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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Nucleoside and nucleotide reverse transcriptase inhibitors
entecavir
J05AF10
Forms & Strengths
- Oral Tablets: 0.5 mg
- Oral Tablets: 1 mg
- Oral Solution: 0.05 mg/mL
Adult Dosing
- Chronic hepatitis B, nucleoside-naive: 0.5 mg orally once daily
- Lamivudine-refractory chronic hepatitis B: 1 mg orally once daily
- Renal impairment (CrCl 30-49 mL/min): 0.5 mg every 48 hours or 0.25 mg daily (naive); 1 mg every 48 hours or 0.5 mg daily (refractory)
- Renal impairment (CrCl 10-29 mL/min): 0.5 mg every 72 hours (naive); 1 mg every 72 hours (refractory)
- Hemodialysis or CAPD: 0.5 mg every 7 days (naive); 1 mg every 7 days (refractory)
Pediatric Dosing
- Children >= 2 years and < 16 years, weight-based dosing for nucleoside-naive chronic hepatitis B
- 10 kg to 11 kg: 0.15 mg (3 mL) once daily
- > 11 kg to 14 kg: 0.2 mg (4 mL) once daily
- > 14 kg to 17 kg: 0.25 mg (5 mL) once daily
- > 17 kg to 22 kg: 0.3 mg (6 mL) once daily
- > 22 kg to 30 kg: 0.35 mg (7 mL) once daily
- > 30 kg: 0.5 mg tablet or 10 mL oral solution once daily
Indications
- Treatment of chronic hepatitis B virus infection in adults and pediatric patients aged 2 years and older with evidence of active viral replication and persistent serum aminotransferase elevations or histologically active disease
Mechanism of Action
- Guanosine nucleoside analogue with activity against hepatitis B virus (HBV) polymerase
- Competes with the natural substrate deoxyguanosine triphosphate to functionally inhibit all three phases of the HBV viral polymerase: base priming, reverse transcription of the negative strand, and synthesis of the positive strand
Contraindications
- Hypersensitivity to entecavir or any component of the product
Adverse Reactions
- Headache
- Fatigue
- Dizziness
- Nausea
- Elevated ALT
- Lactic acidosis and severe hepatomegaly with steatosis (rare, potentially fatal)
- Severe acute exacerbations of hepatitis B upon discontinuation
Drug Interactions
- Drugs that reduce renal function or compete for active tubular secretion (e.g., lamivudine, adefovir, tenofovir) may increase serum concentrations of entecavir or the co-administered drug
- No pharmacokinetic interactions observed with co-administration of lamivudine, adefovir, or tenofovir disoproxil fumarate
Curated Content: Needs Vetting Before Put to Clinical Use