抗病毒藥品 Treatment of chronic hepatitis B in patients with evidence of viral replication and active liver inflammation

Nucleoside Reverse Transcriptase Inhibitor (Anti-HBV)
Telbivudine, a synthetic thymidine nucleoside analogue (L-enantiomer of thymidine), is intracellularly phosphorylated to the active triphosphate form, which competes with the natural substrate, thymidine 5'-triphosphate, to inhibit hepatitis B viral DNA polymerase; enzyme inhibition blocks reverse transcriptase activity thereby reducing viral DNA replication.

Vd: >total body water; Protein binding: ~3%
Metabolism: No metabolites detected
Half-life elimination: (Terminal) 40-49 hours
Time to peak, plasma: 1-4 hours
Excretion: Urine (~42% as unchanged drug)

1. Hypersensitivity to telbivudine or to any of the excipients.
2. Concurrent use with peginterferon alfa-2a.

In hepatitis B-infected women (not coinfected with HIV), the AASLD chronic hepatitis B treatment guidelines suggest antiviral therapy to reduce the risk of perinatal transmission of hepatitis B in HBsAg-positive pregnant women with an HBV DNA >200,000 units/mL.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk and benefits.

Dizziness, headache, abdominal pain, diarrhoea, blood creatine phosphokinase increased, fatigue, rash

600mg PO QD; with or without food

Adolescents ≥16 years: Refer to adult dosing

1. CrCl ≥50 mL/minute: No dosage adjustment is necessary
2. CrCl 30-49 mL/minute: 600 mg every 48 hours
3. CrCl <30 mL/minute (not requiring dialysis): 600 mg every 72 hours
4. ESRD: 600 mg every 96 hours
5. Hemodialysis: Administer after dialysis session

No dosage adjustment necessary.