical uses. Likewise, state the main difference between a thrombus and an embolus. Describe the usual etiologies of arterial versus venous thrombosis, and discuss how prophylactic or interventional drug therapies for these two situations are similar or different. Give a short summary of how and where heparins exert their desired anticoagulant effects, and describe the mechanisms and risks of paradoxic increases in thrombotic events associated with heparin-induced thrombocytopenia. Objectives : Objectives Compare and contrast unfractionated heparins and low–molecular weight (LMW) heparins in terms of mechanisms of action, pharmacokinetics, dosing (schedules), suitability for outpatient therapy, and monitoring of response(s). Summarize the key points that describe the differences between warfarin and heparin: mechanisms, onsets, sites of action, and monitoring. Compare and contrast the actions and uses of aspirin with those of warfarin and heparin, and state the typical “targets” for the lab test that is used to monitor the response to each. Summarize instructions about the use of aspirin for relief of common headache, pain, or fever for an outpatient who is taking warfarin; explain situations in which concomitantly taking both warfarin and aspirin is acceptable and situations in which doing so can be dangerous. Summarize general precautions and guidelines (including drug selection and monitoring) that apply when anticoagulation is indicated for a pregnant woman. In particular, state what the adjustment to the dosage of warfarin should be. Physiology and Pathophysiology of Coagulation : Physiology and Pathophysiology of Coagulation Hemostasis Stage 1—formation of platelet plug Platelet aggregation Stage 2—coagulation Intrinsic coagulation pathway Extrinsic coagulation pathway Keeping hemostasis under control Physiologic removal of clots Thrombosis Arterial thrombosis Venous thrombosis Figure 51-2 Outline of the coagulation cascade showing factors affected by anticoagulant drugs. : Figure 51-2 Outline of the coagulation cascade showing factors affected by anticoagulant drugs. Parenteral Anticoagulants I:Heparin and Related Drugs : Parenteral Anticoagulants I:Heparin and Related Drugs Heparin (unfractionated) Sources Lungs of cattle Intestines of pigs Rapid-acting anticoagulant Uses Pulmonary embolism (PE) Stroke evolving Massive deep venous thrombosis (DVT) Parenteral Anticoagulants I: Heparin and Related Drugs : Parenteral Anticoagulants I: Heparin and Related Drugs Adverse effects – Hemorrhage – Heparin-induced thrombocytopenia – Hypersensitivity reactions Protamine Activated partial thromboplastin time (aPTT) Low-Molecular-Weight Heparins : Low-Molecular-Weight Heparins Heparin preparations composed of molecules that are shorter than those found in unfractionated heparin. Therapeutic use Prevention of DVT following surgery Treatment of established DVT Prevention of ischemic complications Adverse effects and interactions Bleeding Immune-mediated thrombocytopenia Cost Parenteral Anticoagulants II: Direct Thrombin Inhibitors : Parenteral Anticoagulants II: Direct Thrombin Inhibitors Bivalirudin [Angiomax] Therapeutic use Prevent clot formation (combined with aspirin) Mechanism of action Facilitates the actions of antithrombin Prevents the conversion of fibrinogen into fibrin Prevents the activation of factor XIIIa Adverse effects Back pain Nausea Headache Parenteral Anticoagulants II: Direct Thrombin Inhibitors : Parenteral Anticoagulants II: Direct Thrombin Inhibitors Other direct thrombin inhibitors Lepirudin Argatroban Desirudin Warfarin, an Oral Anticoagulant : Warfarin, an Oral Anticoagulant Oral anticoagulant Antagonist vitamin K Blocks the biosynthesis of factors VII, IX, X, and prothrombin Therapeutic uses Long-term prophylaxis of thrombosis Prevention of venous thrombosis and associated pulmonary embolism Prevention of thromboembolism (in patients with prosthetic heart valves) Prevention of thrombosis during atrial fibrillation Warfarin, an Oral Anticoagulant (cont’d) : Warfarin, an Oral Anticoagulant (cont’d) Adverse effects Hemorrhage Fetal hemorrhage and teratogenesis from use during pregnancy Use during lactation Warfarin, an Oral Anticoagulant (cont’d) : Warfarin, an Oral Anticoagulant (cont’d) Drug interactions Drugs that increase anticoagulant effects Drugs that promote bleeding Drugs that decrease anticoagulant effects Heparin Aspirin Acetaminophen Antiplatelet Drugs : Antiplatelet Drugs Aspirin (ASA) Inhibition of cyclooxygenase Adverse effect Increase risk of GI bleeding Ticlopidine [Ticlid] Inhibits ADP-mediated aggregation Adverse effects Hematologic effects Clopidogrel [Plavix] ADP receptor antagonist Antiplatelet Drugs : Antiplatelet Drugs Glycoprotein (GP) IIb/IIIa receptor antagonists Most effective antiplatelet drugs Reversible blockade of platelet GP IIb/IIIa receptors Thrombolytic Drugs : Thrombolytic Drugs Streptokinase [Streptase] Binds plasminogen Uses Acute coronary thrombosis (acute MI) Deep venous thrombosis (DVT) Massive pulmonary emboli Adverse effects Bleeding – Antibody production Hypotension Fever Thrombolytic Drugs : Thrombolytic Drugs Alteplase Binds plasminogen Uses Myocardial infarction Deep vein thrombosis Massive pulmonary emboli Adverse effects Bleeding – Antibody production Hypotension Fever Other Thrombolytic Drugs : Urokinase Retavase Streptokinase vs. Alteplase Other Thrombolytic Drugs You do not have the permission to view this presentation. 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