Entecavir review

Entecavir is an antiviral oral drug used in treating patients with Hepatitis B infection. Entecavir is classified as a nucleoside analog which inhibits the actions of transcription, reverse transcription, and DNA replication in the process of viral replication. It has been reported that entecavir has been more efficacious in treating hepatitis B than its previous agents (adefovir and lamivudine).

Baraclude, the brand name of entecavir is indicated for administration in treating patients infected with Chronic Hepatitis B virus infections in adults. Entecavir is used in treating hepatitis B infections with strong evidence of active viral replications and evidences of either persisting elevations in serum ALT or AST aminotransferases or any histologically active disease.

Entecavir should be taken by a patient on an empty stomach, preferably 2 hours after a meal and two hour prior to the next meal.

The recommended dosage of entecavir for patients inexperienced with nucleoside treatment is at 0.5mg given once daily. For adults and adolescents with a history of Hepatitis B viremia while receiving treatments of lamivudine or any lamivudine or telbivudine resistance mutations, the recommended dose is 1mg once a day.

Entecavir/Baraclude oral solution has 0.05mg of entecavir per milliliter. Hence, 10mL of the solution provides 0.5mg of a dose while as a 20mL solution provides 1mg of entecavir.

The major reported side effects of entecavir use were the aggravation of hepatitis B after stopping drug treatment, and the development of lactic acidosis coupled with severe hepatomegaly with steatosis.

Side effects with lesser threats include shallowness of breath, swelling of gums, lips, face, throats, nausea, gastrointestinal pain such as diarrhea and gas pain, dark-colored urine and clay-colored stools. Skin rashes and even insomnia may also develop.

Discontinued use of entecavir may lead to aggravating the condition of Hepatitis B. It may also cause lactic acidosis, or the build up of lactic acid in the body, as evidenced by unusual muscle pain, severe tiredness, numbness and tingling of extremities. Entecavir use may also develop liver malfunction such as an enlarged liver or development of fat in the liver.

Entecavir has not been found to be contraindicated with any other drug. However, the discontinued use of entecavir may result in aggravation of the disease. For HIV infected patients, taking entecavir without the anti-HIV drugs may result in less potency of the anti-HIV drugs.

The co-administration of entecavir with other antiviral drugs has shown no clinical interactions. Caution should be exercised when co-administering Baraclude with drugs that may reduce kidney function.

Patients taking Baraclude should be under physician care, and should be closely monitored as well to prevent the exacerbation of the condition. Patients should be informed that entecavir does not reduce the risk of hepatitis B transmission.

It is imperative that patients who are offered entecavir therapy must first undergo HIV antibody testing before starting Baraclude. They should be informed that if they are HIV infected and is not receiving effective treatment, entecavir may increase the resistance of the body to HIV medication.

Entecavir has the following structural formula:

Chemical structure of entecavir

• Molecular formula of entecavir is C12H15N5O3
• Chemical IUPAC Name is 2-amino-9-[4-hydroxy-3-(hydroxymethyl)-2-methylidene-cyclopentyl]-3H-purin-6-one
• Molecular weight is 277.279 g/mol
Entecavir available : 0.5mg tablets and 1mg tablets

Brand name(s): Baraclude

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