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There are three types of DTIs, dependent on their interaction with the thrombin molecule. Bivalent DTIs (hirudin and analogs) bind both to the active site and exosite 1, while univalent DTIs bind only to the active site. [1] The third class of inhibitors, which are gaining importance recently, is the allosteric inhibitors.
Heparin cofactor II (HCII), a protein encoded by the SERPIND1 gene, is a coagulation factor that inhibits IIa, and is a cofactor for heparin and dermatan sulfate ("minor antithrombin"). [ 5 ] The product encoded by this gene is a serine protease inhibitor which rapidly inhibits thrombin in the presence of dermatan sulfate or heparin.
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]
Small molecular direct thrombin inhibitors (smDTIs) are non-peptide small molecules that specifically and reversibly inhibit both free and clot-bound thrombin by binding to the active site of the thrombin molecule. They prevent VTE in patients undergoing hip-and knee replacement surgery. [10]
Activated clotting time (ACT), also known as activated coagulation time, is a test of coagulation. [1] [2]The ACT test can be used to monitor anticoagulation effects, such as from high-dose heparin before, during, and shortly after procedures that require intense anticoagulant administration, such as cardiac bypass, interventional cardiology, thrombolysis, extra-corporeal membrane oxygenation ...
Low-molecular-weight heparin (LMWH) is a class of anticoagulant medications. [1] They are used in the prevention of blood clots and, in the treatment of venous thromboembolism (deep vein thrombosis and pulmonary embolism), and the treatment of myocardial infarction.
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).
Rivaroxaban, Apixaban and Edoxaban bind to the active site of factor Xa, regardless of whether factor Xa is bound in the prothrombinase complex or is in its free form. [35] [37] These direct factor Xa inhibitors can be administered orally, as can dabigatran etexilate, which is a direct thrombin inhibitor.