Comparison of three-factor and four-factor prothrombin complex concentrates regarding reversal of the anticoagulant effects of rivaroxaban in healthy volunteers

J Thromb Haemost. 2014 Sep;12(9):1428-36. doi: 10.1111/jth.12599. Epub 2014 Jul 24.

Abstract

Background: Four-factor prothrombin complex concentrates (PCCs), which contain factor II, FVII, FIX, and FX, have shown the potential to reverse the anticoagulant effect of rivaroxaban in healthy volunteers. The purpose of this study was to determine whether a three-factor PCC, which contains little FVII, has a similar effect.

Methods and results: We performed an open-label, single-center, parallel-group study comparing the effect of a three-factor PCC (Profilnine SD) with that of a four-factor PCC (Beriplex P/N) on the pharmacodynamics of rivaroxaban in 35 healthy volunteers. After receiving 4 days of rivaroxaban 20 mg twice daily to obtain supratherapeutic steady-state concentrations, volunteers were randomized to receive a single 50 IU kg(-1) bolus dose of four-factor PCC, three-factor PCC or saline 4 h after the morning dose of rivaroxaban on day 5, and the effects of these interventions on prothrombin time and thrombin generation were determined. Within 30 min, four-factor PCC reduced mean prothrombin time by 2.5-3.5 s, whereas three-factor PCC produced only a 0.6-1.0-s reduction. In contrast, three-factor PCC reversed rivaroxaban-induced changes in thrombin generation more than four-factor PCC.

Conclusions: This study demonstrates the potential of both three-factor and four-factor PCCs to at least partially reverse the anticoagulant effects of rivaroxaban in healthy adults. The discrepant effects of the PCC preparations may reflect differences in the procoagulant components present in each.

Keywords: anticoagulants; hemorrhage; pharmacology; prothrombin complex concentrates; rivaroxaban.

Publication types

  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Anticoagulants / administration & dosage*
  • Area Under Curve
  • Blood Coagulation Factors / administration & dosage*
  • Body Mass Index
  • Drug Administration Schedule
  • Drug Combinations
  • Factor IX / administration & dosage*
  • Factor VII / administration & dosage*
  • Factor VII / therapeutic use
  • Factor X / administration & dosage*
  • Female
  • Healthy Volunteers
  • Hemorrhage / prevention & control
  • Humans
  • Male
  • Middle Aged
  • Morpholines / administration & dosage*
  • Partial Thromboplastin Time
  • Prothrombin / administration & dosage*
  • Prothrombin Time
  • Rivaroxaban
  • Thiophenes / administration & dosage*
  • Thrombin / chemistry
  • Time Factors
  • Treatment Outcome
  • Young Adult

Substances

  • Anticoagulants
  • Blood Coagulation Factors
  • Drug Combinations
  • Morpholines
  • Thiophenes
  • factor IX, factor VII, factor X, prothrombin drug combination
  • prothrombin complex concentrates
  • Factor VII
  • Prothrombin
  • Factor IX
  • Factor X
  • Rivaroxaban
  • Thrombin
  • Profilnine SD