Dosing & Uses
Dosage Forms & Strengths
Chronic Hepatitis B
600 mg PO qDay
Administration: with or without food
CrCl 50 mL/min or higher: normal dose
CrCl 30-49 mL/min: 600 mg PO q48hr
CrCl <30 mL/min: 600 mg PO q72hr
ESRD: 600 mg PO q96hr
Safety and efficacy not established
Well tolerated, most AEs comparable to lamivudine
Elevated serum creatinine kinase (11%); higher incidence than lamivudine
Abdominal pain, upper (6%)
Pharyngolaryngeal pain (5%)
Back pain (4%)
Abdominal pain (3%)
ALT increased (3%)
Abdominal distension (3%)
Hepatitis B exacerbation (2%)
Black Box Warnings
Hepatitis B Treatment
- Severe acute exacerbations of hepatitis B reported in patients who have discontinued therapy for hepatitis B
- Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who discontinue therapy
- Resumption of therapy for hepatitis B may be warranted
- Lactic acidosis and severe hepatomegaly with steatosis (including fatal cases) reported with use of nucleoside analogues alone or in combination
Coadministration with pegylated interferon alfa-2a is contraindicated because of increased risk of peripheral neuropathy
Discontinuation may result in acute exacerbation of hepatitis B
Risk of lactic acidosis, severe hepatomegaly with steatosis
Risk of peripheral neuropathy alone or in combination with pegylated interferon alfa-2a and other interferons (see Contraindications)
Pregnancy & Lactation
Pregnancy Category: B (to register pregnant patients, call 1-800-258-4263)
Lactation: not known if distributed in breast milk, do not nurse
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.
Mechanism of Action
Thymidine nucleoside analog; inhibits HBV DNA polymerase, which blocks reverse transcriptase activity and in turn reduces viral DNA replication.
Half-life, elimination: 40-49 hr
Peak plasma time: 1-4 hr
Concentration: 3.7±1.25 mcg/mL
AUC: 26.1±7.2 mcg/mL
Trough: 0.2-0.3 mcg/mL
Protein bound: 3.3%
Renal clearance: 7.6±2.9 mL/min
Metabolism: None detected in studies
Excretion: urine 42% (passive diffusion)
Dialyzable: 23% (HD)
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