(tel BI vyoo deen)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tyzeka: 600 mg [DSC]
Brand Names: U.S.
- Tyzeka [DSC]
- Antihepadnaviral, Reverse Transcriptase Inhibitor, Nucleoside (Anti-HBV)
Telbivudine, a synthetic thymidine nucleoside analogue (L-enantiomer of thymidine), is intracellularly phosphorylated to the active triphosphate form, which competes with the natural substrate, thymidine 5'-triphosphate, to inhibit hepatitis B viral DNA polymerase; enzyme inhibition blocks reverse transcriptase activity thereby reducing viral DNA replication.
Vd > total body water
No metabolites detected
Urine (~42% as unchanged drug)
Time to Peak
Terminal: 40-49 hours
Use: Labeled Indications
Treatment of chronic hepatitis B with evidence of viral replication and either persistent transaminase elevations or histologically-active disease
Concurrent use with peginterferon alfa-2a
Canadian labeling: Additional contraindications (not in U.S. labeling): Hypersensitivity to telbivudine or any component of the formulation
Chronic hepatitis B: Oral: 600 mg once daily.
Treatment duration (AASLD practice guidelines [Lok, 2009]):
Hepatitis Be antigen (HBeAg) positive chronic hepatitis: Treat ≥1 year until HBeAg seroconversion and undetectable serum HBV DNA; continue therapy for ≥6 months after HBeAg seroconversion.
HBeAg negative chronic hepatitis: Treat >1 year until hepatitis B surface antigen (HBsAg) clearance.
Note: Patients not achieving <2 log decrease in serum HBV DNA after at least 6 months of therapy should either receive additional treatment or be switched to an alternative therapy should either receive additional treatment or be switched to an alternative therapy.
Chronic hepatitis B: Oral: Adolescents ≥16 years: Refer to adult dosing.
Dosing: Renal Impairment
CrCl ≥50 mL/minute: No dosage adjustment is necessary.
CrCl 30-49 mL/minute: 600 mg every 48 hours
CrCl <30 mL/minute (not requiring dialysis): 600 mg every 72 hours
End-stage renal disease (ESRD): 600 mg every 96 hours
Hemodialysis: Administer after dialysis session
Dosing: Hepatic Impairment
No dosage adjustment necessary.
May be administered without regard to food.
May be taken without regard to food.
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Interferon Alfa-2b: May enhance the adverse/toxic effect of Telbivudine. Specifically, the risk for peripheral neuropathy may be increased. Avoid combination
Peginterferon Alfa-2a: May enhance the adverse/toxic effect of Telbivudine. Specifically, the risk for peripheral neuropathy may be increased. Avoid combination
Peginterferon Alfa-2b: May enhance the adverse/toxic effect of Telbivudine. Specifically, the risk for peripheral neuropathy may be increased. Avoid combination
Central nervous system: Fatigue (13%)
Neuromuscular & skeletal: Increased creatine phosphokinase (79%; grades 3/4: 16%, most asymptomatic and transient)
1% to 10%:
Central nervous system: Headache (10%), dizziness (4%), fever (4%), insomnia (3%)
Dermatologic: Skin rash (4%), pruritus (2%)
Endocrine & metabolic: Increased serum lipase (grades 3/4: 2%)
Gastrointestinal: Diarrhea (6%), abdominal pain (3% to 6%), nausea (5%), abdominal distension (3%), dyspepsia (3%)
Hematologic & oncologic: Neutropenia (grades 3/4: 2%)
Hepatic: Increased serum ALT (grades 3/4: 5% to 7%), increased serum AST (grades 3/4: 6%)
Infection: Exacerbation of hepatitis B (2%)
Neuromuscular & skeletal: Arthralgia (4%), back pain (4%), myalgia (3%)
Respiratory: Cough (6%), pharyngolaryngeal pain (5%)
<1% (Limited to important or life-threatening): Hepatomegaly, hyperbilirubinemia, hypoesthesia, increased amylase, lactic acidosis, liver steatosis, myopathy, myositis, paresthesia, peripheral neuropathy, rhabdomyolysis, thrombocytopenia
Concerns related to adverse effects:
• Lactic acidosis/hepatomegaly: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis).
• Myopathy: Use has been associated with myopathy (unexplained muscle aches and/or muscle weakness in conjunction with serum creatine kinase increases) several weeks to months after initiation of telbivudine; interrupt therapy if myopathy is suspected and discontinue therapy if myopathy is diagnosed. Patients taking concomitant medications associated with myopathy should be monitored closely.
• Peripheral neuropathy: May occur alone or in combination with pegylated interferon alfa-2a (concurrent use is contraindicated) or possibly other interferons. Symptoms have been observed within 3 months after initiation of therapy. Interrupt treatment for suspected peripheral neuropathy and discontinue if confirmed; symptoms may be reversible with discontinuation.
• Chronic hepatitis B: [U.S. Boxed Warning]: Severe, acute exacerbation of hepatitis B may occur upon discontinuation. Monitor liver function several months after stopping treatment; reinitiation of antihepatitis B therapy may be required.
• Human immunodeficiency virus: Telbivudine does not exhibit any clinically-relevant activity against HIV type 1.
• Renal impairment: Use caution in patients with moderate-to-severe renal dysfunction and end stage renal disease (ESRD); dosing adjustment required (CrCl <50 mL/minute).
• African-American or Hispanic patients: Safety and efficacy have not been established in Black/African-American or Hispanic patients.
• Coinfections: Safety and efficacy have not been studied in patients coinfected with HIV, hepatitis C virus (HCV) or hepatitis D virus (HDV).
• Liver transplant recipients: Safety and efficacy in liver transplant patients have not been established; monitor renal function in patients receiving concurrent therapy of cyclosporine or tacrolimus.
• Appropriate Use: Not recommended as first-line therapy of chronic HBV due to high rate of resistance; use may be appropriate in short-term treatment of acute HBV (Lok, 2009).
• Resistance: Cross-resistance among hepatitis B antivirals may develop; use caution in patients failing previous lamivudine therapy.
LFTs (eg, AST and ALT) periodically during therapy and for several months following discontinuation of therapy; renal function prior to initiation and periodically during treatment; signs and symptoms of peripheral neuropathy (eg, weakness, paresthesia, leg pain) or myopathy (eg, unexplained muscle pain, tenderness or weakness); serum creatine kinase; HBV DNA (every 3-6 months during therapy); HBeAg and anti-HBe signs/symptoms of HBV relapse/exacerbation after discontinuation of therapy.
Pregnancy Risk Factor
Adverse events were not observed in animal reproduction studies. Based on available information, telbivudine may be used to treat hepatitis b during pregnancy (Liu, 2013). Health professionals are encouraged to contact the antiretroviral pregnancy registry to monitor outcomes of pregnant women exposed to antiretroviral medications (1-800-258-4263).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience abdominal pain, headache, loss of strength and energy, joint pain, insomnia, back pain, dizziness, cough, pharyngitis, nausea, or diarrhea. Have patient report immediately to prescriber signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of lactic acidosis (fast breathing, tachycardia, abnormal heartbeat, vomiting, fatigue, shortness of breath, severe loss of strength and energy, severe dizziness, feeling cold, or muscle pain or cramps), burning or numbness feeling, change in balance, abnormal gait, urinary retention, change in amount of urine passed, abdominal edema, muscle pain, or muscle weakness (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: nucleoside reverse transcriptase inhibitors (NRTIs)
Other brands: Tyzeka