Lethal cerebral hemorrhage after ticagrelor intoxication: a specific antidote is urgently needed

Clin Toxicol (Phila). 2018 Dec;56(12):1200-1203. doi: 10.1080/15563650.2018.1480026. Epub 2018 Jun 11.

Abstract

Background: Ticagrelor is a direct and reversible competitive antagonist of the P2Y12 receptor and inhibits platelet activation. Although adverse bleeding is common, fatal intoxication has never been documented.

Case description: A 47-year-old man died from a severe cerebral hemorrhage secondary to a fall and cranial trauma 4 d after the massive intake of ticagrelor. Iterative platelet transfusions did not improve his condition. Toxicological analyses by liquid chromatography tandem mass spectrometry (LC-MS/MS) revealed high plasma concentrations of ticagrelor (3343 µg/L) and its active metabolite AR-C124910XX (656 µg/L) 10 h after intake. The approximate ingested dose was extrapolated to 1677 mg. Assessment of ADP-induced platelet aggregation and platelet Vasodilator Stimulated Phosphoprotein phosphorylation (VASP), 2 and 3 d after admission, respectively, showed the persistence of platelet inhibition.

Discussion: To the best of our knowledge, no prior fatal cases have been reported and documented with both ticagrelor and AR-C124910XX concentrations. Our findings highlight the need for a specific antidote to manage such complications resulting from ticagrelor overdose.

Keywords: Ticagrelor; antiplatelet therapy; fatal intoxication; platelet transfusion.

Publication types

  • Case Reports

MeSH terms

  • Accidental Falls
  • Antidotes / therapeutic use*
  • Cerebral Hemorrhage / chemically induced*
  • Cerebral Hemorrhage / diagnostic imaging
  • Cerebral Hemorrhage / therapy
  • Fatal Outcome
  • Hemostasis
  • Humans
  • Male
  • Middle Aged
  • Platelet Aggregation Inhibitors / analysis
  • Platelet Aggregation Inhibitors / poisoning*
  • Platelet Transfusion
  • Purinergic P2Y Receptor Antagonists / analysis
  • Purinergic P2Y Receptor Antagonists / poisoning*
  • Tandem Mass Spectrometry
  • Ticagrelor / analysis
  • Ticagrelor / poisoning*
  • Tomography, X-Ray Computed

Substances

  • Antidotes
  • Platelet Aggregation Inhibitors
  • Purinergic P2Y Receptor Antagonists
  • Ticagrelor