Dosing & Uses
Dosage Forms & Strengths
emtricitabine/tenofovir disoproxil fumarate
tablet
- 200mg/300mg
HIV Infection
Indicated in combination with other antiretroviral (ART) agents in adults and adolescents weighing at least 35 kg
One 200 mg/300 mg tablet PO qDay
HIV-1 Pre-exposure Prophylaxis
Indicated in combination with safer sex practices to reduce risk of sexually acquired HIV-1 in at-risk adults and adolescents weighing ≥35 kg
One 200 mg/300 mg tablet PO qDay
See Dosing Considerations
PrEP indications (CDC guidelines)
- Men who have sex with men (MSM) at substantial lrisk of HIV acquisition
- Adult heterosexually active men and women at substantial risk of HIV acquisition
- Adult injection drug users (IDU) at substantial risk of HIV acquisition
- Heterosexually-active women and men whose partners are known to have HIV infection (ie, HIV-discordant couples) to protect the uninfected partner during conception and pregnancy so that an informed decision can be made in awareness of what is known and unknown about benefits and risks of PrEP for mother and fetus
Factors that help identify individuals at high risk for HIV
- Has partner(s) known to be HIV-1 infected or engages in sexual activity within a high prevalence area or social network and 1 or more of the following
-
Factors
- Inconsistent or no condom use
- Diagnosis or sexually transmitted infections
- Exchange of sex for commodities (eg, money, food, shelter, drugs)
- Illicit drug use or alcohol dependence
- Incarceration
- Partner(s) of unknown HIV-1 status with any of the risk factors listed above
Treatment of Hepatitis B / HIV-1 Coinfection (Off-label)
One 200 mg/300 mg tablet PO qDay in combination with other antiretroviral agents
Dosage Modifications
Renal impairment
-
HIV infection
- CrCl ≥50 mL/min: Dose adjustment not necessary
- CrCl 30-49 mL/min: One 200 mg/300 mg tablet PO q48hr
- CrCl <30 mL/min and ESRD requiring dialysis: Not recommended
-
PrEP
- CrCl ≥60 mL/min: Dose adjustment not necessary
- CrCl <60 mL/min: Do not use for pre-exposure prophylaxis
- If a decrease in estimated CrCl observed in an uninfected individual while taking emtricitabine/tenofovir DF for HIV-1 PrEP, evaluate potential causes and reassess potential risks and benefits of continued use
Hepatic impairment
- No substantial alterations in tenofovir pharmacokinetics observed in clinical trials in subjects with hepatic impairment compared with unimpaired subjects
- Pharmacokinetics of emtricitabine have not been studied with hepatic impairment; however, emtricitabine is not significantly metabolized by liver enzymes, so the impact of liver impairment should be limited
Dosing Considerations
All patients should be tested for the presence of chronic hepatitis B virus (HBV) before or when initiating
Before initiating and during use, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein in all patients; in patients with chronic kidney disease, also assess serum phosphorus
HIV infection
- Not recommended for use as a component of a triple nucleoside regimen
- Should not be coadministered with combination products that are complete regimens or already contain emtricitabine or tenofovir (eg, Atripla, Complera, Emtriva, Genvoya, Odefsey, Stribild, Viread)
- Do not coadminister with lamivudine-containing products (eg, Epivir, Combivir, Dutrebis, Epzicom, Triumeq, Trizivir) because of similarities between emtricitabine and lamivudine
- In treatment experienced patients, use should be guided by laboratory testing and treatment history
PrEP
- Individuals must have a negative HIV-1 test immediately prior to initiating emtricitabine/tenofovir AF for HIV-1
- If clinical symptoms consistent with acute viral infection are present and recent (<1 month) exposures are suspected, delay starting PrEP for at least 1 month and reconfirm HIV-1 status or use a test cleared by the FDA as an aid in the diagnosis of HIV-1 infection, including acute or primary HIV-1 infection
- Continuing screening at least once q3months while taking emtricitabine/tenofovir AF
Dosage Forms & Strengths
emtricitabine/tenofovir disoproxil fumarate
tablet
- 100mg/150mg
- 133mg/200mg
- 167mg/250mg
- 200mg/300mg
HIV Infection
Weight <17 kg: Safety and efficacy not established
Indicated in combination with other ART agents for children weighing at least 17 kg who can swallow the tablet whole
Weight ≥17 kg
- 17 to <22 kg: One 100 mg/150 mg tablet PO qDay
- 22 to <28 kg: One 133 mg/200 mg tablet PO qDay
- 28 to <35 kg: One 167 mg/250 mg tablet PO qDay
- ≥35 kg: One 200 mg/300 mg tablet PO qDay
HIV-1 Pre-exposure Prophylaxis
Indicated in combination with safer sex practices for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 in at-risk adults and adolescents weighing at least 35 kg
<35 kg: Safety and efficacy not established
≥35 kg: One 200 mg/300 mg tablet PO qDay
PrEP indications (CDC guidelines)
- Men who have sex with men (MSM) at substantial risk of HIV acquisition
- Adult heterosexually active men and women at substantial risk of HIV acquisition
- Adult injection drug users (IDU) at substantial risk of HIV acquisition
- Heterosexually-active women and men whose partners are known to have HIV infection (ie, HIV-discordant couples) to protect the uninfected partner during conception and pregnancy so that an informed decision can be made in awareness of what is known and unknown about benefits and risks of PrEP for mother and fetus
Factors that help identify individuals at high risk for HIV
- Has partner(s) known to be HIV-1 infected or engages in sexual activity within a high prevalence area or social network and 1 or more of the following
Factors
- Inconsistent or no condom use
- Diagnosis or sexually transmitted infections
- Exchange of sex for commodities (eg, money, food, shelter, drugs)
- Illicit drug use or alcohol dependence
- Incarceration
- Partner(s) of unknown HIV-1 status with any of the risk factors listed above
Dosage Modifications
Renal impairment
- No data are available to make dosage recommendations in pediatric patients infected with HIV-1 infection who have renal impairment
PrEP
- CrCl ≥60 mL/min or greater: Dose adjustment not necessary
- CrCl <60 mL/min: Do not use for pre-exposure prophylaxis
- If a decrease in estimated CrCl observed in an uninfected individual while taking emtricitabine/tenofovir DF for HIV-1 PrEP, evaluate potential causes and reassess potential risks and benefits of continued use
Hepatic impairment
- No substantial alterations in tenofovir pharmacokinetics observed in clinical trials in subjects with hepatic impairment compared with unimpaired subjects
- Pharmacokinetics of emtricitabine have not been studied with hepatic impairment; however, emtricitabine is not significantly metabolized by liver enzymes, so the impact of liver impairment should be limited
Dosing Considerations
All patients should be tested for the presence of chronic hepatitis B virus (HBV) before or when initiating
Before initiating and during use, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein in all patients; in patients with chronic kidney disease, also assess serum phosphorus
HIV infection
- Not recommended for use as a component of a triple nucleoside regimen
- Should not be coadministered with combination products that are complete regimens or already contain emtricitabine or tenofovir (eg, Atripla, Complera, Emtriva, Genvoya, Odefsey, Stribild, Viread)
- Do not coadminister with lamivudine-containing products (eg, Epivir, Combivir, Dutrebis, Epzicom, Triumeq, Trizivir) because of similarities between emtricitabine and lamivudine
- In treatment experienced patients, use should be guided by laboratory testing and treatment history
PrEP
- Individuals must have a negative HIV-1 test immediately prior to initiating emtricitabine/tenofovir AF for HIV-1 PrEP
- If clinical symptoms consistent with acute viral infection are present and recent (<1 month) exposures are suspected, delay starting PrEP for at least 1 month and reconfirm HIV-1 status or use a test cleared by the FDA as an aid in the diagnosis of HIV-1 infection, including acute or primary HIV-1 infection
- Continuing screening at least once q3months while taking emtricitabine/tenofovir AF
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Note: includes adverse effects of any severity rating
Diarrhea
Nausea
Fatigue
Headache
Dizziness
Depression
Insomnia
Abnormal dreams
Rash
1-10%
Note: includes adverse effects grade 2-4
Diarrhea (9%)
Nausea (9%)
Fatigue (9%)
Depression (9%)
Sinusitis (8%)
URI infections (8%)
Dizziness (8%)
Rash event (7%)
Headache (6%)
Nasopharyngitis (5%)
Insomnia (5%)
Vomiting (2%)
Warnings
Black Box Warnings
Posttreatment acute exacerbation of hepatitis B
- Severe acute exacerbations of hepatitis B virus (HBV) reported in HBV-infected patients who have discontinued emtricitabine/tenofovir DF
- Monitor hepatic function with both clinical and laboratory follow-up for at least several months after discontinuing
- If appropriate, initiation of antihepatitis B therapy may be warranted
Pre-exposure prophylaxis (PrEP)
- Use for PrEP must only be prescribed to individuals confirmed to be HIV-negative immediately prior to initiating and periodically (at least every 3 months) during use
- Drug-resistant HIV-1 variants have been identified with use of emtricitabine/tenofovir for a PrEP indication following undetected acute HIV-1 infection
- Do not initiate emtricitabine/tenofovir for PrEP if signs or symptoms of acute HIV-1 infection are present unless negative infection status is confirmed
Contraindications
Hypersensitivity
Do not use as PrEP in HIV-infected individuals or individuals with unknown HIV status
Use as monotherapy in HIV-infected patients
Cautions
Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, reported with nucleoside analogues, including emtricitabine and tenofovir; suspend dosing in those who develop clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity
Do not coadminister with other drugs containing emtricitabine or tenofovir
Severe exacerbation of hepatitis B may occur upon discontinuation (see Black Box Warning)
Immune reconstitution syndrome reported with combination ART; during the initial treatment phase, patients whose immune systems respond may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia [PCP], or tuberculosis); autoimmune disorders (eg, Grave disease, polymyositis, and Guillain-Barré syndrome) have also been reported
PrEP
- Use for HIV-1 PrEP only as part of a comprehensive prevention strategy that includes other prevention measures, such as safer sex practices, because emtricitabine/tenofovir AF is not always effective in preventing acquisition of HIV-1
- If clinical symptoms consistent with acute viral infection are present and recent (<1 month) exposures are suspected, delay starting PrEP for at least one month and reconfirm negative HIV-1 status or use a test approved by the FDA as an aid in the diagnosis of HIV-1 infection, including acute or primary HIV-1 infection; while receiving therapy for PrEP HIV-1 screening tests should be repeated at least every 3 months
Renal toxicity
- Increased risk of new onset or worsening renal impairment
- Obtain estimated CrCl in all patients before initiating
- Routinely monitor calculated creatinine clearance and serum phosphorus
- Avoid use if CrCl <30 mL/min (<60 mL/min for PrEP), hemodialysis, or concurrent or recent use of nephrotoxic drugs
- Tenofovir DF may cause renal toxicity (acute renal failure and/or Fanconi syndrome); avoid administering therapy with concurrent or recent use of nephrotoxic drugs, including NSAIDs; consider alternative to NSAIDs in patients taking tenofovir DF and at risk of renal impairment
Bone effects of tenofovir
- Bone mineral density may decrease; consider assessment of bone mineral density in patients with a history of pathologic fracture or other risk factors for osteoporosis or bone loss
- Osteomalacia associated with proximal renal tubulopathy, manifested as bone pain or pain in extremities and which may contribute to fractures, have been reported
- Consider hypophosphatemia and osteomalacia secondary to proximal renal tubulopathy in patients at risk of renal dysfunction who present with persistent or worsening bone or muscle symptoms while receiving TDF-containing products
Drug interaction overview
-
Drug affecting renal function
- Emtricitabine and tenofovir are primarily excreted by the kidneys by a combination of glomerular filtration and active tubular secretion
- No drug-drug interactions due to competition for renal excretion have been observed; however, coadministration with drugs that are eliminated by active tubular secretion may increase concentrations of emtricitabine, tenofovir, and/or the coadministered drug
-
P-gp and BCRP inhibitors
- Tenofovir DF is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters
- Increased tenofovir absorption may occur if coadministered with inhibitors of these transporters
Pregnancy & Lactation
Pregnancy
Data on the use during pregnancy from observational studies have shown no increased risk of major birth defects
Available data from the Antiretroviral Regnancy Registry (APR) show no increase in the overall risk of major birth defects with first trimester exposure for emtricitabine (2.3%) or tenofovir DF (2.1%) compared with the background rate for major birth defects of 2.7%
Healthcare providers are encouraged to register pregnant women by calling the APR at 1-800-258-4263
Pregnant women with HIV infection should continue antiretroviral drugs according to current guidelines during pregnancy to decrease maternal-fetal viral transmission (https://aidsinfo.nih.gov)
Lactation
Emtricitabine and tenofovir have been shown to be present in human breast milk
HIV-1 infected women
- The CDC recommend that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1
- Because of the potential for HIV transmission (in HIV-negative infants); developing viral resistance (in HIV-positive infants); and adverse reactions in a breastfed infant similar to those seen in adults
- Instruct mothers not to breastfeed
Women taking PrEP
- In HIV-uninfected women, consider the developmental and health benefits of breastfeeding and the mother’s clinical need of drug therapy for HIV-1 PrEP along with any potential adverse effects on the breastfed child from drug therapy and the risk of HIV-1 acquisition due to nonadherence and subsequent mother to child transmission
- Women should not breastfeed if acute HIV-1 infection is suspected because of the risk of HIV-1 transmission to the infant
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Emtricitabine: Nucleoside reverse transcriptase inhibitor (NRTI); following phosphorylation, interferes with HIV viral DNA polymerase and inhibits viral replication; cytosine analogue
Tenofovir: Nucleoside reverse transcriptase inhibitor (NRTI); following hydrolysis and phosphorylation, inhibits HIV-1 reverse transcriptase by competing with AMP as substrate
Administration
Oral Administration
May take with or without food
Swallow tablet whole; do not chew, crush, break, or dissolve
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Patient Handout
Formulary
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