Rivaroxaban

Class	Factor Xa inhibitor
Chemistry	Oxazolidinone
Routes of administration	Oral only
Absorption	Rapidly absorbed High oral bioavailability (~ 80-100%) Maximum blood concentration about 120-240 minutes after administration
Solubility	pKa 13; practically insoluble in water
Distribution	VOD=0.7L/kg; 95% protein-bound
Metabolism	66% is metabolised in the liver: a substrate of CYP3A4 and CYP2J2. Inactive metabolites are excreted by biliary (50%) and renal (50%) routes
Elimination	33% renal excretion of unchanged drug 66% hepatic metabolism
Time course of action	Half life = 7-12 hrs
Target receptor	Factor Xa
Mechanism of action	Rivaroxaban inhibits free factor Xa as well as prothrombinase-bound and clot-associated factor Xa, in contrast to drugs like fondaparinux which only act on free Xa. Factor Xa is the active form of Factor X (activated by either the intrinsic or extrinsic pathway); its job is to cleave prothrombin into thrombin. Thus, rivaroxaban prevents thrombin generation.
Clinical effects	Bleeding, deranged LFTs, nausea and vomiting (in ~ 10%)
Literature reference	TGA PI document
CICM details of understanding	Level 2
Mentioned around Deranged Physiology	Warfarin and other oral anticoagulants
Related SAQs