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Updated Pediatric ARV Guidelines

Updates to the Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection were released on Thursday, November 1, 2012. Please send your comments to ContactUs@aidsinfo.nih.gov by November 15, 2012.

Corrections were made to the guideline. For a description of the changes, please see the correction notice.

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Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection

Nucleoside and Nucleotide Analogue Reverse Transcriptase Inhibitors (NRTIs)

Emtricitabine

(Last updated:11/1/2012; last reviewed:11/1/2012)

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Emtricitabine (FTC, Emtriva)
For additional information see Drugs@FDA: http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm
Formulations
Pediatric oral solution: 10 mg/mL
Capsules: 200 mg
Combination tablets
  • With tenofovir (TDF): 200 mg FTC + 300 mg TDF (Truvada)
  • With TDF and efavirenz (EFV): 200 mg FTC + 300 mg TDF + 600 mg EFV (Atripla)
  • With TDF and rilpivirine (RPV): 200 mg FTC + 300 mg TDF + 25 mg RPV (Complera)
  • With FTC + elvitegravir (EVG) + cobicistat (COBI): 200 mg FTC + 150 mg EVG + 150 mg COBI + 300 mg TDF (Stribild)
Dosing Recommendations

Neonate/infant dose (aged 0–<3 months):
  • Oral solution: 3 mg/kg once daily.

Pediatric dose (aged ≥3 months–17 years):

  • Oral solution:
    6 mg/kg (maximum dose 240 mg) once daily. (Higher maximum dose because the oral solution has 20% lower plasma exposure in pediatric pharmacokinetic analysis.)
  • Capsules (for children who weigh >33 kg):
    200 mg once daily.

Adolescent (aged ≥18 years)/adult dose:

  • Oral solution: 240 mg (24 mL) once daily.
  • Capsules: 200 mg once daily.

Combination Tablets

Truvada

  • Adolescent (aged ≥12 years and ≥35) kg and adult dose: 1 tablet once daily.

Atripla

  • Adolescent (aged ≥12 years and ≥40 kg) and adult dose: 1 tablet once daily.
  • See efavirenz section for pregnancy warning.

Complera

  • Adult dose (aged ≥18 years): 1 tablet once daily.

Stribild:

  • Adult dose (aged ≥18 years): 1 tablet once daily in treatment-naive adults. Administer with food.
Selected Adverse Events
  • Minimal toxicity.
  • Severe acute exacerbation of hepatitis can occur in hepatitis B virus (HBV)-coinfected patients who discontinue FTC.
  • Hyperpigmentation/skin discoloration on palms and/or soles.
  Special Instructions
  • FTC can be given without regard to food; however, administer Atripla on an empty stomach because it also contains EFV.
  • FTC oral solution can be kept at room temperature up to 77°F (25°C) if used within 3 months; refrigerate for longer term storage.
  • Before using FTC, screen patients for HBV.
Metabolism
  • Limited metabolism: No cytochrome P (CYP) 450 interactions.
  • Renal excretion 86%: Competition with other compounds that undergo renal elimination.
  • Dosing of FTC in patients with renal impairment: Decrease dosage in patients with impaired renal function. Consult manufacturer’s prescribing information.
  • Do not use Atripla (fixed-dose combination) in patients with creatinine clearance (CrCl) <50 mL/min or in patients requiring dialysis.
  • Do not use Truvada (fixed-dose combination) in patients with CrCl <30 mL/min or in patients requiring dialysis.
  • Use Complera with caution in patients with severe renal impairment or end-stage renal disease. Increase monitoring for adverse effects because rilpivirine concentrations may be increased in patients with severe renal impairment or end-stage renal disease.
  • If using Stribild, please see the elvitegravir section of the drug appendix for additional information.

Drug Interactions (see also the Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents):

  • Other nucleoside reverse transcriptase inhibitors (NRTIs): Do not use emtricitabine in combination with lamivudine because the agents share similar resistance profiles and lack additive benefit.
  • Renal elimination: Competition with other compounds that undergo renal elimination (possible competition for renal tubular secretion). Drugs that decrease renal function could decrease clearance.
  • Use with Stribild: If using Stribild, please see the elvitegravir section of the drug appendix for additional information.

Major Toxicities:

  • More common: Headache, insomnia, diarrhea, nausea, rash, and hyperpigmentation/skin discoloration (possibly more common in children).
  • Less common (more severe): Neutropenia. Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported. Exacerbations of hepatitis have occurred in HIV/hepatitis B virus-co-infected patients who changed from emtricitabine-containing to non-emtricitabine-containing regimens.

Resistance: The International Antiviral Society-USA (IAS-USA) maintains a list of updated resistance mutations (see http://www.iasusa.org/resistance_mutations/index.html) and the Stanford University HIV Drug Resistance Database offers a discussion of each mutation (see http://hivdb.stanford.edu/pages/GRIP/FTC.html).

Pediatric Use: Emtricitabine is Food and Drug Administration (FDA)-approved for once-daily administration in children starting at birth. Owing to its once-a-day dosing, minimal toxicity, and pediatric pharmacokinetic (PK) data, emtricitabine is commonly used as part of a dual-NRTI backbone in antiretroviral therapy (ART).

A single-dose PK study of emtricitabine liquid solution and capsules was performed in 25 HIV-infected children ages 2 to 17 years.1 Emtricitabine was found to be well absorbed following oral administration, with a mean elimination half-life of 11 hours (range 9.7 to 11.6 hours). Plasma concentrations in children receiving the 6 mg/kg emtricitabine once-daily dose were approximately equivalent to those in adults receiving the standard 200-mg dose.

Based on this dose-finding study, emtricitabine was given at a dose of 6 mg/kg once daily in combination with other antiretroviral (ARV) drugs.2,3 PK results were similar to the preceding dose-finding study.1 Follow-up data extending to Week 96 indicated that 89% of the ARV-naive and 76% of the ARV-experienced children maintained suppression of plasma HIV RNA <400 copies/mL (74% of ARV-naive children and 62% of ARV-experienced children at <50 copies/mL). Minimal toxicity was observed in this trial.

In PACTG P1021, emtricitabine at a dose of 6 mg/kg (maximum 240 mg/day as liquid or 200 mg/day as capsules) in combination with didanosine and efavirenz, all given once daily, was studied in 37 ARV-naive HIV-infected children aged 3 months to 21 years.2 Eighty-five percent of children achieved HIV RNA <400 copies/mL and 72% maintained HIV RNA suppression to <50 copies/mL through 96 weeks of therapy. The median CD4 T lymphocyte count rose by 329 cells/mm3 at Week 96.

A study in South Africa evaluated the PKs of emtricitabine in 20 HIV-exposed infants aged <3 months, given emtricitabine as 3 mg/kg once daily for two, 4-day courses, separated by an interval of ≥2 weeks.4 Emtricitabine exposure (area under the curve [AUC]) in neonates receiving 3 mg/kg emtricitabine once daily was in the range of pediatric patients aged >3 months receiving the recommended emtricitabine dose of 6 mg/kg once daily and adults receiving the once-daily recommended 200-mg emtricitabine dose (AUC approximately 10 hr*ug/mL). Over the first 3 months of life, emtricitabine AUC decreased with increasing age, correlating with an increase in total body clearance of the drug. In a small group of neonates (N = 6) receiving a single dose of emtricitabine 3 mg/kg after a single maternal dose of 600 mg during delivery, the AUC exceeded that seen in adults and older children, but the half-life (9.2 hrs) was similar.5 Extensive safety data are lacking in this age range.

References

  1. Wang LH, Wiznia AA, Rathore MH, et al. Pharmacokinetics and safety of single oral doses of emtricitabine in human immunodeficiency virus-infected children. Antimicrob Agents Chemother. Jan 2004;48(1):183-191. Available at http://www.ncbi.nlm.nih.gov/pubmed/14693538.
  2. McKinney RE, Jr., Rodman J, Hu C, et al. Long-term safety and efficacy of a once-daily regimen of emtricitabine, didanosine, and efavirenz in HIV-infected, therapy-naive children and adolescents: Pediatric AIDS Clinical Trials Group Protocol P1021. Pediatrics. Aug 2007;120(2):e416-423. Available at http://www.ncbi.nlm.nih.gov/pubmed/17646352.
  3. Saez-Llorens X, Violari A, Ndiweni D, et al. Long-term safety and efficacy results of once-daily emtricitabine-based highly active antiretroviral therapy regimens in human immunodeficiency virus-infected pediatric subjects. Pediatrics. Apr 2008;121(4):e827-835. Available at http://www.ncbi.nlm.nih.gov/pubmed/18332076.
  4. Blum M, Ndiweni D, Chittick G, al e. Steady state pharmacokinetic evaluation of emtricitabine in neonates exposed to HIV in utero. 13th Conference on Retroviruses and Opportunistic Infections (CROI); February 5-9, 2006; Denver, CO.
  5. Flynn PM, Mirochnick M, Shapiro DE, et al. Pharmacokinetics and safety of single-dose tenofovir disoproxil fumarate and emtricitabine in HIV-1-infected pregnant women and their infants. Antimicrob Agents Chemother. Dec 2011;55(12):5914-5922. Available at http://www.ncbi.nlm.nih.gov/pubmed/21896911.