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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 ...
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. [ 28 ]
However, newer retrospective cohort studies have not shown adverse cardiovascular events caused by clopidogrel-PPI interactions. Therefore there is no definite evidence on the drug interaction effect on mortality. [38] For patients with high risk of gastrointestinal bleeding, the risk outweighs the possible adverse cardiovascular effects.
Verapamil is a class-IV antiarrhythmic and more effective than digoxin in controlling ventricular rate. [19] Verapamil is not listed as a first line antihypertensive agent by the guidelines provided by JAMA in JNC-8. [20] However, it may be used to treat hypertension if patient has co-morbid atrial fibrillation or other types of arrhythmia. [17 ...
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Andexanet alfa, sold under the brand name Andexxa among others, is an antidote for the medications rivaroxaban and apixaban, when reversal of anticoagulation is needed due to uncontrolled bleeding. [8] It has not been found to be useful for other factor Xa inhibitors. [9] It is given by injection into a vein. [9]
The study found that dabigatran had comparable rates of ischemic stroke or systemic embolism, intracerebral haemorrhage, and all-cause mortality when compared to other anticoagulants like apixaban, edoxaban, and rivaroxaban. Notably, apixaban was associated with a lower risk of gastrointestinal bleeding than dabigatran and the others.
Rivaroxaban inhibits both free and bound Factor Xa in the prothrombinase complex. [33] It is a selective direct factor Xa inhibitor with an onset of action of 2.5 to 4 hours. [34] Inhibition of Factor Xa interrupts the intrinsic and extrinsic pathway of the blood coagulation cascade, inhibiting both thrombin formation and development of thrombi.