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Emtricitabine and Tenofovir Disoproxil Fumarate

Medically reviewed by Drugs.com. Last updated on Sep 17, 2020.

Pronunciation

(em trye SYE ta been & ten OF oh vir dye soe PROX il FUE ma rate)

Index Terms

  • Tenofovir Disoproxil Fumarate and Emtricitabine

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Truvada: emtricitabine 100 mg and tenofovir disoproxil fumarate 150 mg, emtricitabine 133 mg and tenofovir disoproxil fumarate 200 mg, emtricitabine 167 mg and tenofovir disoproxil fumarate 250 mg, emtricitabine 200 mg and tenofovir disoproxil fumarate 300 mg [contains fd&c blue #2 aluminum lake]

Generic: emtricitabine 200 mg and tenofovir disoproxil fumarate 300 mg

Brand Names: U.S.

  • Truvada

Pharmacologic Category

  • Antiretroviral, Reverse Transcriptase Inhibitor, Nucleoside (Anti-HIV)
  • Antiretroviral, Reverse Transcriptase Inhibitor, Nucleotide (Anti-HIV)

Pharmacology

Nucleoside and nucleotide reverse transcriptase inhibitor combination; emtricitabine is a cytosine analogue while tenofovir is an analog of adenosine 5'-monophosphate. Each drug interferes with HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication.

Use: Labeled Indications

HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretroviral agents in adults and pediatric patients weighing ≥17 kg

HIV-1 infection, preexposure prophylaxis: Preexposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in at-risk adults and adolescents weighing ≥35 kg (must have negative HIV-1 test immediately prior to initiation of emtricitabine/tenofovir disoproxil fumarate for HIV-1 PrEP).

Off Label Uses

HIV-1/hepatitis B co-infection, treatment

Based on the Department of Health and Human Services guidelines for the use of antiretroviral agents in adults and adolescents with HIV, emtricitabine/tenofovir is effective and recommended as the nucleoside reverse transcriptase inhibitor backbone of a fully suppressive antiretroviral regimen in patients with HIV-1 co-infected with hepatitis B.

HIV-1 nonoccupational postexposure prophylaxis

Based on the Centers for Disease Control and Prevention, US Department of Health and Human Services updated guidelines for antiretroviral postexposure prophylaxis after sexual, injection drug use, or other nonoccupational exposure to HIV, emtricitabine/tenofovir (in combination with other antiretrovirals) is effective and recommended for postexposure prophylaxis of HIV-1 infection following nonoccupational exposure in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that may contain HIV when that exposure represents a substantial risk for HIV transmission.

HIV-1 occupational postexposure prophylaxis

Based on the US Public Health Service updated guidelines for the management of occupational exposures to human immunodeficiency virus and recommendations for postexposure prophylaxis, emtricitabine/tenofovir (in combination with raltegravir) is an effective and recommended treatment option for postexposure prophylaxis of HIV-1 infection in healthcare personnel following occupational exposure to blood and/or other body fluids that may contain HIV.

Contraindications

As preexposure prophylaxis in patients with unknown or HIV-1 positive status

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to emtricitabine, tenofovir, or any component of the formulation

Dosing: Adult

HIV-1 infection, preexposure prophylaxis:

Persons who inject drugs (off-label use): Oral: One tablet (emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg) once daily (CDC 2018).

Uninfected individuals at high-risk for sexual acquisition: Oral: One tablet (emtricitabine 200 mg/tenofovir disoproxil fumarate300 mg) once daily in combination with safe sex practices (CDC 2018).

HIV-1 infection, postexposure prophylaxis (off-label use):

Nonoccupational exposure: Oral: One tablet (emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg) once daily for 28 days in combination with other antiretroviral agents. Initiate therapy within 72 hours of exposure (HHS [nPEP 2016]).

Occupational exposure: Oral: One tablet (emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg) once daily for 4 weeks with concomitant raltegravir. Initiate therapy as soon as possible after occupational exposure (and within 72 hours) (Kuhar 2013).

HIV-1 infection, treatment: Oral: One tablet (emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg) once daily in combination with other antiretroviral agents.

HIV-1/hepatitis B co-infection, treatment (off-label use): Oral: One tablet (emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg) once daily in combination with other antiretroviral agents (HHS [adult 2019]).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

HIV-1 infection, treatment: Use in combination with other antiretroviral agents. Note: Multiple tablet strengths exist and contain different amounts of emtricitabine and tenofovir.

Children and Adolescents weighing ≥17 kg and who are able to swallow a tablet whole:

<17 kg: Not intended for use; product is a fixed-dose combination; safety and efficacy have not been established in these patients

17 to <22 kg: Oral: One tablet (emtricitabine 100 mg/tenofovir 150 mg) once daily

22 to <28 kg: Oral: One tablet (emtricitabine 133 mg/tenofovir 200 mg) once daily

28 to <35 kg: Oral: One tablet (emtricitabine 167 mg/tenofovir 250 mg) once daily

≥35 kg: Oral: One tablet (emtricitabine 200 mg/tenofovir 300 mg) once daily

Postexposure prophylaxis, nonoccupational (nPEP) (HHS [nPEP] 2016): Limited data available: Adolescents: Oral: One tablet (emtricitabine 200 mg/tenofovir 300 mg) once daily for 28 days in combination with other antiretroviral agents. Initiate therapy within 72 hours of exposure.

Preexposure prophylaxis (PrEP) in uninfected high-risk individuals: Adolescents weighing ≥35 kg: Oral: One tablet (emtricitabine 200 mg/tenofovir 300 mg) once daily; Note: Patients should be screened for HIV infection prior to initiation of therapy and at least once every 3 months; adherence should also be closely monitored (CDC 2018).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Administration

Oral: May be administered with or without food.

Dietary Considerations

Consider calcium and vitamin D supplementation in patients with history of bone fracture or osteopenia.

Storage

Store tablets at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Dispense only in original container.

Drug Interactions

Acyclovir-Valacyclovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Acyclovir-Valacyclovir. Monitor therapy

Adefovir: May diminish the therapeutic effect of Tenofovir Products. Adefovir may increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Adefovir. Avoid combination

Aminoglycosides: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Aminoglycosides. Monitor therapy

Atazanavir: Tenofovir Disoproxil Fumarate may decrease the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Use boosted atazanavir in adults; give combo (atazanavir/ritonavir or atazanavir/cobicistat with tenofovir) as a single daily dose with food. Pediatric patients, pregnant patients, and use of H2-blockers require dose changes. See Lexi Interact monograph. Consider therapy modification

Cabozantinib: MRP2 Inhibitors may increase the serum concentration of Cabozantinib. Monitor therapy

Cidofovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Cidofovir. Monitor therapy

Cladribine: Agents that Undergo Intracellular Phosphorylation may diminish the therapeutic effect of Cladribine. Avoid combination

Cobicistat: May enhance the adverse/toxic effect of Tenofovir Products. More specifically, cobicistat may impair proper tenofovir monitoring and dosing. Monitor therapy

Darunavir: Tenofovir Disoproxil Fumarate may increase the serum concentration of Darunavir. Darunavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Monitor therapy

Didanosine: Tenofovir Disoproxil Fumarate may diminish the therapeutic effect of Didanosine. Tenofovir Disoproxil Fumarate may increase the serum concentration of Didanosine. Management: Avoid use of tenofovir disoproxil fumarate and didanosine when possible. If combined in adults with CrCL greater than 60 mL/min, decrease didanosine to 250 mg daily if 60 kg or more or to 200 mg if less than 60 kg. Avoid if CrCL is less than 60 mL/min. Consider therapy modification

Ganciclovir-Valganciclovir: Tenofovir Products may increase the serum concentration of Ganciclovir-Valganciclovir. Ganciclovir-Valganciclovir may increase the serum concentration of Tenofovir Products. Monitor therapy

Ledipasvir: May increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Avoid this combination if TDF is used as part of the elvitegravir/cobicistat/emtricitabine/TDF product. Consider alternatives when TDF is used with a ritonavir or cobicistat boosted protease inhibitor. Monitor for increased TDF toxicities if combined. Consider therapy modification

Lopinavir: May enhance the nephrotoxic effect of Tenofovir Disoproxil Fumarate. Lopinavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose due to a potential risk of acute renal failure. Diclofenac appears to confer the most risk. Consider therapy modification

Nonsteroidal Anti-Inflammatory Agents (Topical): May enhance the nephrotoxic effect of Tenofovir Products. Monitor therapy

Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy

Simeprevir: Tenofovir Disoproxil Fumarate may decrease the serum concentration of Simeprevir. Simeprevir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Monitor therapy

Tipranavir: Tenofovir Disoproxil Fumarate may decrease the serum concentration of Tipranavir. Tipranavir may decrease the serum concentration of Tenofovir Disoproxil Fumarate. Monitor therapy

Velpatasvir: May increase the serum concentration of Tenofovir Disoproxil Fumarate. Monitor therapy

Voxilaprevir: Tenofovir Disoproxil Fumarate may increase the serum concentration of Voxilaprevir. Voxilaprevir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Also see individual agents.

>10%: Neuromuscular & skeletal: Decreased bone mineral density (13%)

1% to 10%:

Central nervous system: Headache (7%)

Endocrine & metabolic: Weight loss (3%)

Gastrointestinal: Abdominal pain (4%)

Hematologic & oncologic: Abnormal phosphorus levels (<2.0 mg/dL: 10%), decreased neutrophils (5%)

Neuromuscular & skeletal: Bone fracture (2%)

<1%, postmarketing, and/or case reports: Glycosuria, immune reconstitution syndrome, proteinuria

ALERT: U.S. Boxed Warning

Posttreatment acute exacerbation of hepatitis B:

Severe, acute exacerbations of hepatitis B virus (HBV) have been reported in HBV-infected individuals who have discontinued emtricitabine/tenofovir disoproxil fumarate. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in individuals who are infected with HBV and discontinue emtricitabine/tenofovir disoproxil fumarate. If appropriate, initiation of antihepatitis B therapy may be warranted.

Risk of drug resistance with use for preexposure prophylaxis:

Emtricitabine/tenofovir disoproxil fumarate used for HIV-1 preexposure prophylaxis must only be prescribed to individuals confirmed to be HIV-negative immediately prior to initiating and at least every 3 months during use. Drug-resistant HIV-1 variants have been identified with use of emtricitabine/tenofovir disoproxil fumarate for HIV-1 preexposure prophylaxis following undetected acute HIV-1 infection. Do not initiate emtricitabine/tenofovir disoproxil fumarate for HIV-1 preexposure prophylaxis if signs or symptoms of acute HIV-1 infection are present unless negative infection status is confirmed.

Warnings/Precautions

Concerns related to adverse effects:

• Decreased bone mineral density: In clinical trials, tenofovir disoproxil fumarate has been associated with decreases in bone mineral density in HIV-1 infected adults and increases in bone metabolism markers. Serum parathyroid hormone and 1,25 vitamin D levels were also higher. Decreases in bone mineral density have also been observed in clinical trials of HIV-1 infected pediatric patients. Observations in chronic hepatitis B infected pediatric patients (aged 12-18 years) were similar. In all pediatric clinical trials, skeletal growth (height) appears unaffected. Consider monitoring of bone density in adult and pediatric patients with a history of pathologic fractures or with other risk factors for bone loss or osteoporosis. Consider calcium and vitamin D supplementation for all patients; effect of supplementation has not been studied but may be beneficial. Long-term bone health and fracture risk unknown. If abnormalities are suspected, expert assessment is recommended.

• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome, autoimmune hepatitis) later in therapy; further evaluation and treatment may be required.

• Lactic acidosis/hepatomegaly: Lactic acidosis and severe hepatomegaly with steatosis, sometimes fatal, have been reported with use of nucleoside analogues, alone or in combination with other antiretrovirals. Suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (marked transaminase elevation may/may not accompany hepatomegaly and steatosis).

• Osteomalacia and renal dysfunction: May cause osteomalacia with proximal renal tubulopathy. Bone pain, extremity pain, fractures, arthralgias, weakness and muscle pain have been reported. In patients at risk for renal dysfunction, persistent or worsening bone or muscle symptoms should be evaluated for hypophosphatemia and osteomalacia.

• Renal toxicity: Tenofovir disoproxil fumarate may cause renal toxicity (acute renal failure and/or Fanconi syndrome); avoid use with concurrent or recent nephrotoxic therapy (including high dose or multiple NSAID use). Acute renal failure has occurred in HIV-infected patients with risk factors for renal impairment who were on a stable tenofovir regimen to which a high dose or multiple NSAID therapy was added. Consider alternatives to NSAIDS in patients taking tenofovir disoproxil fumarate and at risk for renal impairment. Calculate creatinine clearance and assess serum creatinine, urine glucose, and urine protein prior to initiation of therapy and as clinically appropriate during therapy. In patients with chronic kidney disease, also assess serum phosphorous. IDSA guidelines recommend discontinuing tenofovir (and substituting with alternative antiretroviral therapy) in HIV-infected patients who develop a decline in GFR (a >25% decrease in GFR from baseline and to a level of <60 mL/minute/1.73 m2) during use, particularly in presence of proximal tubular dysfunction (eg, euglycemic glycosuria, increased urinary phosphorus excretion and hypophosphatemia, proteinuria [new onset or worsening]) (IDSA [Lucas 2014]).

Disease-related concerns:

• Chronic hepatitis B: [US Boxed Warning]: Acute, severe exacerbations of hepatitis B virus (HBV) have been reported in HBV-infected individuals who have discontinued emtricitabine/tenofovir disoproxil fumarate. Closely monitor hepatic function with clinical and laboratory follow-up for at least several months in individuals infected with HBV who discontinue this therapy. If appropriate, anti-hepatitis B therapy may be warranted, especially in patients with advanced liver disease or cirrhosis. All individuals with HIV should be tested for HBV prior to initiation of treatment; HBV-uninfected patients should be offered vaccination.

• Comprehensive prevention program: Preexposure prophylaxis (PrEP) should be accompanied by a comprehensive HIV-1 prevention program (eg, risk reduction counseling, access to condoms), with particular emphasis on medication adherence. In addition, regular monitoring (eg, HIV status of patient and partner(s), risk behavior, adherence, adverse effects, sexually transmitted infections that facilitate HIV-1 transmission) is highly recommended. Time from initiation of therapy to maximal protection against HIV-1 is unknown.

• HIV treatment and renal impairment: Use with caution in patients with renal impairment (CrCl <50 mL/minute); dosage adjustment required. Do not use in patients with CrCl <30 mL/minute or requiring hemodialysis. IDSA guidelines recommend avoiding tenofovir in HIV patients with preexisting kidney disease (CrCl <50 mL/minute and not on hemodialysis or GFR <60 mL/minute/1.73 m2) when other effective HIV treatment options exist because data suggest risk of chronic kidney disease (CKD) is increased (IDSA [Lucas 2014]).

• PrEP and renal impairment: Do not use in CrCl <60 mL/minute.

• Resistance risk with PrEP: [US Boxed Warning]: Confirm HIV-1 negative status immediately before and at least every 3 months during therapy. Do not start PrEP if signs or symptoms of acute HIV-1 infection are present unless HIV-1 negative status is confirmed by a test approved by the Food and Drug Administration (FDA) as an aid to detect HIV-1 infection (including acute or primary infection). Risk of drug resistant HIV-1 variants with PrEP use if patient had undetected acute HIV-1 infection. Some HIV-1 tests (eg, rapid tests) do not detect acute HIV-1 infection. Screen PrEP candidates for acute viral infections and potential exposure events (eg, condomless sex/condom breaking during sex with a partner of unknown HIV-1 status or unknown viremic status, or a recent STI) within 1 month of starting PrEP. If infections or events exist, reconfirm HIV-1 negative status. If a screening test indicates possible HIV-1 infection or if symptoms of acute HIV-1 infection develop after a potential exposure, convert the HIV-1 PrEP regimen to an HIV-1 treatment regimen until negative infection status is confirmed.

Concurrent drug therapy issues:

• Duplicate therapy: Do not use concurrently with emtricitabine, lamivudine, tenofovir disoproxil fumarate, tenofovir alafenamide, or any combination of these drugs.

Monitoring Parameters

CBC with differential, reticulocyte count, creatine kinase, CD4 count, HIV RNA plasma levels, serum phosphorus (individuals with chronic kidney disease); serum creatinine, urine glucose and urine protein (prior to initiation and as clinically indicated during therapy), hepatic function tests, bone density (patients with a history of bone fracture or have risk factors for bone loss); testing for hepatitis B virus (HBV) is recommended prior to the initiation of antiretroviral therapy; weight (children).

Patients with HIV and HBV coinfection should be monitored for several months following tenofovir discontinuation.

HIV-1 preexposure prophylaxis (PrEP) (CDC 2018): Pregnancy test for women receiving PrEP (every 3 months); documented negative HIV test (≤1 week before initiating or reinitiating PrEP and at least every 3 months while taking PrEP), assess symptoms of side effects and sexually transmitted infections (STIs) (every 3 months during therapy); renal function (prior to initiation, 3 months after initiation, then every 6 months); testing for HBV (prior to initiation) and STIs (prior to initiation, then every 3 to 6 months, even if asymptomatic).

HIV occupational postexposure prophylaxis (PEP) (Kuhar 2013): Documented HIV test (at baseline and 6 weeks, 12 weeks, and 6 months after exposure); if confirmation that a fourth generation HIV p2 antigen-HIV antibody test is being used, monitor at baseline, 6 weeks and 4 months after exposure. CBC, renal and hepatic function assessments at baseline and 2 weeks after exposure (minimum recommendations, others dictated by clinical assessment).

Reproductive Considerations

The Health and Human Services (HHS) perinatal HIV guidelines consider this a preferred combination for females living with HIV who are not yet pregnant but are trying to conceive.

This combination is recommended for pre-exposure prophylaxis in couples with discordant HIV status who are planning a pregnancy. The partner without HIV should begin therapy 1 month prior to and continue for 1 month after conception is attempted (HHS [perinatal] 2019).

Refer to individual monographs for additional information.

Pregnancy Considerations

The Health and Human Services (HHS) perinatal HIV guidelines consider emtricitabine with tenofovir disoproxil fumarate to be a preferred nucleoside reverse transcriptase inhibitor backbone for initial therapy in antiretroviral-naive pregnant females. Emtricitabine with tenofovir disoproxil fumarate may also be recommended as part of a regimen when acute HIV infection is detected during pregnancy. In addition, this combination is preferred for use in pregnant females living with HIV who have had antiretroviral therapy (ART) in the past but are restarting, or who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). Females who become pregnant while taking this combination may continue if viral suppression is effective and the regimen is well tolerated.

The HHS perinatal guidelines also recommend emtricitabine plus tenofovir disoproxil fumarate as a component of regimens for HIV/hepatitis B virus-coinfected pregnant females.

Refer to individual monographs for additional information.

Patient Education

What is this drug used for?

• It is used to treat HIV infection.

• It is used in HIV negative patients to lower the chance of getting HIV infection through sex.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Nausea

• Diarrhea

• Trouble sleeping

• Dizziness

• Headache

• Nightmares

• Weight loss

• Loss of strength and energy

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Lactic acidosis like fast breathing, fast heartbeat, abnormal heartbeat, vomiting, fatigue, shortness of breath, severe loss of strength and energy, severe dizziness, feeling cold, or muscle pain or cramps.

• Liver problems like dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin.

• Kidney problems like unable to pass urine, blood in the urine, change in amount of urine passed, or weight gain.

• Depression

• Bone pain

• Muscle pain

• Muscle weakness

• Painful extremities

• Infection

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Frequently Asked Questions