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level: Level 2

Questions and Answers List

Anticoagulants

level questions: Level 2

QuestionAnswer
Parenteral Anticoagulants1 Heparin 2 Low-Molecular-Weight Heparins 3 Fondaparinux (Arixtra®) 4 Direct Thrombin Inhibitors
Oral Anticoagulants1 WARFARIN 2 Dabigatran etexilate
are the two traditional anticoagulants used for acute coronary syndromes, deep-vein thrombosis (DVT), pulmonary embolism (PE), and heart surgery Also given to certain people at risk for forming blood clots, such as those with artificial heart valves or who have atrial fibrillation (AF)intravascular coagulation of the blood in any part of the circulatory system, as in the heart, arteries, veins, or capillariesHeparin and warfarin
• Rapid-acting anticoagulant fast-acting, has a short half-life Uses: • Pulmonary embolism (PE), Stroke evolving, Massive deep venous thrombosis (DVT) Sources: ✓Lungs of cattle, Intestines of pigs Adverse effects • Hemorrhage, Thrombocytopenia, Hypersensitivity, Protamine Sulfate as antidote, Activated partial thromboplastin time IT NEEDS MONITORING w/ SPECIAL BLOOD TESTSHeparin (unfractionated)
is produced by chemically splitting heparin into pieces of about one-third of its original size. fewer side effects, longer half-life, and a more predictable dose-dependent response, NO MONITORING req. INHIBITS FACTOR 10a Therapeutic use • Prevention of DVT following surgery • Treatment of established DVT • Prevention of ischemic complications Adverse effects and interactions • Bleeding • thrombocytopeniaLow-Molecular-Weight Heparins
• Synthetic anticoagulant, Selective inhibition longer half-life, less bleeding than LMW Heparins Therapeutic use • Prevention of DVT following surgery • Treatment of acute PE (in conjunction with warfarin) • Treatment of acute DVT (in conjunction with warfarin) Adverse effects • Bleeding • Patients weighing less than 50 kg • Thrombocytopenia • Spinal or epidural hematomaFondaparinux (Arixtra®)
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 • HeadacheDirect Thrombin Inhibitors • Bivalirudin [Angiomax], Lepirudin, Argatroban, Desirudin
• Antagonist to vitamin K; Blocks the biosynthesis of factors VII, IX, X, and prothrombin It takes days to be effective 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 Adverse effects • Hemorrhage (Fetal hemorrhage in pregnant) • Not to be Used during lactation Drug interactions • Drugs that increase anticoagulant effects • Drugs that promote bleedingWARFARIN
• is a new oral direct thrombin inhibitor and the prodrug of dabigatran • is a small molecule that reversibly inhibits both free and clot-bound thrombin by binding to exosite 1 and/or the active site of thrombinDabigatran etexilate
Future of Anticoagulants 1 Molecular targets are __ 2 The two candidate compounds. 1 factor IIa (thrombin) and factor Xa 2 direct thrombin inhibitor (dabigatran etexilate), direct factor Xa inhibitor (rivaroxaban)
an essential cofactor for the synthesis of many clotting factors.Vitamin K
1 Heparin’s action can be reversed with __ 2 __ given orally or intravenously, can counteract warfarin.1 protamine 2 Vitamin K
Specific antidotes for direct oral anticoagulants: 1 for Dabigatran 2 for Apixaban, Betrixaban, Edoxaban, Rivaroxaban. 1 Idarucizumab (IV) 2 Andexanet alfa (IV volus then slow IV infusion)