Classifications: antiretroviral agent; nucleoside reverse transcriptase inhibitor (nrti); Therapeutic:antiretroviral; nrti
Pregnancy Category: B
600 mg tablets
Telbivudine is a nucleoside analogue with activity against hepatitis B virus (HBV) DNA polymerase. Its metabolite inhibits
HBV DNA polymerase (reverse transcriptase) by competing with the natural nucleoside substrate. Incorporation of the metabolite
of telbivudine into HBV viral DNA causes DNA chain termination, resulting in inhibition of HBV replication.
Telbivudine inhibits HBV viral DNA replication, reducing the viral load and preventing infection of new hepatocytes.
Treatment of chronic hepatitis B in patients with evidence of either histologically active disease or evidence of persistent
elevations in serum aminotransferases (ALT or AST).
Hypersensitivity to telbivudine; lactation. Safe use in children <16 y not established.
Moderate to severe renal impairment, hemodialysis; alcoholism; obesity in females; risk of hepatic disease; individuals
with organ transplants; older adults; pregnancy (category B).
Route & Dosage
|Chronic Hepatitis B
Adults/Adolescents (≥16 y): PO 600 mg/d
Clcr ≥50 mL/min: no dosage adjustment
Clcr 3049 mL/min: 600 mg q48h
Clcr <30 mL/min (not requiring dialysis): 600 mg q72h
Clcr <510 mL/min (ESRD): 600 mg q96h
- May be given without regard to food.
- Note dose adjustment for Clcr <50 mL/min.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole: Fatigue and malaise, headache, influenza-like syndrome, post-procedural pain,
. GI: Abdominal pain, diarrhea and loose stools,
dyspepsia, nausea, vomiting. Metabolic: Increased CPK levels, lactic acidosis and severe hepatomegaly with steatosis. Musculoskeletal:
Arthralgia, back pain, myalgia. Respiratory: Cough, nasopharyngitis,
pharyngolaryngeal pain, upper respiratory tract infection. Skin:
Coadministration with drugs that alter renal function may alter plasma concentrations of telbivudine. Anti-HBV activity of
telbivudine is additive with adefovir
and is not antagonized by the hiv nrtis didanosine
Telbivudine is not antagonistic to anti-HIV activity of abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir,
14 h. Distribution:
Minimal protein binding; widely distributed in tissues. Elimination:
Primarily unchanged in urine. Half-Life:
Assessment & Drug Effects
- Monitor for and report S&S of lactic acidosis (e.g., anorexia, nausea, vomiting, bloating, abdominal pain, malaise, tachycardia
or other arrhythmia, and difficulty in breathing).
- Withhold drug and notify physician of any of the following: suspected lactic acidosis, steatosis, or markedly elevated liver
- Lab tests: LFTs during and for several months after discontinuation of telbivudine; periodic serum bicarbonate.
Patient & Family Education
- Follow directions for taking the drug (see Administration).
- Avoid all alcohol consumption while taking this drug.
- Report any of the following to a health care provider: loss of appetite, nausea and vomiting, abdominal pain, palpitations,
or difficulty breathing.