Peringatan Keamanan

There is no information on intentional overdose of telbivudine, but one subject experienced an unintentional and asymptomatic overdose. Healthy subjects who received telbivudine doses up to 1800 mg/day for 4 days had no increase in or unexpected adverse events. A maximum tolerated dose for telbivudine has not been determined.

Telbivudine

DB01265

small molecule approved investigational

Deskripsi

Telbivudine is a synthetic thymidine nucleoside analog with specific activity against the hepatitis B virus. Telbivudine is orally administered, with good tolerance, lack of toxicity and no dose-limiting side effects.

Struktur Molekul 2D

Berat 242.2286
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 15 hours.
Volume Distribusi -
Klirens (Clearance) * 7.6 +/- 2.9 L/h [Normal renal function (Clcr>80 mL/min)] * 5.0 +/- 1.2 L/h [Mild renal function impairement (Clcr=50-80 mL/min)] * 2.6 +/- 1.2 L/h [Moderate renal function impairement (Clcr=30-49 mL/min)] * 0.7 +/- 0.4 L/h [Severe renal function impairement (Clcr<30 mL/min)]

Absorpsi

Absorbed following oral administration. Telbivudine absorption and exposure were unaffected when a single 600–mg dose was administered with a high–fat (~55 g), high–calorie (~950 kcal) meal.

Metabolisme

No metabolites of telbivudine were detected following administration of 14C–telbivudine in humans. Telbivudine is not a substrate, or inhibitor of the cytochrome P450 (CYP450) enzyme system.

Rute Eliminasi

Telbivudine is eliminated primarily by urinary excretion of unchanged drug.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

24 Data
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Telbivudine.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Telbivudine.
Ribavirin Ribavirin may increase the hepatotoxic activities of Telbivudine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Telbivudine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Telbivudine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Telbivudine.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Telbivudine.
Ganciclovir The risk or severity of cytopenia can be increased when Ganciclovir is combined with Telbivudine.
Valganciclovir The risk or severity of cytopenia can be increased when Valganciclovir is combined with Telbivudine.
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Telbivudine.
Bacillus calmette-guerin substrain tice live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Telbivudine.
Bacillus calmette-guerin substrain connaught live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Telbivudine.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Telbivudine.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Telbivudine.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Telbivudine.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Telbivudine.
Human adenovirus e serotype 4 strain cl-68578 antigen The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Telbivudine.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Telbivudine.
Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Telbivudine.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Telbivudine.
Bacillus calmette-guerin substrain russian BCG-I live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain russian BCG-I live antigen can be decreased when used in combination with Telbivudine.
Ropeginterferon alfa-2b The risk or severity of adverse effects can be increased when Ropeginterferon alfa-2b is combined with Telbivudine.
Chikungunya vaccine (live, attenuated) The therapeutic efficacy of Chikungunya vaccine (live, attenuated) can be decreased when used in combination with Telbivudine.
Smallpox (Vaccinia) Vaccine, Live The therapeutic efficacy of Smallpox (Vaccinia) Vaccine, Live can be decreased when used in combination with Telbivudine.

Target Protein

DNA
Protein P P

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18201580
    Matthews SJ: Telbivudine for the management of chronic hepatitis B virus infection. Clin Ther. 2007 Dec;29(12):2635-53. doi: 10.1016/j.clinthera.2007.12.032.
  • PMID: 18069753
    Amarapurkar DN: Telbivudine: a new treatment for chronic hepatitis B. World J Gastroenterol. 2007 Dec 14;13(46):6150-5.
  • PMID: 17724496
    Dusheiko G, Danta M: Telbivudine for the treatment of chronic hepatitis B. Drugs Today (Barc). 2007 May;43(5):293-304.
  • PMID: 17722961
    Keam SJ: Telbivudine. Drugs. 2007;67(13):1917-29.
  • PMID: 17477811
    Ruiz-Sancho A, Sheldon J, Soriano V: Telbivudine: a new option for the treatment of chronic hepatitis B. Expert Opin Biol Ther. 2007 May;7(5):751-61.
  • PMID: 15985003
    Marcellin P, Asselah T, Boyer N: Treatment of chronic hepatitis B. J Viral Hepat. 2005 Jul;12(4):333-45.
  • PMID: 15882124
    Han SH: Telbivudine: a new nucleoside analogue for the treatment of chronic hepatitis B. Expert Opin Investig Drugs. 2005 Apr;14(4):511-9.
  • PMID: 16981973
    Jones R, Nelson M: Novel anti-hepatitis B agents: A focus on telbivudine. Int J Clin Pract. 2006 Oct;60(10):1295-9.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Sebivo
    Tablet • 600 mg • Oral • Canada • Approved
  • Sebivo
    Tablet, film coated • 600 mg • Oral • EU
  • Sebivo
    Tablet, film coated • 600 mg • Oral • EU
  • Sebivo
    Solution • 20 mg/ml • Oral • EU
  • Tyzeka
    Tablet, film coated • 600 mg/1 • Oral • US • Approved
  • Tyzeka
    Solution • 20 mg/1mL • Oral • US • Approved
  • Tyzeka
    Tablet, film coated • 600 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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