Entecavir


Concise Prescribing Info
Indications/Uses
Chronic hepatitis B.
Dosage/Direction for Use
Adult : PO Compensated liver disease: Nucleoside naïve patient: 0.5 mg once daily. In patient with resistance, or concomitant use with lamivudine: 1 mg once daily. Decompensated liver disease: 1 mg once daily.
Dosage Details
Oral
Chronic hepatitis B
Adult: Compensated liver disease: Nucleoside naive patient: 0.5 mg once daily; In patient with resistance, or concomitant use with lamivudine: 1 mg once daily.  Decompensated liver disease: 1 mg once daily.
Child: Compensated liver disease: Nucleoside naive patient: ≥2 years ≥10 kg: 0.015 mg/kg once daily. Max: 0.5 mg daily. In patient with concomitant use with lamivudine: 0.03 mg/kg once daily. Max: 1 mg daily.
Renal Impairment
Compensated liver disease:
Nucleoside naive patient:
 CrCl (mL/min) Dosage
30-49 0.25 mg once daily or 0.5 mg every 48 hours
10-29  0.15 mg once daily or 0.5 mg every 72 hours
<10 0.05 mg once daily or 0.5 mg every 5-7 days

In patient with resistance, or concomitant use with lamivudine:
 CrCl (mL/min) Dosage
30-49  0.5 mg once daily or 1 mg every 48 hours
10-29  0.3 mg once daily, or 0.5 mg every 48 hours, or 1 mg every 72 hours
<10  0.1 mg once daily, or 0.5 mg every 72 hours, or 1 mg every 7 days

Decompensated liver disease: 
 CrCl (mL/min) Dosage
30-49 0.5 mg once daily or 1 mg every 48 hours
10-29 0.3 mg once daily, or 0.5 mg every 48 hours, or 1 mg every 72 hours
<10  0.1 mg once daily, or 0.5 mg every 72 hours, or 1 mg every 7 days

Patient on haemodialysis or CAPD: Nucleoside naive patient: 0.05 mg once daily or 0.5 mg every 5-7 days. In patient with resistance, or concomitant use with lamivudine: 0.1 mg once daily, or 0.5 mg every 72 hours, or 1 mg every 7 days.
Administration
Should be taken on an empty stomach. Take at least 2 hr after a meal & 2 hr before the next meal.
Contraindications
Hypersensitivity.
Special Precautions
Patient with chronic hepatitis B, HIV co-infection, hepatomegaly, lactic acidosis, liver transplant recipient. Renal and hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Hepatorenal syndrome, transient increase in serum transaminases, elevated serum lactate levels.
Blood and lymphatic system disorders: Thrombocytopenia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, dyspepsia, abdominal pain.
General disorders and admin site conditions: Fatigue, pyrexia.
Investigations: Increased serum bilirubin, elevated serum creatinine.
Metabolism and nutrition disorders: Hyperglycaemia.
Nervous system disorders: Headache, dizziness, somnolence.
Psychiatric disorders: Insomnia.
Renal and urinary disorders: Haematuria.
Skin and subcutaneous tissue disorders: Rash, alopecia.
Potentially Fatal: Lactic acidosis associated with severe hepatomegaly and hepatic steatosis; pancreatitis, liver failure, renal failure, severe acute exacerbations of hepatitis B following treatment discontinuation. Rarely, hypersensitivity reaction.
Patient Counseling Information
This drug may cause dizziness, fatigue and somnolence, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor LFTs every 3 months and viral markers for hepatitis B every 3-6 months during treatment, and at least 6 months after treatment discontinuation; HIV status prior therapy initiation. 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. May decrease serum concentration of orlistat. May increase serum levels with immunosuppressants e.g. ciclosporin, tacrolimus.
Food Interaction
Delayed and reduced absorption with food.
Action
Description: Entecavir, a nucleoside reverse transcriptase inhibitor, competitively inhibit hepatitis B viral polymerase by blocking reverse transcriptase activity and consequently reducing viral DNA synthesis.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Delayed and decreased absorption with food. Time to peak plasma concentration: 0.5-1.5 hours.
Distribution: Extensively distributed. Plasma protein binding: Approx 13%.
Metabolism: Partially metabolised in the liver via glucuronide or sulfate conjugation. Undergoes phosphorylation by cellular enzymes to its active metabolite, entecavir triphosphate.
Excretion: Mainly via urine (60-75% as unchanged drug). Terminal elimination half-life: Approx 128-149 hours.
Chemical Structure

Chemical Structure Image
Entecavir

Source: National Center for Biotechnology Information. PubChem Database. Entecavir, CID=135398508, https://pubchem.ncbi.nlm.nih.gov/compound/Entecavir (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C. Protect from light. Use appropriate personal protective equipment (e.g. gloves) for receiving, handling, administration and disposal.
MIMS Class
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. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 23/04/2019.

Anon. Entecavir. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/04/2019.

Buckingham R (ed). Entecavir. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2019.

Entecavir Tablet (Aurobindo Pharma Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/04/2019.

Entecavir Zentiva 0.5 mg Film-Coated Tablets (Winthrop Pharmaceutical UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 23/04/2019.

Joint Formulary Committee. Entecavir. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2019.

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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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