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Ximelagatran (Exanta or Exarta, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin [1] that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy.
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]
Dabigatran is an oral direct thrombin inhibitor. Dabigatran (Pradaxa) was found to be noninferior to Warfarin in prevention of ischemic stroke, as well as intracranial hemorrhage risk and overall mortality for non-valvular atrial fibrillation according to the RE-LY trial. [9]
Compared to warfarin it has fewer interactions with other medications. [12] It is a direct factor Xa inhibitor. [8] In 2007, Pfizer and Bristol-Myers Squibb began the development of apixaban as an anticoagulant. [13] Apixaban was approved for medical use in the European Union in May 2011, and in the United States in December 2012.
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 ...
[14] [15] Renal clearance and degradation account for the most part for the systemic clearance of desulfatohirudins and there is accumulation of the drug in patients with chronic kidney disease. These drugs should not be used in patients with impaired renal function, since there is no specific antidote available to reverse the effects. [14]