Generic
Telbivudine
1 brands available in the market
At a glance
Telbivudine is a synthetic thymidine nucleoside analog used for the treatment of chronic hepatitis B virus (HBV) infection. It inhibits HBV DNA polymerase to stop viral replication.
Description
Telbivudine is a synthetic thymidine nucleoside analog that undergoes intracellular phosphorylation to form the active metabolite telbivudine 5'-triphosphate. This active metabolite competes with thymidine triphosphate, incorporating into viral DNA and causing chain termination, thereby inhibiting HBV replication.
Indications
- Chronic hepatitis B (HBeAg-positive and HBeAg-negative, compensated liver disease)
Therapeutic class
Hepatic Viral Infections (Hepatitis B)
Pharmacological class
Nucleoside Analog (Antiviral)
Pharmacology
Telbivudine is phosphorylated by cellular kinases to form telbivudine 5'-triphosphate. It competes with the natural substrate thymidine triphosphate for HBV DNA polymerase, incorporating into viral DNA and causing chain termination, inhibiting viral replication.
Mechanism of action
Inhibits HBV DNA polymerase to stop viral replication.
Dosage
Adult and Adolescent (≥16 years) Dose (Oral):
- Recommended: 600 mg once daily
- HBeAg-positive: Initiate if HBV DNA <9 log10 copies/mL and ALT ≥2x ULN
- HBeAg-negative: Initiate if HBV DNA <7 log10 copies/mL
- Monitor HBV DNA at 24 weeks; consider alternative therapy if detectable
Administration
- Take orally with or without food
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Fatigue, headache, nausea
- Decreased appetite, diarrhea, abdominal pain
- Muscle pain, joint pain
- Insomnia, rash, fever
Serious:
- Myopathy, rhabdomyolysis
- Peripheral neuropathy
- Lactic acidosis
- Severe exacerbation of hepatitis B (upon treatment discontinuation)
Precautions & warnings
- Do not use in combination with peginterferon alfa-2a (risk of peripheral neuropathy)
- Discontinue if myopathy is diagnosed
- Dose adjustment required in renal impairment
- Not evaluated in liver transplant recipients or decompensated liver disease
- Not evaluated in patients co-infected with HCV, HIV, or HDV
Contraindications
- Hypersensitivity to telbivudine
- Combination with peginterferon alfa-2a
Drug interactions
- Drugs affecting renal function (aminoglycosides, loop diuretics, platinum compounds, vancomycin, amphotericin B): Altered plasma concentrations
- Myopathy-associated drugs (azole antifungals, cyclosporine, corticosteroids, statins): Increased myopathy risk
Food interactions
Alcohol is unsafe with Telbivudine (increased liver damage risk).
Use in pregnancy
Use in Pregnancy: Generally safe; animal studies show low or no adverse effects; limited human data; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited data suggests drug may pass into breast milk and harm the baby; consult your doctor.
Pediatric use
Safety and efficacy not established in children <16 years
Geriatric use
Caution required in elderly patients
Renal / hepatic impairment
Renal Impairment: CrCl <30 (without dialysis): 600 mg every 72 hours; CrCl 30-49: 600 mg every 48 hours; ESRD: 600 mg every 96 hours (post-dialysis); consult your doctor.
Hepatic Impairment: Safe in liver disease; no dose adjustment needed; consult your doctor.
Overdose effects
No overdose information; excessive doses may increase side effects; provide symptomatic treatment.
Storage conditions
Store in the original bottle at 15-30°C; keep out of reach of children.
Chemical structure
Telbivudine