Product Information
Registration Status: ActiveENTECAVIR-TEVA FC TABLETS 1MG is approved to be sold in Singapore with effective from 2021-01-31. It is marketed by TEVA PHARMACEUTICAL INVESTMENTS SINGAPORE PTE LTD, with the registration number of SIN16093P.
This product contains Entecavir 1mg in the form of TABLET, FILM COATED. It is approved for ORAL use.
This product is manufactured by Remedica Ltd. in CYPRUS.
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.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Entecavir is an oral antiviral drug used in the treatment of hepatitis B infection. It is marketed under the trade name Baraclude (BMS). Entecavir is a guanine analogue that inhibits all three steps in the viral replication process, and the manufacturer claims that it is more efficacious than previous agents used to treat hepatitis B (lamivudine and adefovir). It was approved by the U.S. Food and Drug Administration (FDA) in March 2005.
Indication
For the treatment of chronic hepatitis B virus infection in adults with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.
Mechanism of Action
By competing with the natural substrate deoxyguanosine triphosphate, entecavir functionally inhibits all three activities of the HBV polymerase (reverse transcriptase, rt): (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Upon activation by kinases, the drug can be incorporated into the DNA which has the ultimate effect of inhibiting the HBV polymerase activity.
Pharmacokinetics
- Absorption
- Absorption Following oral administration in healthy subjects, entecavir peak plasma concentrations occurred between 0.5 and 1.5 hours. In healthy subjects, the bioavailability of the tablet is 100% relative to the oral solution.
- Distribution
- Metabolism
- Entecavir is not a substrate, inhibitor, or inducer of the cytochrome P450 (CYP450) enzyme system. Entecavir is efficiently phosphorylated to the active triphosphate form.
- Elimination
Clearance
* renal cl=383.2 +/- 101.8 mL/min [Unimpaired renal function] * renal cl=197.9 +/- 78.1 mL/min [Mild impaired renal function] * renal cl=135.6 +/- 31.6 mL/min [Moderate impaired renal function] * renal cl=40.3 +/- 10.1 mL/min [severe impaired renal function] * apparent oral cl=588.1 +/- 153.7 mL/min [Unimpaired renal function] * apparent oral cl=309.2 +/- 62.6 mL/min [Mild impaired renal function] * apparent oral cl=226.3 +/- 60.1 mL/min [Moderate impaired renal function] * apparent oral cl=100.6 +/- 29.1 mL/min [severe impaired renal function] * apparent oral cl=50.6 +/- 16.5 mL/min [severe impaired renal function amnaged with Hemodialysis] * apparent oral cl=35.7 +/- 19.6 mL/min [severe impaired renal function amnaged with CAPD]
Toxicity
Healthy subjects who received single entecavir doses up to 40 mg or multiple doses up to 20 mg/day for up to 14 days had no increase in or unexpected adverse events. If overdose occurs, the patient must be monitored for evidence of toxicity, and standard supportive treatment applied as necessary.
Active Ingredient/Synonyms
Anhydrous entecavir | Entecavir | Entecavir (anhydrous) | Entecavir anhydrous | Entecavirum | Entecavir |
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.