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Heparin, also known as unfractionated heparin (UFH), is a medication and naturally occurring glycosaminoglycan. [3] [4] Heparin is a blood anticoagulant that increases the activity of antithrombin. [5] It is used in the treatment of heart attacks and unstable angina. [3] It can be given intravenously or by injection under the skin. [3]
Thrombin demonstrates a high level of allosteric regulation. [2] Allosterism in thrombin is regulated by the exosites 1 and 2 and the sodium binding site. A recent patent review has shown that the general consensus among researchers is that allosteric inhibitors may provide a more regulatable anticoagulant. [3]
DTIs inhibit thrombin by two ways; bivalent DTIs block simultaneously the active site and exosite 1 and act as competitive inhibitors of fibrin, [13] while univalent DTIs block only the active site and can therefore both inhibit unbound and fibrin-bound thrombin. In contrast, heparin drugs bind in exosite 2 and form a bridge between thrombin ...
Indirect thrombin inhibitors bind to antithrombin to enhance the rate of inactivation of clotting factors, indirectly inactivating thrombin through actions on antithrombin. [42] Heparin is a widely used anticoagulant. It is administered intravenously (into a vein) or subcutaneously (below the skin).
Older terminology distinguishes between two forms of heparin-induced thrombocytopenia: type 1 (mild, nonimmune mediated and self-limiting fall in platelet count) and type 2, the form described above. Currently, the term HIT is used without a modifier to describe the immune-mediated severe form. [4]
Smaller risk of osteoporosis in long-term use. Smaller risk of heparin-induced thrombocytopenia, a potential side effect of heparin. Hepatin's anticoagulant effects are typically reversible with protamine sulfate, while protamine's effect on LMWH is limited. LMWH has less of an effect on thrombin than heparin, but about the same effect on ...
An antithrombotic agent is a drug that reduces the formation of blood clots (). [1] [2] Antithrombotics can be used therapeutically for prevention (primary prevention, secondary prevention) or treatment of a dangerous blood clot (acute thrombus).
Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor. [3] In 2000, argatroban was licensed by the US Food and Drug Administration (FDA) for prophylaxis or treatment of thrombosis in people with heparin-induced thrombocytopenia (HIT).