Epivir-HBV
100mg
Generic Name: lamivudine
Mechanism of Action
Lamivudine is a synthetic nucleoside analogue. Intracellularly, lamivudine is phosphorylated to its active 5′-triphosphate metabolite, lamivudine triphosphate, 3TC-TP. Incorporation of the monophosphate form into viral DNA by HBV reverse transcriptase results in DNA chain termination. 3TC-TP also inhibits the RNA- and DNA-dependent DNA polymerase activities of HIV-1 reverse transcriptase (RT). 3TC-TP is a weak inhibitor of mammalian α, β, and γ-DNA polymerases.
Antiviral Activity
Activity of lamivudine against HBV in cell culture was assessed in HBV DNA-transfected 2.2.15 cells, HB611 cells, and infected human primary hepatocytes. EC50 values (the concentration of drug needed to reduce the level of extracellular HBV DNA by 50%) varied from 0.01 μM (2.3 ng/mL) to 5.6 μM (1.3 mcg/mL) depending upon the duration of exposure of cells to lamivudine, the cell model system, and the protocol used. See the EPIVIR package insert for information regarding activity of lamivudine against HIV.
Indications and Usage
Epivir-HBV is indicated for the treatment of chronic hepatitis B associated with evidence of hepatitis B viral replication and active liver inflammation. This indication is based on 1-year histologic and serologic responses in adult patients with compensated chronic hepatitis B, and more limited information from a study in pediatric patients ages 2 to 17 years
Contraindications
Epivir-HBV Tablets and Epivir-HBV Oral Solution are contraindicated in patients with previously demonstrated clinically significant hypersensitivity to any of the components of the products.
Adverse Reactions
Several serious adverse events reported with lamivudine (lactic acidosis and severe hepatomegaly with steatosis, posttreatment exacerbations of hepatitis B, pancreatitis, and emergence of viral mutants associated with reduced drug susceptibility and diminished treatment response) are also described.
Dosage and Administration
The recommended oral dose of Epivir-HBV for treatment of chronic hepatitis B in adults is 100 mg once daily . Safety and effectiveness of treatment beyond 1 year have not been established and the optimum duration of treatment is not known.
The formulation and dosage of lamivudine in Epivir-HBV are not appropriate for patients dually infected with HBV and HIV. If lamivudine is administered to such patients, the higher dosage indicated for HIV therapy should be used as part of an appropriate combination regimen, and the prescribing information for EPIVIR as well as Epivir-HBV should be consulted.
The recommended oral dose of Epivir-HBV for pediatric patients 2 to 17 years of age with chronic hepatitis B is 3 mg/kg once daily up to a maximum daily dose of 100 mg. Safety and effectiveness of treatment beyond 1 year have not been established and the optimum duration of treatment is not known.
How to Supply
Epivir-HBV Tablets, 100 mg, box of 14 tablets.
Storage
Store at 25°C (77°F), excursions permitted to 15° to 30°C (59° to 86°F).
Please read the package insert for information in details!