This information is intended for healthcare professionals based in Ireland.

PK/PD

Absorption, distribution and metabolism

The pharmacodynamics effects of ELIQUIS® are reflective of the mechanism of action (FXa inhibition)

  • The absolute bioavailability of ELIQUIS® is approximately 50% for doses up to 10 mg. ELIQUIS® is rapidly absorbed with maximum concentrations (Cmax) appearing 3 to 4 hours after tablet intake. Intake with food does not affect ELIQUIS® AUC or Cmax at the 10 mg dose. ELIQUIS® can be taken with or without food.1
  • ELIQUIS® demonstrates linear pharmacokinetics with dose proportional increases in exposure for oral doses up to 10 mg. At doses ≥25 mg ELIQUIS® displays dissolution limited absorption with decreased bioavailability. ELIQUIS® exposure parameters exhibit low to moderate variability reflected by a within-subject and inter-subject variability of ~20% CV* and ~30% CV, respectively.1
  • ELIQUIS® has multiple routes of elimination. Of the administered ELIQUIS® dose in humans, approximately 25% was recovered as metabolites, with the majority recovered in faeces.1 Renal excretion of ELIQUIS® accounts for approximately 27% of total clearance. Additional contributions from biliary and direct intestinal excretion were observed in clinical and nonclinical studies, respectively.
  • ELIQUIS® has a total clearance of about 3.3 l/h and a half-life of approximately 12 hours.1

  Multiple routes of elimination of ELIQUIS®

multiple routes of elimination of eliquis (apixaban) image

Multiple routes of elimination of ELIQUIS®

Drug- drug interactions

No dose adjustment is necessary with many common concomitant therapies¹

  • Amiodarone
  • Atenolol
  • Digoxin
  • Diltiazem
  • Famotidine
  • Naproxen
  • Quinidine
  • Verapamil
  • ELIQUIS® is not recommended in patients receiving strong inhibitors** of both CYP3A4 and P-gp,
    • such as azole antimycotics (e.g. ketoconazole) and HIV protease inhibitors (e.g. ritonavir).1
  • Strong inducers*** of both CYP3A4 and P-gp should be co-administered with caution in patients with NVAF and for the prevention of recurrent DVT and PE, but no dose adjustment of ELIQUIS® is required1. In patients treated for DVT or PE, apixaban use is not recommended since efficacy may be compromised1

 Interactions with medicinal products affecting haemostasis¹

interactions with medicinal products affecting haemostasis image

Food interactions

  • ELIQUIS® is rapidly absorbed with maximum concentrations (Cmax) appearing 3 to 4 hours after tablet intake.1
  • Intake with food does not affect ELIQUIS® AUC or Cmax at the 10 mg dose.1
  • ELIQUIS® can be taken with or without food.1

PK according to age and gender

  • Elderly patients (above 65 years) exhibited higher plasma concentrations than younger patients, with mean AUC values being approximately 32% higher and no difference in Cmax.1
  • Exposure to ELIQUIS® was approximately 18% higher in females than in males.1

*coefficient of variation
**Strong inhibitors may increase ELIQUIS exposure
***Strong inducers may reduce ELIQUIS exposure

Risk Minimisation Materials

The Eliquis (apixaban) Prescriber Guide and Patient Alert Card are risk minimisation materials developed for all indications as an aid to prescribing, in particular they are aimed at increasing awareness about the potential risk of bleeding during treatment with apixaban and providing guidance on how to manage that risk. Printed copies of these educational materials may be obtained by contacting the Bristol-Myers Squibb Medical Information Department (telephone: 1800 749 749; e-mail: medical.information@bms.com). Alternatively, electronic copies can be accessed via the HPRA website at http://www.hpra.ie/homepage/medicines/medicines-information/find-a-medicine.

References:

  1. ELIQUIS® (apixaban) Summary of Product Characteristics.