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Pharmacology: Pharmacodynamics: Mechanism of action: Apixaban is an oral, reversible, direct and selective active site inhibitor of factor Xa (FXa). It does not require a cofactor (antithrombin III) for antithrombotic activity. Apixaban inhibits free and clot-bound FXa and prothrombinase activity, resulting in decreased thrombin generation and thrombus development.
Pharmacokinetics: Apixaban is rapid absorbed with an absolute bioavailability of about 50% and peak plasma concentrations are reached 3-4 hours after oral administration. Plasma protein binding is about 87%. Apixaban is metabolized in the liver mainly via the P450 cytochromes CYP3A4, CYP3A5 and is excreted renally and in the feces as unchanged drug and inactive metabolites. The half-life is about 12 hours.
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