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Ximelagatran showed good efficacy compared with warfarin in several trials in prevention and treatment of deep vein thrombosis and as thromboprophylaxis in atrial fibrillation. [1] Development was stopped by manufacturer AstraZeneca , however, because of reports of liver enzyme derangements and liver failure .
Warfarin is indicated for the prophylaxis and treatment of venous thrombosis and its extension, pulmonary embolism; [9] prophylaxis and treatment of thromboembolic complications associated with atrial fibrillation and/or cardiac valve replacement; [9] and reduction in the risk of death, recurrent myocardial infarction, and thromboembolic events such as stroke or systemic embolization after ...
The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [3] [14] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [15]
Antithrombin (AT) is a small glycoprotein that inactivates several enzymes of the coagulation system. It is a 464-amino-acid protein produced by the liver.It contains three disulfide bonds and a total of four possible glycosylation sites. α-Antithrombin is the dominant form of antithrombin found in blood plasma and has an oligosaccharide occupying each of its four glycosylation sites.
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Tecarfarin is a vitamin K antagonist under development for use as an anticoagulant. [2] A Phase II/III clinical trial in 607 people, comparing it to the established vitamin K antagonist warfarin, found no difference in quality of anticoagulation or side effects between the two drugs in the overall population. [3]
However, in the case of the second generation superwarfarins intended to kill warfarin-resistant rodents, the time of vitamin K administration may need to be prolonged to months, in order to combat the long residence time of the poison. [2] The vitamin K antagonists can cause birth defects . [3]
Heparin is contraindicated for suspected cases of vaccine-induced pro-thrombotic immune thrombocytopenia (VIPIT) secondary to SARS-CoV-2 vaccination, as heparin may further increase the risk of bleeding in an anti-PF4/heparin complex autoimmune manner, in favor of alternative anticoagulant medications (such as argatroban or danaparoid). [7] [8] [9]