[General characteristics of the new oral anticoagulants]

Geriatr Psychol Neuropsychiatr Vieil. 2013 Dec;11(1 Suppl):4-9. doi: 10.1684/pnv.2013.0446.
[Article in French]

Abstract

Treatment with vitamin K antagonists are subject to a common iatrogenic mainly characterized by hemorrhagic stroke. Their narrow therapeutic range associated with variability largely explains this phenomenon. New oral anticoagulants (NOAC) are now available. dabigatran (Pradaxa®) is a direct and specific thrombin inhibitor. It is excreted mainly by the kidney and is the only which can be dialyzed. Rivaroxaban (Xarelto®) and apixaban (Eliquis®) are factor X activated direct inhibitors. They are highly bound to plasma proteins and are metabolized mainly by the liver, via CYP3A4. All NOAC are substrates of P-glycoprotein (P-gp). Due to pharmacological changes, some populations at risk were identified: patients with hepatic impairment, renal impairment, elderly patients or low weight. Some pharmacokinetic or pharmacodynamic drug interactions alter the concentration and the expected impact of NOAC. The NOAC does not require biological monitoring. They interfere with the routine coagulation tests which should be interpreted with caution. Specific tests exist and can be used in case of emergencies. Currently, no antidote is available. The new oral anticoagulant look promising in the elderly. However, certain rules must be followed to reduce the risk of iatrogenic.

Keywords: biological monitoring; new oral anticoagulants; pharmacological characteristics; population at risks.

Publication types

  • English Abstract
  • Review

MeSH terms

  • Administration, Oral
  • Aged
  • Anticoagulants / adverse effects
  • Anticoagulants / pharmacokinetics
  • Anticoagulants / therapeutic use*
  • Benzimidazoles / adverse effects
  • Benzimidazoles / pharmacokinetics
  • Benzimidazoles / therapeutic use
  • Cerebral Infarction / prevention & control*
  • Dabigatran
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Drugs, Investigational / adverse effects
  • Drugs, Investigational / pharmacokinetics
  • Drugs, Investigational / therapeutic use*
  • Humans
  • Iatrogenic Disease
  • Intracranial Hemorrhages / chemically induced
  • Morpholines / adverse effects
  • Morpholines / pharmacokinetics
  • Morpholines / therapeutic use
  • Pyrazoles / adverse effects
  • Pyrazoles / pharmacokinetics
  • Pyrazoles / therapeutic use
  • Pyridones / adverse effects
  • Pyridones / pharmacokinetics
  • Pyridones / therapeutic use
  • Risk Factors
  • Rivaroxaban
  • Stroke / chemically induced
  • Thiophenes / adverse effects
  • Thiophenes / pharmacokinetics
  • Thiophenes / therapeutic use
  • Vitamin K / antagonists & inhibitors
  • beta-Alanine / adverse effects
  • beta-Alanine / analogs & derivatives
  • beta-Alanine / pharmacokinetics
  • beta-Alanine / therapeutic use

Substances

  • Anticoagulants
  • Benzimidazoles
  • Drugs, Investigational
  • Morpholines
  • Pyrazoles
  • Pyridones
  • Thiophenes
  • beta-Alanine
  • Vitamin K
  • apixaban
  • Rivaroxaban
  • Dabigatran