Drugs List

Therapeutic Indications

Uses

Treatment of Human Immunodeficiency Virus 1 (HIV-1) infection in combination with other anti-retroviral agents in adults and children.

Treatment with emtricitabine is based on studies in treatment-naive patients and in treatment-experienced patients with stable virological control. There is no experience in patients who are failing their current regimen or who have failed multiple regimens.

When new regimens are decided for patients who have failed an antiretroviral regimen, the patterns of mutations associated with different medicines and the treatment history should be carefully considered. Resistant testing may be necessary.

Administration

For oral administration, with or without food.

Contraindications

Breastfeeding - (see Lactation)

Children under 4 months of age - see Dosage; Children

Precautions and Warnings

Emtricitabine therapy should be initiated by a physician experienced in the management of HIV.

Patients should be advised that treatment is not a cure for HIV infection and they may still develop opportunistic infections and other complications of HIV infection. Patients should therefore remain under close clinical observation by physicians experienced in the treatment of HIV infection.

Emtricitabine is not recommended as monotherapy for the treatment of HIV infection. It must be used in combination with other anti-retroviral drugs. Emtricitabine should not be used with other products containing emtricitabine or lamivudine.

Patients should be advised that treatment does not prevent the risk of HIV transmission through sexual contact or blood contamination and that appropriate precautions should be continued.

Pregnancy - see Pregnancy section
Advise women of child bearing age to use adequate contraception during treatment with emtricitabine.

Renal impairment (creatinine clearance less than 30 ml/minute) - see Dosage; Renal Impairment
Renal function and the patients clinical response to treatment should be closely monitored in patients with renal impairment.

Blood lipid and glucose levels may increase during antiretroviral therapy. This may be linked to disease control and lifestyle. Refer to established HIV treatment guidelines for monitoring and manage lipid and glucose level disorders as appropriate.

Patients with pre-existing hepatic impairment, including chronic active hepatitis, have an increased risk of developing hepatic function abnormalities during therapy. These patients should be closely monitored and treatment should be interrupted or discontinued if hepatic disease worsens in these patients.

Patients with chronic hepatitis B or C who are treated with combination antiretroviral therapy have an increased risk of developing severe and potentially fatal hepatic adverse effects, and therefore should be closely monitored during treatment. The product literature relating to concurrent treatments for hepatitis B or C should be consulted. If hepatic disease worsens in these patients, interruption or discontinuation of therapy should be considered. In patients with advanced liver disease or cirrhosis discontinuation is not recommended as subsequent exacerbations of hepatitis may lead to hepatic decompensation.
Emtricitabine is active in vitro against hepatitis B virus (HBV). Limited data is available on the safety and efficacy of emtricitabine in patients who are co-infected with HIV and HBV. Patients co-infected with HIV and HBV should be closely monitored with clinical and laboratory follow-up for several months after stopping treatment with emtricitabine for evidence of exacerbations of hepatitis.

Treatment regimens containing nucleoside or nucleotide analogues have been reported to cause mitochondrial dysfunction in HIV-negative infants exposed in utero and/or post-natally. Adverse reactions such as haematological (anaemia, neutropenia), metabolic (hyperlactataemia, hyperlipasemia) and neurological (hypertonia, convulsions, abnormal behaviour) have been reported. Consider in children exposed to nucleoside or nucleotide analogues in utero (including HIV-negative infants) and who present with neurological symptoms or severe clinical findings of unknown cause.

When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunist pathogens may arise. This can lead to the aggravation of symptoms or other serious clinical conditions such as cytomegalovirus retinitis, mycobacterial infections or pneumocystis carinii pneumonia. These reactions are usually observed within the first few weeks or months after treatment initiation. Any inflammatory symptoms should be evaluated and treated appropriately.

Cases of osteonecrosis have been reported in patients with advanced HIV disease and/or long term exposure to combination antiretroviral therapy, although the aetiology of this condition is thought to be due to several factors including corticosteroid use, alcohol consumption, severe immunosuppression, higher body mass index. Patients should be advised to seek medical advice if they experience joint aches or pains, joint stiffness or difficulty in movement.

The oral solution contains sunset yellow (E110) which may cause allergic reactions, including asthma. Allergic reactions (possibly delayed) may also be caused by other components of the solution including methyl parahydroxybenzoate (E218) and propyl parahydroxybenzoate (E216).
The oral solution contains sodium, which should be taken into consideration when treating patients with restricted sodium intake.

If vomiting occurs within 1 hour of a dose the dose should be re-taken.

Warn patients that dizziness may be side effect and that if affected they should not drive or operate machinery.

Pregnancy and Lactation

Pregnancy

Emtricitabine should only be used in pregnancy if necessary.

The safety of emtricitabine in human pregnancy has not been established.

Studies on animals do not indicate direct or indirect harmful effects of emtricitabine to pregnancy, foetal development, parturition or postnatal development.

Women of child bearing potential should be advised to use adequate contraception.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

It is not known whether emtricitabine is excreted in human breast milk.

It is recommended that women with HIV do not breastfeed their infants under any circumstances in order to prevent the transmission of HIV.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Neutropenia
Anaemia
Thrombocytopenia
Headache
Dizziness
Asthenia
Insomnia
Abnormal dreams
Fatigue
Diarrhoea
Nausea
Vomiting
Dyspepsia
Abdominal pain
Flatulence
Anorexia
Dyspnoea
Cough
Pancreatitis
Hepatic impairment
Elevated serum lipase
Elevated amylase including elevated pancreatic amylase
Elevated serum aspartate aminotransferase (AST)
Elevated alanine aminotransferase (ALT)
Hyperbilirubinaemia
Myalgia
Arthralgia
Fever
Rash
Pruritis
Maculopapular rash
Urticaria
Vesiculobullous rash
Pustular rash
Allergic reaction
Skin discolouration (hyperpigmentation)
Elevated creatine kinase
Pain
Osteonecrosis
Angioedema
Immune reactivation syndrome - Inflammatory reaction to asymptomatic or residual opportunistic infections (HIV infected patients with severe immune deficiency)

Presentation

Hard capsules containing 200 mg emtricitabine.

Oral solution containing 10 mg emtricitabine per ml.

Drugs List

Therapeutic Indications

Uses

Treatment of Human Immunodeficiency Virus 1 (HIV-1) infection in combination with other anti-retroviral agents in adults and children.

Treatment with emtricitabine is based on studies in treatment-naive patients and in treatment-experienced patients with stable virological control. There is no experience in patients who are failing their current regimen or who have failed multiple regimens.

When new regimens are decided for patients who have failed an antiretroviral regimen, the patterns of mutations associated with different medicines and the treatment history should be carefully considered. Resistant testing may be necessary.

Dosage

Emtricitabine therapy should be initiated by a physician experienced in the management of HIV.

Emtricitabine is not recommended as monotherapy for the treatment of HIV infection. It must be used in combination with other anti-retroviral drugs. Emtricitabine should not be used with other products containing emtricitabine or lamivudine.

Adults

Elderly

Children

Patients with Renal Impairment

Patients with Hepatic Impairment

Additional Dosage Information

Administration

For oral administration, with or without food.

Contraindications

Breastfeeding - (see Lactation)

Children under 4 months of age - see Dosage; Children

Precautions and Warnings

Emtricitabine therapy should be initiated by a physician experienced in the management of HIV.

Patients should be advised that treatment is not a cure for HIV infection and they may still develop opportunistic infections and other complications of HIV infection. Patients should therefore remain under close clinical observation by physicians experienced in the treatment of HIV infection.

Emtricitabine is not recommended as monotherapy for the treatment of HIV infection. It must be used in combination with other anti-retroviral drugs. Emtricitabine should not be used with other products containing emtricitabine or lamivudine.

Patients should be advised that treatment does not prevent the risk of HIV transmission through sexual contact or blood contamination and that appropriate precautions should be continued.

Pregnancy - see Pregnancy section
Advise women of child bearing age to use adequate contraception during treatment with emtricitabine.

Renal impairment (creatinine clearance less than 30 ml/minute) - see Dosage; Renal Impairment
Renal function and the patients clinical response to treatment should be closely monitored in patients with renal impairment.

Blood lipid and glucose levels may increase during antiretroviral therapy. This may be linked to disease control and lifestyle. Refer to established HIV treatment guidelines for monitoring and manage lipid and glucose level disorders as appropriate.

Patients with pre-existing hepatic impairment, including chronic active hepatitis, have an increased risk of developing hepatic function abnormalities during therapy. These patients should be closely monitored and treatment should be interrupted or discontinued if hepatic disease worsens in these patients.

Patients with chronic hepatitis B or C who are treated with combination antiretroviral therapy have an increased risk of developing severe and potentially fatal hepatic adverse effects, and therefore should be closely monitored during treatment. The product literature relating to concurrent treatments for hepatitis B or C should be consulted. If hepatic disease worsens in these patients, interruption or discontinuation of therapy should be considered. In patients with advanced liver disease or cirrhosis discontinuation is not recommended as subsequent exacerbations of hepatitis may lead to hepatic decompensation.
Emtricitabine is active in vitro against hepatitis B virus (HBV). Limited data is available on the safety and efficacy of emtricitabine in patients who are co-infected with HIV and HBV. Patients co-infected with HIV and HBV should be closely monitored with clinical and laboratory follow-up for several months after stopping treatment with emtricitabine for evidence of exacerbations of hepatitis.

Treatment regimens containing nucleoside or nucleotide analogues have been reported to cause mitochondrial dysfunction in HIV-negative infants exposed in utero and/or post-natally. Adverse reactions such as haematological (anaemia, neutropenia), metabolic (hyperlactataemia, hyperlipasemia) and neurological (hypertonia, convulsions, abnormal behaviour) have been reported. Consider in children exposed to nucleoside or nucleotide analogues in utero (including HIV-negative infants) and who present with neurological symptoms or severe clinical findings of unknown cause.

When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunist pathogens may arise. This can lead to the aggravation of symptoms or other serious clinical conditions such as cytomegalovirus retinitis, mycobacterial infections or pneumocystis carinii pneumonia. These reactions are usually observed within the first few weeks or months after treatment initiation. Any inflammatory symptoms should be evaluated and treated appropriately.

Cases of osteonecrosis have been reported in patients with advanced HIV disease and/or long term exposure to combination antiretroviral therapy, although the aetiology of this condition is thought to be due to several factors including corticosteroid use, alcohol consumption, severe immunosuppression, higher body mass index. Patients should be advised to seek medical advice if they experience joint aches or pains, joint stiffness or difficulty in movement.

The oral solution contains sunset yellow (E110) which may cause allergic reactions, including asthma. Allergic reactions (possibly delayed) may also be caused by other components of the solution including methyl parahydroxybenzoate (E218) and propyl parahydroxybenzoate (E216).
The oral solution contains sodium, which should be taken into consideration when treating patients with restricted sodium intake.

If vomiting occurs within 1 hour of a dose the dose should be re-taken.

Warn patients that dizziness may be side effect and that if affected they should not drive or operate machinery.

Pregnancy and Lactation

Pregnancy

Emtricitabine should only be used in pregnancy if necessary.

The safety of emtricitabine in human pregnancy has not been established.

Studies on animals do not indicate direct or indirect harmful effects of emtricitabine to pregnancy, foetal development, parturition or postnatal development.

Women of child bearing potential should be advised to use adequate contraception.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

It is not known whether emtricitabine is excreted in human breast milk.

It is recommended that women with HIV do not breastfeed their infants under any circumstances in order to prevent the transmission of HIV.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Effects on Ability to Drive and Operate Machinery

There have been no studies into the effects of emtricitabine on the ability to drive and operate machinery, however, dizziness has been reported as a side effect of emtricitabine therapy and patients should be advised to be cautious.

Counselling

Patients should be advised that treatment is not a cure for HIV infection and they may still develop opportunistic infections and other complications of HIV infection.

Advise patients that current anti-retroviral therapy has not been shown to prevent the risk of transmission of HIV to others through sexual contact or blood contamination. Appropriate precautions should continue to be used.

Advise women of child-bearing age to take adequate contraceptive precautions.

Warn patients that dizziness may be side effect and that if affected they should not drive or operate machinery.

Patients should be advised to seek medical advice if they experience joint aches or pains, joint stiffness or difficulty in movement.

Patients should be advised that if a dose is missed within 12 hours of the time it is normally taken, they should take the dose with or without food as soon as possible and resume the normal dosing schedule. If a dose is missed by more than 12 hours they should not take the missed dose, and resume the usual schedule.

If vomiting occurs within one hour of a dose, the dose should be retaken.

Side Effects

Neutropenia
Anaemia
Thrombocytopenia
Headache
Dizziness
Asthenia
Insomnia
Abnormal dreams
Fatigue
Diarrhoea
Nausea
Vomiting
Dyspepsia
Abdominal pain
Flatulence
Anorexia
Dyspnoea
Cough
Pancreatitis
Hepatic impairment
Elevated serum lipase
Elevated amylase including elevated pancreatic amylase
Elevated serum aspartate aminotransferase (AST)
Elevated alanine aminotransferase (ALT)
Hyperbilirubinaemia
Myalgia
Arthralgia
Fever
Rash
Pruritis
Maculopapular rash
Urticaria
Vesiculobullous rash
Pustular rash
Allergic reaction
Skin discolouration (hyperpigmentation)
Elevated creatine kinase
Pain
Osteonecrosis
Angioedema
Immune reactivation syndrome - Inflammatory reaction to asymptomatic or residual opportunistic infections (HIV infected patients with severe immune deficiency)

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Shelf Life and Storage

Capsules
There are no special precautions for storage

Oral solution
Store in a refrigerator between 2 - 8 degrees C
After opening, do not store above 25 degrees C

Further Information

Last Full Review Date: February 2012

Reference Sources

British National Formulary, 62nd Edition (2011) Pharmaceutical Press, London.

BNF for Children (2011-2012) Pharmaceutical Press, London.

Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

Summary of Product Characteristics: Emtriva 200mg Hard Capsules. Gilead Science Ltd. Revised October 2018.
Summary of Product Characteristics: Emtriva 10mg per mL Oral Solution. Gilead Science Ltd. Revised October 2018.

The Renal Drug Handbook. 3rd edition. (2009) ed. Ashley, C and Currie, Radcliffe Publishing Ltd, Abingdon.

US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Emtricitabine Last revised: August 2, 2011
Last accessed: February 6, 2012