[From heparin to apixaban: anticoagulants cut both ways?]

Zentralbl Chir. 2014 Feb;139(1):89-97. doi: 10.1055/s-0032-1328004. Epub 2013 Mar 4.
[Article in German]

Abstract

Background: Regarding anticoagulant therapies there has been a remarkable shift in recent years. The objective of this brief overview is to provide relevant information and guidelines on the advantages and disadvantages of novel anticoagulants addressing specifically the surgical disciplines. Hitherto, conventional anticoagulant therapy in patients with a high thrombosis risk was largely limited to heparins and vitamin-K antagonists (VKA). Their modes of action, the difficulties in managing VKAs (e.g., bridging therapy) and the risk of HIT (heparin-induced thrombocytopenia) associated with heparins are briefly discussed. Novel anticoagulants supposedly eliminate these obstacles. Fondaparinux (Arixtra®) is a fully synthetic pentasaccharide which acts like a heparin but has an increased half life. Fondaparinux has a diminished risk of HIT. However, no specific antidote is currently available for Fondaparinux. The novel oral anticoagulants (NOAC) dabigatran etexilat (Pradaxa®), rivaroxaban (Xarelto®) and apixaban (Eliquis®), also known as "direct" anticoagulants, act independently from antithrombin by inhibiting thrombin, as in the case of dabigatran, or by inhibiting factor Xa, as in the case of rivaroxaban and apixaban. It is assumed that they are suitable for long-term use and do not require laboratory monitoring. Nevertheless, clinical experience is very limited and caution rather than quick conclusions is necessary. Two major drawbacks are on the one hand the risk of drug accumulation in kidney and/or liver disease and, on the other hand, the lack of specific antidotes. In addition, interactions with other medication may have unexpected effects on serum drug levels. Therefore, the analysis of drug levels in the plasma may become necessary in subgroups of patients.

Discussion and conclusion: Studies establishing clear recommendations for the desirable and measurable reference range are needed. Similarly, evidence-based recommendations regarding perioperative prevention of thrombosis are required ("bridging": yes or no?). Irrespective of these issues, the authors predict a further expansion of the use of NOACs.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Administration, Oral
  • Anticoagulants / adverse effects
  • Anticoagulants / pharmacokinetics
  • Anticoagulants / therapeutic use*
  • Benzimidazoles / adverse effects
  • Benzimidazoles / therapeutic use
  • Blood Coagulation Tests
  • Dabigatran
  • Drug Interactions
  • Factor Xa Inhibitors
  • Fondaparinux
  • Heparin / pharmacokinetics
  • Heparin / therapeutic use*
  • Humans
  • International Normalized Ratio
  • Liver Failure / blood
  • Liver Failure / complications
  • Metabolic Clearance Rate / physiology
  • Morpholines / adverse effects
  • Morpholines / therapeutic use
  • Perioperative Care
  • Polysaccharides / adverse effects
  • Polysaccharides / pharmacokinetics
  • Polysaccharides / therapeutic use
  • Pyrazoles / pharmacokinetics
  • Pyrazoles / therapeutic use*
  • Pyridines / adverse effects
  • Pyridines / therapeutic use
  • Pyridones / pharmacokinetics
  • Pyridones / therapeutic use*
  • Renal Insufficiency / blood
  • Renal Insufficiency / complications
  • Rivaroxaban
  • Thiophenes / adverse effects
  • Thiophenes / therapeutic use
  • Thrombocytopenia / blood
  • Thrombocytopenia / chemically induced
  • Thrombocytopenia / drug therapy
  • Thrombosis / blood
  • Thrombosis / drug therapy*
  • Thrombosis / prevention & control
  • Vitamin K / antagonists & inhibitors

Substances

  • Anticoagulants
  • Benzimidazoles
  • Factor Xa Inhibitors
  • Morpholines
  • Polysaccharides
  • Pyrazoles
  • Pyridines
  • Pyridones
  • Thiophenes
  • Vitamin K
  • apixaban
  • Heparin
  • Rivaroxaban
  • Dabigatran
  • Fondaparinux