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

  1. 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.
  2. Monitor renal function (SCr, eGFR, urine protein) due to renal excretion; dose adjustment required when eGFR <50 mL/min.
  3. If stopping emtricitabine in a patient with HIV/HBV co-infection, closely monitor LFTs for 4+ weeks — severe HBV flares have caused liver failure.
  4. 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