African Journal of
Pharmacy and Pharmacology

  • Abbreviation: Afr. J. Pharm. Pharmacol.
  • Language: English
  • ISSN: 1996-0816
  • DOI: 10.5897/AJPP
  • Start Year: 2007
  • Published Articles: 2285

Full Length Research Paper

Pharmacological profile of non-vitamin K antagonist oral anticoagulants

Rose Mary Ferreira Lisboa da Silva
  • Rose Mary Ferreira Lisboa da Silva
  • Department of Internal Medicine, Faculty of Medicine, Federal University of Minas Gerais, Brazil.
  • Google Scholar


  •  Received: 05 February 2017
  •  Published: 08 March 2017

Abstract

The non-vitamin K antagonist oral anticoagulants have been approved since 2008 for the prevention of systemic embolism and stroke in patients with non-valvular atrial fibrillation with prior stroke, transient ischemic attack, or CHA2DS2-VASc score ≥2. According to the latest guidelines of 2016, if CHA2DS2-VASc score ≥2 for all male patients or if CHA2DS2-VASc score ≥3 for all female patients, oral anticoagulants are recommended, and considering shared decision between doctor and patient. However, they are contraindicated in patients with mechanical prosthetic valve and in patients with moderate-to-severe mitral stenosis and atrial fibrillation. They have also been approved for prevention and treatment of deep vein thrombosis and pulmonary embolism. Dabigatran, a direct thrombin inhibitor, was the first to be approved, followed by the factor Xa inhibitors, rivaroxaban, apixaban, and recently, in 2015, edoxaban. They have advantages such as the use of fixed-dose, with infrequent drug interaction, rapid onset of action and do not require monitoring of their anticoagulant action. Nonetheless, they have different half-lives, the need for dose adjustment according to renal function, weight and age of the patient. Its use in pregnant women and children or adolescents is not well established. There are also peculiarities about the risks of bleeding, effects on coagulation tests and specific antidotes. Through this review we discuss the pharmacokinetics and pharmacodynamics characteristics of direct oral anticoagulants, its indications, interactions and contraindications. Analysis of its efficacy, safety and risk-benefit ratio will also be addressed.

 

Key words: Anticoagulants agents, dabigatran, rivaroxaban, apixaban, edoxaban, pharmacokinetics, pharmacodynamics, systemic embolism.