Generic Name

Entecavir

Precaution

Lactic acidosis: Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases have been reported with the use of nucleoside analogues alone or in combination with antiretrovirals.Exacerbations of hepatitis after discontinuation of treatment: Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued anti-hepatitis B therapy, including Entecavir. Lactation: excretion in milk unknown/not recommended

Indication

Chronic hepatitis B

Contra Indication

Entecavir is contraindicated in patients with previously demonstrated hypersensitivity to Entecavir or any component of the product.

Dose

N/A

Side Effect

1-10% Fatigue (1-3%),Headache (2-4%),Dizziness,Nausea <1% Diarrhea,Dyspepsia,Vomiting,Somnolence,Insomnia

Pregnancy Category

Mode of Action

Selective HBV DNA polymerase inhibitor; inhibition blocks reverse transcriptase activity, which in turn reduces viral DNA synthesis

Interaction

Drugs that reduce renal function or compete for active tubular secretion may increase serum conc of either entecavir or co-administered drug.

Pregnancy Category Note

Pregnancy Prospective pregnancy data from the APR are not sufficient to adequately assess the risk of birth defects, miscarriage or adverse maternal or fetal outcomes; use during pregnancy has been evaluated in a limited number of individuals reported to APR and number of exposures to entecavir is insufficient to make a risk assessment compared to a reference population; rate of miscarriage is not reported in APR; all pregnancies have a background risk of birth defect, loss, or other adverse outcomes Lactation Not known whether drug is present in human breast milk, affects human milk production, or has effects on the breastfed infant; when administered to lactating rats, entecavir was present in milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition

Adult Dose

Chronic Hepatitis B Indicated for treatment of CHB with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease Nucleoside inhibitor treatment-naïve with compensated liver disease (adults and adolescents ?16 yr): 0.5 mg PO qDay Lamivudine-refractory or known lamivudine or telbivudine resistance substitutions (adults and adolescents ?16 yr): 1 mg PO qDay Decompensated liver disease (adults): 1 mg PO qDay

Child Dose

Chronic Hepatitis B Indicated for treatment of CHB with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease in children ?2 years and weigh at least 10 kg <2 years: Safety and efficacy not established >16 years: As adult

Renal Dose

Renal Impairment Usual daily dose (0.5 mg) CrCl ?50 mL/min: No dosage adjustment required CrCl 30-49 mL/min: Reduce to 0.25 mg/day or 0.5 mg q48hr CrCl 10-29 mL/min: Reduce to 0.15 mg/day or 0.5 mg q72hr CrCl <10 mL/min, hemodialysis, or CAPD: 0.05 mg/day or 0.5 mg q7days Lamivudine-refractory/decompensated liver disease daily dose (1 mg) CrCl ?50 mL/min: No dosage adjustment required CrCl 30-49 mL/min: Reduce to 0.5 mg/day or 1 mg q48hr CrCl 10-29 mL/min: Reduce to 0.3 mg/day or 1 mg q72hr CrCl <10 mL/min, hemodialysis, or CAPD: 0.1 mg/day or 1 mg q7days

Administration

Should be taken on an empty stomach. Take at least 2 hr after a meal & 2 hr before the next meal. Use oral solution when needed for renal impairment dosage adjustments.