Newer Oral Anticoagulant Agents: A New Era in Medicine

Abstract

After a gap of almost 60 years following the development of warfarin, 2 new categories of oral anticoagulant agents have been approved for clinical use – the direct thrombin inhibitors and factor Xa inhibitors. These agents promise to be more convenient to administer with fixed dosing but still have equivalent efficacy and improved bleeding risk compared to warfarin. The clinical community is looking forward to the widespread usage of these agents but there is also some apprehension regarding bleeding risks, non-availability of specific reversal strategies and lack of specific monitoring parameters. This review article will attempt to educate the reader about three representative drugs from these classes: Dabigatran, Rivaroxaban and Apixaban. We will discuss the historical perspective to the development of these drugs, available research data and pharmacology of these agents. The best strategies for monitoring and reversal of these drugs in special situations will also be touched upon.

Crystal structure of (S)-5-chloro-N-({2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]oxazolidin-5-yl}methyl)thiophene-2-carboxamide

“…In anticoagulants, warfarin and heparin have dominated the market, but they have some defects such as making making patients bleed easily and be prone to thrombocytopenia and osteoporosis (Mega & Carreras, 2012). In recent years, factor Xa inhibitors, the new type of anticoagulant drugs, have received more and more attention, and rivaroxaban is a representative drug of factor Xa inhibitors (Goel & Srivathsan, 2012).…”

Anticoagulant therapy and its impact on dental patients: a review

“…6 This is achieved in two ways; by preventing the formation of a clot, and by slowing the progression of an existing clot. 7 The mechanisms of existing anticoagulant agents are based on our understanding of the coagulation cascade, and with an improved understanding of pharmacology and coagulation pathways, there has been a recent trend towards more specific anticoagulant therapy. 4,7 This trend has occurred due to the limitations of older anticoagulants, such as heparins and vitamin K antagonists (VKA), which can have a narrow therapeutic window and an unpredictable effect on coagulation, requiring laboratory monitoring to ensure safety and efficacy.…”

“…7 The mechanisms of existing anticoagulant agents are based on our understanding of the coagulation cascade, and with an improved understanding of pharmacology and coagulation pathways, there has been a recent trend towards more specific anticoagulant therapy. 4,7 This trend has occurred due to the limitations of older anticoagulants, such as heparins and vitamin K antagonists (VKA), which can have a narrow therapeutic window and an unpredictable effect on coagulation, requiring laboratory monitoring to ensure safety and efficacy. 1,4,[6][7][8][9] One of the most commonly encountered anticoagulants in Australia remains warfarin, despite its unpredictable pharmacological nature.…”

“…4,7 This trend has occurred due to the limitations of older anticoagulants, such as heparins and vitamin K antagonists (VKA), which can have a narrow therapeutic window and an unpredictable effect on coagulation, requiring laboratory monitoring to ensure safety and efficacy. 1,4,[6][7][8][9] One of the most commonly encountered anticoagulants in Australia remains warfarin, despite its unpredictable pharmacological nature. 10 The ability of warfarin to be administered orally meant that it remained the first-choice anticoagulant, over parenteral alternatives such as heparin.…”

“…3,7,8,11 A number of these medications, termed novel oral anticoagulants (NOACs), have been approved for use in Australia by the Therapeutic Goods Administration (TGA). The drugs that have been approved by the TGA at this time are dabigatran (Pradaxa â ), rivaroxaban (Xarelto â ) and apixaban (Eliquis â ), and they are increasingly being used to overcome problems associated with warfarin use.…”