TELBIVUDINE

TELBIVUDINE
(tel-bi'vu-deen)
Tyzeka
Classifications: antiretroviral agent; nucleoside reverse transcriptase inhibitor (nrti);
Therapeutic:antiretroviral
; nrti
Prototype: Lamivudine
Pregnancy Category: B

Availability

600 mg tablets

Action

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.

Therapeutic Effect

Telbivudine inhibits HBV viral DNA replication, reducing the viral load and preventing infection of new hepatocytes.

Uses

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).

Contraindications

Hypersensitivity to telbivudine; lactation. Safe use in children <16 y not established.

Cautious Use

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

Renal Impairment
Clcr ≥50 mL/min: no dosage adjustment
Clcr 30–49 mL/min: 600 mg q48h
Clcr <30 mL/min (not requiring dialysis): 600 mg q72h
Clcr <5–10 mL/min (ESRD): 600 mg q96h

Administration

Oral
  • 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, pyrexia. CNS: Dizziness, insomnia. 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: Rash.

Interactions

Drug: 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 and stavudine. Telbivudine is not antagonistic to anti-HIV activity of abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, or zidovudine.

Pharmacokinetics

Peak: 1–4 h. Distribution: Minimal protein binding; widely distributed in tissues. Elimination: Primarily unchanged in urine. Half-Life: 40–49 h.

Nursing Implications

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 enzymes.
  • 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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