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brand emtriva 200 mg capsule

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Uses

Treatment of HIV Infection

Emtricitabine is used in conjunction with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults, adolescents, and pediatric patients.

Emtricitabine usually is used in multiple-drug regimens that include another HIV nucleoside reverse transcriptase inhibitor (NRTI) (dual NRTIs) and 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. Single-entity emtricitabine is labeled by FDA for use in conjunction with other antiretrovirals in all age groups. Emtricitabine also is commercially available in various fixed-combination preparations that contain a tenofovir prodrug (either tenofovir alafenamide fumarate or tenofovir disoproxil fumarate [tenofovir DF]) with or without a third antiretroviral. These fixed combinations can be used in specific patient groups to decrease pill burden and improve compliance.

If the dual NRTI option of emtricitabine and tenofovir alafenamide is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection, a fixed-combination preparation containing both drugs (emtricitabine/tenofovir alafenamide; Descovy) is commercially available and can be used in adults and adolescents 12 years of age or older weighing at least 35 kg. Emtricitabine/tenofovir alafenamide must be used in conjunction with other antiretrovirals for treatment of HIV-1.

If the dual NRTI option of emtricitabine and tenofovir DF is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection, a fixed-combination preparation containing both drugs (emtricitabine/tenofovir DF; Truvada) is commercially available and can be used in adults, adolescents, and children weighing at least 17 kg. Emtricitabine/tenofovir DF must be used in conjunction with other antiretrovirals for treatment of HIV-1.

If an NNRTI-based regimen of efavirenz, emtricitabine, and tenofovir DF is used for the treatment of HIV-1 infection, a fixed-combination preparation containing all 3 drugs (efavirenz/emtricitabine/tenofovir DF; Atripla) is commercially available and can be used in adults and adolescents 12 years of age or older weighing at least 40 kg. Efavirenz/emtricitabine/tenofovir DF can be used alone as a complete treatment regimen or in conjunction with other antiretrovirals.

If an HIV NNRTI-based regimen of rilpivirine, emtricitabine, and tenofovir alafenamide is used for the treatment of HIV-1 infection, a fixed-combination preparation containing all 3 drugs (emtricitabine/rilpivirine/tenofovir alafenamide; Odefsey) is commercially available and can be used in antiretroviral-naive adults and adolescents 12 years of age or older weighing at least 35 kg with baseline plasma HIV-1 RNA levels of 100,000 copies/mL or less. Emtricitabine/rilpivirine/tenofovir alafenamide also can be used to replace a stable antiretroviral regimen in certain antiretroviral-experienced (previously treated) patients who are virologically suppressed (i.e., plasma HIV-1 RNA levels less than 50 copies/mL). Emtricitabine/rilpivirine/tenofovir alafenamide is used alone as a complete regimen for the treatment of HIV-1 infection.

If an HIV NNRTI-based regimen of rilpivirine, emtricitabine, and tenofovir DF is used for the treatment of HIV-1 infection, a fixed-combination preparation containing all 3 drugs (emtricitabine/rilpivirine/tenofovir DF; Complera) is commercially available and can be used in antiretroviral-naive adults and adolescents 12 years of age or older weighing at least 35 kg with baseline plasma HIV-1 RNA levels of 100,000 copies/mL or less. Emtricitabine/rilpivirine/tenofovir DF also can be used to replace a stable antiretroviral regimen in certain antiretroviral-experienced patients who are virologically suppressed (i.e., plasma HIV-1 RNA levels less than 50 copies/mL). Emtricitabine/rilpivirine/tenofovir DF is used alone as a complete treatment regimen.

A fixed-combination preparation of elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide (EVG/c/FTC/TAF; Genvoya) and a fixed-combination preparation containing elvitegravir, cobicistat, emtricitabine, and tenofovir DF (EVG/c/FTC/TDF; Stribild) also are commercially available for use alone as complete regimens for the treatment of HIV-1 infection. For information on EVG/c/FTC/TAF, see . For information on EVG/c/FTC/TDF, see

The most appropriate antiretroviral regimen cannot be defined for each clinical scenario and selection of specific antiretrovirals for use in multiple-drug regimens should be individualized based on information regarding antiretroviral potency, potential rate of development of resistance, known toxicities, and potential for pharmacokinetic interactions as well as virologic, immunologic, and clinical characteristics of the patient. For information on the general principles and guidelines for use of antiretroviral therapy, including specific recommendations for initial therapy in antiretroviral-naive patients and recommendations for changing antiretroviral regimens,

Antiretroviral-naive Adults and Adolescents

Dual NRTI Options

For initial treatment in HIV-infected adults and adolescents, the US Department of Health and Human Services (HHS) Panel on Antiretroviral Guidelines for Adults and Adolescents states that emtricitabine and tenofovir DF is a recommended dual NRTI option for use in most INSTI-, NNRTI-, and PI-based regimens. This recommendation is based on safety and efficacy data from clinical trials, long term clinical experience, and availability of fixed-combination preparations containing emtricitabine and tenofovir DF.

The HHS panel states that emtricitabine and tenofovir alafenamide is another recommended dual NRTI option for use in most INSTI-, NNRTI-, and PI-based regimens used for initial treatment in antiretroviral-naive adults and adolescents. This recommendation is based on safety and efficacy data from clinical trials, supportive bioequivalence data, and availability of fixed-combination preparations containing emtricitabine and tenofovir alafenamide.

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

A dual NRTI option of emtricitabine and didanosine is not recommended for initial antiretroviral regimens because of inferior virologic efficacy, limited clinical trial experience in antiretroviral-naive patients, and didanosine toxicities (e.g., pancreatitis, peripheral neuropathy).

Emtricitabine and lamivudine should not be used concomitantly at any time since the drugs have similar resistance profiles and concomitant use provides no additional benefit.

Efavirenz, Emtricitabine, and Tenofovir DF

Safety and efficacy of a regimen of efavirenz, emtricitabine, and tenofovir DF are based on results of a randomized, open-label study designed to demonstrate noninferiority of this regimen compared with a regimen of efavirenz, zidovudine, and lamivudine (study 934). In this study, 511 antiretroviral-naive HIV-infected patients (mean age 38 years, 86% male, 59% white, 23% black, median baseline plasma HIV-1 RNA level 5.01 log10 copies/mL [range: 3.56-6.54 log10 copies/mL], mean baseline CD4 T-cell count 245 cells/mm) were randomized to receive a once-daily regimen of efavirenz, emtricitabine, and tenofovir DF or a regimen of efavirenz once daily with the fixed combination of lamivudine and zidovudine (lamivudine/zidovudine; Combivir) twice daily. The primary measure used to assess noninferiority of the regimen of efavirenz, emtricitabine, and tenofovir DF to the regimen of efavirenz and lamivudine/zidovudine was plasma HIV-1 RNA levels at week 48, specifically, the number of patients with HIV-1 RNA levels less than 400 copies/mL. The 487 patients without baseline resistance to efavirenz who underwent randomization and received treatment were the predefined population used for the primary endpoint analysis.

Through week 48, the regimen of efavirenz, emtricitabine, and tenofovir DF met the criteria for noninferiority to the regimen of efavirenz and lamivudine/zidovudine. At week 48, 84 or 80% of adults receiving the efavirenz, tenofovir DF, and emtricitabine regimen and 73 or 70% of adults receiving the efavirenz and lamivudine/zidovudine regimen had plasma HIV-1 RNA levels less than 400 or 50 copies/mL, respectively. At week 48, increases in CD4 T-cell counts were greater in patients receiving the efavirenz, emtricitabine, and tenofovir DF regimen (mean increase of 190 cells/mm) than in those receiving the efavirenz and lamivudine/zidovudine regimen (mean increase of 158 cells/mm). Virologic failure (i.e., individuals who failed to achieve virologic suppression or experienced rebound after achieving virologic suppression) was reported in 2% of those receiving efavirenz, emtricitabine, and tenofovir DF and in 4% of those receiving efavirenz and lamivudine/zidovudine at week 48.

At 144 weeks, 64% of adults receiving the efavirenz, emtricitabine, and tenofovir DF regimen and 56% of those receiving the efavirenz and lamivudine/zidovudine regimen had plasma HIV-1 RNA levels less than 50 copies/mL. The mean increase in CD4 T-cell count from baseline in these groups was 312 and 271 cells/mm, respectively, at 144 weeks.

Emtricitabine, Rilpivirine, and Tenofovir Alafenamide

Efficacy of the fixed combination emtricitabine/rilpivirine/tenofovir alafenamide for the treatment of HIV-1 infection in antiretroviral-naive HIV-infected adults is based on results of clinical trials evaluating a regimen of rilpivirine and emtricitabine/tenofovir DF and clinical trials evaluating a regimen of elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide.

Antiretroviral-experienced Adults and Adolescents

The manufacturer states that a decision to use emtricitabine in previously treated patients should be based on the likelihood that the strain of HIV-1 is susceptible to the drug as assessed by laboratory testing (e.g., genotype testing, phenotype testing) and treatment history.

Study 303

Emtricitabine has been evaluated in a randomized, open-label, multicenter study (study 303) in 440 previously treated adults (mean age: 42 years; 86% male; 64% white; 13% Hispanic; 21% African American; median baseline plasma HIV-1 RNA level: 1.7 log10 copies/mL; mean baseline CD4 T-cell count: 527 cells/mm) who had received a lamivudine-containing regimen that also included 2 other antiretrovirals (background regimen) for at least 12 weeks prior to study entry and had plasma HIV-1 levels of 400 copies/mL or less. Patients in this study were randomized to receive emtricitabine in conjunction with stavudine or zidovudine and a PI or NNRTI or to continue their lamivudine-containing background regimen (i.e., lamivudine in conjunction with stavudine or zidovudine and a PI or NNRTI).

At week 48, 77 and 67% of adults receiving the regimen that included emtricitabine and 82 and 72% of those receiving the regimen that included lamivudine had plasma HIV-1 RNA levels less than 400 or 50 copies/mL, respectively. Virologic failure (i.e., individuals who failed to achieve virologic suppression or experienced rebound after achieving virologic suppression) was reported in 7% of those receiving the emtricitabine-containing regimen and in 8% of those receiving the lamivudine-containing regimen at week 48. Administration of the emtricitabine-containing regimen resulted in a mean increase in CD4 T-cell counts of 29 cells/mm; administration of the lamivudine-containing regimen resulted in a mean increase in CD4 T-cell counts of 61 cells/mm.

Efavirenz, Emtricitabine, and Tenofovir DF

Efficacy of the fixed combination efavirenz/emtricitabine/tenofovir DF (Atripla) was evaluated in a randomized, open-label study (study 073) in antiretroviral-experienced patients who had been receiving a suppressive regimen consisting of at least 2 NRTIs and a PI or NNRTI (mean age 43 years [range 22-73 years]), 88% male, 68% white, 29% black, median CD4 T-cell count 516 cells/mm). Patients had plasma HIV-1 RNA levels less than 200 copies/mL for at least 12 weeks on their existing regimen (96% had plasma HIV-1 levels less than 50 copies/mL), no known HIV-1 substitutions conferring resistance to the components of the fixed combination, and no history of virologic failure; patients were randomized to either switch to efavirenz/emtricitabine/tenofovir DF or continue their existing (baseline) regimen.

At 48 weeks, 89 and 87% of those switched to efavirenz/emtricitabine/tenofovir DF had plasma HIV-1 RNA levels less than 200 and 50 copies/mL, respectively, compared with 88 and 85% of those who remained on their baseline regimen. This difference was not statistically significant. There was no change in CD4 T-cell count from baseline in either group.

Emtricitabine, Rilpivirine, and Tenofovir Alafenamide

The fixed combination emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) can be used to replace a stable antiretroviral regimen for the treatment of HIV-1 in antiretroviral-experienced adults and adolescents 12 years of age or older weighing at least 35 kg who have been virologically suppressed (i.e., plasma HIV-1 RNA levels less than 50 copies/mL) on their current regimen for at least 6 months, have no history of treatment failure, and are infected with HIV-1 with no known substitutions associated with resistance to the antiretroviral components of the fixed combination (i.e., emtricitabine, rilpivirine, tenofovir).

Efficacy of emtricitabine/rilpivirine/tenofovir alafenamide for the treatment of HIV-1 infection in antiretroviral experienced adults is based on results of clinical trials evaluating a regimen of rilpivirine and emtricitabine/tenofovir DF and clinical trials evaluating a regimen of elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide.

Emtricitabine, Rilpivirine, and Tenofovir DF

The fixed combination emtricitabine/rilpivirine/tenofovir DF (Complera) can be used to replace a stable antiretroviral regimen for treatment of HIV-1 infection in antiretroviral-experienced adults and adolescents 12 years of age or older weighing at least 35 kg who have been virologically suppressed (i.e., plasma HIV-1 RNA levels less than 50 copies/mL) on their current regimen for at least 6 months, are currently receiving only their first or second antiretroviral regimen, have no history of virologic failure, and have no current evidence or history of resistance to emtricitabine, rilpivirine, or tenofovir DF.

The efficacy and safety of emtricitabine/rilpivirine/tenofovir DF have been evaluated in a randomized, open-label study (study 106) in 476 virologically suppressed HIV-infected adults (mean age 42 years, 88% male, 77% white, 17% black, 17% Hispanic, mean baseline CD4 T-cell count 584 cells/mm). Patients were receiving their first or second antiretroviral regimen with no history of virologic failure; had no history of resistance to emtricitabine, rilpivirine, or tenofovir DF; and were virologically suppressed (plasma HIV-1 RNA levels less than 50 copies/mL) for at least 6 months. Patients were randomized in a 2:1 ratio to switch to emtricitabine/rilpivirine/tenofovir DF for 48 weeks or to continue receiving their baseline antiretroviral regimen containing a ritonavir-boosted HIV PI for 24 weeks and then switch to emtricitabine/rilpivirine/tenofovir DF for an additional 24 weeks. In patients initially switched to emtricitabine/rilpivirine/tenofovir DF, 89% maintained plasma HIV-1 RNA levels less than 50 copies/mL at 48 weeks; 90% of those who continued to receive their baseline regimen maintained plasma HIV-1 RNA levels less than 50 copies/mL at 24 weeks.

Pediatric Patients

Emtricitabine is used in conjunction with other antiretroviral agents for the treatment of HIV-1 infection in pediatric patients.

The fixed combination emtricitabine/rilpivirine/tenofovir alafenamide or the fixed combination emtricitabine/rilpivirine/tenofovir DF can be used alone as a complete regimen for the treatment of HIV-1 infection in adolescents 12 years of age or older weighing at least 35 kg.

For initial treatment of HIV-infected pediatric patients, the HHS Panel on Antiretroviral Therapy and Medical Management of HIV-infected Children recommends a PI-, NNRTI-, or INSTI-based regimen that includes 2 NRTIs (dual NRTIs).

For use in initial treatment regimens in pediatric patients, the HHS panel states that emtricitabine and zidovudine is a preferred dual NRTI option for antiretroviral-naive neonates, infants, and children younger than 12 years of age and is an alternative dual NRTI option for antiretroviral-naive adolescents 12 years of age or older in early puberty (sexual maturity rating [SMR] 3). These experts also state that emtricitabine and abacavir is a preferred dual NRTI option in children 3 months of age or older and adolescents 12 years of age or older in early puberty (SMR 1-3) who are negative for human leukocyte antigen (HLA)-B*5701.

The HHS panel states that emtricitabine and tenofovir alafenamide is a preferred dual NRTI option for initial treatment regimens in antiretroviral-naive adolescents 12 years of age or older in early puberty (SMR 1-3) with estimated creatinine clearance 30 mL/minute or greater. These experts state that emtricitabine and tenofovir DF is an alternative dual NRTI option for use in antiretroviral-naive children and adolescents 12 years of age or older at SMR 3; however, because decreased bone mineral density (BMD) has been reported in adults and children receiving tenofovir DF, the panel states that the dual option of emtricitabine and tenofovir DF should be used in children 2 years or age or older or adolescents at SMR 1 or 2 only in special circumstances after weighing the potential risk of decreased BMD versus the benefits of the dual NRTI option.

Emtricitabine and didanosine is an alternative (not a preferred) dual NRTI option for initial treatment regimens in children 2 weeks of age or older.

Emtricitabine and lamivudine should not be used concomitantly at any time since the drugs have similar resistance profiles and concomitant use provides no additional benefit.

Antiretroviral regimens containing only NRTIs are not recommended for initial treatment in antiretroviral-naive pediatric patients because of inferior virologic efficacy.

A triple NRTI regimen that includes abacavir, tenofovir DF, and emtricitabine or a triple NRTI regimen that includes tenofovir DF, didanosine, and emtricitabine should not be used at any time in pediatric patients because of the high rate of early virologic failure reported in antiretroviral-naive adults.

For further information on treatment of HIV infection in pediatric patients,

Clinical Experience

Safety and efficacy of emtricitabine in conjunction with other antiretrovirals have been evaluated in 3 open-label, nonrandomized studies in children 3 months to 21 years of age (mean age: 7.9 years; 49% male; 15% white; 24% Hispanic; 61% black; median baseline plasma HIV-1 RNA level: 4.6 log10 copies/mL; mean baseline CD4 T-cell count: 745 cells/mm) who were treatment naive or treatment experienced (i.e., virologic suppression on a lamivudine-containing regimen; emtricitabine substituted for lamivudine). At week 48, 86 or 73% of children had plasma HIV-1 RNA levels less than 400 or 50 copies/mL, respectively. The mean increase in CD4 T-cell counts was 232 cells/mm.

The pharmacokinetics and safety of emtricitabine were evaluated in a dose-finding study in 20 neonates born to HIV-infected mothers.(See Pediatric Use under Warnings/Precautions: Specific Populations, in Cautions.)

Preexposure Prophylaxis for Prevention of HIV-1 Infection

The fixed combination containing emtricitabine and tenofovir DF (emtricitabine/tenofovir DF; Truvada) is 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. The manufacturer states that this indication is based on clinical trials in men who have sex with men (MSM) at high risk for HIV-1 infection and in heterosexual HIV-serodiscordant couples.

Adults at high risk for HIV-1 infection 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 or more 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 (Truvada) is not always effective in preventing acquisition of HIV-1 infection and 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: Warnings/Precautions.)

For additional information on PrEP,

Clinical Experience

Efficacy and safety of a once-daily regimen of emtricitabine/tenofovir DF for HIV-1 PrEP were evaluated in a multinational, randomized, double-blind, placebo-controlled, phase 3 trial (Preexposure Prophylaxis Initiative [iPrEx trial]; NCT00458393) that included 2499 HIV-seronegative men or transgender women (male at birth) who have sex with men and have evidence of high-risk behavior for HIV-1 infection. Study participants (mean age 27 years [range 18-67 years], 5% Asian, 9% black, 18% white, 72% Hispanic/Latino) were randomized to receive emtricitabine/tenofovir DF (a fixed-combination tablet containing 200 mg of emtricitabine and 300 mg of tenofovir DF once daily) or placebo in conjunction with usual prevention strategies (i.e., monthly HIV-1 testing, risk-reduction counseling, condoms, diagnosis and management of sexually transmitted infections) and were followed for 4237 person-years. The primary outcome measure was the incidence of documented HIV seroconversion. There was a 42% reduction in the risk of HIV-1 seroconversion in the group receiving emtricitabine/tenofovir DF (48 individuals receiving emtricitabine/tenofovir DF and 83 individuals receiving placebo seroconverted). Results of a post-hoc case-control study of plasma and intracellular drug concentrations in about 10% of study participants indicated that efficacy of emtricitabine/tenofovir DF PrEP is strongly correlated with adherence since risk reduction appeared to be greatest in those with detectable intracellular tenofovir DF.

Efficacy and safety of emtricitabine/tenofovir DF for PrEP in HIV-1-seronegative partners of serodiscordant heterosexual couples were evaluated in a randomized, double-blind, placebo-controlled, 3-arm trial (Partners Preexposure Prophylaxis [PrEP] trial; NCT00557245) that included 4758 serodiscordant couples in Kenya and Uganda. The infected partners had median plasma HIV-1 RNA levels of 3.9 log10 copies/mL and median CD4 T-cell counts of 495 cells/mm (80% had CD4 T-cell counts of 350 cells/mm or higher). The uninfected partners (mean age 33-34 years, 61-64% male) were randomized to receive emtricitabine/tenofovir DF (a fixed-combination tablet containing 200 mg of emtricitabine and 300 mg of tenofovir DF once daily), tenofovir DF (300 mg of tenofovir DF once daily), or placebo (once daily). Study participants received monthly HIV-1 testing, adherence evaluations, sexual behavior assessments, and safety evaluations. Women received monthly pregnancy tests; if pregnancy occurred, the study drug was interrupted during pregnancy and breast-feeding. After 7827 person-years of follow-up, there were a total of 82 emergent HIV-1 seroconversions (overall observed seroincidence rate of 1.05 per 100 person-years). The risk reduction for the emtricitabine/tenofovir DF group relative to the placebo group was 75%. There were 13 seroconversions in partners randomized to emtricitabine/tenofovir DF and 52 seroconversions in partners randomized to placebo (2 and 3 seroconversions, respectively, occurred during interruption of PrEP for pregnancy). Results of a post-hoc case-control study of plasma and drug concentrations in about 10% of study participants indicated that efficacy of emtricitabine/tenofovir DF PrEP is strongly correlated with adherence since risk reduction appeared to be greatest in those with detectable plasma tenofovir.

Postexposure Prophylaxis following Occupational Exposure to HIV

Emtricitabine is used in conjunction with other antiretrovirals for postexposure prophylaxis of HIV infection following occupational exposure (PEP) in health-care personnel and other individuals 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.

The US Public Health Service (USPHS) states that the preferred regimen for PEP following an occupational exposure to HIV is a 3-drug regimen of raltegravir used in conjunction with emtricitabine and tenofovir DF (may be administered as the fixed combination emtricitabine/tenofovir DF; Truvada). These experts recommend several alternative regimens that include an INSTI, NNRTI, or PI and 2 NRTIs (dual NRTIs). The preferred dual NRTI option for use in PEP regimens is emtricitabine and tenofovir DF (may be administered as the fixed combination emtricitabine/tenofovir DF; Truvada); alternative dual NRTIs are tenofovir DF and lamivudine, lamivudine and zidovudine (may be administered as the fixed combination lamivudine/zidovudine; Combivir), or zidovudine and emtricitabine.

Because management of occupational exposures to HIV is complex and evolving, consultation with an infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or the National Clinicians' Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) is recommended whenever possible. However, initiation of PEP should not be delayed while waiting for expert consultation.

For information on types of occupational exposure to HIV and associated risk of infection, management of occupational exposure to HIV, efficacy and safety of postexposure prophylaxis, and recommendations regarding PEP,

Postexposure Prophylaxis following Nonoccupational Exposure to HIV

Emtricitabine is used in conjunction with other antiretrovirals for 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 that exposure represents a substantial risk for HIV transmission.

When nPEP is indicated following a nonoccupational exposure to HIV, the US Centers for Disease Control and Prevention (CDC) states that the preferred regimen in adults and adolescents 13 years of age or older with normal renal function is either raltegravir or dolutegravir used in conjunction with emtricitabine and tenofovir DF (administered as the fixed combination emtricitabine/tenofovir DF; Truvada). The alternative nPEP regimen recommended in these patients is ritonavir-boosted darunavir used in conjunction with emtricitabine/tenofovir DF (Truvada).

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

For additional information on nonoccupational exposure to HIV and recommendations regarding postexposure prophylaxis,

Dosage and Administration

Administration

Emtricitabine is administered orally once daily without regard to meals.

Single-entity emtricitabine is commercially available as 200-mg capsules or an oral solution containing 10 mg/mL.

Emtricitabine is used in conjunction with other antiretrovirals. Single-entity emtricitabine should not be used concomitantly with any other emtricitabine-containing preparation or with any preparation containing lamivudine.

Fixed Combinations Containing Emtricitabine

Emtricitabine is commercially available in fixed-combination tablets containing emtricitabine and tenofovir alafenamide fumarate (emtricitabine/tenofovir alafenamide; Descovy), fixed-combination tablets containing emtricitabine and tenofovir disoproxil fumarate (emtricitabine/tenofovir DF; Truvada), fixed-combination tablets containing efavirenz, emtricitabine, and tenofovir DF (efavirenz/emtricitabine/tenofovir DF; Atripla), fixed-combination tablets containing rilpivirine, emtricitabine, and tenofovir alafenamide fumarate (emtricitabine/rilpivirine/tenofovir alafenamide; Odefsey), and fixed-combination tablets containing emtricitabine, rilpivirine, and tenofovir DF (emtricitabine/rilpivirine/tenofovir DF; Complera). In addition, emtricitabine is commercially available in fixed-combination tablets containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide fumarate (EVG/c/FTC/TAF; Genvoya) and fixed-combination tablets containing elvitegravir, cobicistat, emtricitabine, and tenofovir DF (EVG/c/FTC/TDF; Stribild). For information on EVG/c/FTC/TAF, see . For information on EVG/c/FTC/TDF, see

Emtricitabine/tenofovir alafenamide (Descovy) tablets are administered orally once daily without regard to meals. For the treatment of human immunodeficiency virus type 1 (HIV-1) infection, emtricitabine/tenofovir alafenamide is used in conjunction with other antiretrovirals.

Emtricitabine/tenofovir DF (Truvada) tablets are administered orally once daily without regard to meals. A fixed-combination tablet containing 200 mg of emtricitabine and 300 mg of tenofovir DF is bioequivalent to a 200-mg capsule of emtricitabine and a 300-mg tablet of tenofovir DF given simultaneously. For the treatment of human immunodeficiency virus type 1 (HIV-1) infection, emtricitabine/tenofovir DF is used in conjunction with other antiretrovirals. For preexposure prophylaxis (PrEP) for prevention of HIV-1 infection, emtricitabine/tenofovir DF is used alone without any other antiretrovirals.

Efavirenz/emtricitabine/tenofovir DF (Atripla) tablets are administered orally once daily on an empty stomach, preferably at bedtime. Administration at bedtime may make efavirenz-related adverse CNS effects more tolerable. A fixed-combination tablet containing 600 mg of efavirenz, 200 mg of emtricitabine, and 300 mg of tenofovir DF is bioequivalent to a 600-mg tablet of efavirenz, 200-mg capsule of emtricitabine, and 300-mg tablet of tenofovir DF when taken in the fasting state. The fixed combination can be used alone as a complete treatment regimen or in conjunction with other antiretrovirals.

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) tablets are administered orally once daily with a meal. The fixed combination is used alone as a complete treatment regimen.

Emtricitabine/rilpivirine/tenofovir DF (Complera) tablets are administered orally once daily with a meal. A fixed-combination tablet containing 200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of tenofovir DF 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. The fixed combination is used alone as a complete treatment regimen.

Because the antiretroviral agents contained in the fixed-combination preparations also may be available in single-entity or other fixed-combination preparations, care should be taken 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 Warnings/Precautions: Other Warnings/Precautions, in Cautions.)

Dosage

Emtricitabine (Emtriva) capsules and oral solution are not bioequivalent. Bioavailability of the oral solution is 80% relative to that of the capsule.

Adult Dosage

Treatment of HIV Infection

For the treatment of HIV-1 infection in adults 18 years of age or older, the usual dosage of emtricitabine (Emtriva) is 200 mg (as the capsule) once daily. Alternatively, when the oral solution containing 10 mg/mL is used, the usual dosage of emtricitabine (Emtriva) is 240 mg (24 mL) once daily.

When emtricitabine/tenofovir alafenamide (Descovy) is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection, adults should receive 1 tablet (200 mg of emtricitabine and 25 mg of tenofovir alafenamide) once daily.

When emtricitabine/tenofovir DF (Truvada) is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection, adults should receive 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF) once daily.

When efavirenz/emtricitabine/tenofovir DF (Atripla) is used for the treatment of HIV-1 infection, adults should receive 1 tablet (600 mg of efavirenz, 200 mg of emtricitabine, and 300 mg of tenofovir DF) once daily.

When emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) is used for the treatment of HIV-1 infection, adults should receive 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 25 mg of tenofovir alafenamide) once daily.

When emtricitabine/rilpivirine/tenofovir DF (Complera) is used for the treatment of HIV-1 infection, adults should receive 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of tenofovir DF) once daily.

Preexposure Prophylaxis for Prevention of HIV-1 Infection

When emtricitabine/tenofovir DF (Truvada) is used for preexposure prophylaxis (PrEP) for prevention of HIV-1 infection in HIV-1-negative adults at high risk, the recommended dosage is 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF) once daily.

PrEP should only be used in high-risk adults (see Uses: Preexposure Prophylaxis for Prevention of HIV-1 Infection) with confirmed HIV-1-negative status. PrEP should not be initiated if signs or symptoms of acute HIV-1 infection are present and recent (within the past month) exposure to HIV-1 is suspected.(See Precautions Related to HIV-1 Preexposure Prophylaxis [PrEP] under Cautions: Warnings/Precautions.)

Postexposure Prophylaxis following Occupational Exposure to HIV

For postexposure prophylaxis of HIV infection following occupational exposure (PEP) in health-care personnel or other individuals, the recommended dosage of emtricitabine is 200 mg (as the capsule) once daily. Emtricitabine usually is used with tenofovir DF or zidovudine in conjunction with a recommended HIV integrase strand transferase inhibitor (INSTI), nonnucleoside reverse transcriptase inhibitor (NNRTI), or HIV protease inhibitor (PI).(See Uses: Postexposure Prophylaxis following Occupational Exposure to HIV.)

When emtricitabine/tenofovir DF (Truvada) is used as the dual NRTI option in PEP regimens, adults should receive 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF) once daily in conjunction with a recommended INSTI, NNRTI, or PI.(See Uses: Postexposure Prophylaxis following Occupational Exposure to HIV.)

When emtricitabine/rilpivirine/tenofovir DF (Complera) is used as a complete regimen for PEP, adults should receive 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of tenofovir DF) once daily.

The PEP regimen should be initiated as soon as possible following occupational exposure to HIV (preferably within hours) and continued for 4 weeks, if tolerated.

Postexposure Prophylaxis following Nonoccupational Exposure to HIV

For postexposure prophylaxis of HIV infection following nonoccupational exposure (nPEP) when the exposure represents a substantial risk for HIV transmission, the usual adult dosage of emtricitabine is 200 mg once daily in conjunction with other antiretrovirals. Emtricitabine usually is used in conjunction with tenofovir DF and a recommended or alternative INSTI, PI, or NNRTI.(See Uses: Postexposure Prophylaxis following Nonoccupational Exposure to HIV.)

When emtricitabine/tenofovir DF (Truvada) is used as the dual NRTI option in nPEP regimens, adults should receive 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF) once daily in conjunction with a preferred or alternative INSTI, PI, or NNRTI.

When emtricitabine/rilpivirine/tenofovir DF (Complera) is used as a complete regimen for nPEP, adults should receive 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of tenofovir DF) once daily.

The nPEP regimen should be initiated as soon as possible (within 72 hours) following nonoccupational exposure to HIV and continued for 28 days. If the exposed individual seeks care more than 72 hours after the exposure, nPEP is not recommended.

Pediatric Dosage

Treatment of HIV Infection

For the treatment of HIV-1 infection in pediatric patients 3 months to 17 years of age, the usual dosage of emtricitabine (Emtriva) is 6 mg/kg (as the oral solution containing 10 mg/mL) once daily (maximum 240 mg daily). Alternatively, children weighing more than 33 kg who can swallow an intact capsule may receive one 200-mg capsule once daily.

The usual dosage of emtricitabine (Emtriva) for the treatment of HIV-1 infection in infants 0-3 months of age is 3 mg/kg (as the oral solution containing 10 mg/mL) once daily.

When emtricitabine/tenofovir alafenamide (Descovy) is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection in adolescents 12 years of age or older weighing at least 35 kg, the recommended dosage is 1 tablet (200 mg of emtricitabine and 25 mg of tenofovir alafenamide) once daily.

When emtricitabine/tenofovir DF (Truvada) is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection in children weighing at least 35 kg, the recommended dosage is 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF) once daily. When emtricitabine/tenofovir DF (Truvada) is used in conjunction with other antiretrovirals for the treatment of HIV-1 infection in children weighing 17 to less than 35 kg who are able to swallow a tablet, the recommended dosage is based on weight; a low-strength fixed-combination tablet of the drug should be used.(See Table 1.)

Table 1. Emtricitabine/tenofovir DF (Truvada®) Dosage for Treatment of HIV-1 Infection in Children Weighing 17 kg or more[230 ]
Weight (kg) Dosage of Emtricitabine/tenofovir DF given Once Daily
17 to less than 22 kg 1 tablet (100 mg of emtricitabine and 150 mg of tenofovir DF)
22 to less than 28 kg 1 tablet (133 mg of emtricitabine and 200 mg of tenofovir DF)
28 to less than 35 kg 1 tablet (167 mg of emtricitabine and 250 mg of tenofovir DF)
35 kg or more 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF)

When efavirenz/emtricitabine/tenofovir DF (Atripla) is used for the treatment of HIV-1 infection in adolescents 12 years of age or older weighing at least 40 kg, the recommended dosage is 1 tablet (600 mg of efavirenz, 200 mg of emtricitabine, and 300 mg of tenofovir DF) once daily.

When emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) is used for the treatment of HIV-1 infection in adolescents 12 years of age or older weighing at least 35 kg, the usual dosage is 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 25 mg of tenofovir alafenamide) once daily.

When emtricitabine/rilpivirine/tenofovir DF (Complera) is used for the treatment of HIV-1 infection in adolescents 12 years of age or older weighing at least 35 kg, the usual dosage is 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of tenofovir DF) once daily.

Special Populations

Hepatic Impairment

While the pharmacokinetics of emtricitabine have not been specifically studied in patients with hepatic impairment, the drug is not metabolized by liver enzymes and clinically important changes in emtricitabine metabolism are not expected if the drug is used in patients with hepatic impairment.

If emtricitabine/tenofovir alafenamide (Descovy) is used for the treatment of HIV-1 infection in patients with mild or moderate hepatic impairment (Child-Pugh class A or B), usual dosage can be used; the fixed combination has not been studied in those with severe hepatic impairment (Child-Pugh class C).

Emtricitabine/tenofovir DF (Truvada) has not been studied in patients with hepatic impairment.

When efavirenz/emtricitabine/tenofovir DF (Atripla) is used for the treatment of HIV-1 infection, usual dosage can be used in patients with mild hepatic impairment; however, caution is advised. The fixed combination is not recommended in those with moderate or severe hepatic impairment.

When emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) is used for the treatment of HIV-1 infection in patients with mild or moderate hepatic impairment (Child-Pugh class A or B), usual dosage can be used; the fixed combination has not been studied in those with severe hepatic impairment (Child-Pugh class C).

When emtricitabine/rilpivirine/tenofovir DF (Complera) is used for the treatment of HIV-1 infection in patients with mild or moderate hepatic impairment (Child-Pugh class A or B), usual dosage can be used; the fixed combination has not been studied in those with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

When emtricitabine (Emtriva) is used for the treatment of HIV-1 infection in adults, dosage should be adjusted in those with creatinine clearance less than 50 mL/minute (see Table 2). The manufacturer states that data are insufficient to make emtricitabine dosage recommendations for treatment of HIV-1 infection in pediatric patients with renal impairment; however, a reduction in the dose and/or increase in dosing interval similar to adjustments for adults should be considered.

Table 2. Emtricitabine (Emtriva®) Dosage for Treatment of HIV-1 Infection in Adults with Renal Impairment[1 ]
Creatinine Clearance (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
less than 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

When emtricitabine/tenofovir alafenamide (Descovy) is used for the treatment of HIV-1 infection, usual dosage can be used in patients with estimated creatinine clearance of 30 mL/minute or greater; the fixed combination is not recommended in those with severe renal impairment (estimated creatinine clearance less than 30 mL/minute).

When emtricitabine/tenofovir DF (Truvada) is used for the treatment of HIV-1 infection in adults, usual dosage can be used in those with mild renal impairment (creatinine clearance 50-80 mL/minute), but calculated creatinine clearance, serum phosphorus, urine glucose, and urine protein should be monitored. If the fixed combination is used in adults with creatinine clearance of 30-49 mL/minute, dosage should be reduced to 1 tablet (200 mg of emtricitabine and 300 mg of tenofovir DF) once every 48 hours; clinical response and renal function should be monitored since dosage has not been evaluated clinically. Emtricitabine/tenofovir DF should not be used for treatment of HIV-1 infection in adults with creatinine clearances less than 30 mL/minute (including hemodialysis patients). Data are insufficient to make dosage recommendations for the fixed combination for treatment of HIV-1 infection in pediatric patients with renal impairment.

When emtricitabine/tenofovir DF (Truvada) is used for PrEP for prevention of HIV-1 infection in HIV-1-negative adults at high risk, usual dosage can be used in those with creatinine clearances of 60 mL/minute or greater, but calculated creatinine clearance, serum phosphorus, urine glucose, and urine protein should be monitored. If creatinine clearance decreases while emtricitabine/tenofovir DF is being used for PrEP, potential causes should be evaluated and potential risks and benefits of continued use should be reassessed. Emtricitabine/tenofovir DF should not be used for PrEP in adults with creatinine clearances less than 60 mL/minute.

When efavirenz/emtricitabine/tenofovir DF (Atripla) is used for the treatment of HIV-1 infection, usual dosage can be used in patients with creatinine clearance of 50 mL/minute or greater. The fixed combination should not be used in those with moderate or severe renal impairment (estimated creatinine clearances less than 50 mL/minute).

When emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) is used for the treatment of HIV-1 infection, usual dosage can be used in patients with estimated creatinine clearance of 30 mL/minute or greater; the fixed combination is not recommended in those with severe renal impairment (estimated creatinine clearance less than 30 mL/minute).

Emtricitabine/rilpivirine/tenofovir DF (Complera) should not be used in patients with renal impairment that is moderate, severe, or end-stage (estimated creatinine clearance less than 50 mL/minute) or requires dialysis.

Cautions

Contraindications

Emtricitabine is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.

The manufacturer states that there are no known contraindications for use of the fixed combination of emtricitabine and tenofovir alafenamide (emtricitabine/tenofovir alafenamide; Descovy).

The fixed combination containing emtricitabine and tenofovir disoproxil fumarate (emtricitabine/tenofovir DF; Truvada) should not be used alone for treatment of HIV-1 infection and should not be used for preexposure prophylaxis of HIV-1 infection in individuals with unknown or positive HIV-1 status.(See Precautions Related to HIV-1 Preexposure Prophylaxis under Warnings/Precautions: Warnings, in Cautions.)

The fixed combination containing efavirenz, emtricitabine, and tenofovir DF (efavirenz/emtricitabine/tenofovir DF; Atripla) is contraindicated in patients who have had a clinically important hypersensitivity reaction (e.g., Stevens-Johnson syndrome, erythema multiforme, toxic skin eruption) to efavirenz; because of the efavirenz component, concomitant use of this fixed combination and voriconazole is contraindicated.

Concomitant use of the fixed combination containing emtricitabine, rilpivirine, and tenofovir alafenamide (emtricitabine/rilpivirine/tenofovir alafenamide; Odefsey) or fixed combination containing emtricitabine, rilpivirine, and tenofovir disoproxil fumarate (emtricitabine/rilpivirine/tenofovir DF; Complera) and certain drugs that induce cytochrome P-450 isoenzyme 3A (CYP3A) or drugs that elevate gastric pH is contraindicated because of the 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 human immunodeficiency virus (HIV) nonnucleoside reverse transcriptase inhibitors (NNRTIs).

When emtricitabine/tenofovir alafenamide, emtricitabine/tenofovir DF, efavirenz/emtricitabine/tenofovir DF, emtricitabine/rilpivirine/tenofovir alafenamide, or emtricitabine/rilpivirine/tenofovir DF are used, the contraindications associated with each drug in the fixed combination should be considered.(See Precautions Related to Use of Fixed Combinations under Warnings/Precautions: Other Warnings/Precautions, in Cautions.)

Warnings/Precautions

Warnings

Lactic Acidosis and Severe Hepatomegaly with Steatosis

Lactic acidosis and severe hepatomegaly with steatosis, including fatalities, have been reported in patients receiving HIV nucleoside reverse transcriptase inhibitors (NRTIs), including emtricitabine with or without a tenofovir prodrug, in conjunction with other antiretroviral agents. Most reported cases have involved women; obesity and long-term therapy with NRTIs also may be risk factors.

Caution should be observed when NRTIs are used in patients with known risk factors for liver disease; however, lactic acidosis and severe hepatomegaly with steatosis have been reported in patients with no known risk factors. Emtricitabine (single-entity or fixed-combination preparations) should be discontinued in any patient with clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (signs of hepatotoxicity include hepatomegaly and steatosis even in the absence of marked increases in serum aminotransferase concentrations).

Individuals with Hepatitis B Virus Infection

Prior to initiating emtricitabine (single-entity or fixed-combination preparations) for treatment of human immunodeficiency virus type 1 (HIV-1) infection, the patient should be tested for chronic hepatitis B virus (HBV).

Although emtricitabine has some activity against HBV, single-entity or fixed-combination preparations containing emtricitabine are not indicated for treatment of chronic HBV infection.

Safety and efficacy of emtricitabine (single-entity or fixed-combination preparations) have not been established in patients with HBV and HIV-1 coinfection. However, when selecting components of an antiretroviral regimen for HIV-infected patients coinfected with HBV, some experts state that emtricitabine and tenofovir alafenamide or emtricitabine and tenofovir DF are preferred dual NRTI options in such patients since these antiretrovirals have activity against both HIV and HBV.

Severe acute exacerbations of HBV infection have been reported in HIV-infected patients following discontinuance of emtricitabine with or without a tenofovir prodrug. In some of these patients, exacerbations of HBV have been associated with hepatic decompensation and hepatic failure. Hepatic function should be closely monitored with clinical and laboratory follow-up for at least several months after stopping emtricitabine therapy (single-entity or fixed-combination preparations) in HIV-infected patients coinfected with HBV. If appropriate, initiation of treatment for HBV infection may be warranted.

Precautions Related to HIV-1 Preexposure Prophylaxis

Only the fixed combination containing emtricitabine and tenofovir DF (emtricitabine/tenofovir DF; Truvada) should be used for PrEP. Emtricitabine should not be used alone for HIV-1 PrEP.

Emtricitabine/tenofovir DF should be used for HIV-1 PrEP only in HIV-1-negative adults at high risk.

A negative HIV-1 test should be confirmed immediately prior to initiation of emtricitabine/tenofovir DF for HIV-1 PrEP and screening for HIV-1 infection should be performed at least once every 3 months during PrEP. Individuals also should be tested for HBV prior to initiation of emtricitabine/tenofovir DF PrEP.(See Individuals with Hepatitis B Virus (HBV) Infection under Cautions: Warnings/Precautions.)

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

Emtricitabine/tenofovir DF PrEP must be used as part of a comprehensive HIV prevention strategy that includes other prevention measures (e.g., safer sex practices). (See REMS.) All uninfected individuals should be counseled 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). All HIV-negative individuals should be informed about and supported in their 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 PrEP is used in individuals with undetected HIV-1 infection. Drug-resistant HIV-1 variants have been identified when emtricitabine/tenofovir DF PrEP was used in such individuals.

Clinicians should consider that 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 emtricitabine/tenofovir DF PrEP, clinicians should evaluate HIV-negative individuals for current or recent signs or symptoms consistent with acute viral infection (e.g., fever, fatigue, myalgia, rash) and ask about any potential exposure events that may have occurred 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 (within 1 month) exposures to HIV-1 are suspected, initiation of emtricitabine/tenofovir DF PrEP should be delayed for at least 1 month and HIV-1 status reconfirmed or a test approved by the US Food and Drug Administration (FDA) for use as an aid in the diagnosis of HIV-1 infection, including acute or primary HIV-1 infection, should be used.

During emtricitabine/tenofovir DF PrEP, if symptoms consistent with acute HIV-1 infection develop following a potential exposure event, the drugs should be discontinued 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.

Uninfected individuals should be counseled to strictly adhere to the recommended emtricitabine/tenofovir DF dosage schedule (see Preexposure Prophylaxis for Prevention of HIV-1 Infection under Dosage: Adult Dosage, in Dosage and Administration). Effectiveness of the fixed combination in reducing the risk of acquiring HIV-1 is strongly correlated with adherence as demonstrated by measurable tenofovir concentrations in clinical trials.

Adverse effects reported in HIV-negative adults receiving emtricitabine/tenofovir DF PrEP are 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

When emtricitabine/tenofovir alafenamide, emtricitabine/tenofovir DF, efavirenz/emtricitabine/tenofovir DF, emtricitabine/rilpivirine/tenofovir alafenamide, or emtricitabine/rilpivirine/tenofovir DF is used, the cautions, precautions, contraindications, and drug interactions associated with each drug in the fixed combination must be considered. Cautionary information applicable to specific populations (e.g., pregnant or nursing women, individuals with hepatic or renal impairment, geriatric patients) should be considered for each drug. For cautionary information related to , , and , see Cautions in the individual drug monographs.

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

Multiple emtricitabine-containing preparations should not be used concomitantly.

Because of similarities between emtricitabine and lamivudine, emtricitabine (single-entity or fixed-combination preparations) should not be used concomitantly with any preparation containing lamivudine. In addition, fixed combinations containing tenofovir DF should not be used concomitantly with adefovir dipivoxil.

Adipogenic Effects

Redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (''buffalo hump''), peripheral wasting, breast enlargement, and general cushingoid appearance, has been reported in patients receiving antiretroviral therapy. The mechanism and long-term consequences of fat redistribution are unknown; a causal relationship has not been established.

Immune Reconstitution Syndrome

Immune reconstitution syndrome has been reported in HIV-infected patients receiving multiple-drug antiretroviral therapy, including emtricitabine. During the initial phase of treatment, HIV-infected patients whose immune systems 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]); such response may necessitate further evaluation and treatment.

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barre syndrome) have also been reported to occur in the setting of immune reconstitution; however, the 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 the 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 the 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 http://www.APRegistry.com.

The US Department of Health and Human Services (HHS) Panel on Treatment of HIV-infected Pregnant Women and Prevention of Perinatal Transmission states that emtricitabine and tenofovir DF is a preferred dual NRTI option for use in conjunction with an HIV integrase strand transfer inhibitor (INSTI), HIV nonnucleoside reverse transcriptase inhibitor (NNRTI), or HIV protease inhibitor (PI) for initial treatment of HIV-1 infection in antiretroviral-naive pregnant women, and is a preferred dual NRTI option in pregnant women coinfected with HBV.

Some experts state that the dual NRTI option of emtricitabine and tenofovir DF used 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 an HIV-1-negative woman receiving emtricitabine/tenofovir DF (Truvada) for HIV-1 PrEP becomes pregnant, careful consideration should be given to whether the PrEP regimen should be continued, taking into account the potential increased risk of HIV-1 infection during pregnancy.

Lactation

Emtricitabine is distributed into human milk in low concentrations.

Because of the risk of adverse effects in the infant and the risk of HIV transmission, HIV-infected women should not breast-feed infants.

Pediatric Use

Safety and efficacy of emtricitabine (Emtriva) have been established for treatment of HIV-1 infection in children 3 months of age and older.

The pharmacokinetics and safety of emtricitabine were evaluated in a dose-finding study in 20 neonates born to HIV-infected mothers. These neonates received zidovudine prophylaxis for 6 weeks. In addition, these neonates received 2 short courses of emtricitabine (3 mg/kg daily for 4 days per course) during the first 12 weeks of life. This dose was well tolerated and was not associated with any safety issues. Systemic exposure (area under the plasma concentration-time curve [AUC]) in infants 0-3 months of age receiving emtricitabine 3 mg/kg daily was similar to that reported in children 3 months to 17 years of age receiving emtricitabine 6 mg/kg daily. All neonates were HIV-1 negative at the end of the study (6 months postpartum); efficacy of emtricitabine for the prevention or treatment of HIV was not determined.

Emtricitabine/tenofovir alafenamide (Descovy) should not be used in pediatric patients younger than 12 years of age or weighing less than 35 kg.

Safety and efficacy of emtricitabine/tenofovir DF (Truvada) for treatment of HIV-1 infection have not been established in pediatric patients weighing less than 17 kg; safety and efficacy of this fixed combination for HIV-1 PrEP have not been established in pediatric patients.

Efavirenz/emtricitabine/tenofovir DF (Atripla): Should not be used in pediatric patients younger than 12 years of age or weighing less than 40 kg.

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

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

Geriatric Use

Experience in those 65 years of age or older is insufficient to determine whether they respond differently to emtricitabine (single-entity or fixed-combination preparations) than younger adults. Dosage should be selected with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.

Hepatic Impairment

Emtricitabine has not been studied in patients with hepatic impairment; impact of hepatic impairment is expected to be minimal.(See Hepatic Impairment under Dosage and Administration: Special Populations.)

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

Emtricitabine/tenofovir DF (Truvada) has not been studied in patients with hepatic impairment. Hepatic impairment does not have a substantial effect on tenofovir DF pharmacokinetics and is expected to have a minimal impact on emtricitabine pharmacokinetics.

Efavirenz/emtricitabine/tenofovir DF (Atripla) is not recommended in patients with moderate or severe hepatic impairment.

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

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

Renal Impairment

Emtricitabine is principally eliminated by the kidney and the pharmacokinetics of the drug are altered in patients with renal impairment. If renal function is impaired, dosage of single-entity emtricitabine (Emtriva) must be adjusted based on creatinine clearance.(See Renal Impairment under Dosage and Administration: Special Populations.)

Emtricitabine/tenofovir alafenamide (Descovy) is not recommended in patients with severe renal impairment (estimated creatinine clearance less than 30 mL/minute).

Emtricitabine/tenofovir DF (Truvada) should not be used for treatment of HIV-1 infection in patients with creatinine clearance less than 30 mL/minute or in those with end-stage renal disease requiring dialysis; dosage adjustments are necessary when the drug is used for treatment of HIV-1 infection in those with creatinine clearance 30-49 mL/minute.(See Renal Impairment under Dosage and Administration: Special Populations.) Emtricitabine/tenofovir DF should not be used for PrEP in HIV-1 uninfected adults with creatinine clearance less than 60 mL/minute. If creatinine clearance decreases while emtricitabine/tenofovir DF is being used for PrEP, potential causes should be evaluated and potential risks and benefits of continued use should be reassessed.

Efavirenz/emtricitabine/tenofovir DF (Atripla) should not be used in patients with moderate or severe renal impairment (estimated creatinine clearance less than 50 mL/minute,).

Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) is not recommended in patients with severe renal impairment (estimated creatinine clearance less than 30 mL/minute).

Emtricitabine/rilpivirine/tenofovir DF (Complera) should not be used in patients with renal impairment that is moderate, severe, or end-stage (estimated creatinine clearance less than 50 mL/minute) or requires dialysis.

Common Adverse Effects

The most common adverse effects in adults receiving emtricitabine in conjunction with other antiretrovirals are mild to moderate headache, diarrhea, nausea, and rash. Adverse effects reported in children 3 months to 21 years of age receiving emtricitabine in clinical studies have been similar to those in adults, with the exception of a higher frequency of hyperpigmentation.

Drug Interactions

The following drug interactions are based on studies using emtricitabine.

Drug interaction studies have also been performed using the fixed combination containing emtricitabine and tenofovir alafenamide (emtricitabine/tenofovir alafenamide; Descovy), fixed combination containing emtricitabine and tenofovir disoproxil fumarate (emtricitabine/tenofovir DF; Truvada), fixed combination containing efavirenz, emtricitabine, and tenofovir DF (efavirenz/emtricitabine/tenofovir DF; Atripla), fixed combination containing emtricitabine, rilpivirine, and tenofovir alafenamide (emtricitabine/rilpivirine/tenofovir alafenamide; Odefsey), or fixed combination containing emtricitabine, rilpivirine, and tenofovir DF (emtricitabine/rilpivirine/tenofovir DF; Complera). When a fixed combinations is used, interactions associated with each drug in the fixed combination should be considered.

Drugs Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions between emtricitabine and drugs metabolized by hepatic microsomal enzymes are unlikely. In vitro studies indicate that emtricitabine does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, or 3A4.

Drugs Metabolized by Uridine Diphosphate-glucuronosyltransferase

Pharmacokinetic interactions between emtricitabine and drugs metabolized by uridine diphosphate-glucuronosyltransferase are unlikely. Emtricitabine does not inhibit glucuronosyltransferase (uridine diphosphoglucuronosyltransferase, UDP-glucuronate β-d-glucuronosyltransferase [acceptor-unspecific]), an enzyme responsible for glucuronidation.

Antiretroviral Agents

HIV Entry and Fusion Inhibitors

Maraviroc

No in vitro evidence of antagonistic antiretroviral effects between maraviroc and emtricitabine.

HIV Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Although not specifically studied, clinically important pharmacokinetic interactions between rilpivirine and emtricitabine are unlikely.

In vitro evidence of additive or synergistic antiretroviral effects between emtricitabine and NNRTIs (e.g., delavirdine, efavirenz, nevirapine). No in vitro evidence of antagonistic antiretroviral effects between emtricitabine and etravirine or rilpivirine.

HIV Nucleoside and Nucleotide Reverse Transcriptase Inhibitors (NRTIs)

In vitro evidence of additive to synergistic antiretroviral effects between emtricitabine and nucleoside and HIV nucleotide reverse transcriptase inhibitors (NRTIs) (e.g., abacavir, stavudine, tenofovir DF, zidovudine).

Lamivudine

Emtricitabine and lamivudine should not be used concomitantly. Because emtricitabine is an analog of lamivudine, the drugs have similar resistance profiles and concomitant use provides no additional benefit.

Stavudine

No clinically important pharmacokinetic interactions between emtricitabine and stavudine.

Tenofovir

No clinically important pharmacokinetic interactions between emtricitabine and tenofovir DF.

Zidovudine

Although not considered clinically important, concomitant use of emtricitabine (200 mg once daily for 7 days) and zidovudine (300 mg twice daily for 7 days) increased zidovudine peak plasma concentrations and area under the concentration-time curve (AUC) by 17 and 13%, respectively, but did not affect emtricitabine peak plasma concentrations or AUC.

HIV Protease Inhibitors (PIs)

Although not specifically studied, pharmacokinetic interactions between darunavir and emtricitabine are unlikely.

No clinically important pharmacokinetic interactions between emtricitabine and indinavir.

In vitro evidence of additive or synergistic antiretroviral effects between emtricitabine and HIV PIs (e.g., amprenavir, nelfinavir, ritonavir, saquinavir, tipranavir). No in vitro evidence of antagonistic antiretroviral effects between emtricitabine and atazanavir or darunavir.

Famciclovir

No clinically important pharmacokinetic interactions between emtricitabine and famciclovir.

HCV Antivirals

HCV Polymerase Inhibitors

Sofosbuvir

Concomitant use of emtricitabine and sofosbuvir does not have a clinically important effect on the pharmacokinetics of either drug. Dosage adjustments are not needed for either drug.

HCV Protease Inhibitors

Simeprevir

No clinically important interactions are expected if simeprevir is used concomitantly with emtricitabine.

HCV Replication Complex Inhibitors

Elbasvir and Grazoprevir

Clinically important pharmacokinetic interactions are not expected if emtricitabine is used concomitantly with the fixed combination of elbasvir and grazoprevir (elbasvir/grazoprevir).

Ledipasvir and Sofosbuvir

Clinically important pharmacokinetic interactions are not expected if emtricitabine is used concomitantly with the fixed combination of ledipasvir and sofosbuvir (ledipasvir/sofosbuvir).

Pharmacokinetics

The pharmacokinetics of emtricitabine in healthy individuals are similar to that in individuals with human immunodeficiency virus type 1 (HIV-1) infection.

Absorption

Following oral administration, emtricitabine is rapidly and extensively absorbed; peak plasma concentrations of the drug are attained within 1-2 hours.

Emtricitabine capsules: Mean absolute oral bioavailability is 93%.

Emtricitabine oral solution: Mean absolute oral bioavailability is 75%.

A fixed-combination tablet containing efavirenz 600 mg, tenofovir disoproxil fumarate (tenofovir DF) 300 mg, and emtricitabine 200 mg (Atripla) is bioequivalent to a 600-mg tablet of efavirenz, a 300-mg tablet of tenofovir DF, and a 200-mg capsule of emtricitabine given simultaneously.

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

A fixed-combination tablet containing emtricitabine 200 mg and tenofovir DF 300 mg (Truvada) is bioequivalent to a 200-mg capsule of emtricitabine and a 300-mg tablet of tenofovir DF given simultaneously.

Food

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

Administration of emtricitabine capsules with food (approximately 1000 kcal high-fat meal) did not affect the area under the concentration-time curve (AUC) of emtricitabine, but resulted in a 29% decrease in peak plasma concentrations of the drug.

Administration of emtricitabine oral solution with a high-fat or low-fat meal did not affect the AUC or peak plasma concentrations of emtricitabine.

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) is similar to that reported in adults receiving 200 mg daily. The AUC reported in neonates receiving emtricitabine 3 mg/kg daily for 4 days is similar to that reported in children 3 months to 17 years of age receiving the recommended dosage.

Peak plasma concentrations and AUC of emtricitabine are increased in adults with renal impairment (creatinine clearance less than 50 mL/minute or end-stage renal disease requiring dialysis) due to reduced renal clearance of the drug. Dosage adjustments are needed.(See Dosage and Administration: Special Populations.)

Distribution

Emtricitabine is less than 4% bound to plasma proteins; binding is independent of drug concentrations over the range of 0.01-200 mcg/mL.

Following oral administration, emtricitabine is distributed into saliva and into vaginal tissue and cervicovaginal fluid.

Emtricitabine crosses the human placenta.

Emtricitabine is distributed into human milk in low concentrations.

Elimination

Metabolism

Emtricitabine 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

Emtricitabine is eliminated in urine (86%) and feces (14%). The drug is eliminated in urine by glomerular filtration and active tubular secretion; 13% of a dose is recovered in urine as 3 metabolites.

Emtricitabine is removed by hemodialysis; it is not known whether the drug is removed by peritoneal dialysis.

Half-life

The plasma elimination half-life of emtricitabine is approximately 10 hours.

Special Populations

Renal clearance of emtricitabine is reduced in adults with renal impairment (creatinine clearance less than 50 mL/minute or end-stage renal disease requiring dialysis).

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