What is the mechanism of action of apixaban?

Mechanism of Action Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development.

How does apixaban inhibit XA?

The factor Xa inhibitors that are currently commercially available include rivaroxaban, apixaban, betrixaban, and edoxaban. These drugs bind to factor Xa and prevent the formation of thrombin by interrupting the extrinsic and intrinsic coagulation cascades.

What is pharmacodynamics of apixaban?

Apixaban inhibits free and clot-bound FXa, as well as prothrombinase activity, which inhibits clot growth [15]. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development. It has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin [16].

What type of anticoagulant is apixaban?

Apixaban is in a class of medications called factor Xa inhibitors. It works by blocking the action of a certain natural substance that helps blood clots to form.

Is apixaban intrinsic or extrinsic?

1 INTRODUCTION. Apixaban is one of the newer oral anticoagulants (NOAC). It works by the direct inhibition of factor Xa, which is formed by both intrinsic and extrinsic coagulation pathways. This prevention of thrombin formation from prothrombin is needed to prevent the conversion of fibrinogen to fibrin.

What Happens When factor Xa is inhibited?

Factor Xa inhibitors are a type of anticoagulant that work by selectively and reversibly blocking the activity of clotting factor Xa, preventing clot formation. They affect both factor Xa within the blood and within a preexisting clot. They do not affect platelet aggregation.

What is the function of factor Xa?

Factor Xa is a serine protease which cleaves prothrombin to generate thrombin and lies at the crossroads of the extrinsic and intrinsic coagulation pathway. Only a small amount of factor Xa is needed to generate many molecules of thrombin.

What is the reversal agent for apixaban?

Coagulation factor Xa (recombinant), inactivated-zhzo (andexanet alfa; Andexxa – Portola) has received accelerated approval from the FDA for urgent reversal of the anticoagulant effect of the direct factor Xa inhibitors apixaban (Eliquis) and rivaroxaban (Xarelto).

What is factor Xa in blood clotting?

What is the pharmacokinetics of apixaban?

The pharmacokinetic properties of apixaban have been described in detail. In healthy male volunteers, apixaban was rapidly absorbed after oral administration, with a time to maximum plasma apixaban concentration of about 1 hour. The elimination half-life for apixaban in healthy subjects is approximately 12 hours.

How is apixaban metabolism?

Apixaban is mainly metabolized by cytochrome p450(CYP)3A4 and to a lesser extent by CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2 Label. 56% of an orally administered dose is recovered in the feces and 24.5-28.8% of the dose is recovered in the urine Label,1,2.