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Emtricitabine

Class: HIV Nucleoside and Nucleotide Reverse Transcriptase Inhibitors
VA Class: AM800
Chemical Name: 5-Fluoro-1-(2R, 5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine
Molecular Formula: C8H10FN3O3S
CAS Number: 143491-57-0
Brands: Emtriva

Emtricitabine is also contained as an ingredient in the following combinations:
Efavirenz, Emtricitabine, and Tenofovir Disoproxil Fumarate
Emtricitabine and Tenofovir Alafenamide
Emtricitabine and Tenofovir Disoproxil Fumarate
Emtricitabine, Rilpivirine Hydrochloride, and Tenofovir Alafenamide
Emtricitabine, Rilpivirine Hydrochloride, and Tenofovir Disoproxil Fumarate

Medically reviewed by Drugs.com on Oct 2, 2020. Written by ASHP.

Warning

    Lactic Acidosis and Hepatomegaly with Steatosis
  • Lactic acidosis and severe hepatomegaly with steatosis, including fatalities, reported in patients receiving HIV nucleoside reverse transcriptase inhibitors (NRTIs) in conjunction with other antiretrovirals. (See Lactic Acidosis and Severe Hepatomegaly with Steatosis under Cautions.)

    HBV Infection
  • Single entity and fixed combinations containing emtricitabine not labeled by FDA for treatment of chronic HBV infection; safety and efficacy not established in HIV-infected patients coinfected with HBV.

  • Severe, acute exacerbations of HBV reported following discontinuance of preparations containing emtricitabine and/or the tenofovir prodrug tenofovir disoproxil fumarate (tenofovir DF) in patients coinfected with HIV-1 and HBV. Monitor hepatic function closely with both clinical and laboratory follow-up for at least several months after emtricitabine or a fixed combination containing emtricitabine and a tenofovir prodrug (tenofovir DF or tenofovir alafenamide) is discontinued in coinfected patients. If appropriate, initiation of HBV treatment may be warranted.

    HIV-1 Preexposure Prophylaxis (PrEP)
  • Prescribe emtricitabine/tenofovir DF (Truvada) for HIV-1 PrEP only for individuals confirmed to be HIV-1-negative immediately prior to initiation of PrEP; confirm HIV-1-negative status periodically (at least every 3 months) during PrEP.

  • Drug-resistant HIV-1 variants have been identified when emtricitabine/tenofovir DF PrEP was used following undetected acute HIV-1 infection. Do not initiate PrEP if signs or symptoms of acute HIV-1 infection are present, unless negative infection status is confirmed. (See Precautions Related to HIV-1 Preexposure Prophylaxis under Cautions.)

Risk Evaluation and Mitigation Strategy (REMS):

FDA approved a REMS for emtricitabine to ensure that the benefits outweigh the risks. The REMS may apply to one or more preparations of emtricitabine and consists of the following: elements to assure safe use. See https://www.accessdata.fda.gov/scripts/cder/rems/.

Introduction

Antiretroviral; HIV nucleoside reverse transcriptase inhibitor (NRTI).

Uses for Emtricitabine

Treatment of HIV Infection

Treatment of HIV-1 infection in adults, adolescents, and pediatric patients; used in conjunction with other antiretrovirals.

Single-entity emtricitabine used with another NRTI (dual NRTIs) in conjunction with an HIV integrase strand transfer inhibitor (INSTI), HIV nonnucleoside reverse transcriptase inhibitor (NNRTI), or HIV protease inhibitor (PI) in INSTI-, NNRTI-, or PI-based regimens. Also commercially available in various fixed combinations containing emtricitabine and a tenofovir prodrug (either tenofovir alafenamide or tenofovir DF) with or without a third antiretroviral; these fixed combinations used in certain patient groups to decrease pill burden and improve compliance.

For initial treatment in HIV-infected adults and adolescents, experts state that emtricitabine and tenofovir alafenamide or emtricitabine and tenofovir DF are recommended dual NRTI options for use in most INSTI-, NNRTI-, and PI-based regimens.

For initial treatment in antiretroviral-naive pediatric patients, experts state that emtricitabine and zidovudine is a preferred dual NRTI option for use with a recommended PI, NNRTI, or INSTI in neonates, infants, and children <12 years of age and an alternative option in adolescents ≥12 years of age in early puberty (sexual maturity rating [SMR] 3). Emtricitabine and abacavir is a preferred dual NRTI option in children ≥3 months of age and in adolescents ≥12 years of age in early puberty (SMR 1–3) who are negative for HLA-B*5701. Emtricitabine and tenofovir alafenamide is a preferred dual NRTI option in adolescents ≥12 years of age in early puberty (SMR 1–3) with estimated Clcr ≥30 mL/minute; emtricitabine and tenofovir DF is an alternative dual NRTI option in adolescents ≥12 years of age at SMR 3, but use in children ≥2 years of age or adolescents at SMR 1 or 2 only in special circumstances after weighing potential risks versus benefits.

Because all 3 drugs have activity against both HIV and HBV, emtricitabine and tenofovir DF or emtricitabine and tenofovir alafenamide are preferred dual NRTI options for antiretroviral regimens in HIV-infected patients coinfected with HBV.

Emtricitabine/tenofovir alafenamide fixed combination (Descovy) can be used in adults and adolescents ≥12 years of age weighing ≥35 kg; used in conjunction with other antiretrovirals for treatment of HIV-1.

Emtricitabine/tenofovir DF fixed combination (Truvada) can be used in adults, adolescents, and children weighing ≥17 kg; used in conjunction with other antiretrovirals for treatment of HIV-1.

Efavirenz/emtricitabine/tenofovir DF fixed combination (Atripla) can be used in adults and adolescents ≥12 years of age weighing ≥40 kg; used alone as a complete treatment regimen or used in conjunction with other antiretrovirals.

Emtricitabine/rilpivirine/tenofovir alafenamide fixed combination (Odefsey) can be used alone as a complete treatment regimen in antiretroviral-naive adults and adolescents ≥12 years of age weighing ≥35 kg with baseline plasma HIV-1 RNA levels ≤100,000 copies/mL; also can be used to replace a stable antiretroviral regimen in antiretroviral-experienced (previously treated) patients who are virologically suppressed (i.e., plasma HIV-1 RNA levels <50 copies/mL) on their current regimen for ≥6 months, have no history of treatment failure, and are infected with HIV-1 with no known substitutions associated with resistance to the components of the fixed combination.

Emtricitabine/rilpivirine/tenofovir DF fixed combination (Complera) can be used alone as a complete treatment regimen in antiretroviral-naive adults and adolescents ≥12 years of age weighing ≥35 kg with baseline plasma HIV-1 RNA levels ≤100,000 copies/mL; also can be used to replace a stable antiretroviral regimen in antiretroviral-experience patients who are virologically suppressed (i.e., plasma HIV-1 RNA levels <50 copies/mL) on their current regimen for ≥6 months, are currently receiving only their first or second antiretroviral regimen, have no history of treatment failure, and have no current evidence or history of resistance to the components of the fixed combination.

Preexposure Prophylaxis for Prevention of HIV-1 Infection (PrEP)

Emtricitabine/tenofovir DF (Truvada) used for preexposure prophylaxis (PrEP) in conjunction with safer sex practices to reduce the risk of sexually acquired HIV-1 in HIV-1-negative adults at high risk.

Adults at high risk include those with partner(s) known to be infected with HIV-1 or those engaging in sexual activity within a high prevalence area or social network and with ≥1 of the following factors: inconsistent or no condom use, diagnosis of sexually transmitted infections, exchange of sex for commodities (e.g., money, food, shelter, drugs), use of illicit drugs, alcohol dependence, incarceration, or partner(s) of unknown HIV-1 status with any of these risk factors.

PrEP with emtricitabine/tenofovir DF not always effective in preventing acquisition of HIV-1 infection; must be used as part of a comprehensive prevention strategy that includes safer sex practices. (See Precautions Related to HIV-1 Preexposure Prophylaxis [PrEP] under Cautions.)

Postexposure Prophylaxis following Occupational Exposure to HIV (PEP)

Postexposure prophylaxis of HIV infection following occupational exposure (PEP) in health-care personnel and others exposed via percutaneous injury (e.g., needlestick, cut with sharp object) or mucous membrane or nonintact skin (e.g., chapped, abraded, dermatitis) contact with blood, tissue, or other body fluids that might contain HIV. Used in conjunction with other antiretrovirals.

USPHS recommends 3-drug regimen of raltegravir in conjunction with emtricitabine and tenofovir DF as the preferred regimen for PEP following occupational exposures to HIV. Several alternative regimens that include an INSTI, NNRTI, or PI and 2 NRTIs (dual NRTIs) also recommended. Preferred dual NRTI option for PEP regimens is emtricitabine and tenofovir DF (may be given as emtricitabine/tenofovir DF; Truvada); alternative dual NRTI options are tenofovir DF and lamivudine, lamivudine and zidovudine (may be given as lamivudine/zidovudine; Combivir), or zidovudine and emtricitabine.

Management of occupational exposures to HIV is complex and evolving; consult infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or National Clinicians’ Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) whenever possible. Do not delay initiation of PEP while waiting for expert consultation.

Postexposure Prophylaxis following Nonoccupational Exposure to HIV (nPEP)

Postexposure prophylaxis of HIV infection following nonoccupational exposure (nPEP) in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that might contain HIV when the exposure represents a substantial risk for HIV transmission. Used in conjunction with other antiretrovirals.

When nPEP indicated in adults and adolescents ≥13 years of age with normal renal function, CDC states preferred regimen is either raltegravir or dolutegravir used in conjunction with emtricitabine and tenofovir DF (given as emtricitabine/tenofovir DF; Truvada); alternative regimen recommended in these patients is ritonavir-boosted darunavir used in conjunction with emtricitabine/tenofovir DF (Truvada).

Consult infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or the National Clinicians’ Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) if nPEP indicated in certain exposed individuals (e.g., pregnant women, children, those with medical conditions such as renal impairment) or if considering a regimen not included in CDC guidelines, source virus is known or likely to be resistant to antiretrovirals, or healthcare provider is inexperienced in prescribing antiretrovirals. Do not delay initiation of nPEP while waiting for expert consultation.

Emtricitabine Dosage and Administration

Administration

Oral Administration

Emtricitabine (Emtriva): Administer orally once daily without regard to meals. Use in conjunction with other antiretrovirals.

Emtricitabine/tenofovir alafenamide (Descovy): Administer orally once daily without regard to meals. Use in conjunction with other antiretrovirals for treatment of HIV-1.

Emtricitabine/tenofovir DF (Truvada): Administer orally once daily without regard to meals. Use in conjunction with other antiretrovirals for treatment of HIV-1; use alone as a complete regimen for PrEP for prevention of sexually transmitted HIV-1.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Administer orally once daily on an empty stomach, preferably at bedtime. Use alone as a complete regimen or in conjunction with other antiretrovirals for treatment of HIV-1.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Administer orally once daily with a meal. Use alone as a complete treatment regimen.

Emtricitabine/rilpivirine/tenofovir DF (Complera): Administer orally once daily with a meal. Use alone as a complete treatment regimen.

Because antiretrovirals contained in the fixed combinations also may be available in single-entity or other fixed-combination preparations, take care to ensure that therapy is not duplicated if a fixed combination is used in conjunction with other antiretrovirals. (See Precautions Related to Use of Fixed Combinations under Cautions.)

Dosage

Emtricitabine (Emtriva) capsules and oral solution are not bioequivalent. (See Bioavailability under Pharmacokinetics.)

Pediatric Patients

Treatment of HIV Infection
Oral

Emtricitabine (Emtriva oral solution containing 10 mg/mL) in infants 0–3 months of age: 3 mg/kg once daily.

Emtricitabine (Emtriva oral solution containing 10 mg/mL) in children and adolescents 3 months to 17 years of age: 6 mg/kg (up to a maximum of 240 mg) once daily.

Emtricitabine (Emtriva capsules) in children weighing >33 kg who can swallow intact capsule: 200 mg once daily.

Emtricitabine/tenofovir alafenamide (Descovy) in adolescents ≥12 years of age weighing ≥35 kg: 1 tablet (emtricitabine 200 mg and tenofovir alafenamide 25 mg) once daily.

Emtricitabine/tenofovir DF (Truvada) in children weighing ≥35 kg: 1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg) once daily.

Emtricitabine/tenofovir DF (Truvada) in children weighing 17 to <35 kg: Base dosage on weight and use a low-strength fixed-combination tablet. (see Table 1)

Table 1. Emtricitabine/tenofovir DF (Truvada) Dosage for Treatment of HIV-1 Infection in Children Weighing ≥17 kg230

Weight (kg)

Dosage of Emtricitabine/tenofovir DF given Once Daily

17 to <22 kg

1 tablet (emtricitabine 100 mg and tenofovir DF 150 mg)

22 to <28 kg

1 tablet (emtricitabine 133 mg and tenofovir DF 200 mg)

28 to <35 kg

1 tablet (emtricitabine 167 mg and tenofovir DF 250 mg)

≥35 kg

1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg)

Efavirenz/emtricitabine/tenofovir DF (Atripla) in adolescents ≥12 years of age weighing ≥40 kg: 1 tablet (efavirenz 600 mg, emtricitabine 200 mg, and tenofovir DF 300 mg) once daily.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) in adolescents ≥12 years of age weighing ≥35 kg: 1 tablet (emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir alafenamide 25 mg) once daily.

Emtricitabine/rilpivirine/tenofovir DF (Complera) in adolescents ≥12 years of age weighing ≥35 kg: 1 tablet (emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg) once daily.

Adults

Treatment of HIV Infection
Oral

Emtricitabine (Emtriva): 200-mg capsule once daily. Alternatively, 240 mg (24 mL) as the oral solution containing 10 mg/mL once daily.

Emtricitabine/tenofovir alafenamide (Descovy): 1 tablet (emtricitabine 200 mg and tenofovir alafenamide 25 mg) once daily.

Emtricitabine/tenofovir DF (Truvada): 1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg) once daily.

Efavirenz/emtricitabine/tenofovir DF (Atripla): 1 tablet (efavirenz 600 mg, emtricitabine 200 mg, and tenofovir DF 300 mg) once daily.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): 1 tablet (emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir alafenamide 25 mg) once daily.

Emtricitabine/rilpivirine/tenofovir DF (Complera): 1 tablet (emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg) once daily.

Preexposure Prophylaxis for Prevention of HIV-1 Infection (PrEP)
HIV-1-negative Adults at High Risk
Oral

Emtricitabine/tenofovir DF (Truvada): 1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg) once daily.

Use PrEP only in high-risk adults confirmed to be HIV-1-negative; do not initiate if signs or symptoms of acute HIV-1 infection are present and recent (<1 month) exposure to HIV-1 is suspected. (See Precautions Related to HIV-1 Preexposure Prophylaxis [PrEP] under Cautions.)

Postexposure Prophylaxis following Occupational Exposure to HIV (PEP)†
Oral

Emtricitabine (Emtriva capsules): 200 mg once daily. Use in conjunction with other antiretrovirals (see Postexposure Prophylaxis following Occupational Exposure to HIV under Uses).

Emtricitabine/tenofovir DF (Truvada): 1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg) once daily. Use in conjunction with a recommended INSTI, NNRTI, or PI (see Postexposure Prophylaxis following Occupational Exposure to HIV [PEP] under Uses).

Emtricitabine/rilpivirine/tenofovir DF (Complera): 1 tablet (emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg) once daily. Use as a complete regimen for PEP.

Initiate PEP as soon as possible following occupational exposure to HIV (preferably within hours); continue for 4 weeks, if tolerated.

Postexposure Prophylaxis following Nonoccupational Exposure to HIV (nPEP)†
Oral

Emtricitabine (Emtriva capsules): 200 mg once daily. Usually used in conjunction with tenofovir DF and a preferred or alternative INSTI, NNRTI, or PI (see Postexposure Prophylaxis following Nonoccupational Exposure to HIV [nPEP] under Uses).

Emtricitabine/tenofovir DF (Truvada): 1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg) once daily. Use in conjunction with a preferred or alternative INSTI, NNRTI, or PI.

Emtricitabine/rilpivirine/tenofovir DF (Complera): 1 tablet (emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg) once daily. Use as a complete regimen for nPEP.

Initiate nPEP as soon as possible (within 72 hours) following nonoccupational exposure that represents a substantial risk for HIV transmission and continue for 28 days.

nPEP not recommended if exposed individual seeks care >72 hours after exposure.

Prescribing Limits

Pediatric Patients

Treatment of HIV Infection
Oral

Emtricitabine (Emtriva) in children 3 months to 17 years of age: Maximum 240 mg (as the oral solution) once daily.

Special Populations

Hepatic Impairment

Treatment of HIV Infection

Emtricitabine not metabolized by liver enzymes; not specifically studied, but clinically important changes in metabolism not expected in patients with hepatic impairment.

Emtricitabine/tenofovir alafenamide (Descovy): Use usual dosage in patients with mild or moderate hepatic impairment (Child-Pugh class A or B); not studied in those with severe hepatic impairment (Child-Pugh class C).

Emtricitabine/tenofovir DF (Truvada): Not studied in hepatic impairment.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Use usual dosage in patients with mild hepatic impairment; caution advised. Not recommended in those with moderate or severe hepatic impairment.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Use usual dosage in patients with mild or moderate hepatic impairment (Child-Pugh class A or B); not studied in those with severe hepatic impairment (Child-Pugh class C).

Emtricitabine/rilpivirine/tenofovir DF (Complera): Use usual dosage in patients with mild or moderate hepatic impairment (Child-Pugh class A or B); not studied in those with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

Treatment of HIV Infection
Oral

Emtricitabine (Emtriva): Reduce dosage in adults with Clcr <50 mL/minute (see Table 2).

Emtricitabine (Emtriva): Data insufficient to make specific emtricitabine dosage recommendations for pediatric patients with renal impairment; consider reducing dose and/or increasing dosing interval.

Table 1. Emtricitabine (Emtriva) Dosage for Treatment of HIV-1 Infection in Adults with Renal Impairment1200

Clcr (mL/minute)

Dosage of Capsules

Dosage of Oral Solution

30–49

200 mg every 48 hours

120 mg every 24 hours

15–29

200 mg every 72 hours

80 mg every 24 hours

<15

200 mg every 96 hours

60 mg every 24 hours

Hemodialysis patients

200 mg every 96 hours; on day of dialysis, give dose after the procedure

60 mg every 24 hours; on day of dialysis, give dose after the procedure

Emtricitabine/tenofovir alafenamide (Descovy): Use usual dosage in patients with estimated Clcr ≥30 mL/minute; not recommended in those with severe renal impairment (estimated Clcr <30 mL/minute).

Emtricitabine/tenofovir DF (Truvada): Use usual dosage in adults with Clcr 50–80 mL/minute; however, monitor calculated Clcr, serum phosphorus, urine glucose, and urine protein. In adults with Clcr 30–49 mL/minute, reduce dosage to 1 tablet (emtricitabine 200 mg and tenofovir DF 300 mg) once every 48 hours; monitor clinical response and renal function since dosage not evaluated clinically. Do not use in adults with Clcr <30 mL/minute (including hemodialysis patients). Data insufficient to make dosage recommendations for treatment of HIV-1 infection in pediatric patients with renal impairment.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Use usual dosage in patients with Clcr ≥50 mL/minute; do not use in those with estimated Clcr <50 mL/minute.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Use usual dosage in patients with estimated Clcr ≥30 mL/minute; not recommended in those with severe renal impairment (estimated Clcr <30 mL/minute).

Emtricitabine/rilpivirine/tenofovir DF (Complera): Do not use in those with moderate, severe, or end-stage renal impairment (estimated Clcr <50 mL/minute) or if dialysis required.

Preexposure Prophylaxis for Prevention of HIV-1 Infection
Oral

Emtricitabine/tenofovir DF (Truvada): Use usual dosage in adults with Clcr ≥60 mL/minute; however, monitor calculated Clcr, serum phosphorus, urine glucose, and urine protein. If Clcr decreases, evaluate potential causes and reassess potential risks and benefits of continued use. Do not use if Clcr <60 mL/minute.

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Cautions for Emtricitabine

Contraindications

  • Known hypersensitivity to emtricitabine or any ingredient in the formulation.

  • Emtricitabine/tenofovir alafenamide (Descovy): Manufacturer states none known.

  • Emtricitabine/tenofovir DF: Do not use alone for treatment of HIV-1 infection; do not use for preexposure prophylaxis of HIV-1 infection in individuals with unknown or positive HIV-1 status. (See Precautions Related to HIV-1 Preexposure Prophylaxis [PrEP] under Cautions.)

  • Efavirenz/emtricitabine/tenofovir DF (Atripla): History of clinically important hypersensitivity reaction (e.g., Stevens-Johnson syndrome, erythema multiforme, toxic skin eruption) to efavirenz; concomitant use with voriconazole contraindicated (because of efavirenz component).

  • Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) or emtricitabine/rilpivirine/tenofovir DF (Complera): Concomitant use with certain drugs that induce CYP3A or elevate gastric pH contraindicated (because of rilpivirine component); substantially decreased plasma concentrations of rilpivirine may occur and may result in loss of virologic response and development of resistance to rilpivirine and/or class resistance to HIV NNRTIs.

  • Fixed combinations containing emtricitabine: Consider contraindications associated with each drug in the fixed combination.

Warnings/Precautions

Warnings

Lactic Acidosis and Severe Hepatomegaly with Steatosis

Lactic acidosis and severe hepatomegaly with steatosis (sometimes fatal) reported in patients receiving HIV NRTIs, including emtricitabine with or without a tenofovir prodrug, in conjunction with other antiretrovirals. Reported most frequently in women; obesity and long-term NRTI therapy also may be risk factors. Cases reported in patients with no known risk factors.

Use emtricitabine (single entity or fixed combinations) with caution in patients with known risk factors for liver disease.

Discontinue if there are clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (e.g., hepatomegaly and steatosis even in the absence of marked increases in serum aminotransferase concentrations).

Individuals with HBV Infection

Test all HIV-infected patients for presence of HBV before initiating antiretroviral therapy.

Emtricitabine (single entity or fixed combinations) not indicated for treatment of chronic HBV infection.

Safety and efficacy not established for treatment of HIV infection in patients coinfected with HBV. (See Treatment of HIV Infection under Uses.)

Severe acute exacerbations of HBV reported following discontinuance of emtricitabine with or without a tenofovir prodrug. HBV exacerbations have been associated with hepatic decompensation and hepatic failure.

If emtricitabine (single entity or fixed combinations) used in patients coinfected with HIV and HBV, closely monitor hepatic function (using both clinical and laboratory follow-up) for at least several months after emtricitabine or fixed combinations containing emtricitabine are discontinued. If appropriate, initiation of HBV treatment may be warranted.

Precautions Related to HIV-1 Preexposure Prophylaxis

Use emtricitabine/tenofovir DF (Truvada) for HIV-1 PrEP only in HIV-1-negative adults at high risk.

Confirm a negative HIV-1 test immediately prior to initiating PrEP and screen for HIV-1 infection at least once every 3 months during PrEP. Also test for HBV prior to initiating PrEP. (See Individuals with HBV Infection under Cautions.)

Emtricitabine/tenofovir DF PrEP not always effective in preventing acquisition of HIV-1 infection.

Must be used as part of a comprehensive HIV prevention strategy that includes other prevention measures (e.g., safer sex practices). (See REMS.) Counsel all uninfected individuals about safer sex practices that include consistent and correct use of condoms, knowledge of their own HIV-1 status and that of their partner(s), and regular testing for other sexually transmitted infections that can facilitate HIV-1 transmission (e.g., syphilis, gonorrhea). Inform and support uninfected individuals regarding efforts to reduce sexual risk behavior.

Because emtricitabine/tenofovir DF alone does not constitute a complete antiretroviral regimen for treatment of HIV-1 infection, HIV-1 resistance-associated mutations may emerge if emtricitabine/tenofovir DF PrEP is used in individuals with undetected HIV-1 infection. Drug-resistant HIV-1 variants have been identified in such individuals.

Many HIV-1 tests (e.g., rapid tests) detect anti-HIV antibodies and may not identify HIV-1 during the acute stage of infection. Prior to initiating PrEP, evaluate HIV-negative individuals for current or recent signs or symptoms consistent with acute viral infections (e.g., fever, fatigue, myalgia, rash) and ask about any potential exposure events within the last month (e.g., unprotected sex, condom broke during sex with HIV-infected partner).

If clinical symptoms consistent with acute viral infection are present and recent (<1 month) exposures to HIV-1 are suspected, delay initiating PrEP for at least 1 month and reconfirm HIV-1 status or use a test approved by FDA as an aid in the diagnosis of HIV-1 infection, including acute or primary HIV-1 infection.

During PrEP, if symptoms consistent with acute HIV-1 infection develop following a potential exposure event, discontinue the drugs until negative infection status is confirmed using a test approved by FDA as an aid in the diagnosis of HIV-1 infection, including acute or primary HIV-1 infection.

Counsel uninfected individuals to strictly adhere to recommended emtricitabine/tenofovir DF dosage schedule. (See Preexposure Prophylaxis [PrEP] for Prevention of HIV-1 Infection under Dosage and Administration.) Effectiveness in reducing risk of acquiring HIV-1 is strongly correlated with adherence.

Adverse effects similar to those reported in HIV-infected patients receiving the drugs for treatment of HIV-1 infection.

Other Warnings/Precautions

Precautions Related to Use of Fixed Combinations

Emtricitabine/tenofovir alafenamide, emtricitabine/tenofovir DF, efavirenz/emtricitabine/tenofovir DF, emtricitabine/rilpivirine/tenofovir alafenamide, emtricitabine/rilpivirine/tenofovir DF: Consider cautions, precautions, contraindications, and interactions associated with each drug in the fixed combination. Consider cautionary information applicable to specific populations (e.g., pregnant or nursing women, individuals with hepatic or renal impairment, geriatric patients) for each drug.

Because the antiretrovirals contained in the fixed-combination preparations also may be available in single-entity or other fixed-combination preparations, take care to ensure that therapy is not duplicated if a fixed combination is used in conjunction with other antiretrovirals.

Do not use multiple emtricitabine-containing preparations concomitantly.

Because of similarities between emtricitabine and lamivudine, do not use emtricitabine (single entity or fixed combinations) concomitantly with any preparation containing lamivudine. In addition, do not use fixed combinations containing tenofovir DF concomitantly with adefovir.

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, breast enlargement, and general cushingoid appearance.

Mechanisms and long-term consequences of adipogenic effects unknown; causal relationship not established.

Immune Reconstitution Syndrome

During initial treatment, HIV-infected patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jirovecii [formerly P. carinii]); this may necessitate further evaluation and treatment.

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barré syndrome) also reported in the setting of immune reconstitution; time to onset is more variable and can occur many months after initiation of antiretroviral therapy.

Specific Populations

Pregnancy

Emtricitabine (Emtriva): Category B.

Emtricitabine/tenofovir alafenamide (Descovy): Insufficient human data to assess risk of birth defects and miscarriage if used in pregnant women.

Emtricitabine/tenofovir DF (Truvada): Category B.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Category D.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Insufficient human data to assess risk of birth defects and miscarriage if used in pregnant women.

Emtricitabine/rilpivirine/tenofovir DF (Complera): Category B.

Antiretroviral Pregnancy Registry at 800-258-4263 or [Web].

Experts state that emtricitabine and tenofovir DF is a preferred dual NRTI option for use in conjunction with an INSTI, NNRTI, or PI for initial treatment of HIV-1 infection in antiretroviral-naive pregnant women, and is a preferred dual NRTI option in pregnant HIV-infected women coinfected with HBV.

Experts state that the dual NRTI option of tenofovir DF and emtricitabine in conjunction with the fixed combination of lopinavir and ritonavir (lopinavir/ritonavir) is a preferred regimen for treatment of HIV type 2 (HIV-2) infection in pregnant women.

If HIV-negative woman receiving emtricitabine/tenofovir DF (Truvada) for HIV-1 PrEP becomes pregnant, carefully consider whether PrEP regimen should be continued, taking into account the potential increased risk of HIV-1 infection during pregnancy.

Lactation

Emtricitabine distributed into human milk in low concentrations.

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.

Pediatric Use

Emtricitabine (Emtriva): Safety and efficacy for treatment of HIV-1 infection in pediatric patients ≥3 months of age is supported by evidence from studies in pediatric patients. Adverse effects reported in children similar to adults. Pharmacokinetics evaluated in a limited number of neonates born to HIV-infected mothers; efficacy in preventing or treating HIV infection in these neonates not determined.

Emtricitabine/tenofovir alafenamide (Descovy): Should not be used in pediatric patients <12 years of age or weighing <35 kg.

Emtricitabine/tenofovir DF (Truvada): Safety and efficacy for treatment of HIV-1 infection not established in pediatric patients weighing <17 kg; safety and efficacy for HIV-1 PrEP not established in pediatric patients.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Do not use in pediatric patients <12 years of age or weighing <40 kg.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Safety and efficacy not established in pediatric patients <12 years of age or weighing <35 kg.

Emtricitabine/rilpivirine/tenofovir DF (Complera): Safety and efficacy not established in pediatric patients <12 years of age or weighing <35 kg.

Geriatric Use

Insufficient experience in those ≥65 years of age to determine whether they respond differently to emtricitabine (single-entity or fixed-combination preparations) than younger adults.

Hepatic Impairment

Emtricitabine not metabolized by liver enzymes; any impact of hepatic impairment expected to be limited. (See Hepatic Impairment under Dosage and Administration.)

Emtricitabine/tenofovir alafenamide (Descovy): Not studied in patients with severe hepatic impairment (Child-Pugh class C).

Emtricitabine/tenofovir DF (Truvada): Not studied in patients with hepatic impairment.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Not recommended in those with moderate or severe hepatic impairment.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Not studied in patients with severe hepatic impairment (Child-Pugh class C).

Emtricitabine/rilpivirine/tenofovir DF (Complera): Not studied in patients with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

Dosage adjustment of emtricitabine (Emtriva) necessary based on degree of renal impairment. Monitor clinical response and renal function in patients with renal impairment. (See Renal Impairment under Dosage and Administration.)

Emtricitabine/tenofovir alafenamide (Descovy): Not recommended in patients with severe renal impairment (estimated Clcr <30 mL/minute).

Emtricitabine/tenofovir DF (Truvada): Do not use for treatment of HIV-1 in patients with Clcr <30 mL/minute or patients with end-stage renal disease requiring dialysis. Do not use for PrEP in HIV-1 uninfected adults with Clcr <60 mL. If Clcr decreases during emtricitabine/tenofovir DF (Truvada) PrEP, evaluate potential causes and reassess potential risks and benefits of continued use.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Do not use in those with estimated Clcr <50 mL/minute.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey): Not recommended in those with severe renal impairment (estimated Clcr <30 mL/minute).

Emtricitabine/rilpivirine/tenofovir DF (Complera): Do not use in those with moderate, severe, or end-stage renal impairment (estimated Clcr <50 mL/minute) or if dialysis required.

Common Adverse Effects

Mild to moderate headache, GI effects (diarrhea, nausea), rash.

Interactions for Emtricitabine

Emtricitabine does not inhibit CYP1A2, 2A6,2B6, 2C9, 2C19, 2D6, or 3A4. Interactions with drugs metabolized by these CYP isoenzymes unlikely.

Emtricitabine does not inhibit glucuronosyltransferase (uridine diphosphoglucuronosyltransferase, UDP-glucuronate β-d-glucuronosyltransferase [acceptor-unspecific]), an enzyme responsible for glucuronidation. Pharmacokinetic interactions unlikely.

The following drug interactions are based on studies using emtricitabine. Interaction studies also have been performed using emtricitabine/tenofovir alafenamide, emtricitabine/tenofovir DF, efavirenz/emtricitabine/tenofovir DF, emtricitabine/rilpivirine/tenofovir alafenamide, or emtricitabine/rilpivirine/tenofovir DF. When a fixed combinations containing emtricitabine is used, consider interactions associated with each drug in the fixed combination.

Specific Drugs

Drug

Interaction

Comments

Abacavir

In vitro evidence of additive or synergistic antiretroviral effects

Atazanavir

No in vitro evidence of antagonistic antiretroviral effects

Darunavir

Pharmacokinetic interaction unlikely

No in vitro evidence of antagonistic antiretroviral effects

Delavirdine

In vitro evidence of additive or synergistic antiretroviral effects

Didanosine

Concomitant use with emtricitabine not recommended in antiretroviral-naive adults (inferior virologic efficacy, limited clinical trial experience, didanosine toxicities); considered alternative (not a preferred) dual NRTI in antiretroviral-naive children ≥2 weeks of age

Efavirenz

In vitro evidence of additive or synergistic antiretroviral effects

Elbasvir and grazoprevir

Fixed combination of elbasvir and grazoprevir (elbasvir/grazoprevir): Clinically important pharmacokinetic interactions with emtricitabine not expected

Etravirine

No in vitro evidence of antagonistic antiretroviral effects

Famciclovir

Pharmacokinetic interaction unlikely

Indinavir

No effect on pharmacokinetics of either drug

Lamivudine

In vitro evidence of additive antiretroviral effects

Do not use concomitantly with emtricitabine (no potential benefit)

Ledipasvir

Fixed combination of ledipasvir and sofosbuvir (ledipasvir/sofosbuvir): Clinically important pharmacokinetic interactions with emtricitabine not expected

Maraviroc

No in vitro evidence of antagonistic antiretroviral effects

Nelfinavir

In vitro evidence of additive to synergistic antiretroviral effects

Nevirapine

In vitro evidence of additive or synergistic antiretroviral effects

Rilpivirine

Pharmacokinetic interactions unlikely

No in vitro evidence of antagonistic antiretroviral effects

Ritonavir

In vitro evidence of additive or synergistic antiretroviral effects

Saquinavir

In vitro evidence of additive or synergistic antiretroviral effects

Simeprevir

Clinically important interactions with emtricitabine not expected

Sofosbuvir

No clinically important pharmacokinetic interactions with emtricitabine

Dosage adjustments not needed for either drug

Stavudine

Pharmacokinetic interaction unlikely

In vitro evidence of additive or synergistic antiretroviral effects

Concomitant use with emtricitabine not recommended (increased toxicities)

Tenofovir

No clinically important pharmacokinetic interactions

In vitro evidence of additive to synergistic antiretroviral effects

No in vitro evidence of antagonistic antiviral effects against HBV

Tipranavir

In vitro evidence of additive antiretroviral effects

Zidovudine

In vitro evidence of additive or synergistic antiretroviral effects

Emtricitabine Pharmacokinetics

Absorption

Bioavailability

Pharmacokinetics in healthy individuals similar to those in individuals with HIV-1 infection.

Rapidly and extensively absorbed; peak plasma concentrations of emtricitabine attained within 1–2 hours.

Emtricitabine capsules: Bioavailability is 93%.

Emtricitabine oral solution: Bioavailability is 75%.

Fixed-combination tablet containing efavirenz 600 mg, emtricitabine 200 mg, and tenofovir DF 300 mg (efavirenz/emtricitabine/tenofovir DF; Atripla) is bioequivalent to a 600-mg tablet of efavirenz, 200-mg capsule of emtricitabine, and 300-mg tablet of tenofovir DF taken simultaneously in fasting state.

Fixed-combination tablet containing emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg (emtricitabine/rilpivirine/tenofovir DF; Complera) taken with a meal is bioequivalent to a 200-mg emtricitabine capsule, 25-mg rilpivirine tablet, and 300-mg tenofovir DF tablet taken simultaneously with a meal.

Fixed-combination tablet containing emtricitabine 200 mg and tenofovir DF 300 mg (emtricitabine/tenofovir DF; Truvada) is bioequivalent to a 200-mg capsule of emtricitabine and 300-mg tablet of tenofovir DF.

Food

Food does not have a clinically important effect on emtricitabine absorption.

Special Populations

Pharmacokinetics in pediatric patients 3 months to 17 years of age receiving recommended emtricitabine dosage (6 mg/kg daily [up to 240 mg daily] as the oral solution or 200-mg capsule once daily) similar to those reported in adults receiving 200 mg daily. AUC reported in neonates receiving 3 mg/kg daily for 4 days similar to that reported in children 3 months to 17 years of age receiving the recommended dosage.

Peak plasma concentrations and AUC of emtricitabine increased in patients with renal impairment (Clcr <50 mL/minute or end-stage renal disease requiring dialysis) due to reduced renal clearance of the drug. Dosage adjustments needed. (See Renal Impairment under Dosage and Administration.)

Distribution

Extent

Emtricitabine distributed into saliva and into vaginal tissue and cervicovaginal fluid following oral administration.

Crosses human placenta.

Distributed into human milk in low concentrations.

Plasma Protein Binding

<4 %.

Elimination

Metabolism

Undergoes oxidation and conjugation with glucuronic acid.

Intracellularly, emtricitabine is phosphorylated and converted by cellular enzymes to the active metabolite, emtricitabine 5′-triphosphate.

Elimination Route

Excreted in urine (86%) and feces (14%). Eliminated by glomerular filtration and active tubular secretion.

Removed by hemodialysis; not known whether removed by peritoneal dialysis.

Half-life

10 hours.

Special Populations

Renal impairment reduces renal clearance.

Stability

Storage

Oral

Capsules

Emtricitabine (Emtriva): 25°C (may be exposed to 15–30°C).

Solution

Emtricitabine (Emtriva): 2–8°C until dispensed. For patient use, store at 25°C (may be exposed to 15–30°C); use within 3 months.

Tablets

Emtricitabine/tenofovir DF (Truvada), efavirenz/emtricitabine/tenofovir DF (Atripla), emtricitabine/rilpivirine/tenofovir DF (Complera): 25°C (may be exposed to 15–30°C). Store in original container; keep tightly closed.

Emtricitabine/tenofovir alafenamide, emtricitabine/rilpivirine/tenofovir alafenamide: <30°C. Dispense in original container; keep tightly closed.

Actions and Spectrum

  • Emtricitabine is an HIV NRTI. Inactive until converted intracellularly to an active 5′-triphosphate metabolite.

  • Active in vitro against HIV-1 and HIV-2. Also has some activity against HBV.

  • Inhibits replication of HIV by interfering with viral RNA-directed DNA polymerase (reverse transcriptase).

  • HIV-1 with reduced susceptibility to emtricitabine have been produced in vitro and have emerged during therapy with the drug.

  • HIV resistant to emtricitabine may be cross-resistant to some other NRTIs (e.g., lamivudine).

  • Cross-resistance between emtricitabine and PIs is highly unlikely since the drugs have different target enzymes. Cross-resistance between emtricitabine and NNRTIs is considered to be low since the drugs bind at different sites on reverse transcriptase and have different mechanisms of action.

Advice to Patients

  • Critical nature of compliance with HIV therapy and importance of remaining under the care of a clinician. Importance of taking as prescribed; do not alter or discontinue antiretroviral regimen without consulting clinician.

  • Importance of using emtricitabine (Emtriva), emtricitabine/tenofovir alafenamide (Descovy), or emtricitabine/tenofovir DF (Truvada) in conjunction with other antiretrovirals for treatment of HIV-1 infection—not for monotherapy.

  • Efavirenz/emtricitabine/tenofovir DF (Atripla), emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey), or emtricitabine/rilpivirine/tenofovir DF (Complera) can be used alone as a complete treatment regimen.

  • Antiretroviral therapy is not a cure for HIV infection; opportunistic infections and other complications associated with HIV disease may still occur.

  • Advise HIV-infected patients that effective antiretroviral treatment regimens can decrease HIV-1 concentrations in blood and genital secretions and strict adherence to such regimens in conjunction with risk-reduction measures may decrease, but cannot absolutely eliminate, the risk of secondary transmission of HIV to others. Importance of continuing to practice safer sex (e.g., using latex or polyurethane condoms to minimize sexual contact with body fluids), never sharing personal items that can have blood or body fluids on them (e.g., toothbrushes, razor blades), and never reusing or sharing needles.

  • Emtricitabine/tenofovir DF (Truvada) medication guide must be provided to and reviewed with all HIV-negative individuals each time emtricitabine/tenofovir DF is dispensed for HIV-1 PrEP. (See REMS.) Advise such individuals of the importance of confirming that they are HIV-1-negative before starting PrEP, importance of regular HIV-1 testing (at least every 3 months) during PrEP, importance of strictly adhering to recommended dosage schedule and not missing any doses, and importance of using a complete prevention strategy that also includes other measures (e.g., consistent condom use, testing for other sexually transmitted infections such as syphilis and gonorrhea that may facilitate HIV-1 transmission, reducing sexual risk behavior). Advise uninfected individuals that PrEP does not protect all individuals from acquiring HIV-1 and to report any symptoms of acute HIV-1 infection (e.g., fever, headache, fatigue, arthralgia, vomiting, myalgia, diarrhea, pharyngitis, rash, night sweats, cervical and inguinal adenopathy) immediately to a clinician.

  • Importance of reading patient information provided by the manufacturer.

  • Advise patients that lactic acidosis and severe hepatomegaly with steatosis, including fatalities, have occurred in patients receiving emtricitabine or other NRTIs in conjunction with other antiretrovirals. Importance of contacting clinician if symptoms suggestive of lactic acidosis or hepatotoxicity (e.g., nausea, vomiting, unusual/unexpected stomach discomfort, weakness) occur.

  • Inform patients that testing for HBV infection recommended before antiretroviral therapy initiated. Also advise patients that severe acute exacerbations of HBV infection have been reported following discontinuance of emtricitabine (single-entity or fixed-combination preparations) in HIV-infected patients coinfected with HBV.

  • Redistribution/accumulation of body fat may occur; cause and long-term health effects unknown.

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Advise HIV-infected women not to breast-feed.

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Emtricitabine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

200 mg

Emtriva

Gilead

Solution

10 mg/mL

Emtriva

Gilead

Emtricitabine Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

100 mg with Tenofovir Disoproxil Fumarate 150 mg

Truvada

Gilead

133 mg with Tenofovir Disoproxil Fumarate 200 mg

Truvada

Gilead

167 mg with Tenofovir Disoproxil Fumarate 250 mg

Truvada

Gilead

200 mg with Tenofovir Disoproxil Fumarate 300 mg

Truvada

Gilead

200 mg with Tenofovir Alafenamide 25 mg

Descovy

Gilead

200 mg with Tenofovir Alafenamide Fumarate 25 mg (of tenofovir alafenamide) and Rilpivirine Hydrochloride 25 mg (of rilpivirine)

Odefsey

Gilead

200 mg with Tenofovir Disoproxil Fumarate 300 mg and Efavirenz 600 mg

Atripla

Bristol-Myers Squibb and Gilead

200 mg with Tenofovir Disoproxil Fumarate 300 mg and Rilpivirine Hydrochloride 25 mg (of rilpivirine)

Complera

Gilead

200 mg with Tenofovir Alafenamide Fumarate 10 mg (of tenofovir alafenamide), Elvitegravir 150 mg, and Cobicistat 150 mg

Genvoya

Gilead

200 mg with Tenofovir Disoproxil Fumarate 300 mg, Elvitegravir 150 mg, and Cobicistat 150 mg

Stribild

Gilead

AHFS DI Essentials™. © Copyright 2021, Selected Revisions October 12, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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