Rivaroxaban for the treatment and prevention of thromboembolic disease

J Pharm Pharmacol. 2015 Aug;67(8):1119-32. doi: 10.1111/jphp.12387. Epub 2015 Jun 9.

Abstract

Objectives: A number of direct oral anticoagulants are now available and offer alternative strategies for anticoagulation therapy. Rivaroxaban, a direct oral Factor Xa inhibitor, is approved for use across several thromboembolic indications. This article aims to provide an overview of the key pharmacological characteristics of rivaroxaban and the rationale and evidence for the use of different dose regimens across its licenced indications, and offer practical guidance to healthcare professionals on responsible use. References were sourced via PubMed searches using the search string (rivaroxaban AND (pharmacokinetics OR pharmacodynamics OR (clinical studies) OR (drug interaction)) NOT review NOT (children OR pediatrics OR paediatrics OR adolescent)).

Key findings: Rivaroxaban exhibits predictable pharmacokinetics and pharmacodynamics, and thus does not require routine coagulation monitoring, unlike vitamin K antagonists (e.g. warfarin). Rivaroxaban also has a lower potential for drug-drug and food-drug interactions compared with warfarin; however, co-administration with strong inhibitors of both cytochrome P450 3A4 and P-glycoprotein is not recommended. The data indicate that dose adjustment is not necessary for age, gender or body weight. The dosing regimens of rivaroxaban vary depending on the indication, and phase III studies have demonstrated a favourable benefit-risk profile of rivaroxaban compared with traditional standard of care.

Summary: Rivaroxaban may offer an anticoagulant option that could simplify and improve the management of patients with thromboembolic disorders.

Keywords: anticoagulant; pharmacodynamics; pharmacokinetics; rivaroxaban; thromboembolism.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Administration, Oral
  • Anticoagulants / pharmacology
  • Anticoagulants / therapeutic use*
  • Atrial Fibrillation / drug therapy
  • Clinical Trials as Topic
  • Cytochrome P-450 CYP3A / metabolism
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Factor Xa Inhibitors / pharmacology
  • Factor Xa Inhibitors / therapeutic use*
  • Humans
  • Pulmonary Embolism / drug therapy
  • Rivaroxaban / pharmacology
  • Rivaroxaban / therapeutic use*
  • Thromboembolism / drug therapy*
  • Thromboembolism / physiopathology
  • Venous Thrombosis / drug therapy

Substances

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