Last Updated June 10, 2016
Nucleoside reverse transcriptase inhibitor antiretroviral
Indication: treatment of HIV infection in combination with other antiretrovirals. Together with tenofovir, recommended for treatment of HIV/hepatitis B coinfection.
SA Formulary lists off-label uses: reduction of perinatal transmission of HIV, pre-exposure prophylaxsis, and postexposure prophylaxis, all in combination with other antiretrovirals.
Mechanism of action†: a cytosine analogue that is phosphorylated intracellularly to emtricitabine 5’-triphosphate, which interferes with HIV viral RNA–dependent DNA polymerase inhibiting viral replication.
Pharmacokinetics: renal excretion 86%. Half-life: serum = 10 hours; intracellular = > 20 hours.
Adult Dose: 200 mg once daily. Take without regard to meals.
Use in Renal or Hepatic Insufficiency: Use with caution in renal and hepatic impairment.
Dosage for patients with chronic kidney disease or end-stage renal disease‡:
If using emtricitabine/tenofovir:
Use in Pregnancy and Breastfeeding†: Category B. Excreted into breast milk.
Use in Children: Included in recommended antiretroviral regimens for children.*
US Prescribing Information Boxed Warning†: lactic acidosis/hepatomegaly with steatosis has been reported with nucleoside analogues with fatal cases reported. Use with caution in patients with risk factors for liver disease and suspend treatment if a patient develops signs and symptoms.
US Prescribing Information Boxed Warning†: hepatitis B virus testing should be done prior to initiation of emtricitabine and caution used in coinfected patients.
Use with caution in patients with hepatitis B infection; rebound hepatitis may occur following therapy withdrawal.
Included in recommended regimens in pregnancy, lactation, children.*
Minimal toxicity, hyperpigmentation†/skin discoloration,† headache, nausea, vomiting, rash.
*South Africa National Department of Health Consolidated Guidelines, 2015.
†Information from US prescribing information.
‡Recommendation from South African Renal Society, 2008.