The drug "Ursodez" is a hepatoprotective drug. The medication has a choleretic, hypolipidemic, cholelitic effect, has a hypocholesterolemic and slight immunomodulatory effect. The active substance is ursodeoxycholic acid. The drug does not have a “pill” dosage form. "Ursodez" is made in the form of capsules.
Activity mechanism
The active substance of the drug has the ability to integrate into the membranes of hepatocytes, stabilizing their structure. The result is the protection of cells from damaging factors, the activity of acid bile salts.
The therapeutic effect of the drug is thus manifested in a decrease in the cytotoxic effect. Against the background of cholestasis, Ca2 + -dependent alpha-protease is activated, exocytosis is stimulated. The Ursodez product (instructions for use indicates this) significantly reduces the content of toxic bile acids (deoxycholic, lithocholic, chenodeoxycholic and others) with an increased concentration in patients with chronic liver diseases.
When taking the medicine, there is a decrease in the secretion and synthesis of cholesterol, inhibition of its absorption in the intestine. Due to this, the saturation of bile with this compound is reduced. The drug has the ability to competitively reduce the absorption of lipophilic acids in the intestine, increase their fractional turnover on the basis of enterohepatic circulation. The medication stimulates the elimination of toxic acids, increasing passage.
The mechanism of action of the drug is also based on the screening of non-polar bile acids. Due to this, non-toxic mixed micelles are formed. The tool enhances the solubility of cholesterol in the biliary system, stabilizes the production and secretion of bile. The medicine also reduces its lithogenicity, increases the concentration of acids, thereby provoking an increase in the activity of pancreatic and gastric secretion.
When taking capsules, complete or partial dissolution of the stones is noted. By reducing the saturation of bile, cholesterol mobilization from calculi increases. Immunomodulating activity is manifested due to the effect on the corresponding reactions in the liver. The drug helps to reduce the expression of a number of histocompatibility antigens. The medication also affects the level of T-lymphocytes, reduces the number of eosinophils.
Pharmacokinetics
The absorption of the drug "Ursodez" (instructions for use indicates this) in the small intestine is due to the process of passive diffusion. At the same time, about 90% of the active component is absorbed. In the ileum, the substance is absorbed by active transport. The highest content of the active ingredient reaches in about an hour. The compound is characterized by a high percentage of protein binding - up to 99%. Ursodeoxycholic acid is able to penetrate the placental barrier.
The therapeutic effectiveness of the drug depends on the concentration of the active component in bile. With regular systematic administration, this
bile acid becomes the main in serum. The concentration of ursodeoxycholic acid is about 48%.
The compound is metabolized through liver cells. As a result, glycine and taurine conjugates are formed. Decay products are secreted into the bile. About 50-70% of the medication taken is excreted in feces. A small amount of the drug is transported to the colon. There it is cleaved by bacteria (7-dehydroxylation).
Litocholic acid, which is formed as a result of this process, undergoes partial absorption from the large intestine, however, it undergoes sulfation in the liver and is excreted in the form of sulfolithocholyl tauric or sulfolithocholylglycine conjugate.
Indications
The medicine "Ursodez" is recommended as symptomatic therapy for biliary primary cirrhosis without signs of decompensation. An agent for dissolving medium and small cholesterol stones with an active gall bladder is shown. Prescribe medication for biliary reflux gastritis.
Contraindications
Means “Ursodez” instruction for use does not allow for appointment if the patient has x-ray positive (with an increased concentration of Ca2 +) gallstones, intolerance to the components of the medication. Contraindications include liver cirrhosis at the stage of decompensation, severe disorders of the pancreas, kidneys. The drug is not recommended for people with non-functioning gall bladder, acute pathologies of its inflammatory nature, as well as diseases of the intestines and bile ducts. Do not prescribe medication to pregnant and lactating. The drug is contraindicated in adults and children weighing less than 34 kg.
Side effects
In some cases, undesirable consequences develop when taking the drug "Ursodez." Instructions for use warns about the likelihood of nausea, diarrhea, vomiting. Calcined gallstones can form on the basis of treatment. Increased activity of liver transaminases, abdominal pain, allergic manifestations (including urticaria, including) are also among the undesirable consequences of taking the drug “Ursodez”.
Patient reviews indicate good tolerance to the drug. Subject to doctor’s instructions, side effects are unlikely. In some cases, transient decompensation was observed during the treatment of biliary cirrhosis. As a rule, after stopping the medication, this phenomenon is independently eliminated.
The drug "Ursodez." Price. Instruction manual
The drug is taken in the evening. The daily dosage for dissolving stones is an average of 10 mg / kg. For individuals weighing up to 60 kg, it corresponds to 2 capsules per day, up to 81 kg - 3, up to 100 kg - 4, more than 100 - 5. Duration of admission is from six months to 12 months. After dissolution of calculi, to prevent the formation of new ones, administration is recommended for another several months.
Treatment of biliary cirrhosis is carried out at a dose of 250 mg / day. Course duration - from 10-14 days. up to six months. In some cases, the duration of therapy increases to two years. As a symptomatic treatment, a medication is prescribed at 10-15 mg / day. With a weight of up to 34 kg, a suspended form of the product is recommended. The cost of the drug in the form of capsules is from one hundred rubles.
Does Ursodez have any analogues?
There are a lot of drugs that contain the same active substance. Among them are such funds as Ursodox, Ursoliv. One of the most popular is the drug "Ursosan". Indications for use of this medication are somewhat wider. In particular, it is prescribed for cystic liver fibrosis, chronic sclerosing cholangitis.
Many patients are interested in what is better: the drug "Ursodez" or "Ursosan." It should be said that the doctor selects one or another remedy in accordance with the nature, course of the pathology and tolerability of the drug by the patient. In diseases of the liver, gall bladder self-medication is highly not recommended. Before taking any drug, a specialist examination and consultation is necessary.
Monitoring the effectiveness of therapy should be carried out every 6 months. In this regard, regular ultrasound and X-ray examination are prescribed during the first year of treatment. If, in the first six months, the dissolution of the stones did not happen, then, most likely, the continuation of the course is impractical due to inefficiency.
Additional Information
To ensure the successful dissolution of calculi, it is necessary that the stones are only cholesterol, and their size does not exceed 15 or 20 millimeters. In this case, the gallbladder should be filled no more than half, and the bile ducts must retain their full function.
In the case of the appointment of prolonged treatment exceeding a month, a biochemical analysis should be performed to assess the activity of transaminases in the liver. In addition, the concentration of bilirubin and other compounds should be monitored. While maintaining high rates stop taking the means "Ursodez." The reviews of many experts, however, are positive regarding the effectiveness of the drug.
Conclusion
If there is no result, another medication may be prescribed or the treatment tactics completely reviewed. Before using the drug, you should familiarize yourself with the annotation.