ТЕНОФОВІРУ ДИЗОПРОКСИЛУ ФУМАРАТ/ЕФАВІРЕНЗ/ЕМТРИЦИТАБІН ТАБЛЕТКИ 300 МГ/600 МГ/200 МГ TENOFOVIR DISOPROXIL FUMARATE/EFAVIRENZ/EMTRICITABINE TABLETS 300 MG/600 MG/200 MG

उत्पाद अवलोकन

About ТЕНОФОВІРУ ДИЗОПРОКСИЛУ ФУМАРАТ/ЕФАВІРЕНЗ/ЕМТРИЦИТАБІН ТАБЛЕТКИ 300 МГ/600 МГ/200 МГ TENOFOVIR DISOPROXIL FUMARATE/EFAVIRENZ/EMTRICITABINE TABLETS 300 MG/600 MG/200 MG

The preparation contains tenofovir disoproxil fumarate and is used in combination antiretroviral therapy. The source indicates indications for HIV-1 infection and chronic hepatitis B.

Composition

Active substance: tenofovir disoproxil fumarate — 300 mg, which corresponds to 245 mg of tenofovir disoproxil. Excipients include lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, pregelatinized starch, and magnesium stearate.

The Opadry II Light Blue (Y-30–10671-A) coating contains hypromellose, indigo carmine (E 132), lactose monohydrate, titanium dioxide (E 171), and triacetin.

Indications

For HIV-1 infection, the preparation is prescribed to HIV-1-infected patients in combination with other antiretroviral medicinal products. It is also used in HIV-1-infected adolescents aged 12 to <18 years with resistance to nucleoside reverse transcriptase inhibitors or toxicity that precludes the use of first-line agents.

The choice of preparation for patients who have previously received antiretroviral therapy should be based on individual resistance testing data or treatment history.

For chronic hepatitis B, the preparation is intended for adults with compensated liver disease, evidence of active viral replication, persistently elevated serum alanine aminotransferase levels, and histological evidence of active inflammation and/or fibrosis, as well as in cases of confirmed lamivudine-resistant hepatitis B.

Pharmacological properties

Tenofovir disoproxil fumarate is the fumarate salt of the prodrug tenofovir disoproxil. After absorption, tenofovir disoproxil is converted into tenofovir, a nucleoside monophosphate analogue, and subsequently into the active metabolite tenofovir diphosphate.

Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and HBV polymerase through competitive binding with the natural substrate — deoxyribonucleotide — and DNA chain termination after incorporation.

The intracellular half-life of tenofovir diphosphate is 10 hours in activated peripheral blood mononuclear cells and 50 hours in resting cells.

Source: Compendium