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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 ...
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]
Apixaban is a highly selective, orally bioavailable, and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin, the final enzyme in the coagulation cascade that is responsible for fibrin clot formation. [ 27 ]
Subanalysis of Phase III ARISTOTLE Trial of Eliquis® (apixaban) Demonstrated Consistent Results Versus Warfarin in Patients with Nonvalvular Atrial Fibrillation with or without Valvular Heart ...
Andexanet alfa is used to stop life-threatening or uncontrollable bleeding in people who are taking rivaroxaban or apixaban. [8] Studies in healthy volunteers show that the molecule binds factor Xa inhibitors and counters their anti-Xa-activity. [11] The first published clinical trial was a prospective, open label, single group study. [12]
Augustus John Rush (born December 15, 1942) is an internationally renowned psychiatrist. He is a professor emeritus in Duke-NUS Medical School at the National University of Singapore (NUS), [ 1 ] and adjunct professor of psychiatry and behavioral sciences at Duke University School of Medicine . [ 2 ]
A 2011 trial, APPRAISE-2, showed patients receiving apixaban 5 mg twice daily against placebo after acute coronary syndrome experienced an 150% increased rate of major bleeding episodes without a significant reduction in recurrent ischemic events, so the trial was terminated early. A greater number of intracranial and fatal bleeding events ...
In other trials with new anticoagulants as in ARISTOTLE for apixaban 30,5% took aspirin at inclusion, in the ROCKET-AF trial for rivaroxaban 38,5% and in ENGAGE AF-TIMI 48 for edoxaban 29%. The baseline prevalence of prior myocardial infarction was 17% in RE-LY and 12% in ENGAGE, respectively, raising questions regarding the indication for ...