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Entecavir (Baraclude)

Antiviral agent for chronic hepatitis B.

Trade name Baraclude

Entecavir is in the nucleoside reverse transcriptase inhibitors (NRTIs) family of medications.

 

 

Entecavir is a nucleoside analog, that belongs to a class of carbocyclic nucleosides and inhibits reverse transcription, DNA replication and transcription in the viral replication process. 

 

Entecavir reduces the amount of HBV in the blood by reducing its ability to multiply and infect new cells.

It is mainly used to treat chronic hepatitis B infection in adults and children two years and older with active viral replication and active disease.

It is also used to prevent HBV reinfection after liver transplant and to treat HIV patients infected with HBV. 

 

 

Other nucleoside and nucleotide analogues include lamivudine, telbivudine, adefovir dipivoxil, and tenofovir. 

 

It prevents the hepatitis B virus from multiplying by blocking reverse transcriptase.

It is weakly active against HIV, but is not recommended for use in HIV-HBV co-infected patients without a fully suppressive anti-HIV regimen.

Oral agent with about 70% bioavailability.

Protein binding 13%.

Metabolism Is negligible.

Half-life of 128-149 hours.

Renal excretion 62-73%.

An oral antiviral drug used in the treatment of hepatitis B virus (HBV) infection.

Prevents the hepatitis B virus from multiplying and reduces the amount of virus excretion.

Used to treat HIV patients infected with HBV, but it is not active against HIV.

Used prophylactically to prevent reactivation of HBV in HBV seropositive patients with malignancy and on chemotherapy.

Available as 0.5 mg and 1 mg tablets, and oral solution of 0.05 mg/mL

Administered on an empty stomach, at least 2 hours before a meal and 2 hours after a meal.

The majority of patients on  entecavir have little to no side effects.

Adverse reactions include: headache, fatigue, dizziness, nausea, diarrhea, dyspepsia, vomiting, somnolence and insomnia.

 

Common side effects include: headache, nausea, high blood sugar, and decreased kidney function.

 

 

Severe side effects include: hepatomegaly, high blood lactate levels, and liver inflammation if the medication is stopped.

 

 

Appears to be no harm from use during pregnancy, but no adequate and well-controlled studies exist in pregnant women.

 

Entecavir by mouth is effective.

Laboratory test abnormalities: increase in alanine transaminase (ALT), hematuria, glycosuria, and an increase in lipase.

Periodic monitoring of hepatic function and hematology are recommended.

May be associated with hematuria.

Monitoring of hepatic function and blood counts are recommended.

A guanosine analogue with marked activity against HBV DNA polymerase.

After 48 weeks of treatment 67% of patients with chronic hepatitis B with a positive hepatitis B e antigen and 90% negative for HbeAg had undetectable serum HBV DNA levels.

 

Entecavir is taken by mouth as a tablet or solution. 

 

 

Treatment is recommended for children more than 2 years old who weigh up to 30 kg. 

 

 

Entecavir is recommended on an empty stomach at least 2 hours before or after a meal.

 

 

Dose adjustments are recommended for people with decreased kidney function.

 

 

Baraclude 0.5 mg and 1 mg tablets.

 

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