BLACK BOX WARNING
- lactic acidosis and severe hepatomegaly with steatosis (class NRTI toxicity)
- severe acute exacerbation of hepatitis B after discontinuation in HBV-coinfected patients
emtricitabine
Brand: Emtriva, component of Truvada, Biktarvy, Descovy, etc.
⚠ BBW Prototype: tenofovir-disoproxil-fumarate
Drug Class: nucleoside reverse transcriptase inhibitor (NRTI)
Drug Family: antiretroviral
Subclass: cytidine analog NRTI
Organ Systems: infectious-disease
Mechanism of Action
Phosphorylated to emtricitabine triphosphate; competes with deoxycytidine triphosphate for incorporation into viral DNA; once incorporated, acts as a chain terminator. Also active against hepatitis B virus.
HIV reverse transcriptase (nucleoside active site)
Indications
- HIV-1 infection (as part of combination ART — virtually always in combination, not used alone)
- hepatitis B infection (also active)
Contraindications
- emtricitabine hypersensitivity
Adverse Effects
Common
- skin hyperpigmentation (palms/soles — occurs in darker-skinned patients)
- nausea
- headache
Serious
- lactic acidosis and severe hepatomegaly with steatosis (class NRTI effect)
- severe acute exacerbation of hepatitis B upon discontinuation
Pharmacokinetics (ADME)
| Absorption | 93% oral bioavailability; not significantly affected by food |
| Distribution | widely distributed; low protein binding |
| Metabolism | minimal; some oxidation and glucuronidation |
| Excretion | renal (86% as unchanged drug and metabolites); dose adjustment in CKD |
| Half-life | 10 hours |
| Onset | 1–2 hours |
| Peak | 1–2 hours |
| Duration | 24 hours |
| Protein Binding | <4% |
| Vd | moderate |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| lamivudine | cross-resistance and overlapping mechanism; do not combine | major |
| drugs causing lactic acidosis (metformin, NRTIs) | additive mitochondrial toxicity; lactic acidosis risk | moderate |
Nursing Considerations
- Emtricitabine is virtually always used in combination tablets (e.g., Truvada = emtricitabine + tenofovir DF; Biktarvy = bictegravir + emtricitabine + tenofovir AF); verify patient is not receiving duplicate NRTI therapy.
- Monitor renal function (SCr, eGFR, urine protein) due to renal excretion; dose adjustment required when eGFR <50 mL/min.
- If stopping emtricitabine in a patient with HIV/HBV co-infection, closely monitor LFTs for 4+ weeks — severe HBV flares have caused liver failure.
- Counsel patients on the skin hyperpigmentation — benign and reversible.
Clinical Pearls
- Emtricitabine and tenofovir are the most widely used NRTI backbone of modern ART; the emtricitabine/tenofovir combination (Truvada) is also the backbone of pre-exposure prophylaxis (PrEP) for HIV prevention.
- Emtricitabine and lamivudine have virtually identical mechanisms, resistance profiles, and activity against HBV; they are considered interchangeable but should never be combined due to redundancy.
Safety Profile
Pregnancy safe
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.