Ursodez is a hepatoprotective medicine. The drug has a choleretic, hypolipidemic, choleretic effect, has a hypocholesterolemic and slight immunomodulatory effect. The active substance is ursodeoxycholic acid. The drug does not have a "tablet" dosage form. Ursodez is produced 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. As a result, cells are protected from damaging factors, the activity of acidic bile s alts.
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. Means "Ursodez" (instructions for use indicates this) significantly reduces the content of bile toxic acids (deoxycholic, lithocholic, chenodeoxycholic and others) with their increased concentration in patients withchronic liver pathologies.
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 decreases. 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 drug stimulates the excretion of toxic acids, increasing the passage.
The mechanism of action of the drug is also based on the screening of non-polar bile acids. This results in non-toxic mixed micelles. The agent enhances the solubility of cholesterol in the biliary system, stabilizes the production and secretion of bile. The drug 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 stones is noted. By reducing the saturation of bile, the mobilization of cholesterol from calculi increases. Immunomodulatory activity is manifested by influencing the corresponding reactions in the liver. The drug helps to reduce the expression of a number of histocompatibility antigens. The drug also affects the level of T-lymphocytes, reduces the number of eosinophils.
Pharmacokinetics of the drug
Absorption of the drug "Ursodez" (instructions for use indicates this) in the small intestine is carried out due to the process of passive diffusion. Absorbed at the same timeabout 90% of the active ingredient. In the ileum, the substance is absorbed by active transport. The active ingredient reaches its highest content in about an hour. The compound has a high percentage of protein binding - up to 99%. Ursodeoxycholic acid is able to cross the placental barrier.
The therapeutic efficacy of the drug depends on the concentration of the active ingredient in the bile. With regular systematic intake, this bile acid becomes the main one in the blood serum. The concentration of ursodeoxycholic acid is about 48%.
The compound is metabolized by passing through the liver cells. As a result, glycine and taurine conjugates are formed. The breakdown products are secreted into the bile. About 50-70% of the drug taken is excreted in the feces. A small amount of the drug is transported to the large intestine. There it is broken down by bacteria (7-dehydroxylation).
Litocholic acid, which is formed as a result of this process, is partially absorbed from the large intestine, but undergoes sulfation in the liver and is excreted as sulfolithocholyltaurine or sulfolithocholylglycine conjugate.
Indications
The drug "Ursodez" is recommended as a symptomatic therapy for primary biliary cirrhosis without signs of decompensation. A remedy for dissolving medium and small cholesterol stones with an active gallbladder is shown. Prescribe medication for biliaryreflux gastritis.
Contraindications
Means "Ursodez" instructions for use does not allow for the appointment if the patient has X-ray positive (with an increased concentration of Ca2 +) gallstones, intolerance to the components of the drug. Contraindications include cirrhosis of the liver at the stage of decompensation, severe disorders of the pancreas, kidneys. The drug is not recommended for people with a non-functioning gallbladder, its acute pathologies of an inflammatory nature, as well as diseases of the intestines and bile ducts. Do not prescribe medication to pregnant and lactating women. The remedy is contraindicated for 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 of the likelihood of nausea, diarrhea, vomiting. On the basis of treatment, calcified gallstones can form. Increased activity of liver transaminases, abdominal pain, allergic manifestations (including urticaria) are also undesirable consequences of taking the drug "Ursodez".
Reviews of patients indicate a good tolerability of the drug. When prescribed by a doctor, side effects are unlikely. In some cases, during the treatment of biliary cirrhosis, transient decompensation was noted. As a rule, after stopping the medication, this phenomenon is eliminated on its own.
Ursodez preparation. Price. Instruction
The remedy is taken in the evening. The daily dosage for the dissolution of stones is an average of 10 mg / kg. For persons 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 - from six months to 12 months. After the stones have dissolved, it is recommended to take them for several more months to prevent the formation of new ones.
Biliary cirrhosis is treated at a dose of 250 mg/day. Course duration - from 10-14 days. up to half a year. In some cases, the duration of therapy is increased to two years. As a symptomatic treatment, the drug 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 analogues?
Preparations that contain the same active substance are produced quite a lot. Among them, it is worth mentioning such means as Ursodox, Ursoliv. One of the most popular is the drug "Ursosan". Indications for the use of this medication are somewhat wider. In particular, it is prescribed for cystic fibrosis of the liver, chronic sclerosing cholangitis.
Many patients are interested in what is better: 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 the tolerance of the drug by the patient. In diseases of the liver, gallbladder, self-medication is highly recommended. Before taking anythe drug requires examination and consultation of a specialist.
Monitoring the effectiveness of therapy should be carried out every 6 months. In this regard, regular ultrasound and x-ray examinations 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 it is not advisable to continue the course due to inefficiency.
Additional information
To ensure successful dissolution of calculi, it is necessary that the stones are only cholesterol, and their size does not exceed 15 or 20 millimeters. At the same time, the gallbladder should be no more than half full, and the bile ducts should retain their full function.
In the case of a long-term treatment exceeding a month, a biochemical analysis should be carried out 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 Ursodez. 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 may be completely revised. Before using the drug, you should read the annotation.
