Emtricitabine

Dosage Forms & Strengths

capsule

• 200mg

oral solution

• 10mg/mL

HIV Infection

Capsule: 200 mg PO qDay

Oral Solution: 240 mg PO qDay

Renal Impairment

CrCl 50 mL/min or more: capsule 200 mg PO qDay; oral solution: 240 mg PO qDay

CrCl 30-49 mL/min: capsule 200 mg PO q48hr; oral solution: 120 mg PO qDay

CrCl 15-29 mL/min: capsule 200 mg PO q72hr; oral solution: 80 mg PO qDay

CrCl <15 mL/min: capsule 200 mg PO q96hr; oral solution: 60 mg PO qDay

Administration on day of hemodialysis: Administer after dialysis

Dosage Forms & Strengths

capsule

• 200mg

oral solution

• 10mg/mL

HIV Infection

Indicated for treatment of HIV infection in combination with other antiretroviral agents

Oral solution

• <3 months: 3 mg/kg PO qDay 
• 3 months to 17 years: 6 mg/kg PO qDay; not to exceed 240 mgday (note: oral solution has 20% lower plasma exposure, so maximum daily dose is higher for the oral solution)

Capsule (weight >33 kg)

• 200 mg PO qDay

Renal Impairment

Reduce dose and/or increase dosing interval

Mechanism of Action

Nucleoside reverse transcriptase inhibitor (NRTI); cytosine analog phosphorylated to emtricitabine 5'-triphosphate causing inhibition of HIV and RNA dependent DNA polymerase

Pharmacokinetics

Bioavailability: 93%

Protein Bound: <4%

Metabolism: Oxidation

Dialyzable: 30% removed by hemodialysis

Excretion: Urine (86%); feces (14%)

Half-Life: 10 hr

Peak PlasmaTime: 1-2 hr

Concentration: 1.8±0.7 mcg/m

LAUC: 10±3.1 hr.mcg/mL

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store the capsules at room temperature and away from excess heat and moisture (not in the bathroom). Store the solution in the refrigerator, but do not freeze it. If you prefer not to refrigerate the solution, you may store it at room temperature for up to 3 months. Discard any unused solution that has not been refrigerated after 3 months.

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

EMTRIVA® is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.

Additional important information regarding the use of EMTRIVA for the treatment of HIV-1 Infection:

• EMTRIVA should not be coadministered with ATRIPLA®, COMPLERA®, STRIBILD™, TRUVADA®, or lamivudine-containing products [See WARNINGS AND PRECAUTIONS].
• In treatment-experienced patients, the use of EMTRIVA should be guided by laboratory testing and treatment history [See CLINICAL PHARMACOLOGY].

Serious side effects have been reported including:

• Some people who have taken medicines like emtricitabine (a nucleoside analog) have developed a serious condition called lactic acidosis (buildup of an acid in the blood). Lactic acidosis can be a medical emergency and may need to be treated in the hospital. Call your healthcare provider right away if you get the following signs of lactic acidosis.
  • You feel very weak or tired.
  • You have unusual (not normal) muscle pain.
  • You have trouble breathing.
  • You have stomach pain with nausea and vomiting.
  • You feel cold, especially in your arm and legs.
  • You feel dizzy or lightheaded.
  • You have a fast or irregular heartbeat.
• Some people who have taken medicines like emtricitabine have developed serious liver problems called hepatotoxicity, with liver enlargement (hepatomegaly) and fat in the liver (steatosis). Call your healthcare provider right away if you get the following signs of liver problems.
  • Your skin or the white part of your eyes turns yellow (jaundice).
  • Your urine turns dark.
  • Your bowel movements (stools) turn light in color.
  • You don't feel like eating food for several days or longer.
  • You feel sick to your stomach (nausea).
  • You have lower stomach area (abdominal) pain.
• You may be more likely to get lactic acidosis or liver problems if you are female, very overweight (obese), or have been taking nucleoside analog medicines, like emtricitabine, for a long time.
• Changes in body fat have been seen in some patients taking emtricitabine and other anti-HIV-1 medicines. These changes may include increased amount of fat in the upper back and neck ("buffalo hump"), breast, and around the main part of your body (trunk). Loss of fat from the legs, arms and face may also happen. The cause and long term health effects of these conditions are not known at this time.
• If you are also infected with the Hepatitis B Virus (HBV), you need close medical follow-up for several months after stopping treatment with emtricitabine. Follow-up includes medical exams and blood tests to check for HBV that is getting worse. Patients with HBV infection, who take emtricitabine and then stop it, may get "flare-ups" of their hepatitis. A "flare-up" is when the disease suddenly returns in a worse way than before.

• Do not take emtricitabine if you are allergic to any ingredient in it. 

You should not take emtricitabine if you are allergic to it.

Emtricitabine should not be taken together with any HIV combination medicine that contains emtricitabine or lamivudine. This includes:

• Atripla (efavirenz, emtricitabine, and tenofovir);
• Combivir (lamivudine and zidovudine);
• Complera (rilpivirine, emtricitabine, and tenofovir);
• Epivir (lamivudine);
• Epzicom (abacavir and lamivudine);
• Trizivir (abacavir, lamivudine, and zidovudine); and
• Truvada (emtricitabine and tenofovir).

To make sure you can safely take emtricitabine, tell your doctor if you have any of these other conditions:

• liver disease (especially hepatitis B if you also have HIV);
• kidney disease; or
• if you have used a medicine similar to emtricitabine in the past, such as abacavir (Ziagen), didanosine (Videx), lamivudine (Epivir, Combivir, Epzicom, Trizivir), stavudine (Zerit), tenofovir (Viread), zalcitabine (Hivid), zidovudine (Retrovir), or emtricitabine combinations (Atripla, Complera, Truvada).

Some people develop a life-threatening condition called lactic acidosis while taking emtricitabine. You may be more likely to develop lactic acidosis if you are overweight or have liver disease, if you are a woman, or if you have taken HIV or AIDS medications for a long time. Talk with your doctor about your individual risk.

FDA pregnancy category B. Emtricitabine is not expected to harm an unborn baby. However, HIV can be passed to your baby if you are not properly treated during pregnancy. Take all of your HIV medicines as directed to control your infection.

If you are pregnant, your name may be listed on a pregnancy registry. This is to track the outcome of the pregnancy and to evaluate any effects of emtricitabine on the baby.

Women with HIV or AIDS should not breast feed a baby. Even if your baby is born without HIV, the virus may be passed to the baby in your breast milk.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

The following adverse reactions are discussed in other sections of the labeling:

• Lactic acidosis/severe hepatomegaly with steatosis [See BOXED WARNING, WARNINGS AND PRECAUTIONS].
• Severe acute exacerbations of Hepatitis B [See BOXED WARNING, WARNINGS AND PRECAUTIONS].
• Immune reconstitution syndrome [See WARNINGS AND PRECAUTIONS].

Adverse Reactions from Clinical Trials Experience

More than 2,000 adult subjects with HIV-1 infection have been treated with EMTRIVA alone or in combination with other antiretroviral agents for periods of 10 days to 200 weeks in clinical trials.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions (incidence greater than or equal to 10%, any severity) identified from any of the 3 large controlled clinical trials include headache, diarrhea nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough, and rhinitis.

Studies 301A and 303- Treatment Emergent Adverse Reactions: The most common adverse reactions that occurred in subjects receiving EMTRIVA with other antiretroviral agents in clinical trials 301A and 303 were headache, diarrhea, nausea, and rash, which were generally of mild to moderate severity. Approximately 1% of subjects discontinued participation in the clinical trials due to these events. All adverse reactions were reported with similar frequency in EMTRIVA and control treatment groups with the exception of skin discoloration which was reported with higher frequency in the EMTRIVA treated group.

Skin discoloration, manifested by hyperpigmentation on the palms and/or soles was generally mild and asymptomatic. The mechanism and clinical significance are unknown.

A summary of EMTRIVA treatment-emergent clinical adverse reactions in Studies 301A and 303 is provided in Table 2.

Table 2 : Selected Treatment-Emergent Adverse Reactions (All Grades, Regardless of Causality) Reported in ≥ 3% of EMTRIVA-Treated Subjects in Either Study 301A or 303 (0-48 Weeks)

Studies 301A and 303- Laboratory Abnormalities: Laboratory abnormalities in these trials occurred with similar frequency in the EMTRIVA and comparator groups. A summary of Grades 3-4 laboratory abnormalities is provided in Table 3 below.

Table 3 : Treatment-Emergent Grades 3-4 Laboratory Abnormalities Reported in ≥ 1% of EMTRIVA-Treated Subjects in Either Study 301A or 303

Study 934- Treatment Emergent Adverse Reactions: In Study 934, 511 antiretroviralna�ve subjects received either VIREAD® + EMTRIVA administered in combination with efavirenz (N=257) or zidovudine/lamivudine administered in combination with efavirenz (N=254). Adverse reactions observed in this trial were generally consistent with those seen in previous trials in treatment-experienced or treatment-na�ve subjects (Table 4).

Table 4 : Selected Treatment-Emergent Adverse Reactionsa (Grades 2-4) Reported in ≥ 5% in Any Treatment Group in Study 934 (0-144 Weeks)

Study 934 - Laboratory Abnormalities: Significant laboratory abnormalities observed in this trial are shown in Table 5.

Table 5 : Significant Laboratory Abnormalities Reported in ≥ 1% of Subjects in Any Treatment Group in Study 934 (0-144 Weeks)

Assessment of adverse reactions is based on data from Study 203, an open label, uncontrolled trial of 116 HIV-1-infected pediatric subjects who received emtricitabine through 48 weeks. The adverse reaction profile in pediatric subjects was generally comparable to that observed in clinical trials of EMTRIVA in adult subjects. Hyperpigmentation was more frequent in children. Additional adverse reactions identified from this trial include anemia.

Selected treatment-emergent adverse events, regardless of causality, reported in subjects during 48 weeks of treatment were the following: infection (44%), hyperpigmentation (32%), increased cough (28%), vomiting (23%), otitis media (23%), rash (21%), rhinitis (20%), diarrhea (20%), fever (18%), pneumonia (15%), gastroenteritis (11%), abdominal pain (10%), and anemia (7%). Treatment-emergent grades 3-4 laboratory abnormalities were experienced by 9% of pediatric subjects, including elevated amylase ( > 2.0 x ULN) (n=4), decreased neutrophils ( < 750/mm³) (n=3), elevated ALT ( > 5 x ULN) (n=2), elevated CPK ( > 4 x ULN) (n=2) and one subject each with elevated bilirubin ( > 3.0 x ULN), elevated GGT ( > 10 x ULN), elevated lipase ( > 2.5 x ULN), decreased hemoglobin ( < 7 g/dL), and decreased glucose ( < 40 mg/dL).

Read the entire FDA prescribing information for Emtriva (Emtricitabine)

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Emtricitabine can be taken with or without food. Take the medicine at the same time each day.

Measure liquid medicine with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.

If a child is taking this medication, tell your doctor if the child has any changes in weight. Emtricitabine doses are based on weight in children.

While using emtricitabine , you may need frequent blood tests. Your kidney and liver function may also need to be checked.

Do not take emtricitabine as your only HIV medication. HIV/AIDS is usually treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice. Every person with HIV or AIDS should remain under the care of a doctor.

If you have hepatitis B you may develop liver symptoms after you stop taking this medication, even months after stopping. Your doctor may want to check your liver function for several months after you stop using emtricitabine.

Get your prescription refilled before you run out of medicine completely. Your disease may become resistant to emtricitabine if you stop taking the medication even for a short time.

Store emtricitabine capsules at room temperature away from moisture, heat, and direct light.

Store emtricitabine liquid in the refrigerator. Do not freeze.

You may store the liquid at room temperature, but you must use it within 3 months.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Taking this medication will not prevent you from passing HIV to other people. Do not have unprotected sex or share razors or toothbrushes. Talk with your doctor about safe ways to prevent HIV transmission during sex. Sharing drug or medicine needles is never safe, even for a healthy person.

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

In the U.S.

• Emtriva

Available Dosage Forms:

• Capsule
• Solution

Therapeutic Class: Antiretroviral Agent

Pharmacologic Class: Nucleoside Reverse Transcriptase Inhibitor

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For emtricitabine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to emtricitabine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of emtricitabine in children.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of emtricitabine in the elderly. However, elderly patients are more likely to have age-related heart, kidney, or liver problems, which may require caution and an adjustment of dose in patients receiving emtricitabine.

Pregnancy

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking emtricitabine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using emtricitabine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Orlistat

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of emtricitabine. Make sure you tell your doctor if you have any other medical problems, especially:

• Hepatitis B virus (HBV) infection—Should not be used in patients with this condition. You or your child may receive emtricitabine to treat HIV infection even if you also have hepatitis B virus infection. Your doctor will want to follow you closely for several months once you stop taking emtricitabine.

• Kidney disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

(em trye SYE ta been)

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

Cmax and AUC are increased in patients with CrCl less than 50 mL/minute or ESRD requiring dialysis.

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:

• 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).

More frequently reported side effects include: increased serum alanine aminotransferase, increased serum amylase, increased serum aspartate aminotransferase, and neutropenia. See below for a comprehensive list of adverse effects.

Applies to emtricitabine: oral capsule, oral solution

General

The most common side effects reported during any of 3 large controlled clinical trials were headache, diarrhea, nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough, and rhinitis.

During 2 clinical trials, the most common side effects associated with emtricitabine in combination with other antiretrovirals were headache, diarrhea, nausea, and rash. Most were of mild to moderate severity. Treatment was discontinued due to these adverse effects in approximately 1% of patients.

Side effects have been reported for emtricitabine when taken in combination with other antiretroviral agents.[Ref]

Dermatologic

Dermatological side effects have included rash event (any Grade: up to 30%; Grades 2 to 4: 7%). "Rash event" included rash, pruritus, maculopapular rash, urticaria, vesiculobullous rash, pustular rash, exfoliative rash, generalized rash, macular rash, pruritic rash, vesicular rash, and allergic reaction. Skin discoloration (palmar-plantar hyperpigmentation) has been reported.[Ref]

Nervous system

Nervous system side effects have included dizziness (any Grade: up to 25%; Grades 2 to 4: 8%), headache (any Grade: up to 22%; Grades 2 to 4: 6%), insomnia (any Grade: up to 16%; Grades 2 to 4: 5%), paresthesia (any Grade: up to 6%), neuropathy/peripheral neuritis (any Grade: 4%), and somnolence.[Ref]

Gastrointestinal

Gastrointestinal side effects have included diarrhea (any Grade: 23%; Grades 2 to 4: 9%), nausea (any Grade: up to 18%; Grades 2 to 4: 9%), vomiting (any Grade: 9%; Grades 2 to 4: 2%), and dyspepsia (any Grade: up to 8%).[Ref]

Metabolic

Metabolic side effects have included blood glucose changes (less than 40 or greater than 250 mg/dL; up to 3%), hyperglycemia (greater than 250 mg/dL; 2%), and increased fasting cholesterol (greater than 240 mg/dL; 22%), triglycerides (greater than 750 mg/dL; up to 10%), serum amylase (greater than 2 times ULN: up to 5%; greater than 175 units/L: 8%), fasting triglycerides (greater than 750 mg/dL; 4%), pancreatic amylase (greater than 2 times ULN; up to 2%), serum lipase (greater than 2 times ULN; up to 1%), and alkaline phosphatase (greater than 550 units/L; 1%). Redistribution/accumulation of body fat including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement, and "cushingoid appearance" have been observed in patients receiving antiretroviral therapy.[Ref]

Respiratory

Respiratory side effects have included rhinitis (any Grade: up to 18%), increased cough (any Grade: 14%), sinusitis (Grades 2 to 4: 8%), upper respiratory tract infections (Grades 2 to 4: 8%), and nasopharyngitis (Grades 2 to 4: 5%).[Ref]

Other

Other side effects have included asthenia (any Grade: up to 16%), abdominal pain (any Grade: up to 14%), and fatigue (Grades 2 to 4: 9%).[Ref]

Musculoskeletal

Increased creatine kinase (greater than 990 units/L in males and 845 units/L in females) has been reported in 9% of patients.[Ref]

Musculoskeletal side effects have included elevated creatine kinase (greater than 4 times ULN; up to 12%), myalgia (any Grade: up to 6%), and arthralgia (any Grade: up to 5%).[Ref]

Psychiatric

Psychiatric side effects have included abnormal dreams (any Grade: up to 11%), depressive disorders (any Grade: up to 9%), and depression (Grades 2 to 4: 9%).

Hepatic

Hepatic side effects have included elevated AST (greater than 5 times ULN; up to 6%), ALT (greater than 5 times ULN; up to 5%), and bilirubin (greater than 2.5 times ULN; up to 1%). Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of emtricitabine and other nucleoside analogs alone or in combination with other antiretroviral agents. Severe acute exacerbations of hepatitis B have been reported in patients coinfected with HIV-1 and hepatitis B after discontinuation of emtricitabine and were associated with liver failure and liver decompensation in some patients.[Ref]

Increased AST (greater than 180 units/L in males and 170 units/L in females) has been reported in 3% of patients. Increased ALT (greater than 215 units/L in males and 170 units/L in females) has been reported in 2% of patients.[Ref]

Immunologic

Immunologic side effects have included immune reconstitution syndrome. Autoimmune disorders (e.g., Graves' disease, polymyositis, and Guillain-Barre syndrome) have been reported in the setting of immune reconstitution.

Hematologic

Hematologic side effects have included decreased neutrophils (less than 750/mm3; up to 5%).[Ref]

Genitourinary

Genitourinary side effects have included hematuria (greater than 75 RBC/HPF; 3%) and glycosuria (3 plus; less than 1%).

Some side effects of emtricitabine may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Emtricitabine has been assigned to pregnancy category B by the FDA. The incidence of fetal variations and malformations was not increased in embryofetal toxicity studies performed with emtricitabine in mice at exposures approximately 60-fold higher and in rabbits at approximately 120-fold higher than human exposures at the recommended daily dose. There are no controlled data in human pregnancy. Emtricitabine is only recommended for use during pregnancy when benefit outweighs risk.

To monitor fetal outcomes of pregnant women exposed to emtricitabine, an antiretroviral Pregnancy Registry as been established. Healthcare providers are encouraged to register patients by calling 1-800-258-4263 (USA).

LactMed Record Number

657

Last Revision Date

20170808

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.