Vaskulárna medicína 1/2019

Rivaroxaban – metabolism, pharmacologic properties and drug interactions

Rivaroxaban represents a selective direct inhibitor of activated coagulation factor X (FXa). The absorbtion of rivaroxaban is quick, reaching maximum plasma concentration 2-4 hours following its administration. Peroral bioavailability is high (80-100 %) and pharmacokinetic variability is considered to be moderate (coefficient of variation 30-40 %). The drug is administered in several indications in adults: prophylaxis of venous thromboembolism (VTE) following elective knee or hip replacement surgical intervention, therapy and secondary prophylaxis of VTE, prophylaxis of ischemic stroke and embolism in individuals diagnosed with nonvalvular atrial fibrillation (NVAF) with risky characteristics, and in the prophylaxis of atherothrombotic episodes following an acute coronary syndrome in subjects with increased levels of cardiac biomarkers. Unlike the vitamin K antagonists (VKAs), these anticoagulant drugs offer predictable pharmacokinetic and pharmacodynamic properties, a low probability of drug-drug interactions, and can be administered in fixed doses with no requirement for regular monitoring of coagulation parameters. However, adjustments of dose are needed in individuals with impaired renal functions.

Keywords: antikoagulancia, rivaroxaban, tromboembolie, fibrilace síní, farmakodynamika