Oral antiretroviral agent.
Has a bioavailability 25%, protein binding of < 1%, anhalf-life of 17 hours and is renally excreted.
An oral drug that belongs to a class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase, an enzyme crucial to viral production.
Tenofovir disoproxil fumarate is a prodrug form of tenofovir.
This drug is available in a fixed-dose combination with emtricitabine in a product with the brand name Truvada for once-a-day dosing.
Atripla, a fixed-dose triple combination of tenofovir, emtricitabine and efavirenz, providing a single daily dose for the treatment of HIV.
Truvada-tenovir disoproxil fulmarate 300mg/emitricitabine 200 mg.
Truvada as an antiretroviral preexposure prophylaxis reduces the risk of HIV acquisition among men having sex with men, and among heterosexuals.
Truvada approved for preexposure prophylaxis of HIV for adults at high risk.
Daily use of antiretroviral drugs can reduce the risk of HIV acquisition through sexual interourse.
In adolescents infected with hepatitis B virus (HBV), once-daily tenofovir treatment for 72 weeks effectively suppresses HBV DNA and normalizes alanine aminotransferase (ALT) values, regardless of prior HBV treatment (Murray KF et al).
89 percent of tenofovir-treated patients achieved a virologic response, defined as HBV DNA <400 copies/mL, compared with none of the placebo-treated patients, and no tenofovir resistance was seen in the above study.
Emitricitabine/tenofovir is only partially effective for preventing HIV, with a 75% risk reduction demonstrated in the Partners PrEP study.
Approved for the treatment of HIV, and chronic hepatitis B.
Indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults.
Has activity against wild-type and lamivudine-resistant HBV.
Most common side effects include: nausea, vomiting, diarrhea, and asthenia and less frequent side effects include hepatotoxicity, abdominal pain, and flatulence.
May cause renal toxicity at elevated levels with acute renal failure, Fanconi syndrome, proteinuria or tubular necrosis due to accumulation of the drug in proximal tubules.
May increase didanosine’s concentration and decrease the concentration of atazanavir sulfate.
Drug level monitoring is useful to prvent renal and hepatic toxicity.
Prophylactic use can reduce rates of HIV infection.
Dosage for hepatitis B is 300 mg daily with normal renal function.