Telbivudine

Oral
Chronic hepatitis B

ESRD: 600 mg 96 hrly, after dialysis session.

CrCl (mL/min)	Dosage
<30 (not requiring dialysis)	600 mg 72 hrly.
30-49	600 mg 48 hrly.

May be taken with or without food.

Hypersensitivity. Lactation. Concurrent use w/ peginterferon alfa-2a.

Patient w/ cirrhosis, hepatomegaly or other risk factors for liver disease. Renal impairment. Pregnancy.

Cough, dizziness, fatigue, GI effects (e.g. abdominal pain, diarrhoea, nausea, vomiting, dyspepsia), rash, arthralgia, myalgia, myopathy, malaise, back pain, nasopharyngitis, headache, flu or flu-like symptoms, insomnia; increased serum amylase, lipase, creatine phosphokinase, alanine aminotransferase levels; peripheral neuropathy, rhabdomyolysis.
Potentially Fatal: Lactic acidosis, severe hepatomegaly w/ steatosis.

PO: B

Monitor hepatic function (e.g. AST and ALT) periodically during therapy and for several mth following discontinuation of therapy; renal function; signs and symptoms of peripheral neuropathy or myopathy; serum creatine kinase; hepatitis B virus (HBV) DNA 3-6 mthly during therapy; HBeAg and anti-HBe signs/symptoms of HBV relapse/exacerbation after discontinuation of therapy.

Altered plasma concentration w/ drugs that affect renal function (e.g. aminoglycosides, loop diuretics, platinum compounds, vancomycin, amphotericin B). May increase risk of myopathy w/ other drugs associated w/ myopathy (e.g. azole antifungals, ciclosporin, corticosteroids, erythromycin, fibrates, HMG-CoA reductase inhibitors, penicillamine, zidovudine).
Potentially Fatal: Increased risk of peripheral neuropathy w/ peginterferon alfa-2a.

Description: Telbivudine is phosphorylated intracellularly to the active triphosphate form, which competes w/ thymidine 5'-triphosphate, the natural substrate of hepatitis B virus (HBV) reverse transcriptase, resulting to DNA chain termination and inhibition of HBV replication.
Pharmacokinetics:
Absorption: Absorbed from the GI tract. Time to peak plasma concentration: Approx 3 hr.
Distribution: Widely distributed into tissues. Plasma protein binding: Approx 3.3%.
Metabolism: Undergoes phosphorylation by cellular kinases to form the active metabolite, telmivudine-5'-triphosphate.
Excretion: Via urine, as unchanged drug. Terminal elimination half-life: 30-53.6 hr.

Source: National Center for Biotechnology Information. PubChem Database. Telbivudine, CID=159269, https://pubchem.ncbi.nlm.nih.gov/compound/Telbivudine (accessed on Jan. 23, 2020)

Store at 25°C.

Antivirals

J05AF11 - telbivudine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.

Anon. Telbivudine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 21/09/2015.

Anon. Telbivudine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/09/2015.

Buckingham R (ed). Telbivudine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/09/2015.

Tyzeka Film-Coated Tablet, Tyzeka Solution (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 21/09/2015.