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entecavir (Baraclude)

Indications: 1) chronic hepatitis B 2) treatment of HBV in the HIV/HBV co-infected adult patient who does not qualify for HAART 3) cirrhosis due to hepatitis B [4] * preferred over lamivudine - more effective than lamivudine (about 10%) [2] - with higher barrier to resistance than lamivudine [7] Dosage: 1) 0.5 mg PO QD 2) 1 mg PO QD (if lamivudine-resistant) 3) take on empty stomach (2 hours before or after meal) 4) optimal duration of treatment unknown Tabs: 0.5, 1 mg Oral solution: 0.5. mg/mL Pharmacokinetics: 1) food interferes with absorption 2) renal clearance Dosage adjustment in renal failure: creatinine clearance % standard dose 30-49 mL/min 50% 10-29 mL/min 30% < 10 mL/min 10% Monitor: - liver function tests periodically & for several months after discontinuation [6] Adverse effects: 1) headache 2) fatigue 3) nausea 4) dizziness 5) lactic acidosisis a concern 6) liver, lung, brain & skin tumors in rodents given high doses 7) case report in which a human immunodeficiency virus (HIV) variant containing the M184V resistance substitution was documented during Baraclude treatment for chronic hepatitis B virus (HBV) infection in an HIV/HBV co-infected patient who was not simultaneously receiving highly active antiretroviral therapy (HAART) [3] Drug interactions: - drugs that reduce renal function or compete for active tubular secretion may affect levels of either drug Mechanism of action: 1) guanosine nucleoside analog 2) inhibits hepatitis B viral DNA polymerase 3) resistance does not occur within 1 year [2]

Interactions

drug interactions

General

antiviral agent

Properties

MISC-INFO: pregnancy-category C

Database Correlations

PUBCHEM correlations

References

  1. Prescriber's Letter 12(5): 2005 New Drug: Baraclude (Entecavir) Detail-Document#: 210508 (subscription needed) http://www.prescribersletter.com
  2. Chang T-T et al, A comparison of entecavir and lamivudine for HBeAg-positive chronic hepatitis B. New Engl J Med 2006; 354:1001 PMID: 16525137 - Lai C0L et al, Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. New Engl J Med 2006; 354: 1011 PMID: 16525138 - Hoognagle JH, Hepatitis B - Preventable and now treatable. New Engl J Med 2006; 354:1074 PMID: 16525145
  3. FDA MedWatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Baraclude
  4. Shim JH et al Efficacy of entecavir in treatment-naive patients with hepatitis B virus-related decompensated cirrhosis. J Hepatol 2010 Feb; 52:176. PMID: 20006394
  5. http://www.baraclude.com
  6. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  7. NEJM Knowledge+ Complex Medical Care