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Side effects may include bleeding, most commonly from the nose, gastrointestinal tract (GI) or genitourinary system. [2] Compared to the risk of bleeding with warfarin use, direct factor Xa inhibitors have a higher risk of GI bleeding, but lower risk of bleeding in the brain. [2]
The p-methoxy group of apixaban connects to S1 pocket of FXa but does not appear to have any interaction with any residues in this region of FXa. The pyrazole N-2 nitrogen atom of apixaban interacts with Gln-192 and the carbonyl oxygen interacts with Gly-216. The phenyl lactam group of apixaban is positioned between Tyr-99 and Phe-174 and due ...
Dabigatran, sold under the brand name Pradaxa among others, is an anticoagulant used to treat and prevent blood clots and to prevent stroke in people with atrial fibrillation. [ 6 ] [ 7 ] Specifically it is used to prevent blood clots following hip or knee replacement and in those with a history of prior clots. [ 6 ]
Apixaban was approved for medical use in the European Union in May 2011, and in the United States in December 2012. [7] [8] [14] It is on the World Health Organization's List of Essential Medicines. [15] In 2022, it was the 27th most commonly prescribed medication in the United States, with more than 19 million prescriptions.
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]
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.
Prasugrel, a third generation thienopyridine, is metabolized more efficiently than clopidogrel and ticlopidine in the body and therefore it prevents platelet activation to a greater extent. Studies have shown prasugrel to reduce the risk of stent thrombosis and myocardial infarction to much greater level than clopidogrel. [ 26 ]
Idarucizumab is a non-competitive inhibitor that forms complexes with dabigatran to counteract its anticoagulant effect within minutes of administration. [8] It binds to dabigatran that is free or bound to thrombin, as well as dabigatran's active metabolites. [9]
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