In vivo increase in thrombin generation by four-factor prothrombin complex concentrate in apixaban-treated healthy volunteers

J Thromb Haemost. 2015 Oct;13(10):1799-805. doi: 10.1111/jth.13115. Epub 2015 Sep 21.

Abstract

Background: Four-factor prothrombin complex concentrate (PCC) (Cofact; Sanquin Blood Supply) 50 IU kg(-1) increased thrombin generation beyond baseline values in healthy, rivaroxaban-treated subjects.

Objective: To assess whether infusion with doses of 37.5 IU kg(-1) and 25 IU kg(-1) PCC reverses the anticoagulant effect of high-dose apixaban, another oral direct factor Xa inhibitor.

Methods: In a randomized, double-blind, placebo-controlled, crossover study, six healthy subjects received twice-daily apixaban 10 mg for 3.5 days followed by a single bolus of 37.5 IU kg(-1) PCC, 25 IU kg(-1) PCC, or placebo. The primary outcome was the effect of PCC 15 min after infusion on thrombin generation (endogenous thrombin potential [ETP]); secondary outcomes were the immediate effect of PCC on prothrombin time (PT) and the effect of PCC as compared with placebo over a period of 24 h on ETP and PT.

Results: Fifteen minutes after infusion of 37.5 IU kg(-1) and 25 IU kg(-1) PCC, ETP increased from 41% ± 11% to 56% ± 23% (P = 0.06) and from 44% ± 12% to 51% ± 15% (P = 0.03), respectively. ETP significantly differed over time between 37.5 IU kg(-1) PCC and placebo during 24 h after infusion (P < 0.01). Both PCC doses restored apixaban-induced PT prolongation after 15 min (P < 0.01), and this was sustained over a period of 24 h.

Conclusion: Both 37.5 IU kg(-1) PCC and 25 IU/kg PCC improved coagulation parameters in healthy subjects, suggesting partial reversal of the anticoagulant effect of apixaban. This implies that PCC might be considered in patients with apixaban-associated bleeding. However, ETP was not immediately restored to pre-apixaban levels, suggesting that these doses are too low to instantly and fully restore hemostasis at peak apixaban levels.

Keywords: anticoagulants; apixaban; factor Xa inhibitors; hemorrhage; prothrombin complex concentrates; randomized controlled trial.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Biomarkers / blood
  • Blood Coagulation / drug effects*
  • Blood Coagulation Factors / administration & dosage*
  • Blood Coagulation Tests
  • Cross-Over Studies
  • Double-Blind Method
  • Drug Administration Schedule
  • Factor Xa Inhibitors / administration & dosage*
  • Healthy Volunteers
  • Humans
  • Injections, Intravenous
  • Male
  • Netherlands
  • Pyrazoles / administration & dosage*
  • Pyridones / administration & dosage*
  • Thrombin / metabolism*
  • Time Factors
  • Young Adult

Substances

  • Biomarkers
  • Blood Coagulation Factors
  • Factor Xa Inhibitors
  • Pyrazoles
  • Pyridones
  • prothrombin complex concentrates
  • apixaban
  • Thrombin