Telbivudine
Pronunciation: (tel-BIV-ue-deen)Class: Antiviral
Trade Names:
Tyzeka
- Tablets 600 mg
- Solution, oral 100 mg per 5 mL
Pharmacology
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Telbivudine is phosphorylated by cellular kinases to the active triphosphate form. The telbivudine 5triphosphate is incorporated into viral DNA, causing DNA chain termination that results in inhibition of hepatitis B virus (HBV) replication.
Pharmacokinetics
Absorption
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.
Distribution
Plasma protein binding is low (3.3%). Vd exceeds total body water, suggesting wide distribution into tissues.
Metabolism
Metabolites were not detected.
Elimination
Terminal half-life is 40 to 49 h. Elimination is primarily as unchanged drug in the urine.
Special Populations
Renal Function ImpairmentDosage adjustment is recommended in patients with CrCl less than 50 mL/min.
Hepatic Function ImpairmentNo differences in pharmacokinetics based on hepatic function impairment.
ElderlyNo differences in pharmacokinetics based on age.
GenderNo differences in pharmacokinetics based on gender.
RaceNo differences in pharmacokinetics based on race.
Indications and Usage
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.
Contraindications
Standard considerations.
Dosage and Administration
Adults and Adolescents 16 yr of age and olderPO 600 mg once daily.
Renal Function ImpairmentAdults and Adolescents 16 yr of age and older
PO
CrCl 30 to 49 mL/min Tablets600 mg every 48 h.
Oral solution400 mg (20 mL) daily.
CrCl less than 30 mL/min (not requiring dialysis) Tablets600 mg every 72 h.
Oral solution200 mg (10 mL) once daily.
ESRD Tablets600 mg every 96 h.
General Advice
- May be taken without regard to meals.
Storage/Stability
Store at 59° to 86°F. Use oral solution within 2 mo after opening. Do not freeze.
Drug Interactions
Drugs that alter renal function (eg, cyclosporine, tacrolimus)May alter telbivudine plasma concentrations.
Pegylated interferon alfa-2aCoadministration may be associated with an increased risk of peripheral neuropathy occurrence and severity.
Laboratory Test Interactions
None well documented.
Adverse Reactions
CNS
Fatigue (13%); headache (10%); dizziness, pyrexia (4%); insomnia (3%); hypoesthesia, paresthesia (postmarketing).
Dermatologic
Rash (4%); pruritus (2%).
GI
Diarrhea, upper abdominal pain (6%); nausea (5%); abdominal distension, abdominal pain, dyspepsia (3%).
Hepatic
Hepatitis B exacerbation (2%).
Hematologic-Lymphatic
Neutropenia (2%).
Lab Tests
Elevated creatine kinase (13%); increased ALT (7%); increased AST (6%); increased lipase (2%).
Metabolic-Nutritional
Lactic acidosis (postmarketing).
Musculoskeletal
Arthralgia, back pain (4%); myalgia (3%); rhabdomyolysis (postmarketing).
Respiratory
Cough (6%); pharyngolaryngeal pain (5%).
Precautions
WarningsLactic 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. |
MonitorMonitor 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. |
Pregnancy
Category B .
Lactation
Undetermined.
Children
Safety and efficacy not established in children younger than 16 yr of age.
Elderly
Use with caution, taking into consideration the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Renal Function
Dose adjustment is recommended in patients with CrCl less than 50 mL/min.
Hepatic Function
No dosage adjustment is needed based on hepatic function impairment.
Liver transplant patients
Safety and efficacy not established.
Myopathy
Has been reported several weeks to months after starting therapy.
Peripheral neuropathy
Has been reported.
Overdosage
Symptoms
No adverse reactions were noted with dosages of up to 1,800 mg/day for 4 days.
Patient Information
- Advise patients to read the patient information leaflet before using product the first time and with each refill.
- Inform patients that they will be under the care of a health care provider while taking telbivudine and to discuss any new symptoms.
- Advise patients to promptly report unexplained muscle weakness, tenderness, or pain.
- Explain to patients that telbivudine is not a cure for hepatitis B and that the long-term benefits and relationship of treatment response to outcome are unknown.
- Inform patients that deterioration of liver disease may occur in some cases if treatment is discontinued, and to discuss any change in their regimen with a health care provider.
- Inform patients that treatment has not been shown to reduce HBV transmission through sexual contact.
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telbivudine - Includes detailed dosage instructions.
