Pharmacodynamics and pharmacokinetics
The composition determines the effect of this medicine. Its active component is ursodeoxycholic acid . Ursodeoxycholic acid has high polar properties and creates non-toxic mixed micelles with toxic bile acids. This leads to a decrease in the ability of gastric reflux to damage cell membranes with the appearance of reflux esophagitis and biliary reflux gastritis . In addition, the drug Ursosan creates double molecules that enter the cell membranes of hepatocytes, epithelial cells of the gastrointestinal tract, and cholangiocytes. These molecules stabilize them and make them immune to the influence of cytotoxic micelles.
The active substance of the drug also reduces the content of bile acids, which are toxic to hepatocytes, and stimulates choleresis, saturated with bicarbonates. Thanks to this, intrahepatic cholestasis disappears. Ursodeoxycholic acid reduces the lithogenic index of bile and cholesterol by preventing its absorption in the intestine, reducing secretion in bile, and inhibiting synthesis in the liver. As a result, cholesterol gallstones dissolve. The product also prevents the appearance of new stones.
The drug acts as an immunomodulatory agent by inhibiting the expression of HLA-2 and HLA-1 and improving the normal killer activity of lymphocytes . In addition, it prevents the development of fibrosis in people with primary biliary cirrhosis , as well as alcoholic steatohepatitis and cystic fibrosis . Reduces the likelihood of varicose veins in the esophagus, slows down premature aging and cell death.
The active substance of the drug is absorbed from the small intestine by passive diffusion (absorption rate is approximately 90%), and in the ileum by active transport. The maximum concentration is reached after approximately 60-180 minutes.
The degree of binding to plasma proteins is up to 99%. With chronic use, ursodeoxycholic acid becomes the main bile acid in the blood serum. The therapeutic effect of the drug depends on its content in bile.
The drug is broken down in the liver with the formation of metabolic such as glycine and taurine conjugate. They are secreted into bile. Approximately 60% of the total dosage is excreted in bile. Some of the active substance is also transported to the colon, where it is broken down by bacteria. Lithocholic acid is absorbed to a small extent from the colon, sulfated in the liver and excreted as sulfolithocholylglycine or sulfolitocholyltaurine conjugate.
Effect of the drug
According to the study, it has been proven that ursodeoxycholic acid is quickly absorbed in the intestine and is integrated into liver cells and provides them with protection from various negative factors, including toxic and alcohol damage. When taking the medicine, congestion in the organ decreases and the removal of acids accelerates.
Ursosan, the instructions for use emphasize this, has a choleretic effect. The active substance is capable of:
- Reduce cholesterol production in the liver and slow down its absorption in the intestines.
- Reduce the saturation of bile with cholesterol.
- Increase the content of bile acids.
- Increase the solubility of cholesterol in the biliary system.
Indications for use of Ursosan
On forums people often ask what pills can help with in this or that case. Experts do not recommend taking them without consulting a doctor. Only he can determine whether there are indications for the use of Ursosan. In addition, he selects the desired treatment regimen.
If you have been prescribed Ursosan tablets, the indications for use are usually as follows:
- uncomplicated cholelithiasis ;
- the need to prevent recurrent stone formation after cholecystectomy ;
- acute hepatitis;
- alcohol disease and primary biliary cirrhosis ;
- biliary dyskinesia
- cystic fibrosis of the liver;
- biliary dyspeptic syndrome;
- toxic liver damage;
- chronic active hepatitis ;
- non-alcoholic steatohepatitis;
- atresia of the intrahepatic biliary tract;
- primary sclerosing cholangitis ;
- biliary reflux gastritis and reflux esophagitis ;
- the need to prevent liver damage when taking hormonal contraceptives and cytostatics.
Contraindications
This drug should not be used in case of hypersensitivity to its components, non-functioning gallbladder, chronic hepatitis , pancreatitis , acute cholecystitis , liver cirrhosis (with decompensation), acute cholangitis , acute infectious diseases of the gallbladder, diseases of the bile ducts, pregnancy , breastfeeding , bile -gastrointestinal fistula, gallstones with high Ca2+ content, inflammatory diseases of the small and large intestines, liver failure , renal failure , empyema of the gallbladder, obstruction of the biliary tract.
Contraindications for use
- hypersensitivity;
- X-ray positive (high calcium) gallstones;
- non-functioning gallbladder;
- bile-gastrointestinal fistula;
- acute cholecystitis;
- acute cholangitis;
- liver cirrhosis in the stage of decompensation;
- liver and/or kidney failure;
- obstruction of the biliary tract;
- acute infectious diseases of the gallbladder and bile ducts;
- empyema of the gallbladder.
Although Ursosan has no age restrictions for use, the drug capsules are used with caution in children aged 2 to 4 years due to possible difficulty in swallowing them.
Side effects of Ursosan
Reviews of side effects appear infrequently. However, if any unwanted reactions occur, you should definitely consult a doctor.
The following side effects of Ursosan are known:
- vomit;
- exacerbation of psoriasis ;
- nausea;
- diarrhea;
- transient increase in the activity of liver transaminases;
- constipation;
- painful sensations in the back;
- allergy;
- alopecia.
In rare cases, gallstones may become calcified.
Instructions for use of Ursosan (Method and dosage)
For those who have been prescribed Ursosan tablets, the instructions for use indicate that they should be taken orally with liquid.
The medicine has different dosage regimens depending on the disease. For those who are interested in how to take Ursosan: before or after meals, it is also reported that this is individual, depending on the indications for use.
In the case of diffuse liver diseases and cholelithiasis , the course of treatment can last from several months to several years, the daily dosage is usually 10-15 mg per 1 kg of the patient’s body weight (2-5 capsules). For cholelithiasis, the daily dosage is taken once immediately before bedtime. Treatment is carried out until the stones dissolve, and then another 3 months to ensure that the stones do not form again. For diffuse liver diseases, the instructions for use of Ursosan indicate that the daily dosage should be divided into 2-3 doses. The product should be taken during meals.
After cholecystectomy and for the purpose of preventing recurrent cholelithiasis , 250 mg is usually prescribed 2 times a day. The course lasts several months.
For primary biliary cirrhosis, the medicine is taken in a dosage of 10-15 mg per 1 kg of patient body weight per day. If necessary, it can be increased to 20 mg per 1 kg. The dosage should be divided into 2-3 doses. The course of treatment lasts from 6 months to several years.
If the patient has non-alcoholic steatohepatitis , take 13-15 mg per 1 kg of the patient’s weight per day. The dosage should be divided into 2-3 doses. The course of treatment can last from 6 months to several years.
In the case of biliary reflux gastritis and reflux esophagitis, the medicine is taken 1 capsule (250 mg) per day immediately before bedtime. Therapy is carried out from 10 days to 6 months. If necessary, it can be extended up to 2 years.
For liver damage , biliary atresia alcoholic liver disease, the daily dosage is usually 10-15 mg per 1 kg of patient weight. The daily dosage should be divided into 2-3 doses. The course is designed for six months, a year or more.
If the patient has primary sclerosing cholangitis , the doctor usually prescribes 12-15 mg per 1 kg of the patient’s body weight per day. If necessary, the dosage can be increased to 20 mg per 1 kg of weight. The total daily dose is divided by the patient into 2-3 doses. The course of admission is from six months to several years.
For cystic fibrosis, the drug is taken in dosages of 20-30 mg per kg per day. The dose should be divided into 2-3 doses. The course lasts from six months to several years.
For children over 2 years old, the amount of the drug taken per day is determined individually by a specialist. Typically 10-20 mg per kg per day is prescribed.
In order to eliminate severe and dangerous jaundice, specialists in some cases prescribe this remedy to newborns. Therapy is designed for 2-4 weeks. Instructions for use of Ursosan for newborns indicate that the dosage for children of this age is a quarter of a capsule every day. The powder in it is poured onto a saucer. Then it is divided into four equal parts, one of which is given to the baby. It must first be dissolved in water or breast milk. If treatment is successful, the course can be reduced to 10 days. In this case, you need to monitor the level of bilirubin in the blood every week. On average, its level decreases by 50 units per week. Once the blood concentration reaches 100 mg/ml, the medicine can be discontinued.
Ursosan dosage
Ursosan is taken orally with a sufficient amount of water.
- Diffuse liver diseases, cholelithiasis (cholesterol gallstones and biliary sludge) - continuously for a long time (from several months to several years) in a daily dose of 10 to 12-15 mg/kg (2-5 caps.). For diffuse liver diseases, the daily dose of Ursosan is divided into 2-3 doses, the capsules are taken with food. For cholelithiasis, the entire daily dose of Ursosan is taken once at night. The duration of treatment for dissolving stones is until complete dissolution, plus another 3 months. for the prevention of recurrent stone formation.
- For biliary reflux gastritis and reflux esophagitis, Ursosan is taken 250 mg/day (1 capsule) before bedtime. The course of treatment is from 10–14 days to 6 months, if necessary – up to 2 years.
- After cholecystectomy, to prevent recurrent cholelithiasis, Ursosan is used at a dose of 250 mg 2 times a day for several months.
- Toxic, drug-induced liver damage, alcoholic liver disease and biliary atresia - 10-15 mg/kg/day in 2-3 doses. Duration of therapy is 6–12 months. and more.
- Primary biliary cirrhosis - 10-15 mg/kg/day (if necessary - up to 20 mg/kg) in 2-3 doses. The duration of therapy is from 6 months. up to several years.
- Primary sclerosing cholangitis - 12–15 mg/kg/day (up to 20 mg/kg) in 2–3 doses. The duration of therapy is from 6 months. up to several years.
- Non-alcoholic steatohepatitis - 13-15 mg/kg/day in 2-3 doses. The duration of therapy is from 6 months. up to several years.
- Cystic fibrosis - 20-30 mg/kg in 2-3 doses. The duration of therapy is from 6 months. up to several years or for life.
For children over 2 years of age, Ursosan is prescribed individually at a dose of 10–20 mg/kg/day.
Analogues of Ursosan
Level 4 ATC code matches:
Ursodex
Henofalk
Ursoliv
Ursofalk
Choludexan
Ursohol
Ursodez
Urdoxa
Livodex
The names of analogues of this drug are presented in the following list:
- Ursolak
- Ursoliv
- Ursolysin
- Ursomax
- Ursonost
- Ursofalk
- Ursohol
- Essentiale
- Choludexan
All analogues of Ursosan have their own characteristics of action and application. None of them should be replaced independently without consulting a doctor. The price of analogues may vary depending on the amount of medicine in one package. However, in most cases their cost is higher than the described drug in a similar quantity.
Let's take a closer look at some Ursosan analogues.
Ursofalk or Ursosan - which is better?
In most cases, when choosing between these two drugs, experts believe that the first remedy is better. This has been confirmed by many clinical observations, patient reviews and many years of practice. People who have taken both drugs note that Ursofalk is easier to tolerate. And experts report that it dissolves gallstones faster and improves liver condition.
However, the difference between Ursosan and Ursofalk for each specific case can only be understood in practice. There are people for whom a medicine like Ursosan is more suitable. So you can first prescribe a course of Ursofalk, and, if the treatment is not effective enough, move on to another drug. In this way, the best treatment method can be selected.
Ursosan or Essentiale - which is better?
As a hepatoprotector , Essentiale is much more effective in maintaining liver function. In addition, this remedy does not have as many side effects. So for those who choose the drug when it is necessary to normalize liver function, doctors in most cases recommend a second remedy. Ursosan is more expensive and has less effect on the cellular structure.
Urdoxa or Ursosan - which is better?
Urdoxa is a domestically produced product, which is a generic version of Ursosan. However, all the necessary components for its manufacture are purchased abroad. Thus, all the components in it are the same as in the original drug. In fact, these are complete analogues, and the difference between them lies only in the country of origin. Many, however, choose a domestic product, since its cost is much lower.
Ursoliv or Ursosan - which is better?
Both drugs have the same main component. Some patients tolerate one drug better, while others tolerate the other. In this situation, individual effectiveness can only be verified in practice. All this depends on the characteristics of the body, so you should start taking one of the remedies, and if it does not help, move on to another. There are no objective signs to help determine the effectiveness of each of these drugs. Many patients prefer to try each of the remedies and then choose the most effective one.
Reviews about Ursosan
Reviews of drug treatment can often be found on specialized forums. Doctors also express their opinions. They note the effectiveness of this drug. Patient reviews are also mostly positive. Some also take it as a prophylactic in cases where a large load on the liver is expected.
With regard to use for newborns, doctors' reviews of Ursosan usually report that the treatment was effective. Parents turn to them when their children develop jaundice. Those who gave the medicine according to the specialist’s instructions leave reviews about Ursosan, which say that the drug helped.
Ursosan price, where to buy
This medicine can be bought in Ukraine, Belarus and Russia. How much this drug costs depends largely on the number of capsules in one package.
You can buy this product in Moscow and other Russian cities at the following prices:
- price of Ursosan 100 tablets (250 mg) - approximately 1,500 rubles;
- price of Ursosan 50 capsules – approximately 800 rubles;
- the price of a package of 10 capsules is approximately 200 rubles.
Average price of Ursosan in Ukraine:
- capsules of 50 pieces per package – approximately 600 hryvnia;
- capsules of 100 pieces per package - approximately 1000 hryvnia;
- capsules of 10 pieces per package - approximately 100 hryvnia.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Ursosan capsules 250 mg 10 pcs. Pro.Med.Cs
146 rub. order - Ursosan capsules 250 mg 50 pcs. ZiO-Zdorovye CJSC
RUR 768 order
- Ursosan forte tab. p.p.o. 500 mg 100 pcs. PRO.MED.CS Prague j.s.
RUB 2915 order
- Ursosan forte tab. p.p.o. 500 mg 50 pcs. PRO.MED.CS Prague j.s.
RUB 1,532 order
- Ursosan caps. 250 mg No. 100 ZiO-Zdorovye ZAO
RUB 1,541 order
Pharmacy Dialogue
- Ursosan (caps. 250 mg No. 50)ZiO-Zdorovye CJSC
RUR 749 order
- Ursosan (tab.p.pl/vol.500mg No. 50)Pro.Med.Cs.
RUB 1,652 order
- Ursosan (caps. 250 mg No. 100)ZiO-Zdorovye CJSC
RUB 1,558 order
- Ursosan (caps. 250 mg No. 10) Pro.Med.Cs.
RUB 176 order
- Ursosan (caps. 250 mg No. 50)ZiO-Zdorovye CJSC
RUR 792 order
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Pharmacy24
- Ursosan 250 mg No. 100 capsules PRO.MED.CS Prague a.t., Czech Republic/ PRO.MED.CS Prague a.s., Czech Republic
1022 UAH.order
PaniPharmacy
- Ursosan capsule Ursosan caps. 250 mg No. 50, PRO.MED.CS Prague
610 UAH. order
- Ursosan capsule Ursosan caps. 250 mg No. 100, PRO.MED.CS Prague
1048 UAH order
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Composition and release form
Ursosan, the instructions for use indicate this, contains ursodeoxycholic acid. Today, hepoprotective drugs based on it are considered the most effective.
The medicine is produced in the form of gelatin capsules filled with a mixture of white powder and powder granules in an amount of 250 mg. You can purchase Ursosan in blister packs of 10 or 20 capsules. The medicine is also offered in polyethylene jars containing 10, 20, 50 or 100 capsules. Cardboard packages must contain instructions for use.
