Trade names Baraclude MedlinePlus a605028 CAS ID 142217-69-4 | AHFS/Drugs.com Monograph Molar mass 277.279 g/mol | |
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Pronunciation /ɛnˈtɛkəvɪər/ en-TEK-a-vir or en-TE-ka-veer License data EU EMA: BaracludeUS FDA: Entecavir Pregnancycategory AU: B3US: C (Risk not ruled out) | ||
How to pronounce entecavir baraclude memorizing pharmacology flashcard
Entecavir (ETV), sold under the brand name Baraclude, is an antiviral medication used in the treatment of hepatitis B virus (HBV) infection. In those with both HIV/AIDS and HBV antiretroviral medication should also be used. Entecavir is taken by mouth as a tablet or solution.
Contents
- How to pronounce entecavir baraclude memorizing pharmacology flashcard
- Medical uses
- Pregnancy and breastfeeding
- Side effects
- Mechanism of action
- Administration
- History
- Patent information
- References
Common side effects include headache, nausea, high blood sugar, and decreased kidney function. Severe side effects include enlargement of the liver, high blood lactate levels, and liver inflammation if the medication is stopped. While there appears to be no harm from use during pregnancy, this use has not been well studied. Entecavir is in the nucleoside reverse transcriptase inhibitors (NRTIs) family of medications. It prevents the hepatitis B virus from multiplying by blocking reverse transcriptase.
Entecavir was approved for medical use in 2005. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. In the United States as of 2015 it is not available as a generic medication. The wholesale price is about 392 USD for a typical month supply as of 2016 in the United States.
Medical uses
Entecavir is mainly used to treat chronic hepatitis B infection in adults and children 2 years and older with active viral replication and evidence of active disease with elevations in liver enzymes. It is also used to prevent HBV reinfection after liver transplant and to treat HIV patients infected with HBV. Entecavir is weakly active against HIV, but is not recommended for use in HIV-HBV co-infected patients without a fully suppressive anti-HIV regimen as it may select for resistance to lamivudine and emtricitabine in HIV.
The efficacy of entecavir has been studied in several randomized, double-blind, multicentre trials. Entecavir by mouth is effective and generally well tolerated treatment.
Pregnancy and breastfeeding
It is considered pregnancy category C in the United States, and currently no adequate and well-controlled studies exist in pregnant women.
Side effects
The majority of people who use entecavir have little to no side effects. The most common side effects include headache, fatigue, dizziness, and nausea. Less common effects include trouble sleeping and gastrointestinal symptoms such as sour stomach, diarrhea, and vomiting.
Serious side effects from entecavir include lactic acidosis, liver problems, liver enlargement, and fat in the liver.
Laboratory tests may show an increase in alanine transaminase (ALT), hematuria, glycosuria, and an increase in lipase. Periodic monitoring of hepatic function and hematology are recommended.
Mechanism of action
Entecavir is a nucleoside analog, or more specifically, a deoxyguanosine analogue that belongs to a class of carbocyclic nucleosides and inhibits reverse transcription, DNA replication and transcription in the viral replication process. Other nucleoside and nucleotide analogues include lamivudine, telbivudine, adefovir dipivoxil, and tenofovir.
Entecavir reduces the amount of HBV in the blood by reducing its ability to multiply and infect new cells.
Administration
Entecavir is take by mouth as a tablet or solution. Doses are based on a person's weight. The solution is recommended for children greater than 2 years old that weigh up to 30 kg. Entecavir is recommended on an empty stomach at least 2 hours before or after a meal, generally at the same time everyday. It is not used in children younger than 2 years old. Dose adjustments are also recommended for people with decreased kidney function.
History
Patent information
Bristol-Myers Squibb was the original patent holder for Baraclude, the brand name of entecavir in the US and Canada. The drug patent expiration for Baraclude was in 2015. On August 26, 2014, Teva Pharmaceuticals USA gained FDA approval for generic equivalents of Baraclude 0.5 mg and 1 mg tablets; Hetero Labs received such approval on August 21, 2015; and Aurobindo Pharma on August 26, 2015.