Absorption Time of Eliquis (Apixaban)
Eliquis (apixaban) is rapidly absorbed after oral administration, with maximum plasma concentrations (Cmax) appearing 3 to 4 hours after ingestion. 1
Pharmacokinetic Profile of Apixaban
Absorption Characteristics
- Apixaban has an absolute bioavailability of approximately 50% 1
- Onset of action is rapid, occurring within 1-4 hours after oral administration 2
- Peak plasma concentration (Cmax) is reached at 3-4 hours post-dose 1, 3
- Food does not affect the bioavailability of apixaban, meaning it can be taken with or without meals 1, 3
Distribution and Elimination
- Plasma protein binding is approximately 87% 1
- Terminal elimination half-life is approximately 12 hours 1, 3
- Multiple elimination pathways:
- 27% renal excretion
- Remaining elimination via biliary excretion and direct intestinal excretion 1
Clinical Implications of Apixaban's Absorption Profile
Anticoagulant Effect Timeline
- Anticoagulant effect begins shortly after absorption starts
- The pharmacodynamic effect correlates closely with plasma concentration 4
- Full anticoagulant effect is achieved when peak plasma levels are reached (3-4 hours)
- Effect on coagulation parameters:
- Prolongs prothrombin time (PT)
- Increases International Normalized Ratio (INR)
- Extends activated partial thromboplastin time (aPTT) 1
Perioperative Management Considerations
- For high-risk endoscopic procedures, apixaban should be discontinued 2 days before the procedure in patients with normal renal function (CrCl >80 mL/min) 2
- The rapid onset and offset of action (about 24 hours) of direct oral anticoagulants including apixaban must be considered when planning procedures 2
Special Population Considerations
- Renal impairment: Apixaban is less affected by renal impairment (only
25% renal elimination) compared to other DOACs like dabigatran (80% renal elimination) 2 - Hepatic impairment: Changes in anti-FXa activity were similar in patients with mild-to-moderate hepatic impairment and healthy subjects 1
Important Clinical Pearls
- Unlike vitamin K antagonists (e.g., warfarin), apixaban has a predictable pharmacokinetic profile that doesn't require routine monitoring 5
- In cases of overdose, activated charcoal may be effective if administered within 3 hours of ingestion 2
- The short absorption time and predictable pharmacokinetics contribute to apixaban's favorable safety profile compared to traditional anticoagulants 5
- When transitioning between anticoagulants, the rapid onset of apixaban's action (within hours) must be considered to avoid periods of either inadequate or excessive anticoagulation
Remember that the rapid absorption profile of apixaban (peak levels at 3-4 hours) is a key factor in its clinical utility but also requires careful timing when discontinuing before procedures or managing potential bleeding complications.