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Prior to the introduction of direct factor Xa inhibitors, vitamin K antagonists such as warfarin were the only oral anticoagulants for over 60 years, and together with heparin have been the main blood thinners in use. People admitted to hospital requiring blood thinning were started on an infusion of heparin infusion, which thinned blood ...
An anticoagulant, commonly known as a blood thinner, is a chemical substance that prevents or reduces the coagulation of blood, prolonging the clotting time. [1] Some occur naturally in blood-eating animals, such as leeches and mosquitoes , which help keep the bite area unclotted long enough for the animal to obtain blood.
[1] [2] Antithrombotics can be used therapeutically for prevention (primary prevention, secondary prevention) or treatment of a dangerous blood clot (acute thrombus). In the U.S., the American College of Chest Physicians publishes clinical guidelines for clinicians for the use of these drugs to treat and prevent a variety of diseases.
Anticoagulants and anti-platelet agents (together "antithrombotics") are amongst the most commonly used medications. Anti-platelet agents include aspirin , dipyridamole , ticlopidine , clopidogrel , ticagrelor and prasugrel ; the parenteral glycoprotein IIb/IIIa inhibitors are used during angioplasty .
[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] Its anticoagulant properties make it useful to prevent blood clotting in blood specimen test tubes and kidney dialysis ...
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]
The most commonly used anticoagulants in clinical practice, warfarin and the heparin series of anticoagulants and fondaparinux, act to inhibit the action of Factor Xa in various degrees. Traditional models of coagulation developed in the 1960s envisaged two separate cascades, the extrinsic (tissue factor (TF)) pathway and the intrinsic pathway.
For many years dual treatment with the cyclooxygenase-1 (COX-1) inhibitor aspirin and clopidogrel was routine practice and served as the main antiplatelet agents for the prevention of thrombotic events as they have the capability to powerfully manipulate platelet biology, which plays a central part in thrombosis.