(em trye SYE ta been)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Emtriva: 200 mg [contains fd&c blue #2 (indigotine)]
Emtriva: 10 mg/mL (170 mL) [contains edetate disodium, fd&c yellow #6 (sunset yellow), methylparaben, propylene glycol, propylparaben; cotton candy flavor]
Brand Names: U.S.
- Antiretroviral, Reverse Transcriptase Inhibitor, Nucleoside (Anti-HIV)
Nucleoside reverse transcriptase inhibitor; emtricitabine is a cytosine analogue which is phosphorylated intracellularly to emtricitabine 5'-triphosphate which interferes with HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication.
Converted intracellularly to the active triphosphate form; undergoes minimal biotransformation via oxidation and glucuronide conjugation
Urine (86% primarily as unchanged drug, 13% as metabolites, 9% of dose as oxidative metabolite; 4% as glucuronide metabolite); feces (14%)
Clearance: Renal clearance is greater than creatinine clearance; thus, emtricitabine may be eliminated by both glomerular filtration and active tubular secretion
Time to Peak
Plasma: 1 to 2 hours
Normal renal function:
Infants, Children, and Adolescents: Elimination half-life (emtricitabine):
Single dose: 11 hours
Multiple dose: 7.9 to 9.5 hours
Infants 0 to 3 months (n=20; median age: 26 days): 12.1 ± 3.1 hours
Infants 3 to 24 months (n=14): 8.9 ± 3.2 hours
Children 25 months to 6 years (n=19): 11.3 ± 6.4 hours
Children 7 to 12 years (n=17): 8.2 ± 3.2 hours
Adolescents 13 to 17 years (n=27): 8.9 ± 3.3 hours
Adults: Emtricitabine: 10 hours; Intracellular half-life (emtricitabine 5'-triphosphate): 39 hours
Special Populations: Renal Function Impairment
Cmax and AUC are increased in patients with CrCl less than 50 mL/minute or ESRD requiring dialysis.
Special Populations: Children
Exposure is similar to adults. In neonates, the AUC was similar to the AUC observed in children at least 3 months to 17 years of age.
Use: Labeled Indications
HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretroviral agents.
Off Label Uses
HIV-1 nonoccupational postexposure prophylaxis
Based on the Centers for Disease Control and Prevention, US Department of Health and Human Services updated guidelines for antiretroviral postexposure prophylaxis after sexual, injection drug use, or other nonoccupational exposure to HIV, emtricitabine (in conjunction with other antiretrovirals) is effective and recommended as postexposure prophylaxis of HIV-1 infection following nonoccupational exposure (nPEP) in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that may contain HIV when that exposure represents a substantial risk for HIV transmission.
HIV-1 occupational postexposure prophylaxis
Based on the US Public Health Service updated guidelines for the management of occupational exposures to human immunodeficiency virus and recommendations for postexposure prophylaxis, emtricitabine (in combination with tenofovir disoproxil fumarate and raltegravir) is an effective and recommended treatment option for postexposure prophylaxis of HIV-1 infection in healthcare personnel following occupational exposure (oPEP) to blood and/or other body fluids that may contain HIV.
Hypersensitivity to emtricitabine or any component of the formulation
HIV-1 infection, treatment: Oral:
Capsule: 200 mg once daily
Solution: 240 mg once daily
HIV-1 nonoccupational postexposure prophylaxis (nPEP) (off-label use): Oral: Capsule: 200 mg once daily; initiate therapy within 72 hours of exposure and continue for 28 days in combination with other antiretrovirals (3-drug regimen) Note: The fixed-dose emtricitabine and tenofovir disoproxil fumarate combination product is recommended for these components of the 3-drug regimen (HHS [nPEP] 2016).
HIV-1 occupational postexposure prophylaxis (oPEP) (off-label use): Oral: Capsule: 200 mg once daily in combination with tenofovir disoproxil fumarate and raltegravir; initiate therapy as soon as possible after occupational exposure (and within 72 hours) and continue for 4 weeks; Note: The fixed-dose emtricitabine and tenofovir disoproxil fumarate combination product is recommended for these components of the regimen (Kuhar 2013).
Refer to adult dosing.
HIV-1 infection, treatment: Oral: Note: Due to bioavailability differences, dosage forms are not bioequivalent; oral solution and capsules should not be interchanged on a mg:mg basis.
Infants 1 to <3 months: Solution: 3 mg/kg/dose once daily
Infants ≥3 months, Children, and Adolescents ≤17 years:
Capsule: Children >33 kg and able to swallow capsule whole: 200 mg once daily
Solution: 6 mg/kg once daily; maximum: 240 mg/day
Adolescents ≥18 years: Refer to adult dosing.
HIV-1 nonoccupational postexposure prophylaxis (nPEP) (off-label use) (HHS [nPEP] 2016): Oral: Note: Initiate therapy within 72 hours of exposure and continue for 28 days in combination with other antiretroviral agents.
Infants 1 to <3 months: Solution: 3 mg/kg/dose once daily
Infants ≥3 months and Children:
Capsules: Patient weight >33 kg and able to swallow capsule whole: 200 mg once daily
Solution: 6 mg/kg/dose once daily; maximum daily dose: 240 mg/day
Adolescents: Refer to adult dosing.
Dosing: Renal Impairment
Adolescents ≥ 18 years and Adults:
CrCl ≥50 mL/minute: No dosage adjustment necessary.
CrCl 30 to 49 mL/minute: Capsule: 200 mg every 48 hours; solution: 120 mg every 24 hours
CrCl 15 to 29 mL/minute: Capsule: 200 mg every 72 hours; solution: 80 mg every 24 hours
CrCl <15 mL/minute: Capsule: 200 mg every 96 hours; solution: 60 mg every 24 hours
Hemodialysis: Capsule: 200 mg every 96 hours; solution: 60 mg every 24 hours; administer after hemodialysis on dialysis days (~30% removed during a 3-hour dialysis)
Infants, Children, and Adolescents <18 years: There are no specific dosage adjustments provided in the manufacturer's labeling; however, may consider a reduction in the dose and/or an increase in the dosing interval similar to dosage adjustments for adults.
Dosing: Hepatic Impairment
There are no dosage adjustments provided in the manufacturer’s labeling; however, not hepatically metabolized, so impact of hepatic impairment would be minimal.
Administer with or without food.
Capsules: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Oral solution: Store at 2°C to 8°C (36°F to 46°F). Use within 3 months if stored at 25°C (77°F) with excursions permitted to 15°C to 30°C (59°F to 86°F).
LamiVUDine: May enhance the adverse/toxic effect of Emtricitabine. Avoid combination
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy
Clinical trials were conducted in patients receiving other antiretroviral agents, and it is not possible to correlate frequency of adverse events with emtricitabine alone. The range of frequencies of adverse events is generally comparable to comparator groups, with the exception of hyperpigmentation, which occurred more frequently in patients receiving emtricitabine. Unless otherwise noted, percentages are as reported in adults.
Central nervous system: Dizziness (4% to 25%), headache (6% to 22%), insomnia (5% to 16%), abnormal dreams (2% to 11%)
Dermatologic: Hyperpigmentation (children: 32%; adults: 2% to 4%; primarily of palms and/or soles but may include tongue, arms, lip and nails; generally mild and nonprogressive without associated local reactions such as pruritus or rash), skin rash (17% to 30%; includes hypersensitivity reaction, maculopapular rash, pruritus, pustular rash, vesiculobullous rash)
Gastrointestinal: Diarrhea (children: 20%; adults: 9% to 23%), vomiting (children: 23%; adults: 9%), nausea (13% to 18%), abdominal pain (8% to 14%), gastroenteritis (children: 11%)
Infection: Infection (children: 44%)
Neuromuscular & skeletal: Weakness (12% to 16%), increased creatine phosphokinase (grades 3/4: 11% to 12%)
Otic: Otitis media (children: 23%)
Respiratory: Cough (children: 28%; adults; 14%), rhinitis (children: 20%; adults: 12% to 18%), pneumonia (children: 15%)
Miscellaneous: Fever (children: 18%)
1% to 10%:
Central nervous system: Depression (6% to 9%), paresthesia (5% to 6%), neuritis (≤4%), neuropathy (≤4%)
Endocrine & metabolic: Increased serum triglycerides (grades 3/4: 4% to 10%), increased amylase (grades 3/4: children: 9%; adults: 2% to 5%), hyperglycemia (grades 3/4: 2% to 3%)
Gastrointestinal: Dyspepsia (4% to 8%), increased serum lipase (grades 3/4: ≤1%)
Genitourinary: Hematuria (grades 3/4: 3%)
Hematologic & oncologic: Anemia (children: 7%), neutropenia (grades 3/4: children: 2%; adults: 5%)
Hepatic: Increased serum transaminases (grades 3/4: 2% to 6%), increased serum alkaline phosphatase (>550 units/L: 1%), increased serum bilirubin (grades 3/4: 1%)
Neuromuscular & skeletal: Myalgia (4% to 6%), arthralgia (3% to 5%)
Respiratory: Sinusitis (8%), upper respiratory tract infection (8%), pharyngitis (5%)
<1%, postmarketing, and/or case reports: Immune reconstitution syndrome
Concerns related to adverse effects:
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Lactic acidosis/hepatomegaly: Lactic acidosis and severe hepatomegaly with steatosis, sometimes fatal, have been reported with use of nucleoside analogs, alone or in combination with other antiretrovirals. Suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (marked transaminase elevation may/may not accompany hepatomegaly and steatosis).
• Chronic hepatitis B: [US Boxed Warning]: Safety and efficacy during coinfection of HIV-1 and HBV have not been established; acute, severe exacerbations of HBV have been reported following discontinuation of antiretroviral therapy. Not indicated for treatment of chronic hepatitis B. Closely monitor hepatic function with clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue this therapy. If appropriate, anti-hepatitis B therapy may be warranted. All patients with HIV should be tested for HBV prior to initiation of treatment.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment required.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Duplicate therapy: Concomitant use of other emtricitabine-containing products should be avoided.
Dosage form specific issues:
• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated with hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007).
Viral load, CD4, liver function tests; serum creatinine; hepatitis B testing is recommended prior to initiation of therapy.
Pregnancy Risk Factor
Adverse events were not observed in animal reproduction studies. Emtricitabine has a high level of transfer across the human placenta; no increased risk of overall birth defects has been observed according to data collected by the antiretroviral pregnancy registry. Maternal antiretroviral therapy may increase the risk of preterm delivery, although available information is conflicting possibly due to variability of maternal factors (disease severity; initiation of therapy); however, maternal antiretroviral medication should not be withheld due to concerns of preterm birth. Information related to stillbirth, low birth weight, and small for gestational age infants is limited. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children who develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential mitochondrial dysfunction. Cases of lactic acidosis and hepatic steatosis related to mitochondrial toxicity have been reported with use of nucleoside reverse transcriptase inhibitors (NRTIs). These adverse events are similar to other rare but life-threatening syndromes which occur during pregnancy (eg, HELLP syndrome). In general nucleoside reverse transcriptase inhibitors are well tolerated and the benefits of use generally outweigh potential risk.
Combination antiretroviral therapy (cART) therapy is recommended for all HIV-infected pregnant women to keep the viral load below the limit of detection and reduce the risk of perinatal transmission. When HIV is diagnosed during pregnancy in a woman who has never received antiretroviral therapy, cART should begin as soon as possible after diagnosis. The Health and Human Services (HHS) Perinatal HIV Guidelines consider emtricitabine with tenofovir disoproxil fumarate to be a preferred NRTI backbone for initial therapy in antiretroviral-naive pregnant women. The guidelines also consider emtricitabine plus tenofovir disoproxil fumarate a recommended dual NRTI backbone in regimens for HIV/HBV-coinfected pregnant women. Use caution with hepatitis B coinfection; hepatitis B flare may occur if emtricitabine is discontinued. The pharmacokinetics of emtricitabine are not significantly altered during pregnancy. In general, women who become pregnant on a stable cART regimen may continue that regimen if viral suppression is effective, appropriate drug exposure can be achieved, contraindications for use in pregnancy are not present, and the regimen is well tolerated. Monitoring during pregnancy is more frequent than in non-pregnant adults; cART should be continued postpartum.
For HIV-infected couples planning a pregnancy, maximum viral suppression with cART is recommended prior to conception for the HIV-infected partner(s) and expert consultation is recommended; modification of therapy (if needed) and optimization of the woman’s health should be done prior to conception. HIV-infected women not planning a pregnancy may use any available type of contraception, considering possible drug interactions and contraindications of the specific method. In addition, consistent use of condoms is also recommended (even during pregnancy) to prevent transmission of HIV or other sexually transmitted diseases.
Health care providers are encouraged to enroll pregnant women exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or www.APRegistry.com). Health care providers caring for HIV-infected women and their infants may contact the National Perinatal HIV Hotline (888-448-8765) for clinical consultation (HHS [perinatal] 2016).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience dizziness, nightmares, loss of strength and energy, headache, insomnia, abdominal pain, nausea, vomiting, diarrhea, or rhinorrhea. Have patient report immediately to prescriber signs of lactic acidosis (fast breathing, tachycardia, abnormal heartbeat, vomiting, fatigue, shortness of breath, severe loss of strength and energy, severe dizziness, feeling cold, or muscle pain or cramps), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), depression, skin discoloration, or signs of infection (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: nucleoside reverse transcriptase inhibitors (NRTIs)
Other brands: Emtriva