Apixaban - a novel oral anticoagulant
Apixaban is a novel oral anticoagulant. It is possible to directly, reversibly, and highly selectively block the active site of factor Xa, blocking the conversion of prothrombin to thrombin, and thereby preventing thrombosis. As compared with rivaroxaban, apixaban also prevents thrombosis by indirectly inhibiting thrombin-induced platelet aggregation and reducing thrombin production. It is mainly used to prevent venous thromboembolism events in adult patients undergoing elective hip or knee replacement. In addition to the indications listed above, it is used to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation; To reduce the risk of deep vein thrombosis and recurrent pulmonary embolism; It is used to treat deep vein thrombosis and pulmonary embolism.
Absorption of apixaban is predominantly in the small intestine. There is a first-pass effect, and at an oral dose of 10mg, the absolute bioavailability of apixaban is approximately 50%, with no effect of food on its bioavailability. The plasma protein binding rate of apixaban in humans is about 87%, and it is mainly bound to albumin. The volume of distribution was about 21L and was mainly distributed in the extracellular fluid. The total plasma clearance was approximately 3.3L/h, and the renal clearance was approximately 0.9L/h, with an apparent elimination half-life of approximately 12h.
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