Product Information
Registration Status: ActiveELIQUIS TABLET 2.5MG is approved to be sold in Singapore with effective from 2012-12-24. It is marketed by PFIZER PTE LTD, with the registration number of SIN14279P.
This product contains Apixaban 2.5mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by BRISTOL-MYERS SQUIBB MANUFACTURING COMPANY in PUERTO RICO, andBRISTOL-MYERS SQUIBB S.R.L (Primary and secondary packager) in ITALY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Apixaban is an oral, direct, and highly selective factor Xa (FXa) inhibitor (of both free and prothrombinase-bound FXa independently of antithrombin III) for the prevention and treatment of thromboembolic diseases. It is marketed under the name Eliquis. FDA approved on December 28, 2012.
Indication
Apixaban is to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. It has also been used to lower the risk of developing venous thrombosis post-orthopedic surgical procedures.
Mechanism of Action
Apixaban acts by directly inhibiting, in a reversible manner, free and clot-bound factor Xa to inhibit coagulation.
Pharmacokinetics
- Absorption
- Apixaban is absorbed in the stomach and small intestine. For doses up to 10 mg, the absolute bioavailability is about 50%. For oral administration, absorption is not affected by the presence of food, and it takes about 3-4 hours to achieve maximum plasma concentrations. For large oral doses equal or greater than 25 mg, absorption is dissolution limited and bioavailability is decreased. Most of the absorption occurs in the distal small intestine and the ascending colon.
- Distribution
- The steady state volume of distribution is 21 L.
- Metabolism
- Apixaban mainly undergoes o-demethylation and hydroxylation to metabolites. The major site of biotransformation is at the 3-oxopiperidinyl moiety. The main enzyme responsible for metabolism is CYP3A4/5 while CYP1A2, 2C8, 2C9, 2C19, and 2J2 are minor metabolic enzymes. There are no active metabolites and unchanged apixaban is the primary circulating entity.
- Elimination
Clearance
About 27% of total apixaban is renally cleared.
Toxicity
Major bleeding events.
Active Ingredient/Synonyms
apixabán | apixabanum | Apixaban |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.