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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
tenofovir disoproxil and emtricitabine
J05AR03
Forms & Strengths
- Tablet: 300 mg tenofovir disoproxil fumarate / 200 mg emtricitabine
Adult Dosing
- HIV-1 treatment: 1 tablet orally once daily in combination with other antiretrovirals
- Pre-exposure prophylaxis (PrEP): 1 tablet orally once daily
Pediatric Dosing
- Pediatric patients weighing >= 35 kg: 1 tablet orally once daily
Indications
- Treatment of HIV-1 infection in adults and pediatric patients weighing >= 35 kg
- Pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 in adults and adolescents weighing >= 35 kg
Mechanism of Action
- Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI)
- Tenofovir disoproxil fumarate is a prodrug of tenofovir, an acyclic nucleoside phosphonate nucleotide reverse transcriptase inhibitor (NtRTI)
- Both agents inhibit HIV-1 reverse transcriptase by competing with natural substrates and terminating the viral DNA chain
Contraindications
- Previous hypersensitivity to any of the active substances (tenofovir, emtricitabine)
- Use as PrEP in individuals with unknown or positive HIV-1 status
Adverse Reactions
- Lactic acidosis and severe hepatomegaly with steatosis
- Exacerbation of hepatitis B upon discontinuation
- New-onset or worsening renal impairment (including Fanconi syndrome)
- Decreased bone mineral density
- Common: diarrhea, nausea, fatigue, headache, dizziness, depression, insomnia
Drug Interactions
- Didanosine: Tenofovir increases systemic exposure of didanosine; co-administration is generally not recommended
- HIV protease inhibitors (atazanavir, darunavir): Tenofovir may decrease concentrations; monitor for toxicity and efficacy
- Nephrotoxic drugs (NSAIDs, aminoglycosides, high-dose or multiple NSAIDs): Increased risk of renal toxicity
- Drugs eliminated by active renal tubular secretion (cidofovir, acyclovir, valacyclovir, ganciclovir): May increase concentration of emtricitabine or tenofovir
Curated Content: Needs Vetting Before Put to Clinical Use