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Parenteral anticoagulants: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines.
- Source :
-
Chest [Chest] 2012 Feb; Vol. 141 (2 Suppl), pp. e24S-e43S. - Publication Year :
- 2012
-
Abstract
- This article describes the pharmacology of approved parenteral anticoagulants. These include the indirect anticoagulants, unfractionated heparin (UFH), low-molecular-weight heparins (LMWHs), fondaparinux, and danaparoid, as well as the direct thrombin inhibitors hirudin, bivalirudin, and argatroban. UFH is a heterogeneous mixture of glycosaminoglycans that bind to antithrombin via a unique pentasaccharide sequence and catalyze the inactivation of thrombin, factor Xa, and other clotting enzymes. Heparin also binds to cells and plasma proteins other than antithrombin causing unpredictable pharmacokinetic and pharmacodynamic properties and triggering nonhemorrhagic side effects, such as heparin-induced thrombocytopenia (HIT) and osteoporosis. LMWHs have greater inhibitory activity against factor Xa than thrombin and exhibit less binding to cells and plasma proteins than heparin. Consequently, LMWH preparations have more predictable pharmacokinetic and pharmacodynamic properties, have a longer half-life than heparin, and are associated with a lower risk of nonhemorrhagic side effects. LMWHs can be administered once daily or bid by subcutaneous injection, without coagulation monitoring. Based on their greater convenience, LMWHs have replaced UFH for many clinical indications. Fondaparinux, a synthetic pentasaccharide, catalyzes the inhibition of factor Xa, but not thrombin, in an antithrombin-dependent fashion. Fondaparinux binds only to antithrombin. Therefore, fondaparinux-associated HIT or osteoporosis is unlikely to occur. Fondaparinux exhibits complete bioavailability when administered subcutaneously, has a longer half-life than LMWHs, and is given once daily by subcutaneous injection in fixed doses, without coagulation monitoring. Three additional parenteral direct thrombin inhibitors and danaparoid are approved as alternatives to heparin in patients with HIT.
- Subjects :
- Antithrombins agonists
Arginine analogs & derivatives
Chondroitin Sulfates administration & dosage
Chondroitin Sulfates adverse effects
Dermatan Sulfate administration & dosage
Dermatan Sulfate adverse effects
Dose-Response Relationship, Drug
Fondaparinux
Heparin administration & dosage
Heparin adverse effects
Heparin, Low-Molecular-Weight administration & dosage
Heparin, Low-Molecular-Weight adverse effects
Heparitin Sulfate administration & dosage
Heparitin Sulfate adverse effects
Hirudins administration & dosage
Hirudins adverse effects
Humans
Infusions, Intravenous
Peptide Fragments administration & dosage
Peptide Fragments adverse effects
Pipecolic Acids administration & dosage
Pipecolic Acids adverse effects
Polysaccharides administration & dosage
Polysaccharides adverse effects
Recombinant Proteins administration & dosage
Recombinant Proteins adverse effects
Sulfonamides
Thrombin antagonists & inhibitors
Thrombosis blood
United States
Evidence-Based Medicine
Fibrinolytic Agents administration & dosage
Practice Guidelines as Topic
Societies, Medical
Thrombosis drug therapy
Thrombosis prevention & control
Subjects
Details
- Language :
- English
- ISSN :
- 1931-3543
- Volume :
- 141
- Issue :
- 2 Suppl
- Database :
- MEDLINE
- Journal :
- Chest
- Publication Type :
- Academic Journal
- Accession number :
- 22315264
- Full Text :
- https://doi.org/10.1378/chest.11-2291