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Emtricitabine

Pronunciation

(em trye SYE ta been)

Index Terms

  • BW524W91
  • Coviracil
  • FTC

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

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Capsule, Oral:

Emtriva: 200 mg [contains fd&c blue #2 (indigotine)]

Solution, Oral:

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.

  • Emtriva

Pharmacologic Category

  • Antiretroviral, Reverse Transcriptase Inhibitor, Nucleoside (Anti-HIV)

Pharmacology

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.

Absorption

Rapid, extensive

Metabolism

Converted intracellularly to the active triphosphate form; undergoes minimal biotransformation via oxidation and glucuronide conjugation

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

Time to Peak

Plasma: 1-2 hours

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

Protein Binding

<4%

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 mo to 17 years of age.

Use: Labeled Indications

Treatment of HIV infection in combination with at least two other antiretroviral agents

Contraindications

Hypersensitivity to emtricitabine or any component of the formulation

Dosage

Oral:

Children:

0 to 3 months: Solution: 3 mg/kg/day

3 months to 17 years:

Capsule: Children >33 kg: 200 mg once daily

Solution: 6 mg/kg once daily; maximum: 240 mg/day

Adults: Note: Emtricitabine is a component of recommended initial regimens in all treatment-naive patients (coadministered with dolutegravir and tenofovir, with raltegravir and tenofovir, or with darunavir/ritonavir and tenofovir); as a component of a recommended initial regimen only for treatment-naive patients with pre-ART CrCl>70 mL/minute (coadministered with elvitegravir/cobicistat and tenofovir); and as a component of a recommended initial regimen only for treatment-naive patients who are HLA-B*5701 negative (coadministered with dolutegravir and abacavir) (HHS [adult] 2015).

Capsule: 200 mg once daily

Solution: 240 mg once daily

Dosage adjustment in renal impairment: Adults (consider similar adjustments in children):

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 (including hemodialysis patients): Capsule: 200 mg every 96 hours; solution: 60 mg every 24 hours; administer after dialysis

Dosage adjustment in hepatic impairment: No dosage adjustment required.

Administration

May be administered with or without food.

Dietary Considerations

May be taken with or without food.

Storage

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).

Drug Interactions

Ganciclovir-Valganciclovir: May enhance the adverse/toxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Hematologic toxicity with zidovudine is of particular concern. Ganciclovir-Valganciclovir may increase the serum concentration of Reverse Transcriptase Inhibitors (Nucleoside). Management: Monitor patients receiving any of these combination closely for toxicity of the reverse transcriptase inhibitor. Avoid zidovudine. Intravitreal implants would not be affected. Consider therapy modification

LamiVUDine: May enhance the adverse/toxic effect of Emtricitabine. Avoid combination

Ribavirin (Oral Inhalation): May enhance the hepatotoxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Monitor therapy

Ribavirin (Systemic): May enhance the hepatotoxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Monitor therapy

Adverse Reactions

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%), fever (children 18%), 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); rash (17% to 30%; includes pruritus, maculopapular rash, vesiculobullous rash, pustular rash, and allergic reaction)

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%)

Neuromuscular & skeletal: Weakness (12% to 16%), CPK increased (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: Infection (children 44%)

1% to 10%:

Central nervous system: Depression (6% to 9%), neuropathy/neuritis (4%)

Endocrine & metabolic: Serum triglycerides increased (grades 3/4: 4% to 10%), disordered glucose homeostasis (grades 3/4: 2% to 3%), serum amylase increased (grades 3/4: children 9%; adults 2% to 5%), serum lipase increased (grades 3/4: ≤1%)

Gastrointestinal: Dyspepsia (4% to 8%), serum amylase increased (grades 3/4: 8%)

Genitourinary: Hematuria (grades 3/4: 3%)

Hematologic: Anemia (children: 7%), neutropenia (grades 3/4: children 2%; adults 5%)

Hepatic: Transaminases increased (grades 3/4: 2% to 6%), alkaline phosphatase increased (>550 units/L: 1%), bilirubin increased (grades 3/4: 1%)

Neuromuscular & skeletal: Creatinine kinase increased (grades 3/4: 9%), myalgia (4% to 6%), paresthesia (5% to 6%), arthralgia (3% to 5%)

Respiratory: Upper respiratory tract infection (8%), sinusitis (8%), pharyngitis (5%)

<1% (Limited to important or life-threatening): Immune reconstitution syndrome

ALERT: U.S. Boxed Warning

Lactic acidosis/severe hepatomegaly with steatosis:

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs alone or in combination with other antiretrovirals.

Posttreatment exacerbation of hepatitis B:

Emtricitabine is not approved for the treatment of chronic hepatitis B virus (HBV) infection, and the safety and efficacy of emtricitabine have not been established in patients coinfected with HBV and HIV-1. Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued emtricitabine. 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 emtricitabine. If appropriate, initiation of anti-HBV therapy may be warranted.

Warnings/Precautions

Concerns related to adverse effects:

• Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance).

• 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: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis).

Disease-related concerns:

• Chronic hepatitis B: [U.S. Boxed Warning]: Safety and efficacy during coinfection of HIV 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. All patients with HIV should be tested for HBV prior to initiation of treatment. Caution in patients with known or suspected hepatitis B or C infection (monitoring of liver function is recommended). In HBV coinfected patients, acute HBV infection exacerbations have occurred following discontinuation; monitor hepatic function closely for several months.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment required.

Concurrent drug therapy issues:

• Duplicate therapy: Concomitant use of other emtricitabine-containing products should be avoided.

• Lamivudine: Concomitant use of lamivudine or lamivudine-containing products should be avoided; cross-resistance may develop.

Monitoring Parameters

Viral load, CD4, liver function tests; hepatitis B testing is recommended prior to initiation of therapy

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events were not observed in animal 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. Cases of lactic acidosis/hepatic steatosis syndrome related to mitochondrial toxicity have been reported in pregnant women with prolonged use of nucleoside analogues. It is not known if pregnancy itself potentiates this known side effect; however, women may be at increased risk of lactic acidosis and liver damage. In addition, these adverse events are similar to other rare but life-threatening syndromes which occur during pregnancy (eg, HELLP syndrome). Hepatic enzymes and electrolytes should be monitored in women receiving nucleoside analogues and clinicians should watch for early signs of the syndrome. In addition, mitochondrial dysfunction may develop in infants following in utero exposure. A pharmacokinetic study shows a slight decrease in emtricitabine serum levels during the third trimester and immediately postpartum; however, there is no clear need to adjust the dose. The DHHS Perinatal HIV Guidelines consider emtricitabine with tenofovir to be a preferred NRTI backbone in antiretroviral-naive pregnant women. The DHHS Perinatal HIV Guidelines consider emtricitabine plus tenofovir a recommended dual NRTI/NtRTI backbone for HIV/HBV coinfected pregnant women.

Regardless of CD4 count or HIV RNA copy number, all HIV-infected pregnant women should receive a combination antiretroviral (ARV) drug regimen. A combination of antepartum, intrapartum, and infant ARV prophylaxis is recommended. ARV therapy should be started as soon as possible in women with symptomatic infection. Although earlier initiation may be more effective in reducing the perinatal transmission of HIV, initiation may be delayed until after 12 weeks gestation in women who do not require immediate treatment after careful consideration of maternal conditions (eg, nausea and vomiting) and the potential risks of first trimester fetal exposure for specific agents. A scheduled cesarean delivery at 38 weeks gestation is recommended for all women with HIV RNA >1,000 copies/mL or unknown concentrations near delivery in order to decrease transmission. If ARV therapy must be interrupted for <24 hours during the peripartum period, stop then restart all medications simultaneously in order to decrease the chance of developing resistance. Long-term follow-up is recommended for all infants exposed to ARV medications. In couples who want to conceive, the HIV-infected partner should attain maximum viral suppression prior to conception.

Health care providers are encouraged to enroll pregnant women exposed to antiretroviral medications in the Antiretroviral Pregnancy Registry (1-800-258-4263 or www.APRegistry.com). Healthcare providers caring for HIV-infected women and their infants may contact the National Perinatal HIV Hotline (888-448-8765) for clinical consultation (HHS [perinatal], 2014).

Patient Education

• 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, loss of strength and energy, headache, insomnia, abdominal pain, nausea, vomiting, diarrhea, or rhinorrhea. Have patient report immediately to prescriber signs of too much lactic acid in the blood (lactic acidosis; fast breathing, fast heartbeat, abnormal heartbeat, vomiting, drowsiness, shortness of breath, feeling very tired or weak, severe dizziness, feeling cold, or muscle pain or cramps), signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), depression, skin discoloration, change in body fat, nightmares, 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 healthcare 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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