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Anti-Xa activity in apixaban overdose: a case report
James Barton1, Anselm Wong1,2, Andis Graudins1,2
1a Monash Clinical Toxicology, Program of Emergency Medicine , Monash Health , Victoria , Australia.
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.
Insights
This case study details a significant apixaban overdose, monitoring its concentration and elimination. The patient recovered with rapid resolution of anticoagulation, showing no benefit from clotting factor replacement.
Area of Science:
- Pharmacology
- Toxicology
- Clinical Medicine
Background:
- Apixaban is a direct factor Xa inhibitor used for anticoagulation.
- Overdose cases are rare, necessitating understanding of its pharmacokinetic profile.
Observation:
- A 53-year-old male ingested 200 mg of apixaban along with multiple other medications and alcohol.
- He developed hypotension requiring noradrenaline and presented with a peak apixaban concentration of 1022.6 ng/ml.
- Minor bleeding at a central line site resolved with compression; Vitamin K and Prothrombinex-VF had no effect.
Findings:
- Apixaban elimination followed first-order kinetics with a half-life of 7.4 hours.
- Plasma apixaban levels normalized to therapeutic range within 10 hours post-ingestion.
- No significant bleeding complications occurred despite high apixaban concentrations.
Implications:
- This case provides valuable data on apixaban pharmacokinetics in overdose.
- Current reversal agents may not be effective for apixaban-induced anticoagulation.
- Understanding apixaban elimination is crucial for managing overdose scenarios.
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