Anti-Xa activity in apixaban overdose: a case report

Clin Toxicol (Phila). 2016 Nov;54(9):871-873. doi: 10.1080/15563650.2016.1204453. Epub 2016 Jul 20.

Abstract

Introduction: Apixaban is a novel oral anticoagulation agent that exerts its effect through direct factor Xa inhibition. We present a case of multi-drug overdose including apixaban with associated apixaban concentrations.

Case: A 53 year-old man presented to our metropolitan hospital following a deliberate self-poisoning with 200 mg apixaban, 35 mg ramipril, 105 mg bisoprolol, 280 mg atorvastatin, 6 mg colchicine, 37.4 mg magnesium, 4 × 500 mg paracetamol/9.5 mg codeine/5 mg phenylephrine and alcohol. He developed hypotension that was treated with noradrenaline. His initial and peak apixaban concentration was 1022.6 ng/ml and was associated with only minor bleeding from his femoral central line insertion site, which improved with local compression. Vitamin K 10 mg (at 9 h post-ingestion) and Prothrombinex-VF 2000 units (at 13 h post-ingestion) were also administered without any observed effect on coagulation studies. Apixaban elimination appeared to display first-order kinetics with an elimination half-life of 7.4 h. His plasma apixaban concentration was within the therapeutic dose range 10 h post-ingestion and he recovered uneventfully.

Conclusion: A case of apixaban overdose with associated apixaban concentrations is presented. There was rapid resolution of anticoagulation with no demonstrable benefit of currently available clotting factor replacement.

Keywords: Factor Xa inhibitors; oral anticoagulants; toxicokinetics.

Publication types

  • Case Reports

MeSH terms

  • Administration, Oral
  • Antifibrinolytic Agents / administration & dosage
  • Blood Coagulation Factors / administration & dosage
  • Drug Overdose
  • Factor Xa / drug effects*
  • Factor Xa / metabolism
  • Factor Xa Inhibitors / administration & dosage
  • Factor Xa Inhibitors / pharmacokinetics
  • Factor Xa Inhibitors / poisoning*
  • Half-Life
  • Humans
  • Male
  • Middle Aged
  • Pyrazoles / administration & dosage
  • Pyrazoles / pharmacokinetics
  • Pyrazoles / poisoning*
  • Pyridones / administration & dosage
  • Pyridones / pharmacokinetics
  • Pyridones / poisoning*
  • Vitamin K / administration & dosage*

Substances

  • Antifibrinolytic Agents
  • Blood Coagulation Factors
  • Factor Xa Inhibitors
  • Pyrazoles
  • Pyridones
  • Vitamin K
  • prothrombin complex concentrates
  • apixaban
  • Factor Xa