Baraclude tabs 0.5mg #30

Baraclude user manual

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Composition

The coated tablet contains the active substance entecavir in two dosages: 0.5 mg and 1.0 mg.
Additional components: polysorbate, hypromellose, magnesium stearate, povidone, pink (1.0 mg) or white (0.5 mg) Opadry dye depending on the dosage, crospovidone, MCC, lactose monohydrate.

Form of issue

Baraclude 0.5 mg: tablets in a white film membrane, triangular in shape. On both sides are different markings: "1611" and "BMS".
Baraclude 1.0 mg: tablets in a pink film membrane. The form of the tablets is triangular. On both sides are different markings: "1612" and "BMS".

pharmachologic effect

Antiviral medication.
The active ingredient is an analog of guanosine nucleoside with a pronounced, selective, potent activity that manifests itself with respect to HBV polymerase - hepatitis B virus.
Entecavir is able to phosphorylate to form an active triphosphate, which has an intracellular half-life of 15 hours.
The concentration of entecavir triphosphate within the cell directly depends on the level of entecavir outside the cell, but no significant accumulation of active substance after the initial "plateau" index is recorded.
As a result of competition with its own, natural substrate, deoxyguanosine triphosphate inhibits the functional activity of the polymerase of the virus, acting immediately on 3 links:
    synthesizing a positive strand of HBV DNA;
    reverse transcription of the negative strand of pregenomic mRNA;
    priming of polymerase HBV.
Triphosphate entecavir is a rather weak inhibitor of polymerase of cellular DNA, and at high concentrations it does not adversely affect mitochondrial DNA synthesis.

Pharmacodynamics and pharmacokinetics

The active ingredient is absorbed from the digestive tract for a short time, and the maximum concentration is recorded after 0.5-1.5 hours.
After repeated application of the antiviral agent in a dose of 0.1-1.0 mg, a proportional increase in AUC, Cmax values ​​is recorded. The state of equilibrium is achieved on the 6-10th day of therapy in the treatment according to the scheme (1 time per day). Fatty food prevents the absorption of the active substance, reducing the AUC by 20%, and Cmax by 45%.
The drug penetrates well into the tissues of the body, with plasma proteins binds to 13%. The active ingredient is not an inhibitor, substrate or enzyme inducer in the P450 system.
For Baraclude, cumulation of entecavir is characteristic. Medication is excreted through the renal system through tubular secretion, glomerular filtration.

Indications for use Baraclude

The medication is intended for patients suffering from chronic viral hepatitis B with various lesions of the hepatic system:
    liver disease in the stage of decompensation;
    pathology of the liver in the stage of compensation in the presence of diagnosed viral replication, reliable signs of inflammation / fibrosis in the liver, with increased ALT, AST.

Contraindications

    individual intolerance;
    age restriction - up to 18 years;
    rare forms of hereditary lactose intolerance;
    glucose-galactose malabsorption;
    lack of lactase.

Side effects

In patients with decompensated form of lesions of the liver system, lactic acidosis is noted, which is characterized by:
    nausea;
    general weakness;
    pain in the abdomen, epigastrium;
    rapid breathing;
    weakness in the muscles;
    sharp weight loss;
    severe shortness of breath.

Other reactions:

    dyspepsia;
    diarrheal syndrome;
    vomiting;
    drowsiness;
    nausea;
    sleep disorders, insomnia;
    dizziness;
    skin rashes;
    fast fatiguability;
    anaphylactoid reactions;
    increased liver transaminases.
In addition, in persons suffering from decompensated liver damage, the following negative reactions were recorded:
    kidney failure (rare);
    a drop in the indicator of bicarbonate in the blood;
    increased bilirubin;
    an increase in lipase activity of 3 or more times;
    decrease in the number of platelets less than 50 thousand / mm3;
    increased ALT;
    a decrease in the albumin concentration of less than 2.5 g / dl.

Instructions for use Baraclude (Method and dosage)

Tablets are taken on an empty stomach, inside (a break between taking food and tablets - at least 2 hours).
With compensated lesions of the hepatic system, 0.5 mg once a day is prescribed. Dosage is doubled to 1.0 mg per day in diagnosing resistance to lamivudine (HCV viremia).
Persons with decompensated lesions of the hepatic system are prescribed 1.0 mg once a day. In case of renal failure, the dosage is selected taking into account the QC index.

Overdose

Data on cases of overdose by Baraclude are rather limited. Healthy volunteers who received the medication according to the scheme: 20 mg per day for 2 weeks, or once to 40 mg, no adverse reactions were noted.
It is recommended to conduct post-syndrome therapy depending on clinical manifestations.

Interaction

Because the active component is excreted mainly through the renal system, simultaneous therapy with medications that affect the functioning of the renal system and change the tubular secretion, can provoke an increase in the concentration of entecavir and these drugs.
Clinical interactions with lamivudine, tenofovir, adenovir are not registered.

Storage conditions

Transportation and storage of tablets should be carried out with a temperature of 15-25 degrees.
Shelf life - 2 years.

special instructions

The therapy with nucleoside analogues (including Baraclude) together with antiretroviral medications (and in monotherapy too) can cause lactic acidosis, expressed hepatomegaly, which is accompanied by steatosis.
A lethal outcome is possible. The risk factors include:
    hepatomegaly (increase in liver size);
    long-term therapy with nucleoside analogues;
    overweight;
    female.
With laboratory confirmation of lactic acidosis, the registration of a clinical picture of this condition, Baraclude therapy is canceled.
Against the background of antiviral therapy, there may be an exacerbation of hepatitis, which does not require special therapy. Rare, fatal complications are rare. Upon completion of treatment, control over the indicators of the functional state of the liver system is mandatory. A second course of antiviral therapy is conducted as needed.

Therapy of patients with hepatitis B and HIV infection

In the treatment of Baraclude, the lack of adequate antiretroviral therapy can lead to the formation of resistant strains of the human immunodeficiency virus. Entecavir is not recommended for HIV therapy, since its effectiveness in this direction has not been sufficiently studied.

Therapy of patients with hepatitis B, C, D

There are no reliable data on the efficacy of Baraclude in this group of patients.

Therapy of patients with lesions of the hepatic system in the stage of decompensation

Patients with diseases of the hepatic system of class C (Child-Pugh classification) are at high risk of developing severe adverse reactions from the liver. In such patients, the risk of lactic acidosis, hepatorenal syndrome increases significantly, which requires more careful monitoring (assessment of blood biochemical parameters, monitoring of renal function).

Therapy of patients resistant to lamivudine

It was noted that if there is a mutating resistance in the HCV virus to Lamivudine, the resistance to entecavir increases. That is why in resistant patients it is necessary to carry out constant monitoring of the viral load and to identify resistance mutations by means of examinations.

Therapy of patients with renal system pathology

A dosage adjustment is required.

Therapy of patients after liver transplantation

The effectiveness and safety of therapy with Entecavir in this group of citizens are unknown.
After liver transplantation, patients receive immunosuppressants (Tacrolimus, Cyclosporine), which can affect the functioning of the kidney system.
Treatment with Baraclude does not reduce the risk of HCV transmission, which requires special precautions.

Children

Pediatrics can only be used after the 18th birthday.

In pregnancy and lactation

Controlled, adequate studies in pregnant women were not conducted. Treatment Baraclude during pregnancy is possible only when assessing the possible risk to the fetus and the expected benefits for the mother.
It is recommended to stop breastfeeding during antiviral therapy.

Reviews about Baraclude

Patients leave positive responses about the drug, emphasizing its good tolerability. Reviews of Baraclude on the forums indicate the effectiveness of the drug in the therapy of viral hepatitis B with lesions of the hepatic system.
Patients note that only with prolonged treatment it is possible to achieve negative results of PCR. In some cases, patients reported insomnia at the beginning of antiviral therapy.