telbivudine (Discontinued)

Brand and Other Names:Tyzeka
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Dosing & Uses

AdultPediatric

Dosage Forms & 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

Safety and efficacy not established

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Adverse 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

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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)

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Pregnancy & 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.

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Pharmacology

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)

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Images

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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.