Baraklyud, 30 pcs., 1 mg, film-coated tablets

pharmachologic effect

Antiviral medication.

The active component is an analogue of guanosine nucleoside with pronounced, selective, powerful activity, which manifests itself against HBV polymerase - hepatitis B virus .

Entecavir is capable of phosphorylation to form an active triphosphate, which has an intracellular half-life of 15 hours.

The concentration of entecavir triphosphate inside the cell directly depends on the level of entecavir outside the cell, but no significant accumulation of the active substance is recorded after the initial plateau.

As a result of competition with its own natural substrate, desoquiguanosine triphosphate suppresses the functional activity of the virus polymerase, affecting 3 links at once:

• synthesis of the positive strand of HBV DNA;
• reverse transcription of negative strand pregenomic mRNA;
• HBV polymerase priming.

Entecavir triphosphate is a fairly weak inhibitor of cellular DNA polymerases, and at high concentrations does not have a negative effect on mitochondrial DNA synthesis.

Contraindications

• lactose intolerance, glucose-galactose malabsorption, lactase deficiency;
• age under 18 years;
• lactation (or feeding should be stopped);
• hypersensitivity to the components of Baraklud.

With caution: pregnancy.

Pharmacodynamics and pharmacokinetics

The active component is absorbed from the digestive tract within a short period of time, and the maximum concentration is recorded after 0.5-1.5 hours.

After repeated use of the antiviral agent at a dose of 0.1-1.0 mg, a proportional increase in AUC and Cmax is recorded. A state of equilibrium is achieved on days 6-10 of therapy when treated according to the treatment regimen (once a day). Fatty foods interfere with the absorption of the active substance, reducing AUC by 20% and Cmax by 45%.

The drug penetrates well into body tissues and binds to plasma proteins by 13%. The active substance is not an inhibitor, substrate or enzyme inducer in the P450 system.

Baraklyuda is characterized by the accumulation of entecavir. The medication is excreted through the renal system by tubular secretion and glomerular filtration .

Compound

Active substance: entecavir, 1 tablet – 0.5 or 1 mg.

Auxiliary components of Baraclude tablets:

• microcrystalline cellulose,
• crospovidone,
• magnesium stearate,
• povidone,
• lactose monohydrate,
• dye: in tablets 0.5 mg – Opadry white (macrogol 400, hypromellose 3cP, hypromellose 6cP, titanium dioxide, polysorbate 80), in tablets 1 mg – Opadry pink (titanium dioxide, macrogol 400, hypromellose 6cP, iron dye red oxide E172 , CFR21).

Side effects

In patients with a decompensated form of damage to the hepatic system, lactic acidosis , which is characterized by:

• nausea;
• general weakness;
• pain in the abdominal cavity, epigastrium;
• rapid breathing;
• muscle weakness;
• sudden weight loss;
• severe shortness of breath.

Other reactions:

• dyspepsia;
• diarrhea syndrome;
• vomit;
• drowsiness;
• nausea;
• sleep disorders, insomnia;
• dizziness;
• skin rashes;
• fast fatiguability;
• anaphylactoid reactions;
• increased liver transaminases.

Additionally, the following negative reactions were recorded in persons suffering from decompensated liver damage:

• renal failure (rare);
• a drop in bicarbonate levels in the blood;
• increased bilirubin ;
• increase in lipase activity by 3 or more times;
• decrease in platelet less than 50 thousand/mm3;
• increased ALT;
• decrease in albumin concentration less than 2.5 g/dl.

Side effects

1. From the digestive system, the patient may feel the addition of dyspeptic manifestations, for example, there will be complaints of nausea, vomiting is possible, and loose stools are also noted.
2. On the part of the nervous system, drowsiness develops, a headache occurs, there may be fatigue, and dizziness is also possible.
3. In addition, the manifestation of anaphylactoid reactions on the part of the body cannot be ruled out. Dermatological side effects will include rashes and alopecia.
4. On the metabolic side: with a decompensated lesion, a clinical picture of lactic acidosis may develop, which will be expressed by the following symptoms: the patient will notice general fatigue, nausea, vomiting, and abdominal pain is possible. In addition, there is a sudden decrease in body weight, shortness of breath is noted, breathing becomes more frequent, and muscle weakness is also possible.
5. Laboratory changes: decreased bicarbonate concentrations, increased ALT and bilirubin, and albumin concentrations.

Instructions for use Baraklyud (Method and dosage)

The tablets are taken on an empty stomach, orally (the break between meals and tablets is at least 2 hours).

In case of compensated damage to the hepatic system, 0.5 mg is prescribed once a day. The dosage is doubled to 1.0 mg per day if resistance to lamivudine ( HCV viremia ) is diagnosed.

Persons with decompensated lesions of the hepatic system are prescribed 1.0 mg 1 time per day. In case of renal failure, the dosage is selected taking into account the QC indicator.

Release form

The dosage form of Baraklyuda is film-coated tablets:

• 0.5 mg: triangular, off-white or white in color, with “1611” on one side and BMS on the other;
• 1 mg: Triangular shaped, pink in color, marked “1612” on one side and BMS on the other.

Tablets are packaged in 10 pcs. in blisters, 3 blisters are packed in a cardboard box.

special instructions

Therapy with nucleoside analogues (including Baraklud) together with antiretroviral medications (and in monotherapy too) can cause lactic acidosis, severe hepatomegaly, which is accompanied by steatosis.

Possible death. Risk factors include:

• hepatomegaly (increase in liver size);
• long-term therapy with nucleoside analogues;
• overweight;
• female.

With laboratory confirmation of lactic acidosis and registration of the clinical picture of this condition, Baraclude therapy is canceled.

Against the background of antiviral therapy, exacerbation of hepatitis is possible, which does not require special therapy. Severe, fatal complications rarely occur. Upon completion of treatment, monitoring of indicators of the functional state of the hepatic system is mandatory. A repeated course of antiviral therapy is carried out as needed.

Treatment of patients suffering from hepatitis B and HIV infection

When treated with Baraklud, 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 area has not been sufficiently studied.

Treatment of patients with hepatitis B, C, D

There are no reliable data on the effectiveness of Baraklud in the treatment of 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 class C (Child-Pugh classification) have a high risk of developing severe negative reactions from the liver. hepatorenal syndrome increases significantly , which requires more careful monitoring (assessment of biochemical blood parameters, monitoring the functioning of the renal system).

Treatment of patients resistant to lamivudine

It has been noted that in the presence of mutating resistance to Lamivudine in the HCV virus, resistance to entecavir increases. That is why in resistant patients it is necessary to constantly monitor the viral load and identify resistance mutations through examinations.

Treatment of patients with pathology of the renal system

Correction of the dosage regimen is required.

Treatment of patients after liver transplantation

The effectiveness and safety of Entecavir therapy in this group of citizens is unknown.

After a liver transplant, patients receive immunosuppressants ( Tacrolimus, Cyclosporine ), which can affect the functioning of the renal system.

Treatment with Baraklud does not reduce the risk of HCV transmission, which requires special precautions.

Indications

Indications for treatment with Baraklud are the following types of hepatitis B:

• acute with prolonged or severe course;
• chronic newly diagnosed;
• treated without sufficient effect with other drugs;
• in combination with delta infection;
• in combination with HIV infection.

The specific regimen for using Baraklud, the duration of its use, the possibility and need for combination with other antiviral drugs can only be determined by a specialist (infectious disease specialist or gastroenterologist).

Analogues of Baraklyuda

Level 4 ATX code matches:
Zeffix

Zidovudine

Lamivudine

Structural analogues have not been developed. Medicines with similar pharmacological effects:

• Alfarekin;
• Pegasis;
• Intron A.

Drug interactions

With the simultaneous use of drugs that compete at the level of tubular secretion or cause renal dysfunction, an increase in the serum concentration of entecavir or these drugs is possible.

The interaction of entecavir with other drugs that affect renal function or are excreted by the kidneys has not been studied. When co-prescribing such drugs with entecavir, the patient should be under constant medical supervision.

Overdose

There is no complete data on the characteristics of an overdose of Baraklud. The drug developers noted that patients who regularly took the drug for two weeks in an amount not exceeding 20 mg per day did not experience any adverse effects. The same result was observed in people after a single dose of 40 mg.

But if signs of intoxication with Baraclude still appear, then the medication should be discontinued and urgently consult a doctor. Measures to eliminate an overdose will depend on the nature of the painful symptoms.

Analogs

Only a doctor can replace a prescription drug with another medication with an effect identical to Baraclude.

Abacavir-ABC

"Medicine Technology" (Russia)

Cost: (60 pcs.) – 3897 rub.

The drug is included in the list of vital medications and has a strong antiviral effect. Not used in monotherapy, intended exclusively for complex therapeutic measures.

The therapeutic effect is provided by the active component - abacavir, which has a strong antiviral effect. The drug should not be taken in case of intolerance to the constituent components, liver pathologies, children under 3 years of age, pregnancy and breastfeeding. Abacavir is considered a safe drug and is generally well tolerated, but if an allergic reaction occurs, it can be life-threatening.

The drug is produced in the form of coated tablets. Packaged in blister packs of 10 pieces.

Pros:

• Helps well
• Strong action.

Flaws:

• During treatment, intolerance may develop
• Increases the risk of heart attacks.

Allokin-alpha

RKNPK RosMedTechnologies (RF)

Cost: (3 pcs.) – 3852 rub., (6 pcs.) – 7477 rub.

A drug with antiviral and immunomodulatory effects. Indicated for the treatment of acute herpes infection, diseases caused by viral or bacterial pathogens, exacerbation of hepatitis B, influenza type A and B.

The active substance is alloferon (or oligopeptide). Activates the body's production of interferon and at the same time stimulates the activity of natural killer cells of the immune system. Thanks to this action, there is an accelerated recognition of infection, identification of infected cells and their destruction.

Allokin-alpha is not prescribed in the presence of hypersensitivity of the body, pregnancy and lactation, age less than 18 years, autoimmune pathologies.

The drug is produced in the form of a powder or lyophilisate for the preparation of injection solutions containing 10 and 100 mcg of active substance. Packaged in ampoules of 1 g. Injections are administered under the skin.

Pros:

• Combined action
• Pronounced antiviral effect.

Flaws:

• May cause exacerbation of herpes rashes
• High price.

Mode of application

The instructions for use recommend drinking Baraklyud on an empty stomach: the interval between taking tablets and food should be at least 2-2.5 hours (before or after a meal).

Cost: 11674 rub.

The dosage is calculated in accordance with the indications and diagnosis of the patient. The daily amount of the drug recommended by the manufacturer is 500 mcg. For patients with resistance to the substance lamivudine, the dosage is doubled, it is 1000 mcg.

Patients with kidney pathologies need to adjust the daily dose of drugs.

The duration of the course of Baraklyuda depends on the severity of the diagnosis and the individual indications of the patient - it takes from one year to several years. If necessary, a repeat treatment regimen is prescribed.

During pregnancy and breastfeeding

There have been no comprehensive studies of the effects of drugs on the body during pregnancy. For this reason, the use of Baraclude is not recommended. Prescription is possible only in case of a threat to health and the impossibility of replacing it with another means.

There is also no information about whether entecavir passes into breast milk or not. Breastfeeding should be discontinued during the course of Baraklud.

Precautionary measures

Due to the fact that Baraclude tablets are an antiviral agent, they are not recommended to be combined with alcoholic beverages or alcohol-containing drugs. Otherwise, there is a multiple increase in side effects, which negatively affects the functioning of the central nervous system and increases the load on the liver.

It has been noted that after stopping the use of antiviral drugs (including entecavir), there is an exacerbation of hepatitis. Most often, the acute stage goes away on its own, without any therapy. But the development of life-threatening conditions, even the death of patients, also occurs. So far, scientists and doctors have not been able to decipher the background of this phenomenon. To avoid fatal developments, after completing the course of Barakluda, it is necessary to periodically check the functioning of the liver in order to take timely measures.

Taking the medicine does not affect the possibility of infection with the causative agent of hepatitis, so it is necessary to take the necessary precautions.

Pharmacological properties

The antiviral medication contains the main substance entecavir. Once in the human body, it is converted into active triphosphate. It has a long half-life. This is a competitor of another nucleoside in terms of viral polymerase activity.

The mechanism of the antiviral action of the main substance of entecavir is to stop the emergence of new copies of the virus. It remains in tissues for a long time. Due to the long half-life of the active ingredient, the tablets can be taken once a day. The main advantage for patients with an inflamed liver is the absence of biotransformation in the affected organ. Metabolites of the substance are excreted from the body by the kidneys.

Baraklyud 1 mg No. 30 tablets

Indications for the drug Baraklyud

Chronic hepatitis B in adults with:

• compensated liver damage and the presence of viral replication, increased levels of serum transaminases (ALT or AST) and histological signs of inflammation in the liver and/or fibrosis;
• decompensated liver damage.

Contraindications

• hypersensitivity to entecavir or any other component of the drug;
• rare hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• children under 18 years of age.

Use during pregnancy and breastfeeding

There are no adequate and well-controlled studies in pregnant women.

Baraclude can be taken during pregnancy if the potential benefit outweighs the potential risk to the fetus.

There is no data on the penetration of entecavir into human milk. Breastfeeding while using the drug is not recommended.

Side effects

• From the digestive system: rarely (≥1/1000, <1/100) - diarrhea, dyspepsia, nausea, vomiting.
• From the central nervous system: often (≥1/100, <1/10) - headache, fatigue; rarely (≥1/1000, <1/100) - insomnia, dizziness, drowsiness.
• From the immune system: anaphylactoid reaction.
• From the skin and subcutaneous tissue: alopecia, rash.
• From the liver: increased transaminase activity.
• Metabolism: lactic acidosis (general fatigue, nausea, vomiting, abdominal pain, sudden weight loss, shortness of breath, rapid breathing, muscle weakness), especially in patients with decompensated liver damage.

In addition, in patients with decompensated liver damage, the following additional side effects were observed: often - a decrease in the concentration of bicarbonate in the blood, an increase in ALT activity and bilirubin concentration by more than 2 times compared to ULN, albumin concentration less than 2.5 g/dl, an increase lipase activity is more than 3 times higher than normal, platelet concentration is below 50,000/mm3; rarely - renal failure.

Interaction

Since entecavir is eliminated primarily by the kidneys, concomitant administration of entecavir and drugs that reduce renal function or compete at the level of tubular secretion may increase serum concentrations of entecavir or these drugs. When entecavir was co-administered with lamivudine, adefovir or tenofovir, no significant drug interactions were identified. The interactions of entecavir with other drugs that are excreted by the kidneys or affect renal function have not been studied. Patients should be monitored closely if entecavir is co-administered with these drugs.

Directions for use and dosage

Orally, on an empty stomach (i.e., no less than 2 hours after meals and no later than 2 hours before the next meal).

The recommended dose of entecavir is 0.5 mg once a day. In patients resistant to lamivudine (i.e., patients with hepatitis B virus viremia that persists during a history of lamivudine therapy or patients with confirmed resistance to lamivudine), it is recommended to prescribe entecavir 1 mg once daily.

In patients with decompensated liver disease, it is recommended to administer 1 mg of entecavir once daily.

Patients with renal failure. The clearance of entecavir decreases with a decrease in creatinine Cl. It is recommended to adjust the dose of entecavir in patients with creatinine Cl <50 ml/min, incl. those on hemodialysis and long-term outpatient peritoneal dialysis, according to the table.

Overdose

There are isolated reports of cases of entecavir overdose in patients. In a study of healthy volunteers receiving up to 20 mg of the drug per day for 14 days or single doses of up to 40 mg, no unexpected side effects were reported. In case of overdose, the patient should be closely monitored medically and, if necessary, receive standard supportive therapy.

special instructions

When treated with nucleoside analogues as monotherapy and in combination with antiretroviral drugs, cases of lactic acidosis and severe hepatomegaly with steatosis have been described, sometimes leading to the death of the patient.

Symptoms that may indicate the development of lactic acidosis: general fatigue, nausea, vomiting, abdominal pain, sudden weight loss, shortness of breath, rapid breathing, muscle weakness.

Risk factors are female gender, obesity, long-term use of nucleoside analogs, and hepatomegaly. If these symptoms appear or laboratory confirmation of lactic acidosis is obtained, treatment with the drug should be discontinued.

Cases of exacerbation of hepatitis after discontinuation of antiviral therapy have been described, incl. entecavir. Most of these cases resolved without treatment. However, severe exacerbations, including fatal ones, may develop. The causal relationship of these exacerbations with discontinuation of therapy is unknown. After stopping treatment, liver function should be periodically monitored. If necessary, antiviral therapy can be resumed.

Patients with combined hepatitis B/HIV infection. It should be taken into account that when prescribing entecavir to patients co-infected with HIV who are not receiving antiretroviral therapy, there may be a risk of developing resistant strains of HIV. Entecavir has not been studied for the treatment of HIV infection and is not recommended for such use.

Patients with combined hepatitis B/hepatitis C/hepatitis D infection. There are no data on the effectiveness of entecavir in patients with combined hepatitis B/hepatitis C/hepatitis D infections.

Patients with decompensated liver damage. There is a high risk of developing serious side effects from the liver, in particular in patients with decompensated liver disease class C according to the Child-Pugh classification. These patients are also at greater risk of developing lactic acidosis and specific renal side effects such as hepatorenal syndrome. In this regard, patients should be carefully monitored to identify clinical signs of lactic acidosis and renal dysfunction, and appropriate laboratory tests should be performed in this group of patients (liver enzyme activity, lactic acid concentration in the blood, serum creatinine concentration).

Lamivudine-resistant patients. The presence of resistance mutations in the hepatitis B virus to lamivudine increases the risk of developing resistance to entecavir. In this regard, lamivudine-resistant patients require frequent monitoring of the viral load and, if necessary, appropriate testing to identify resistance mutations.

Patients with impaired renal function. For patients with impaired renal function, adjustment of the dosage regimen is recommended.

Patients who have undergone liver transplantation. The safety and effectiveness of entecavir in patients undergoing liver transplantation are unknown. Renal function should be carefully monitored before and during treatment with entecavir in patients who have undergone liver transplantation and are receiving immunosuppressants that may affect renal function, such as cyclosporine and tacrolimus.

General information for patients. Patients should be informed that entecavir therapy does not reduce the risk of transmission of hepatitis B and therefore appropriate precautions should be taken.

Each tablet of the drug contains 120.5 mg (0.5 mg tablets) or 241 mg (1 mg tablets) of lactose. In this regard, patients with rare hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption are not recommended to take the drug.

Storage conditions for the drug Baraklyud

At a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf life of the drug Baraklyud

2 years.