Telbivudine

Indications

Telbivudine is used for: Chronic hepatitis B

Adult Dose

Oral Chronic hepatitis B Adult: 600 mg once daily.

Child Dose

Safety and efficacy not established Child: >16 yr: 600 mg once daily.

Renal Dose

Renal impairment: ESRD: 600 mg 96 hrly, after dialysis session. CrCl (ml/min) Dosage Recommendation <30 (not requiring dialysis) 600 mg 72 hrly. 30-49 600 mg 48 hrly.

Administration

May be taken with or without food.

Contra Indications

Hypersensitivity. Lactation. Concurrent use w/ peginterferon alfa-2a.

Precautions

Patient w/ cirrhosis, hepatomegaly or other risk factors for liver disease. Renal impairment. Pregnancy. Monitoring Parameters Monitor hepatic function (e.g. AST and ALT) periodically during therapy and for several mth following discontinuation of therapy; renal function; signs and symptoms of peripheral neuropathy or myopathy; serum creatine kinase; hepatitis B virus (HBV) DNA 3-6 mthly during therapy; HBeAg and anti-HBe signs/symptoms of HBV relapse/exacerbation after discontinuation of therapy. Lactation: not known if distributed in breast milk, do not nurse

Pregnancy-Lactation

Pregnancy Category: B Lactation: not known if distributed in breast milk, do not nurse

Interactions

Increased risk of peripheral neuropathy when used with peginterferon alfa-2a.

Side Effects

Side effects of Telbivudine : >10% Fatigue (13%), Elevated serum creatinine kinase (11%); 1-10% Headache (10%), Cough (6%), Diarrhea (6%), Abdominal pain, upper (6%), Nausea (5%), Pharyngolaryngeal pain (5%), Arthralgia (4%), Pyrexia (4%), Rash (4%), Back pain (4%), Dizziness (4%), Abdominal pain (3%), Myalgia (3%), ALT increased (3%), Dyspepsia (3%), Insomnia (3%), Abdominal distension (3%), Pruritus (2%), Hepatitis B exacerbation (2%) <1% Peripheral neuropathy, Myopathy/myositis Potentially Fatal: Lactic acidosis and severe hepatomegaly.

Mode of Action

Telbivudine is a synthetic thymidine nucleoside analogue. It undergoes intracellular phosphorylation to form its active metabolite, telbivudine triphosphate. Telbivudine triphosphate inhibits hepatitis B viral DNA polymerase; enzyme inhibition blocks reverse transcriptase thus reducing viral DNA replication. It is used in the treatment of chronic hepatitis B infection.