Parenteral Anticoagulants: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines

摘要: This article describes the pharmacology of approved parenteral anticoagulants. These include indirect anticoagulants, unfractionated heparin (UFH), low-molecular-weight heparins (LMWHs), fondaparinux, and danaparoid, as well direct thrombin inhibitors hirudin, bivalirudin, argatroban. UFH is a heterogeneous mixture glycosaminoglycans that bind to antithrombin via unique pentasaccharide sequence catalyze inactivation thrombin, factor Xa, other clotting enzymes. Heparin also binds cells plasma proteins than causing unpredictable pharmacokinetic pharmacodynamic properties triggering nonhemorrhagic side effects, such heparin-induced thrombocytopenia (HIT) osteoporosis. LMWHs have greater inhibitory activity against Xa exhibit less binding heparin. Consequently, LMWH preparations more predictable properties, longer half-life heparin, are associated with lower risk effects. can be administered once daily or bid by subcutaneous injection, without coagulation monitoring. Based on their convenience, replaced for many clinical indications. Fondaparinux, synthetic pentasaccharide, catalyzes inhibition but not in an antithrombin-dependent fashion. Fondaparinux only antithrombin. Therefore, fondaparinux-associated HIT osteoporosis unlikely occur. exhibits complete bioavailability when subcutaneously, has LMWHs, given injection fixed doses, Three additional danaparoid alternatives patients HIT.