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Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 52 Anticoagulant, Antiplatelet, and Thrombolytic Drugs
2Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Physiology and Pathophysiology of Coagulation Hemostasis Stage 1: formation of platelet plug Platelet aggregation Platelet aggregation Stage 2: coagulation Intrinsic coagulation pathway Intrinsic coagulation pathway Extrinsic coagulation pathway Extrinsic coagulation pathway Keeping hemostasis under control Physiologic removal of clots Thrombosis Arterial thrombosis Venous thrombosis
3Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Overview of Drugs for Thromboembolic Disorders Three major groups Anticoagulants Antiplatelets Thrombolytics See Table 52-1
4Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Anticoagulants Reduce the formation of fibrin Two mechanisms of action Inhibit the synthesis of clotting factors Inhibit the activity of clotting factors
5Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Heparin and Heparin Derivatives Heparin (unfractionated) Enhances antithrombin Sources Lungs of cattle Lungs of cattle Intestines of pigs Intestines of pigs Rapid-acting anticoagulant Administered by injection only IV IV Continuous and intermittent Deep subQ Deep subQ
6Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Heparin (Unfractionated) Therapeutic uses Preferred anticoagulant during pregnancy and when rapid anticoagulation is required Pulmonary embolism (PE) Stroke evolving Massive deep venous thrombosis (DVT) Open heart surgery Renal dialysis Low-dose therapy postoperatively Disseminated intravascular coagulation (DIC) Adjunct to thrombolytic therapy
7Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Heparin (Unfractionated) Adverse effects Hemorrhage Heparin-induced thrombocytopenia Hypersensitivity reactions Contraindicated Thrombocytopenia Uncontrollable bleeding During and immediately after surgery of the eye, brain, or spinal cord Antidote for OD: protamine sulfate Activated partial thromboplastin time (aPTT)
8Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Low-Molecular-Weight Heparins Heparin preparations composed of molecules that are shorter than those found in unfractionated heparin Therapeutic uses Prevention of DVT following surgery Including replacement of hip, knee Including replacement of hip, knee Treatment of established DVT Prevention of ischemic complications Patients with unstable angina, non–Q-wave MI, and STEMI Patients with unstable angina, non–Q-wave MI, and STEMI
9Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Low-Molecular-Weight Heparins Administered subQ Dosage based on body weight Antidote for toxicity: protamine sulfate Costs more than unfractionated heparin Does not require monitoring; can be given at home Adverse effects and interactions Bleeding (but less than with unfractionated heparin) Immune-mediated thrombocytopenia Severe neurologic injury for patients undergoing spinal puncture or spinal epidural anesthesia
10Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Other LMW Heparin In the United States, three LMW heparins are available: Enoxaparin Dalteparin Tinzaparin
11Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Warfarin, an Oral Anticoagulant Originally discovered while cattle were observed ingesting spoiled clover silage Used as rat poison Failed suicide attempt with large dose brought renewed clinical interest Clinical use Oral anticoagulant with delayed onset Vitamin K antagonist Blocks biosynthesis of factors VII, IX, and X and prothrombin
12Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Warfarin, an Oral Anticoagulant Therapeutic uses Not useful in emergencies Long-term prophylaxis of thrombosis Prevention of venous thrombosis and associated pulmonary embolism Prevention of venous thrombosis and associated pulmonary embolism Prevention of thromboembolism (in patients with prosthetic heart valves) Prevention of thromboembolism (in patients with prosthetic heart valves) Prevention of thrombosis during atrial fibrillation Prevention of thrombosis during atrial fibrillation
13Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Warfarin, an Oral Anticoagulant Monitoring treatment Prothrombin time (PT) International normalized ratio (INR) Adverse effects Hemorrhage (vitamin K for toxicity) Fetal hemorrhage and teratogenesis from use during pregnancy Use during lactation Other adverse effects
14Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Warfarin, an Oral Anticoagulant Drug interactions Drugs that increase anticoagulant effects Drugs that promote bleeding Drugs that decrease anticoagulant effects Heparin Aspirin Acetaminophen
15Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Warfarin, an Oral Anticoagulant Warfarin overdose Vitamin K Dietary vitamin K Contrasts between warfarin and heparin
16Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Direct Thrombin Inhibitors Direct inhibition of thrombin (unlike heparin, which enhances the activity of antithrombin) Dabigatran Etexilate Approved in 2010 Oral prodrug undergoes conversion to dabigatran Advantages of dabigatran: doesn’t require monitoring of anticoagulation, little risk of adverse interactions, same dose can be used for all patients regardless of age or weight
17Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Direct Thrombin Inhibitors Hiruden Analog: Bivalirudin (Angiomax) Prevents clot formation (combined with aspirin) in patients with unstable angina who are undergoing coronary angioplasty Mechanism of action Facilitates the actions of antithrombin Facilitates the actions of antithrombin Prevents conversion of fibrinogen to fibrin Prevents conversion of fibrinogen to fibrin Prevents activation of factor XIII Prevents activation of factor XIII Adverse effects Bleeding Bleeding Back pain Back pain Nausea, headache Nausea, headache
18Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Other Direct Thrombin Inhibitors Lepirudin (Refludan) Argatroban (formerly known as Acova) Desirudin (Ipravask) Dabigatran (Pradaxa)
19Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Selective Factor Xa Inhibitors Produce selective inhibition of factor Xa Fondaparinux Activation of antithrombin Injection Rivaroxaban Binds directly with factor Xa to cause inactivation Oral
20Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Fondaparinux (Arixtra) Synthetic anticoagulant Selective inhibition Therapeutic uses Prevention of DVT following surgery Treatment of acute PE (in conjunction with warfarin) Treatment of acute DVT (in conjunction with warfarin) Adverse effects Bleeding Avoid in patients weighing less than 50 kg Thrombocytopenia Spinal or epidural hematoma
21Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Rivaroxaban (Xarelto) Oral anticoagulant approved in 2011 Does not require laboratory monitoring Patients who received rivaroxaban were found to be much less likely to experience DVT, VTE, PE, or death
22Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Antithrombin (AT) Endogenous compound that suppresses coagulation, primarily by inhibiting thrombin and factor Xa Used to prevent thrombosis in patients with inherited AT deficiency Two preparations, marketed as Atryn and Thrombate III
23Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Antiplatelet Drugs Aspirin (ASA) Inhibition of cyclooxygenase Adverse effect Increases risk for GI bleeding Increases risk for GI bleeding Ticlopidine (Ticlid) Inhibits ADP-mediated aggregation Adverse effects Hematologic effects Hematologic effects Clopidogrel (Plavix) ADP receptor antagonist
24Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Aspirin (ASA) Therapeutic uses Ischemic stroke Transient ischemic attack (TIA) Chronic stable angina Unstable angina Coronary stenting Acute MI Previous MI Primary prevention of MI
25Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Aspirin (ASA) Adverse effects Bleeding GI bleeding and hemorrhagic stroke Enteric-coated tablets may not reduce the risk for GI bleeding
26Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Clopidogrel (Plavix) Therapeutic uses Prevents blockage of coronary artery stents Reduces thrombotic events in patients with acute coronary syndromes MI, ischemic stroke, and vascular death MI, ischemic stroke, and vascular death Similar adverse effects to those of aspirin Use with caution in combination with other drugs that promote bleeding
27Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Antiplatelet Drugs Glycoprotein (GP) IIb/IIIa receptor antagonists Most effective antiplatelet drugs “Super aspirins” Reversible blockade of platelet GP IIb/IIIa receptors
28Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Other Antiplatelet Drugs Dipyridamole Dipyrindamole + aspirin Aggrenox Cilostazol
29Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Thrombolytic Drugs Streptokinase (Streptase); Alteplase (tPa) Major adverse effect – bleeding (minor oozing to life-threatening amount) Likely sites of bleeding Recent wounds, needle puncture sites, invasive procedure sites Recent wounds, needle puncture sites, invasive procedure sites Anticoagulants increase the risk for hemorrhage Blood replacement may need to be considered
30Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Minimizing the Risk of Bleeding Minimizing physical manipulation of the patient Avoiding subQ and IM injections Minimizing invasive procedures Minimizing concurrent use of anticoagulants (eg, heparin, warfarin, dabigatran) Minimizing concurrent use of antiplatelet drugs (eg, aspirin, clopidogrel)
31Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Streptokinase (Streptase) Binds to plasminogen to form active complex Therapeutic uses Acute coronary thrombosis (acute MI) Deep venous thrombosis (DVT) Massive pulmonary emboli Adverse effects Bleeding – excessive fibrinolysis can be reversed with IV aminocaproic acid (Amicar) Antibody production Hypotension Fever
32Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Alteplase (tPa) Converts plasminogen to plasmin Given in accelerated schedule Therapeutic uses Myocardial infarction Ischemic stroke Massive pulmonary emboli
33Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Alteplase (tPa) Adverse effects Bleeding Risk for intracranial bleeding higher than with streptokinase Risk for intracranial bleeding higher than with streptokinase Fever Advantages Does not cause allergic reactions Does not induce hypotension
34Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Other Thrombolytic Drugs Tenecteplase Reteplase
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