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Oral antithrombotic treatment in 2012 - new molecules, new processes

Publication at First Faculty of Medicine, Third Faculty of Medicine |
2012

Abstract

There are two new groups of anticoagulants being introduced into pharmacotherapy of patients indicated for anticoagulation therapy for the purpose of prevention and treatment of venous thrombosis and prophylaxis of thromboembolic events - gatrans and xabans. The former group, represented by dabigatran directly inhibits thrombin.

The latter group includes two medications developed for clinical use - rivaroxaban and apixaban - inhibit the Xa factor. Apart from the above mentioned peroral effects as such, other benefits of these medications include a quick onset of action (counted in tens of minutes), sufficiently long duration of their effect enabling them to be administered in one or two doses per day, and predictability of their effects, with little individual variation, which makes constant monitoring during the course of treatment unnecessary.

Their shared disadvantage is the lack of knowledge of a specific antidote. For prophylaxis of thromboembolic events in patients suffering from atrial fibrillation, i.e. their most important indication, dabigatran and rivaroxaban have been approved for therapeutic use, apixaban is currently going through the registration proceedings.

In comparison to the hitherto used warfarin, there are clear advantages on the side of the new medications, both in terms of the lack of necessity to monitor the therapy, but also in terms of improved safety and efficacy. For another of the important indications - prevention of thromboembolic diseases in patients with prosthetic joints - all three substances are being used.

For the remaining widespread indication - treatment of venous thrombosis, pulmonary embolism and secondary prophylaxis of such events - approvals for rivaroxaban and dabigatran are being expected. Apart from these established medications, another three are in the stage of clinical evaluation: edoxaban, otamixaban, betrixaban, etc.