Emtricitabine
EMTRIVA
What it isCytidine-analog reverse-transcriptase inhibitor; HIV treatment and combination PrEP.
Why this oneExcellent tolerability and dual hepatitis-B activity keep it paired with tenofovir across treatment and prevention.
What limits itStopping can trigger a severe hepatitis-B flare; renal impairment requires adjustment.
FDA-approved for
- HIV infection (2003)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection (in combination with other antiretrovirals) | Adults >=18 y | Capsule 200 mg QD (or oral solution 240 mg QD) | 200 mg QD | 200 mg QD (capsule); 240 mg QD (solution) |
| HIV-1 infection (in combination with other antiretrovirals) | Pediatric 0-3 months | Oral solution 3 mg/kg QD | 3 mg/kg QD | 3 mg/kg QD |
| HIV-1 infection (in combination with other antiretrovirals) | Pediatric 3 months-17 y | Oral solution 6 mg/kg QD (max 240 mg); if >33 kg and can swallow capsules, capsule 200 mg QD | 6 mg/kg QD (max 240 mg) | 240 mg QD |
Renal Adults — CrCl >=50: no adjustment; 30-49: capsule 200 mg q48h or solution 120 mg q24h; 15-29: capsule 200 mg q72h or solution 80 mg q24h; <15 or hemodialysis: capsule 200 mg q96h or solution 60 mg q24h (dose after dialysis on dialysis days). Pediatric renal impairment: insufficient data.
Hepatic Undefined
Instructions
- Take once daily, with or without food.
- Test for hepatitis B virus infection prior to or when initiating.
- In CrCl <50 mL/min, monitor clinical response and renal function closely (dose-interval adjustments not clinically validated).
Cautions
- Severe acute hepatitis B exacerbation after discontinuation in HIV-1/HBV coinfection (boxed): test for HBV before starting; monitor closely for months after stopping; anti-HBV therapy may be warranted.
- Immune reconstitution syndrome, incl. autoimmune disorders with later onset (Graves' disease, polymyositis, Guillain-Barre).
- Lactic acidosis and severe hepatomegaly with steatosis, incl. fatal cases (nucleoside analogs): suspend treatment if suggestive findings.
- Renally eliminated: reduce dosing frequency in renal impairment (CrCl <50).
Adverse reactions
- Headache
- Diarrhea
- Nausea
- Fatigue
- Dizziness
- Depression
- Insomnia
- Abnormal dreams
- Rash
- Abdominal pain
- Asthenia
- Increased cough
- Rhinitis
- Skin hyperpigmentation of palms/soles (very common in pediatric patients)
Pregnancy APR data (>2,700 first-trimester exposures) show no increase in overall major birth defects (2.4% vs 2.7% background); pregnancy registry 1-800-258-4263.
Lactation Do not breastfeed — risk of postnatal HIV-1 transmission, viral resistance in HIV-positive infants, and adverse reactions in the infant; emtricitabine is present in human milk.
⚠ BOXED WARNING
- Severe acute exacerbation of hepatitis B on discontinuation
Cost, est. cash$10–$500/month
Generic entry2018
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Emtricitabine ballicule
