Adefovir
HEPSERA
What it isNucleotide analog inhibiting HBV polymerase; chronic hepatitis B.
Why this oneIt retains activity against lamivudine-resistant virus.
What limits itDose-dependent nephrotoxicity and a low resistance barrier mean tenofovir and entecavir have replaced it. Hepatitis can flare on stopping.
FDA label
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| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Chronic hepatitis B (adequate renal function) | Adults | 10 mg QD | 10 mg QD (optimal duration unknown) | 10 mg QD |
| Chronic hepatitis B (adequate renal function) | Peds >=12 yr (not recommended <12 yr) | 10 mg QD | 10 mg QD | 10 mg QD |
Renal Adults: CrCl >=50: 10 mg q24h; 30-49: 10 mg q48h; 10-29: 10 mg q72h; hemodialysis: 10 mg q7d following dialysis. No recommendation for non-HD CrCl <10 or for adolescents with renal impairment
Hepatic No adjustment needed (label: no change in dosing required in hepatic impairment)
Instructions
- Oral, with or without food
- Offer HIV antibody testing before initiating
- Monitor hepatic function closely for at least several months after discontinuation
- Monitor renal function during treatment, esp. in at-risk patients
Cautions
- Severe acute hepatitis exacerbation on discontinuation — monitor hepatic function after stopping
- Nephrotoxicity (delayed, gradual creatinine rise) with chronic use — monitor renal function; adjust dosing interval
- HIV resistance may emerge in unrecognized/untreated HIV — test before starting
- Lactic acidosis / severe hepatomegaly with steatosis, incl. fatal cases
- Do not use concurrently with tenofovir disoproxil fumarate or tenofovir alafenamide products
- Clinical resistance: use with lamivudine in lamivudine-resistant HBV; consider modifying treatment if HBV DNA remains >1000 copies/mL
Adverse reactions
- Asthenia, headache, abdominal pain, nausea (>5%, compensated liver disease)
- Increased creatinine (most common in pre-/post-transplant lamivudine-resistant patients)
Pregnancy Insufficient prospective data (Antiretroviral Pregnancy Registry 1-800-258-4263)
Lactation Unknown if present in human milk; weigh benefits of breastfeeding vs need for drug
⚠ BOXED WARNINGS
- Severe acute exacerbation of hepatitis B on discontinuation
- Nephrotoxicity
- Lactic acidosis
- HIV resistance
Classes and tags
Clinical profile
Mechanism of action: Adefovir ballicule
