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Factor Xa inhibitors

Factor Xa is positioned at the juncture of the extrinsic and intrinsic coagulation pathways proximal to thrombin.

Agents are approved for prevention of stroke and systemic embolism in nonvalvular atrial fibrillation, and treatment and prevention of venous thromboembolism and consistently shown to be noninferior to warfarin in safety and efficacy

These agents have a favorable benefit-risk profile for treatment and prevention of thrombotic events but may cause worsening acute major bleeding, which is associated with substantial morbidity and mortality.

Oral factor Xa inhibitors are fiven at fixed dose and do not require monitoring.

Do not interfere with diet and had fewer interactions with other drugs.

Drug elimination involves multiple pathways.

Rapid onset of action obviates the need for heparin in the acute management of venous thrombosis.

Rapid onset of action of such agents as significant implications for appropriate timing of the initiation of such drugs following a surgical procedure, given the need for wound hemostasis.

Oral factor Xa inhibitors rivaroxaban, edoxaban and apixaban.

Oral factor Xa inhibitor metabolism inhibited bt diltiazem.

Renal clearance is 66% in the case of rivaroxaban, 25% in the case of apixaban and 35% in the case of edoxaban.

Compared to warfarin’s half-life of 20-60 hours, half-lives of antidote indicated for patients treated with rivaroxaban or apixaban, when reversal of anticoagulation is needed due to life-threatening or uncontrolled bleeding.

 

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