Emtricitabine, Tenofovir disoproxil fumarate
Indications
Emtricitabine, Tenofovir disoproxil fumarate is used for:
Emtricitabine
Indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection in adults and for postexposure prophylaxis of HIV infection in health care workers and others exposed occupationally or nonoccupationally via percutaneous injury or mucous membrane or nonintact skin contact with blood, tissues, or other body fluids associated with risk for transmission of the virus.
Tenofovir disoproxil
Tenofovir is indicated in combination with other antiretroviral agents for the management of HIV-1 infection in adults and pediatric patients 2 years of age and older. It is also indicated for the treatment of chronic hepatitis B in adults and pediatric patients 12 years of age and older [FDA label]. This drug is also a component of multiple products used for the management of HIV-1 infection [F3418], [F3421]. Safety and effectiveness of tenofovir disoproxil in pediatric patients younger than 2 years of age has not been established to this date [FDA label].
Indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection in adults and for postexposure prophylaxis of HIV infection in health care workers and others exposed occupationally or nonoccupationally via percutaneous injury or mucous membrane or nonintact skin contact with blood, tissues, or other body fluids associated with risk for transmission of the virus.
Tenofovir disoproxil
Tenofovir is indicated in combination with other antiretroviral agents for the management of HIV-1 infection in adults and pediatric patients 2 years of age and older. It is also indicated for the treatment of chronic hepatitis B in adults and pediatric patients 12 years of age and older [FDA label]. This drug is also a component of multiple products used for the management of HIV-1 infection [F3418], [F3421]. Safety and effectiveness of tenofovir disoproxil in pediatric patients younger than 2 years of age has not been established to this date [FDA label].
Adult Dose
Child Dose
Renal Dose
Administration
Contra Indications
Precautions
Pregnancy-Lactation
Interactions
Adverse Effects
Side effects of Emtricitabine, Tenofovir disoproxil fumarate :
Mechanism of Action
Emtricitabine
Emtricitabine works by inhibiting reverse transcriptasem preventing transcription of HIV RNA to DNA. Emtricitabine is a synthetic nucleoside analogue of cytidine. It is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate, which is responsible for the inhibition of HIV-1 reverse transcriptase. It competes with the natural substrate deoxycytidine 5'-triphosphate and incorporates into nascent viral DNA, resulting in early chain termination. Therefore emtricitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate deoxycytidine 5'-triphosphate and by its incorporation into viral DNA. By inhibiting HIV-1 reverse transcriptase, emtricitabine can help to lower the amount of HIV, or "viral load", in a patient's body and can indirectly increase the number of immune system cells (called T cells or CD4+ T-cells).
Tenofovir disoproxil
Tenofovir belongs to a class of antiretroviral drugs known as nucleotide analog reverse transcriptase inhibitors (NtRTIs), which block reverse transcriptase, an enzyme necessary for viral production in HIV-infected individuals. This enables the management of HIV viral load through decreased viral replication [FDA label]. Tenofovir disoproxil fumarate is the fumarate salt of the prodrug _tenofovir disoproxil_. Tenofovir disoproxil is absorbed and converted to its active form, _tenofovir_, a nucleoside monophosphate (nucleotide) analog. Tenofovir is then converted to the active metabolite, _tenofovir diphosphate_, a chain terminator, by constitutively expressed enzymes in the cell. Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and the Hepatitis B polymerase by direct binding competition with the natural deoxyribonucleotide substrate (deoxyadenosine 56-triphosphate) and, after integration into DNA, causes viral DNA chain termination [F3442], [FDA label]. **A note on resistance** HIV-1 isolates with decreased susceptibility to tenofovir have been identified in cell culture studies. These viruses expressed a _K65R_ substitution in reverse transcriptase and showed a 2H 4 fold decrease in susceptibility to treatment with tenofovir [FDA label].
Emtricitabine works by inhibiting reverse transcriptasem preventing transcription of HIV RNA to DNA. Emtricitabine is a synthetic nucleoside analogue of cytidine. It is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate, which is responsible for the inhibition of HIV-1 reverse transcriptase. It competes with the natural substrate deoxycytidine 5'-triphosphate and incorporates into nascent viral DNA, resulting in early chain termination. Therefore emtricitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate deoxycytidine 5'-triphosphate and by its incorporation into viral DNA. By inhibiting HIV-1 reverse transcriptase, emtricitabine can help to lower the amount of HIV, or "viral load", in a patient's body and can indirectly increase the number of immune system cells (called T cells or CD4+ T-cells).
Tenofovir disoproxil
Tenofovir belongs to a class of antiretroviral drugs known as nucleotide analog reverse transcriptase inhibitors (NtRTIs), which block reverse transcriptase, an enzyme necessary for viral production in HIV-infected individuals. This enables the management of HIV viral load through decreased viral replication [FDA label]. Tenofovir disoproxil fumarate is the fumarate salt of the prodrug _tenofovir disoproxil_. Tenofovir disoproxil is absorbed and converted to its active form, _tenofovir_, a nucleoside monophosphate (nucleotide) analog. Tenofovir is then converted to the active metabolite, _tenofovir diphosphate_, a chain terminator, by constitutively expressed enzymes in the cell. Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and the Hepatitis B polymerase by direct binding competition with the natural deoxyribonucleotide substrate (deoxyadenosine 56-triphosphate) and, after integration into DNA, causes viral DNA chain termination [F3442], [FDA label]. **A note on resistance** HIV-1 isolates with decreased susceptibility to tenofovir have been identified in cell culture studies. These viruses expressed a _K65R_ substitution in reverse transcriptase and showed a 2H 4 fold decrease in susceptibility to treatment with tenofovir [FDA label].