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Drugs reference index «Telbivudine»

Telbivudine

Pronunciation: (tel-BIV-ue-deen)Class: Antiviral

Trade Names:Tyzeka- Tablets 600 mg- Solution, oral 100 mg per 5 mL

Sebivo (Canada)

Pharmacology

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 Impairment

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.

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 older

PO 600 mg once daily.

Renal Function ImpairmentAdults and Adolescents 16 yr of age and older

PO

CrCl 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.

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-2a

Coadministration 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

Warnings

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

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.

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.

Copyright © 2009 Wolters Kluwer Health.

  • Telbivudine MedFacts Consumer Leaflet (Wolters Kluwer)
  • telbivudine Advanced Consumer (Micromedex) - Includes Dosage Information
  • Tyzeka Prescribing Information (FDA)
  • Tyzeka Consumer Overview

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