Effect of Activated Charcoal on Rivaroxaban Complex Absorption

Area of Science:

• Pharmacokinetics
• Drug Absorption
• Toxicology

Background:

• Rivaroxaban is an anticoagulant with a narrow therapeutic index.
• Activated charcoal is a common adsorbent used to treat poisonings and overdoses.
• The efficacy of activated charcoal in reducing rivaroxaban exposure requires quantification.

Purpose of the Study:

• To quantify the impact of activated charcoal (AC) on rivaroxaban exposure in healthy volunteers.
• To evaluate the effect of delayed AC administration on rivaroxaban absorption.

Main Methods:

• Open-label, incomplete cross-over study in 12 healthy volunteers.
• Single-dose rivaroxaban (40 mg) administered alone or with AC at 2, 5, or 8 hours post-dose.
• Pharmacokinetic analysis using non-linear mixed-effect modeling.

Main Results:

• Activated charcoal significantly reduced rivaroxaban exposure.
• Reductions were 43% at 2h, 31% at 5h, and 29% at 8h post-dose.
• Model simulations indicated potential effects even beyond 8 hours post-dose.

Conclusions:

• Activated charcoal effectively reduces rivaroxaban exposure, irrespective of administration time up to 8 hours.
• AC administration is a viable strategy for managing rivaroxaban overdose or accidental ingestion.
• This study supports the use of AC as an antidote to limit rivaroxaban absorption.