Entecavir

These indications are based on manufacturer information for both originator and generic products. For product specific registered indications, please refer to product specific manufacturer information

Registered South African indications:

• Chronic HBV 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

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients 

Cautions

• Pregnancy 
• Breastfeeding 
• Moderate to severe renal impairment 
• Decompensated hepatic disease 
• Children 
• Risk factors for hepatic disease
• Liver transplant recipients 
• Co-infection with hepatitis C or D 
• HIV positive patients not on highly active antiretroviral therapy 
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab 

Infections caused by: Hepatitis B virus

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

Chronic hepatitis B virus infection in adults with active viral replication, persistently elevated serum aminotransferases or histologically active disease
- Nucleoside naive patients 

• Oral (tab): 0.5mg, dly

- Lamivudine-refractory patients
- Decompensated liver disease 

• Oral (tab): 1mg, dly

Take on an empty stomach (more than 2 hours before/after a meal)

In patients with decompensated liver disease or cirrhosis, treatment cessation is not recommended

 In HBeAg positive patients, treatment should be administered at least until 12 months after achieving HBe seroconversion or until HBs seroconversion or there is loss of efficacy

 In HBeAg negative adult patients, treatment should be administered at least until HBs seroconversion or there is evidence of loss of efficacy

Not established for use in children below 16 years in South Africa

Pregnancy 

• FDA Pregnancy Category C 

Breastfeeding

• Caution; not recommended 

Renal Impairment

• Moderate to severe: Caution; dose adjustment recommended

Hepatic Impairment 

• No dose adjustment recommended

Elderly 

• No dose adjustment recommended  

Central Nervous System Disorders

• Headache
• Dizziness
• Somnolence
• Fatigue 
• Insomnia 

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea
• Dyspepsia

Hepatobiliary Disorders

• Increased transaminases
• Hepatic decompensation 

Endocrine and Metabolic Disorders

• Lactic acidosis 

Skin and Subcutaneous Tissue Disorders

• Rash
• Alopecia

Immune, Blood and Lymphatic Disorders

• Anaphylactoid reactions 

• Agents that decrease renal function
• Agents that compete for active tubular secretion 
• Lamivudine
• Adefovir dipivoxil
• Tenofovir disoproxil fumarate

• Hepatic function

Specific cases may require:

• Renal function
• HIV status

Entecavir is intracellularly phosphorylated to guanosine triphosphate, which competes with natural substrates to inhibit hepatitis B viral polymerase. Enzyme inhibition blocks reverse transcriptase activity thereby reducing viral DNA synthesis.

Spectrum of activity: Hepatitis B virus 

Tablet 0.5mg

• Baraclude (Bristol-Myers Squibb) originator

Tablet 1mg

• Baraclude (Bristol-Myers Squibb) originator