Direct thrombin inhibitors

Br J Clin Pharmacol. 2011 Oct;72(4):581-92. doi: 10.1111/j.1365-2125.2011.03916.x.

Abstract

Heparins and vitamin K antagonists have been the primary agents used for anticoagulation in certain cardiovascular and thromboembolic diseases for over 50 years. However, they can be difficult to administer and are fraught with limitations. In response to the need for new anticoagulants, direct thrombin inhibitors (DTIs) have been developed and investigated for their utility in prophylaxis and treatment of venous thromboembolism (VTE), heparin-induced thrombocytopenia (HIT), acute coronary syndromes (ACS), secondary prevention of coronary events after ACS, and nonvalvular atrial fibrillation. Currently, four parenteral direct inhibitors of thrombin activity are FDA-approved in North America: lepirudin, desirudin, bivalirudin and argatroban. Of the new oral DTIs, dabigatran etexilate is the most studied and promising of these agents. This review discusses the clinical indications and efficacy of these direct thrombin inhibitors as well as future directions in anticoagulant therapy.

Publication types

  • Review

MeSH terms

  • Anticoagulants / pharmacology
  • Antithrombins / pharmacology*
  • Arginine / analogs & derivatives
  • Benzimidazoles / therapeutic use
  • Dabigatran
  • Hirudins / pharmacology
  • Humans
  • Peptide Fragments / pharmacology
  • Pipecolic Acids / therapeutic use
  • Pyridines / therapeutic use
  • Recombinant Proteins / pharmacology
  • Sulfonamides
  • Thrombin / antagonists & inhibitors
  • Thrombin / therapeutic use
  • Venous Thromboembolism / prevention & control

Substances

  • Anticoagulants
  • Antithrombins
  • Benzimidazoles
  • Hirudins
  • Peptide Fragments
  • Pipecolic Acids
  • Pyridines
  • Recombinant Proteins
  • Sulfonamides
  • Arginine
  • Thrombin
  • Dabigatran
  • argatroban
  • bivalirudin