"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 rapidly inhibits the replication of hepatitis viruses .
Before taking the drug, an annotation must be studied. What does the instructions for use indicate? "Baraclud" - a drug that is designed to trigger the reverse course of fibrotic processes in patients with cirrhosis.
The composition of the drug
The drug is produced in two dosage options - 0.5 and 1 mg of the active ingredient of entecavir, visually differing in color of the dye (white or pink, respectively).
The composition of the drug also includes:
- polysorbate;
- magnesium stearate;
- lactose monohydrate;
- hypromellose;
- povidone;
- dye Opadry.
pharmachologic effect
The active ingredient entecavir, which is an analogue of the nucleoside of guanosine, has a pronounced selective effect on the hepatitis B virus.
Entecavir is phosphorylated to active triphosphate with a half-life of about 15 hours, the intracellular content of which is associated with the concentration of entecavir outside the cell. In this case, there is no noticeable accumulation of the active substance in the body. The medicine "Baraclude", the instructions for use of which indicates its high efficiency, suppresses the activity of the virus polymerase, having an effect on three factors simultaneously:
- synthesis of a positive strand of HBV DNA;
- reverse transcription of the negative strand of pregenomic mRNA;
- HBV enzyme priming.
Triphosphate does not belong to strong inhibitors of cellular DNA enzymes, even with a significant content it does not affect mitochondrial DNA synthesis.
Drug action
The active substance of the drug is able to be absorbed from the digestive system in a short time and reaches its maximum 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 achieving balance on the 6-10th day of a single dose of the drug per day. Eating fatty foods significantly complicates the absorption of entecavir, reducing the Cmax and AUC indices by 45% and 20%, respectively.
The drug is rapidly absorbed into the tissue and binds to plasma proteins by 13%. The active component of the drug does not apply to substrates, inhibitors or enzyme inducers in the P450 system. It is able to accumulate in the body and excreted through the renal system through glomerular filtration and tubular secretions.
Indications for use
The drug "Baraclude" is recommended to be taken in the complex treatment of hepatitis B:
- With symptoms of ongoing viral reduplication and an increase in the degree of transaminase activity in the blood serum, in the presence of histological manifestations of ongoing liver inflammation.
- Unrepaired liver lesions.
Significant relief of symptoms of liver disease occurs after taking the drug "Baraclude." Tablets for use recommends taking patients with chronic hepatitis B, complicated by the following liver diseases:
- under decompensation;
- pathological conditions of the liver in the stage of compensation 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 lactase enzyme in the body;
- age less than 18 years.
Persons with kidney failure should take the drug as directed and under the constant supervision of a doctor.
Reception "Baraclude" during pregnancy is not recommended, during therapy it is necessary to stop breast-feeding.
Side effects
Various digestive disorders can be observed during treatment with Baraclude. Instructions for use clearly describe such side effects:
- digestion disorder;
- diarrhea;
- nausea and vomiting;
- dyspepsia.
Migraines, insomnia or drowsiness, loss of appetite and allergic reactions can 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 a decompensated type of liver damage, lactaciadosis can be observed, which is characterized by:
- general muscle weakness;
- rapid breathing and the appearance of shortness of breath;
- nausea
- a significant decrease in body weight;
- pain in the peritoneum, epigastrium.
Also, taking the drug can cause other body reactions:
- elevated liver transaminases ;
- skin rashes;
- anaphylactoid reactions.
In patients also suffering from decompensated liver lesions, in addition, the following reactions of the body were manifested:
- renal failure (in rare cases);
- high bilirubin in the blood;
- a decrease in platelet count to 50 thousand / mm 3 and below;
- a decrease in blood bicarbonate;
- increased ALT;
- more than three-fold increase in lipase activity;
- low albumin.
Medication "Baraclude": method of application and dose
The drug should be taken on an empty stomach, the time interval from the last meal to the drug should be more than two hours.
With compensated liver damage, it is recommended to take "Baraclude" at 0.5 mg daily. If resistance to lamivudine is detected, the dosage must be doubled.
Patients with unrepaired liver lesions are prescribed 1 mg daily. For the elderly and patients with renal failure, the dose must be adjusted depending on the level of QC (creatinine concentration) in the blood.
Overdose
Information on cases of overdose of the drug is not enough.
Clinical trials volunteers received a daily dosage of 20 mg for a two-week period, or they were given a single increased dose of 40 mg of Baraclude. The instruction for use claims that no negative effects have been identified.
Syndromic treatment under the control of clinical manifestations is recommended.
Interaction with other drugs
Due to the fact that the active component of entecavir is excreted primarily 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 the tubular secretion can lead to an increase in the content of these substances and the active substances in the body of entecavir medicines.
Interactions of "Baraclude" with adenovir, tenofovir, lamivudine were not recorded.
Precautionary measures
Taking the drug in patients resistant to lamivudine leads to a risk of resistance.
There is also information about the occurrence of exacerbations of hepatitis after discontinuation of the drug "Baraclude." Instructions for use describe the relief of such exacerbations without additional therapy.
special instructions
Reception "Baraclude" as part of monotherapy, and with complex treatment with other antiretroviral agents, can lead to lactic acidosis, hepatomegaly, accompanied by steatosis. 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 use of the drug "Baraclude" notes the possibility of the 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 pathology of the renal system, dose adjustment is necessary.
The safety and effectiveness of using Baraclude for the treatment of patients after liver transplantation are not known and require special care.
Storage conditions and cost
Storage and transportation of tablets should be carried out in a 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, for certain categories of citizens, the gratuitous issue of the Baraclude medicine has been established. Instructions for use fix this fact.
The price of funds in pharmacies in Moscow starts from 12 thousand rubles.
Patient opinions
Indicates the high effectiveness of the drug "Baraclude" instructions for use. The price, reviews of which testify to its democracy in comparison with the analogues of the drug, ranges from 12-17 thousand per pack, in which 30 tablets. This makes the drug quite popular and in demand among patients in the treatment of hepatitis B.
Negative reviews mainly mention the contraindications and side effects of the drug, such as insomnia and nausea.