Severe acute exacerbations of hepatitis B (HBV) have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued emtricitabine. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue emtricitabine. If appropriate, initiation of anti-HBV therapy may be warranted.
HIV-1 infection, treatment: Oral:
Capsule: 200 mg once daily in combination with other antiretrovirals.
Solution: 240 mg once daily in combination with other antiretrovirals.
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).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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: No dosage adjustment necessary; administer after hemodialysis on dialysis days (HHS [adult] 2022).
There are no dosage adjustments provided in the manufacturer’s labeling; however, not hepatically metabolized, so impact of hepatic impairment would be minimal.
(For additional information see "Emtricitabine: Pediatric drug information")
Note: Due to bioavailability differences, oral dosage forms are not bioequivalent; oral solution and capsules should not be interchanged on a mg:mg basis. Gene mutation and antiretroviral (ARV) resistance patterns should be evaluated (refer to https://www.iasusa.org/ for more information) when necessary.
HIV-1 infection, treatment: Note: Use in combination with other ARV agents. Oral:
Infants 1 to <3 months: Oral solution: 3 mg/kg/dose once daily.
Infants ≥3 months, Children, and Adolescents ≤17 years:
Oral solution: 6 mg/kg/dose once daily; maximum daily dose: 240 mg/day.
Capsules: Patient weight >33 kg and able to swallow capsule whole: 200 mg once daily.
Adolescents ≥18 years:
Capsules: 200 mg once daily.
Oral solution: 240 mg once daily.
HIV-1 nonoccupational postexposure prophylaxis (nPEP) (HHS [nPEP] 2016): Note: Initiate therapy within 72 hours of exposure and continue for 28 days in combination with other ARV agents. Oral:
Infants 1 to <3 months: Oral solution: 3 mg/kg/dose once daily.
Infants ≥3 months and Children:
Oral solution: 6 mg/kg/dose once daily; maximum daily dose: 240 mg/day.
Capsules: Patient weight >33 kg and able to swallow capsule whole: 200 mg once daily.
Adolescents: The combination product is recommended (see emtricitabine and tenofovir disoproxil fumarate monograph).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Monitor clinical response and renal function closely. Dialysis: 30% of the dose is removed by hemodialysis (over 3 hours).
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.
Adolescents ≥18 years:
CrCl ≥50 mL/minute: No dosage adjustment necessary.
CrCl 30 to 49 mL/minute: Capsule: 200 mg every 48 hours; oral solution: 120 mg every 24 hours.
CrCl 15 to 29 mL/minute: Capsule: 200 mg every 72 hours; oral solution: 80 mg every 24 hours.
CrCl <15 mL/minute: Capsule: 200 mg every 96 hours; oral solution: 60 mg every 24 hours.
Hemodialysis: Capsule: 200 mg every 24 hours; solution: 240 mg every 24 hours; administer after hemodialysis on dialysis days (HHS [adult 2019]).
No dosage adjustments are required (HHS [pediatric] 2018).
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Emtriva: 200 mg [contains fd&c blue #2 (indigotine)]
Generic: 200 mg
Solution, Oral:
Emtriva: 10 mg/mL (170 mL) [contains edetate (edta) disodium, fd&c yellow #6 (sunset yellow), methylparaben, propylene glycol, propylparaben; cotton candy flavor]
May be product dependent
Administer with or without food.
Oral: May be administered without regard to food
HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretroviral agents.
HIV-1 nonoccupational postexposure prophylaxis; HIV-1 occupational postexposure prophylaxis
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. 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.
>10%:
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
Hypersensitivity to emtricitabine or any component of the formulation
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).
Disease-related concerns:
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment required.
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).
Hyperpigmentation may occur at a higher frequency in pediatric patients compared to adults (children: 32%; adults: 2% to 6%).
Some dosage forms may contain propylene glycol; in neonates large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Betibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Betibeglogene Autotemcel. Risk X: Avoid combination
Cladribine: Agents that Undergo Intracellular Phosphorylation may diminish the therapeutic effect of Cladribine. Risk X: Avoid combination
Elivaldogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid combination
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy
Food decreases peak plasma concentrations, but does not alter the extent of absorption or overall systemic exposure. Management: Administer without regard to meals.
The Health and Human Services (HHS) perinatal HIV guidelines consider emtricitabine a preferred nucleoside reverse transcriptase inhibitor for patients with HIV infection who are not yet pregnant but are trying to conceive.
Emtricitabine is a recommended component for pre-exposure prophylaxis (PrEP) in patients at risk for HIV infection who are planning a pregnancy. The partner without HIV should begin therapy 20 days prior to attempting conception. Up to 20 days of therapy are required to achieve protective drug concentrations in cervicovaginal tissue, therefore continued use of condoms to prevent HIV exposure is recommended during this time. PrEP should continue for 28 days after attempting conception or condomless sex exposure.
Viral suppression sustained below the limits of detection with antiretroviral therapy (ART) and modification of therapy (if needed) is recommended in all patients with HIV infection who are planning a pregnancy. Optimization of the health of the person who will become pregnant and a discussion of the potential risks and benefits of ART during pregnancy is also recommended prior to conception. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV infection may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2021).
Emtricitabine has a high level of transfer across the human placenta.
No increased risk of overall teratogenic effects has been observed according to data collected by the antiretroviral pregnancy registry. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm delivery, stillbirth, low birth weight, and small-for-gestational-age infants. Actual risks may be influenced by maternal factors, such as disease severity, GA at initiation of therapy, and specific ART regimen; therefore, close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children not diagnosed with HIV infection but who were exposed to ART in utero or as a neonate and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential metabolic dysfunction.
The Health and Human Services (HHS) perinatal HIV guidelines consider emtricitabine a preferred nucleoside reverse transcriptase inhibitor (NRTI) for pregnant patients with HIV infection who are antiretroviral-naive, who have had ART therapy in the past but are restarting, or who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). In addition, patients who become pregnant while taking emtricitabine may continue if viral suppression is effective and the regimen is well tolerated.
The HHS perinatal HIV guidelines consider emtricitabine with tenofovir disoproxil fumarate or tenofovir alafenamide to be a preferred NRTI backbone for initial therapy in antiretroviral-naive patients who are pregnant. The guidelines also consider emtricitabine plus tenofovir disoproxil fumarate or tenofovir alafenamide a recommended dual NRTI backbone in regimens for patients who are HIV/hepatitis B virus-coinfected and pregnant.
Emtricitabine is a recommended component for pre-exposure prophylaxis (PrEP) in uninfected patients at risk for HIV infection who are pregnant. Emtricitabine is also a preferred component of an initial regimen when acute HIV infection is detected during pregnancy.
The pharmacokinetics of emtricitabine are not significantly altered during pregnancy and dosing adjustments are not needed.
ART is recommended for all pregnant people with HIV infection to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Therapy should be individualized following a discussion of the potential risks and benefits of treatment during pregnancy. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers are encouraged to enroll patients exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or http://www.APRegistry.com).
Health care providers caring for pregnant patients with HIV infection and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2021).
Emtricitabine is present in breast milk.
Breast milk concentrations may be higher than those in the maternal serum. Emtricitabine can be detected in the serum of breastfed infants.
Emtricitabine is a recommended component of an initial regimen when acute HIV infection is detected in patients who are breastfeeding. Breastfeeding should be interrupted and not continued if infection is confirmed. Milk may be expressed and stored while waiting for confirmation.
Emtricitabine is a recommended component for pre-exposure prophylaxis (PrEP) in uninfected patients at risk for HIV infection who are breastfeeding.
Maternal or infant antiretroviral therapy does not completely eliminate the risk of postnatal HIV transmission. In addition, multiclass-resistant virus has been detected in breastfeeding infants despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services (HHS) perinatal HIV guidelines do not recommend breastfeeding for patients with HIV infection when safer infant feeding options are available.
Information is available for counseling and managing patients with HIV infection who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2021).
Viral load, CD4, liver function tests; serum creatinine; hepatitis B testing is recommended prior to or when initiating therapy.
Nucleoside reverse transcriptase inhibitor; emtricitabine is a cytidine analogue which is phosphorylated intracellularly to emtricitabine 5'-triphosphate which interferes with HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication.
Absorption: Rapid, extensive
Protein binding: <4%
Metabolism: Converted intracellularly to the active triphosphate form; undergoes minimal biotransformation via oxidation and glucuronide conjugation
Bioavailability: Capsule: 93%; solution: 75%; Note: Relative bioavailability of solution to capsule: 80%
Half-life elimination: 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
Time to peak, plasma: 1 to 2 hours
Excretion: 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
Altered kidney function: Cmax and AUC are increased in patients with CrCl less than 50 mL/minute or ESRD requiring dialysis.
Pediatric: 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.
Capsules (Emtricitabine Oral)
200 mg (per each): $19.31
Capsules (Emtriva Oral)
200 mg (per each): $21.46
Solution (Emtriva Oral)
10 mg/mL (per mL): $0.89
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