[Natural and synthetic glycosaminoglycans. Molecular characteristics as the basis of distinct drug profiles].
For several decades, anticoagulants based on glycosaminoglycans (GAG) are drugs of choice in the therapy and prophylaxis of thromboembolic diseases. In principle, it has to be differentiated between the natural GAG-anticoagulants, which are molecular mixtures with complex composition, and the synthetic GAG-anticoagulants, which are chemically defined oligosaccharides. The former include unfractionated heparin, the various low molecular weight heparins and danaparoid. Representatives of the second group are fondaparinux, idraparinux and the hexadecasaccharide SR123781A. They share a common mechanism of action together with the endogenous antithrombotic heparan sulfate, i.e. the catalysis of the antithrombin-mediated inhibition of factor Xa. Besides, considerable structural differences between the various GAG-anticoagulants result in rather distinct product characteristics. This concerns their pharmacodynamics, pharmacokinetics as well as practice-related aspects such as dosage, monitoring, accumulation tendency, antagonisation and HIT-Typ II.
Alban
S
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Pharmazeutisches Institut, Christian-Albrechts-Universität zu Kiel, Gutenbergstr. 76, 24118 Kiel. salban@pharmazie.uni-kiel.de
D000925:Anticoagulants / Q000737:chemistry / Q000627:therapeutic use*; D000991:Antithrombins / Q000627:therapeutic use; D065427:Factor Xa Inhibitors; D006025:Glycosaminoglycans / Q000096:biosynthesis / Q000138:chemical synthesis / Q000145:classification / Q000627:therapeutic use*; D006493:Heparin / Q000627:therapeutic use; D006495:Heparin, Low-Molecular-Weight / Q000627:therapeutic use; D006801:Humans; D008024:Ligands; D011134:Polysaccharides / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013923:Thromboembolism / Q000188:drug therapy*
D000925:Anticoagulants; D000991:Antithrombins; D065427:Factor Xa Inhibitors; D006025:Glycosaminoglycans; D006495:Heparin, Low-Molecular-Weight; D008024:Ligands; D011134:Polysaccharides; C446839:SR 123781A; D006493:Heparin