Trade Names:Tyzeka- Tablets 600 mg- Solution, oral 100 mg per 5 mLSebivo (Canada)
Telbivudine is phosphorylated by cellular kinases to the active triphosphate form. The telbivudine 5î“¸triphosphate is incorporated into viral DNA, causing DNA chain termination that results in inhibition of hepatitis B virus (HBV) replication.
C max is approximately 3.7 mcg/mL and occurs between 1 and 4 h. Steady state is achieved after approximately 5 to 7 days.
Plasma protein binding is low (3.3%). Vd exceeds total body water, suggesting wide distribution into tissues.
Metabolites were not detected.
Terminal half-life is 40 to 49 h. Elimination is primarily as unchanged drug in the urine.
Dosage adjustment is recommended in patients with CrCl less than 50 mL/min.Hepatic Function Impairment
No differences in pharmacokinetics based on hepatic function impairment.Elderly
No differences in pharmacokinetics based on age.Gender
No differences in pharmacokinetics based on gender.Race
No differences in pharmacokinetics based on race.
Treatment of chronic hepatitis B in adults with evidence of viral replication and either evidence of persistent elevations in serum aminotransaminases or histologically active disease.
PO 600 mg once daily.Renal Function ImpairmentAdults and Adolescents 16 yr of age and older
POCrCl 30 to 49 mL/min Tablets
600 mg every 48 h.Oral solution
400 mg (20 mL) daily.CrCl less than 30 mL/min (not requiring dialysis) Tablets
600 mg every 72 h.Oral solution
200 mg (10 mL) once daily.ESRD Tablets
600 mg every 96 h.
Store at 59° to 86°F. Use oral solution within 2 mo after opening. Do not freeze.
May alter telbivudine plasma concentrations.Pegylated interferon alfa-2a
Coadministration may be associated with an increased risk of peripheral neuropathy occurrence and severity.
None well documented.
Fatigue (13%); headache (10%); dizziness, pyrexia (4%); insomnia (3%); hypoesthesia, paresthesia (postmarketing).
Rash (4%); pruritus (2%).
Diarrhea, upper abdominal pain (6%); nausea (5%); abdominal distension, abdominal pain, dyspepsia (3%).
Hepatitis B exacerbation (2%).
Elevated creatine kinase (13%); increased ALT (7%); increased AST (6%); increased lipase (2%).
Lactic acidosis (postmarketing).
Arthralgia, back pain (4%); myalgia (3%); rhabdomyolysis (postmarketing).
Cough (6%); pharyngolaryngeal pain (5%).
Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with use of nucleoside analogs alone or in combination with antiretrovirals. Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued anti–hepatitis B therapy, including telbivudine.
Monitor hepatic function for at least several months in patients who discontinue anti–hepatitis B therapy. Monitor for signs and symptoms of unexplained muscle pain, tenderness, or weakness. Monitor renal function in elderly patients and in patients taking drugs that may alter renal function.
Category B .
Safety and efficacy not established in children younger than 16 yr of age.
Use with caution, taking into consideration the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Dose adjustment is recommended in patients with CrCl less than 50 mL/min.
No dosage adjustment is needed based on hepatic function impairment.
Safety and efficacy not established.
Has been reported several weeks to months after starting therapy.
Has been reported.
No adverse reactions were noted with dosages of up to 1,800 mg/day for 4 days.
Copyright © 2009 Wolters Kluwer Health.