entecavir (Baraclude)
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Indications
- chronic hepatitis B
- treatment of HBV in the HIV/HBV co-infected adult patient who does not qualify for HAART
- 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
- 0.5 mg PO QD
- 1 mg PO QD (if lamivudine-resistant)
- take on empty stomach (2 hours before or after meal)
- optimal duration of treatment unknown
Tabs: 0.5, 1 mg Oral solution: 0.5. mg/mL
Dosage adjustment in renal failure
Table
| creatinine clearance | % standard dose |
|---|---|
| 30-49 mL/min | 50% |
| 10-29 mL/min | 30% |
| < 10 mL/min | 10% |
Pharmacokinetics
- food interferes with absorption
- renal clearance
Monitor
- liver function tests periodically & for several months after discontinuation[6]
Adverse effects
- headache
- fatigue
- nausea
- dizziness
- lactic acidosisis a concern
- liver, lung, brain & skin tumors in rodents given high doses
- 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
- guanosine nucleoside analog
- inhibits hepatitis B viral DNA polymerase
- resistance does not occur within 1 year[2]
More general terms
References
- ↑ Prescriber's Letter 12(5): 2005 New Drug: Baraclude (Entecavir) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210508&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 2.0 2.1 2.2 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: https://www.ncbi.nlm.nih.gov/pubmed/16525137
Lai C0L et al, Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. New Engl J Med 2006; 354: 1011 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16525138
Hoognagle JH, Hepatitis B - Preventable and now treatable. New Engl J Med 2006; 354:1074 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16525145 - ↑ 3.0 3.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Baraclude
- ↑ 4.0 4.1 Shim JH et al Efficacy of entecavir in treatment-naive patients with hepatitis B virus-related decompensated cirrhosis. J Hepatol 2010 Feb; 52:176. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20006394
- ↑ <Internet> http://www.baraclude.com
- ↑ 6.0 6.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 NEJM Knowledge+ Complex Medical Care