Telbivudine

Trade Names:
Tyzeka
- Tablets 600 mg

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. Steady state is achieved after approximately 5 to 7 days and occurred between 1 and 4 h.

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 t _½ is 40 to 49 h. Elimination is primarily as unchanged drug in the urine.

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

PO 600 mg once daily.

PO CrCl 30 to 49 mL/min: 600 mg once every 48 h. CrCl less than 30 (not requiring dialysis): 600 mg once every 72 h. End-stage renal disease: 600 mg once every 96 h.

Storage/Stability

Store in original container at 59° to 86°F.

Drug Interactions

May alter telbivudine plasma concentrations.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Fatigue, malaise (12%); headache (11%); dizziness, pyrexia (4%); insomnia (3%).

Dermatologic

Rash (4%).

EENT

Nasopharyngitis (11%); pharyngolaryngeal pain (5%).

GI

Diarrhea/loose stools, nausea, vomiting (7%); dyspepsia (3%).

Hematologic-Lymphatic

Neutropenia (2%); thrombocytopenia (less than 1%).

Lab Tests

Increased CPK (9%); increased ALT (4%); increased AST (3%); elevated lipase (2%).

Musculoskeletal

Arthralgia, back pain (4%); myalgia (3%).

Respiratory

Upper respiratory tract infection (14%); cough (7%).

Miscellaneous

Abdominal pain (12%); influenza and influenza-like symptoms, postprocedural pain (7%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 16 yr of age.

Elderly

Use with caution, considering 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.

Exacerbation of hepatitis

Severe acute exacerbations of hepatitis B have occurred after discontinuation of anti-hepatitis B therapy.

Lamivudine-resistant hepatitis B

No adequate studies are available for telbivudine treatment of patients with established lamivudine-resistant HBV infection.

Liver transplant patients

Safety and efficacy of telbivudine in liver transplant patients not established.

Myopathy

Has been reported several weeks to months after starting therapy.

Overdosage

Symptoms

No adverse reactions were noted with doses 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 changes 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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