Dosing and uses of Tyzeka (telbivudine)
Adult dosage forms and strengths
tablet
- 600mg
Chronic Hepatitis B
September 30, 2016: Product discontinued; discontinuation of the product is not due to manufacturing, product quality, safety or efficacy concerns; generic equivalents are not available, but other therapeutic alternatives are available
600 mg PO qDay with or without food
Renal Impairment
CrCl 50 mL/min or higher: normal dose
CrCl 30-49 mL/min: 600 mg PO q48hr
CrCl <30 mL/min: 600 mg PO q72hr
ESRD: 600 mg PO q96hr
Pediatric dosage forms and strengths
Safety and efficacy not established
Tyzeka (telbivudine) adverse (side) effects
Well tolerated, most AEs comparable to lamivudine
>10%
Fatigue (13%)
Elevated serum creatinine kinase (11%); higher incidence than lamivudine
1-10%
Headache (10%)
Cough (6%)
Diarrhea (6%)
Abdominal pain, upper (6%)
Nausea (5%)
Pharyngolaryngeal pain (5%)
Arthralgia (4%)
Pyrexia (4%)
Rash (4%)
Back pain (4%)
Dizziness (4%)
Abdominal pain (3%)
Myalgia (3%)
ALT increased (3%)
Dyspepsia (3%)
Insomnia (3%)
Abdominal distension (3%)
Pruritus (2%)
Hepatitis B exacerbation (2%)
<1%
Peripheral neuropathy
Myopathy/myositis
Warnings
Black box warnings
Hepatitis B Treatment
- Severe acute exacerbations of hepatitis B reported in patients who have discontinued therapy for hepatitis B
- Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who discontinue therapy
- Resumption of therapy for hepatitis B may be warranted
Lactic Acidosis
- Lactic acidosis and severe hepatomegaly with steatosis (including fatal cases) reported with use of nucleoside analogues alone or in combination
Contraindications
Hypersensitivity
Coadministration with pegylated interferon alfa-2a is contraindicated because of increased risk of peripheral neuropathy
Cautions
Discontinuation may result in acute exacerbation of hepatitis B
Renal impairment
Risk of lactic acidosis, severe hepatomegaly with steatosis
Risk of peripheral neuropathy alone or in combination with pegylated interferon alfa-2a and other interferons (see Contraindications)
Pregnancy and lactation
Pregnancy category: B (to register pregnant patients, call 1-800-258-4263)
Lactation: not known if distributed in breast milk, do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Tyzeka (telbivudine)
Mechanism of action
Thymidine nucleoside analog; inhibits HBV DNA polymerase, which blocks reverse transcriptase activity and in turn reduces viral DNA replication
Pharmacokinetics
Half-life, elimination: 40-49 hr
Peak plasma time: 1-4 hr
Concentration: 3.7±1.25 mcg/mL
AUC: 26.1±7.2 mcg/mL
Trough: 0.2-0.3 mcg/mL
Protein bound: 3.3%
Renal clearance: 7.6±2.9 mL/min
Metabolism: None detected in studies
Excretion: urine 42% (passive diffusion)
Dialyzable: 23% (HD)
