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adefovir (adefovir dipivoxil, Hepsera): Dosing and Uses

 

Classes: Hepatitis B/Hepatitis C Agents; Hepatitis B, NRTIs

Medically reviewed by Min Clinic Staff | Updated: January 2026

Dosing and uses of adefovir dipivoxil, Hepsera (adefovir)

 

Adult dosage forms and strengths

tablet

  • 10mg

 

Chronic Hepatitis B

10 mg PO qDay

 

Renal Impairment

CrCl ≥ 50 mL/min: Dose adjustment not necessary

CrCl 30-49 mL/min: 10 mg PO q48hr

CrCl 10-29 mL/min: 10 mg PO q72hr

Hemodialysis: 10 mg qWeek following dialysis

 

Pediatric dosage forms and strengths

tablet

  • 10mg

 

Chronic Hepatitis B

<12 years old: Not recommended

≥12 years old: Administer as in adults, 10 mg PO qDay

 

Renal Impairment

CrCl ≥ 50 mL/min: Dose adjustment not necessary

CrCl 30-49 mL/min: 10 mg PO q48hr

CrCl 10-29 mL/min: 10 mg PO q72hr

Hemodialysis: 10 mg qWeek following dialysis

 

adefovir dipivoxil, Hepsera (adefovir) adverse (side) effects

>10%

Hematuria (11% vs 10% in placebo-treated)

Asthenia (13% vs. 14% placebo)

Hepatitis exacerbation (25%)

 

1-10%

Nausea (5%)

Flatulence (4%)

Diarrhea (3%)

Dyspepsia (3%)

Headache (9%)

Rash (1-10%)

Pruritus (1-10%)

Dyspepsia (5-9%)

Cough (6-8%)

Rhinitis (5%)

Increased AST/ALt

Abnormal liver function

Renal failure

Renal insufficiency

Increased serum Cr (2-3%)

Hypophosphatemia

 

Postmarketing Reports

Metabolism and nutrition disorders: Hypophosphatemia

Gastrointestinal disorders: Pancreatitis

Musculoskeletal system and connective tissue disorders: Myopathy, osteomalacia (manifested as bone pain and may contribute to fractures), both associated with proximal renal tubulopathy

Renal and urinary disorders: Renal failure, Fanconi syndrome, proximal renal tubulopathy

 

Warnings

Black box warnings

Severe acute exacerbations of hepatitis reported following discontinuing drug; monitor hepatic function

Chronic use may result in nephrotoxicity in patients with renal impairment or in those at risk of renal dysfunction; dose adjustment may be required

Resistance to HIV NRTIs may emerge in patients with chronic hepatitis B in whom HIV infection is unrecognized or untreated

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, reported with nucleoside analogs alone or in combination with other antiretrovirals; obesity and prolonged nucleoside exposure may be risk factors

 

Contraindications

Hypersensitivity

 

Cautions

Discontinuation may result in severe acute exacerbation of hepatitis B

Patients who discontinue treatment: Monitor hepatic function for several months

Patients with renal dysfunction: Risk of nephrotoxicity (monitor and adjust dose accordingly)

Coadministration with drugs that reduce renal function may increase adefovir serum concentration

Do not administer with tenofovir (additive toxicity)

May increase HIV resistance in untreated patients who are HIV+

Risk of lactic acidosis, severe hepatomegaly with steatosis

To monitor fetal outcomes, Pregnancy Registry established: 1-800-258-4263

 

Pregnancy and lactation

Pregnancy category: C (Pregnancy Registry: 1-800-258-4263)

Lactation: Unknown if excreted in breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of adefovir dipivoxil, Hepsera (adefovir)

Mechanism of action

Acyclic nucleotide analog; inhibits HBV DNA polymerase; inhibition blocks reverse transcriptase activity, which in turn reduces viral DNA synthesis

 

Absorption

Bioavailability: 59%

Peak plasma time: 0.58-4 hr

Peak plasma concentration: 18.4±6.26 ng/mL

AUC: 220±70 ng•hr/mL

 

Distribution

Protein Bound: ≤ 4%

Vd: 317-467 mL/kg

 

Metabolism

Rapidily converted to adefovir from the diester prodrug, adefovir dipivoxiL

Metabolites: Adefovir (active)

 

Elimination

Half-life: 7.48±1.65 hr

Renal clearance: 231±48.9 mL/min

Excretion: Urine; renal glomerular filtration, active tubular secretion

Dialyzable: Yes