[Direct oral anticoagulant, useful pharmacological characteristics in clinical practice]

Therapie. 2015 May-Jun;70(3):243-9. doi: 10.2515/therapie/2014206. Epub 2014 Dec 24.
[Article in French]

Abstract

Direct oral anticoagulants offer an alternative to vitamin K antagonist drugs in the prevention and treatment of thromboembolic events. Unlike the latter, they inhibit directly and specifically coagulation factors (Xa, IIa). Their pharmacological properties allow a fixed dose administration and no biological monitoring for the majority of patients. However, their pharmacokinetics dependent of membrane transporters (P-gp) and cytochrome P450 (CYP3A4) expose them to significant drug-drug interactions. Dose adjustment may then become necessary as in some clinical situations, such as kidney and liver failure. However, some questions remain open, particularly on the optimal handling of these molecules in some population (elderly patients, renal and hepatic impairment or polymedicated).

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Administration, Oral
  • Anticoagulants / pharmacokinetics
  • Anticoagulants / pharmacology
  • Anticoagulants / therapeutic use*
  • Cytochrome P-450 CYP3A / metabolism
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Humans
  • Thromboembolism / prevention & control*

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Anticoagulants
  • Cytochrome P-450 CYP3A