"Baraclude" refers to antiretroviral drugs, is included in the group of nucleoside analogues. It is prescribed for the treatment of chronic HBV infections. The active component of the drug entecavir promptly inhibits the replication of hepatitis viruses.
Before taking the drug, the annotation must be studied. What does the instructions for use indicate? "Baraclud" (Baraclud) - a drug that is designed to start the reverse flow of fibrotic processes in patients with cirrhosis of the liver.
Composition of the drug
The drug is produced in two dosage options - 0, 5 and 1 mg of the active ingredient of entecavir, visually different in color of the dye (white or pink, respectively).
The composition of the drug also includes:
- polysorbate;
- magnesium stearate;
- lactose monohydrate;
- hypromellose;
- povidone;
- Opadry dye.
Pharmacological action
The active ingredient entecavir, which is an analogue of the guanosine nucleoside, has a pronounced selective effect on the hepatitis B virus.
Entecavir is phosphorylated to an active triphosphate with a half-life of about 15 hours, the intracellular content of which is related to the concentration of entecavir outside the cell. At the same time, there is no noticeable accumulation of the active substance in the body. The drug "Baraclude", the instruction for the use of which indicates its high efficiency, inhibits the activity of the polymerase of the virus, affecting simultaneously three factors:
- synthesis of HBV positive DNA strand;
- reverse transcription of the negative strand of pregenomic mRNA;
- HBV enzyme priming.
Triphosphate is not a strong inhibitor of cellular DNA enzymes, even with a significant content it does not affect mitochondrial DNA synthesis.
Drug action
The active substance of the drug can be absorbed from the digestive system in a short time and reaches its highest content 30-90 minutes after taking the pill.
A commensurate increase in the Cmax and AUC indices occurs with the subsequent use of 0.1-1 mg of the drug "Baraclude". Instructions for use indicate the achievement of balance on the 6-10th day of a single dose of the drug per day. The use of fatty foods significantly complicates the absorption of entecavir, reducingCmax and AUC indices by 45% and 20% respectively.
The drug is rapidly absorbed into tissues and is 13% bound to plasma proteins. The active component of the drug does not apply to substrates, inhibitors or enzyme inducers according to the P450 system. It is able to accumulate in the body and be excreted through the renal system through glomerular filtration and tubular secretions.
Indications for use
Medication "Baraclude" is recommended to be taken in the complex treatment of hepatitis B:
- With symptoms of ongoing viral replication and an increase in the degree of transaminase activity in the blood serum, in the presence of histological manifestations of current inflammation of the liver.
- Unrepaired liver damage.
Significant relief of the symptoms of liver disease occurs after taking the drug "Baraclude". Tablets instructions for use recommend taking patients with chronic hepatitis B, complicated by the following liver diseases:
- being in the stage of decompensation;
- pathological conditions of the liver in the recovery stage with established viral replication, diagnosed manifestations of liver fibrosis with increased AST and ALT.
Contraindications
The drug "Baraclude" has the following contraindications:
- increased susceptibility to entecavir and other substances that make up the drug;
- hereditary lactose intolerance, glucose-galactose malabsorption, deficiency or absence of the enzyme lactase in the body;
- ageunder 18 years old.
Persons with renal insufficiency should take the drug as directed and under constant medical supervision.
Baraclud is not recommended during pregnancy, during therapy it is necessary to stop breastfeeding.
Side effects
Various disorders of the digestive system may be observed during treatment with Baraclude. Instructions for use clearly describe such side effects:
- indigestion;
- diarrhea;
- nausea and vomiting;
- dyspepsia.
Migraines, insomnia or drowsiness, decreased appetite and allergic reactions may also occur.
The use of the drug as the only therapeutic agent or in combination with other antiretroviral drugs can cause severe hepatomegaly with steatosis, which can lead to the death of the patient.
In patients with decompensated liver damage, lactic acidosis may be observed, which is characterized by:
- general muscle weakness;
- rapid breathing and shortness of breath;
- nauseous;
- significant weight loss;
- pain in the peritoneum, epigastrium.
Also, taking the drug can cause other reactions of the body:
- elevated liver transaminases;
- skin rashes;
- anaphylactoid reactions.
In patients also suffering fromdecompensated lesions of the liver, in addition, the following reactions of the body were manifested:
- renal failure (in rare cases);
- high blood bilirubin;
- lower platelet count to 50,000/mm3 and below;
- lower blood levels of bicarbonate;
- increased ALT;
- more than threefold increase in lipase activity;
- low albumin content.
Medication "Baraclude": method of administration and doses
The drug should be taken on an empty stomach, the time interval from the last meal to taking the drug should be more than two hours.
With compensated liver damage, it is recommended to take "Baraclud" at a dose of 0.5 mg daily. If resistance to lamivudine is detected, the dosage should be doubled.
Patients with uncompensated liver damage are prescribed 1 mg daily. For the elderly and patients with renal insufficiency, the dose must be adjusted depending on the level of CK (concentration of creatinine) in the blood.
Overdose
There is not enough information on cases of drug overdose.
Volunteers in clinical trials received a daily dose of 20 mg for a two-week period or were given a single increased dose of 40 mg of Baraclude. Instructions for use states that no negative effects have been identifiedwas.
Posyndromic treatment under clinical control recommended.
Interaction with other drugs
Due to the fact that the active component of entecavir is excreted from the body mainly through the renal system, complex therapy in combination with other drugs that have a direct or indirect effect on the functioning of the kidneys and affect tubular secretion may lead to an increase in the content in the body entecavir and the active substances of these medicines.
Interactions of "Baraclud" with adenovir, tenofovir, lamivudine were not recorded.
Precautions
In patients who are refractory to lamivudine, the drug is at risk of developing resistance.
There is also information about the occurrence of exacerbations of hepatitis after stopping the medication "Baraclud". Instructions for use describe the relief of such exacerbations without additional therapy.
Special Instructions
Acceptance of "Baraclud" both as monotherapy and in complex treatment with other antiretroviral agents can lead to lactic acidosis, hepatomegaly, accompanied by steatosis. However, there is a risk of death.
The following categories of patients are at risk:
- suffering from hepatomegaly;
- treated with nucleoside analogues;
- overweight;
- female patients.
Instructions for the use of the drug "Baraclude" notes the possibility of formation of resistant strains of HIV. The active component of the drug entecavir is not recommended for the treatment of human immunodeficiency virus, since its effectiveness in this direction has not yet been fully studied.
In the treatment of patients with pathologies of the renal system, it is necessary to adjust the dose of the drug.
The safety and efficacy of using Baraclude in the treatment of liver transplant patients is not known and requires special precautions.
Storage conditions and cost
Storage and transportation of tablets should be carried out in the temperature range of 15-25 °C. The drug is suitable for use for two years from the date of manufacture.
The drug is included in a special group of vital medicines, and therefore certain categories of citizens are given free distribution of the drug "Baraclud". The instructions for use record this fact.
The price of funds in pharmacies in Moscow starts from 12 thousand rubles.
Patient opinions
Indicates the high effectiveness of the drug "Baraclud" instructions for use. The price, reviews of which testify to its democratic nature in comparison with analogues of the drug, ranges from 12-17 thousand per package, in which there are 30 tablets. It doesthe drug is quite popular and in demand among patients in the treatment of hepatitis B.
Negative reviews mainly mention contraindications and side effects of the drug, such as insomnia and nausea.
