Products
Emtricitabine is commercially available as a monopreparation in the form of capsules and as an oral solution (Emtriva, combination products, generics). It has been approved in many countries since 2004.
Structure and properties
Emtricitabine (C8H10FN3O3S, Mr = 247.2 g/mol) is a thioanalog of cytidine with a fluorine atom at the 5-position. It exists as a white powder that is soluble in water. It is a prodrug that is biotransformed intracellularly to the active metabolite emtricitabine 5′-triphosphate. Emtricitabine has a very similar structure to lamivudine (3TC).
Effects
Emtricitabine (ATC J05AF09) has antiviral properties against HIV. The effects are due to inhibition of the viral enzyme reverse transcriptase, which transcribes viral RNA into DNA and is important in viral replication. The activated agent is incorporated into viral DNA, leading to chain termination.
Indications
- For treatment of infection with HIV as part of combination antiretroviral therapy.
- HIV pre-exposure prophylaxis (see there).
Dosage
According to the professional information. The drugs are taken once a day, regardless of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Emtricitabine, unlike many other HIV medications, does not interact with CYP450. Interactions are possible with drugs that are tubularly secreted like emtricitabine.
Adverse effects
The most common possible adverse effects include headache, diarrhea, nausea, fatigue, dizziness, depression, sleep disturbances, skin rash, abdominal pain, weakness, cough, rhinitis, and increased skin pigmentation in children. Emtricitabine may rarely cause lactic acidosis and severe liver enlargement.
