Entecavir


Generic Medicine Info
Indications and Dosage
Oral
Chronic hepatitis B
Adult: Compensated liver disease: Nucleoside treatment-naive patients: 0.5 mg once daily; Lamivudine-refractory patients: 1 mg once daily. Decompensated liver disease patients: 1 mg once daily.
Child: Dosage recommendations may vary among countries. Refer to specific product guidelines.
Renal Impairment
Nucleoside treatment-naive patients:
CrCl (mL/min) Dosage 
<10
0.05 mg once daily or 0.5 mg every 5-7 days. 
10-29
0.15 mg once daily or 0.5 mg every 72 hours. 
30-49
0.25 mg once daily or 0.5 mg every 48 hours.
≥50
0.5 mg once daily. 

Lamivudine-refractory or decompensated liver disease patients:
CrCl (mL/min) Dosage
<10
0.1 mg once daily or 0.5 mg every 72 hours.
10-29
0.3 mg once daily or 0.5 mg every 48 hours.
30-49
0.5 mg once daily.
≥50
1 mg once daily.

Patient on haemodialysis or CAPD: Nucleoside treatment-naive patients: 0.05 mg once daily or 0.5 mg every 5-7 days. Lamivudine-refractory or decompensated liver disease patients: 0.1 mg once daily or 0.5 mg every 72 hours. Dosage recommendations may vary among countries. Refer to country-specific product guidelines.
Administration
May be taken with or without food. For patients w/ compensated liver disease & nucleoside treatment-naïve, take w/ or w/o food.
Should be taken on an empty stomach. For patients w/ decompensated liver disease or w/ compensated liver disease who are lamivudine-refractory, take on an empty stomach more than 2 hr before or 2 hr after meals.
Contraindications
Hypersensitivity.
Special Precautions
Patient with risk factors for liver disease (e.g. prolonged nucleoside inhibitor use, obesity, female gender); HIV co-infection. Liver transplant recipient. Not for use in HIV/hepatitis B virus co-infected patients not receiving HAART. Renal and hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: HIV resistance (patients with untreated HIV infection or without highly active antiretroviral therapy [HAART]).
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, dyspepsia.
General disorders and administration site conditions: Fatigue.
Nervous system disorders: Headache, dizziness, somnolence.
Psychiatric disorders: Insomnia.
Skin and subcutaneous tissue disorders: Rash, alopecia.
Potentially Fatal: Lactic acidosis, severe hepatomegaly with steatosis; severe acute exacerbations of hepatitis B following treatment discontinuation.
Monitoring Parameters
Screen for HIV status prior therapy initiation. Monitor LFTs periodically during treatment and several months after discontinuation. Assess for signs and symptoms of lactic acidosis and hepatotoxicity.
Drug Interactions
Concomitant use with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of either medicinal product.
Food Interaction
Decreased absorption with food.
Action
Description: Entecavir is a nucleoside reverse transcriptase inhibitor which competes with natural substrates to inhibit hepatitis B viral polymerase enzyme thereby blocking reverse transcriptase activity thus reducing viral DNA synthesis.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Decreased absorption with food. Time to peak plasma concentration: 30-90 minutes.
Distribution: Extensively distributed. Plasma protein binding: Approx 13%.
Metabolism: Partially metabolised in the liver via glucuronide or sulfate conjugation.
Excretion: Mainly via urine (60-73% as unchanged drug). Terminal elimination half-life: Approx 128-149 hours.
Chemical Structure

Chemical Structure Image
Entecavir

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 135398508, Entecavir. https://pubchem.ncbi.nlm.nih.gov/compound/Entecavir. Accessed June 28, 2022.

Storage
Store below 30°C. Protect from light. Use appropriate personal protective equipment (e.g. gloves) for receiving, handling, administration, and disposal. Storage instructions may vary among countries. Refer to specific product guidelines.
MIMS Class
Antivirals
ATC Classification
J05AF10 - entecavir ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
References
Anon. Entecavir. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/05/2022.

Baraclude (DKSH Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 05/05/2022.

Baraclude 0.05 mg/mL Oral Solution (Bristol-Myers Squibb Pharma EEIG). MHRA. https://products.mhra.gov.uk. Accessed 05/05/2022.

Baraclude 0.5 mg Film-coated Tablets (Bristol-Myers Squibb Pharma EEIG). MHRA. https://products.mhra.gov.uk. Accessed 05/05/2022.

Baraclude 1 mg Film-coated Tablets (Bristol-Myers Squibb Pharma EEIG). MHRA. https://products.mhra.gov.uk. Accessed 05/05/2022.

Baraclude Tablet, Film Coated, Solution (E.R. Squibb & Sons, L.L.C.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 05/05/2022.

Buckingham R (ed). Entecavir. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/05/2022.

Joint Formulary Committee. Entecavir. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/05/2022.

Novartis New Zealand Limited. Entecavir 0.5 mg and 1 mg Film-coated Tablet data sheet 03 December 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 20/06/2022.

Disclaimer: This information is independently developed by MIMS based on Entecavir from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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