active substance: ursodeoxycholic acid
1 capsule contains 250 mg of ursodesoxycholic acid
auxiliary substances: corn starch, silicon dioxide colloidal, magnesium stearate, titanium dioxide (E 171), gelatin, purified water, sodium lauryl sulfate.
Basic physico-chemical properties: white opaque hard gelatin capsules of size "0", containing white pressed powder or granules.
Drugs used to treat liver and biliary tract. Agents used in biliary pathology.
Code ATH A05A A02.
Means used in liver diseases, lipotropic substances.
A05v ATH code.
A small amount of ursodesoxycholic acid is found in human bile.
After oral administration, it reduces the saturation of bile cholesterol, suppressing its absorption in the intestine and reducing the secretion of cholesterol in the bile. Perhaps, thanks to the dispersion of cholesterol and the formation of liquid crystals there is a gradual dissolution of gallstones.
According to our present knowledge I believe that the effect of ursodeoxycholic acid in liver disease and cholestasis due to the relative lipophilic substitution, such detergents toxic bile acid cytoprotective hydrophilic non-toxic ursodeoxycholic acid, to improve the secretory capacity of hepatocytes and immunoregulatory processes.
the use of children
The user from the clinical reports concerns the long - term use of ursodesoxycholic acid (for a period of up to 10 years) in the treatment of children with hepatobiliary disorders associated with cystic fibrosis. There is evidence that the use of ursodesoxycholic acid can reduce proliferation in the bile ducts, stop the progression of histological changes and even eliminate hepatobiliary changes, provided the beginning of therapy in the early stages of cystic fibrosis. For better treatment efficacy with the use of ursodeoxycholic acid should be initiated immediately after the diagnosis of cystic fibrosis.
After oral administration, ursodeoxycholic acid is rapidly absorbed in the jejunum and upper ileum intestine by passive transport, and in the terminal the ileum by active transport. The absorption rate is usually 60-80%. After absorption of bile acid in the liver is subject to almost complete conjugation with the amino acids glycine and taurine and then excreted in the bile. Clearance of the first pass through the liver is up to 60%.
Depending on the daily dose and the primary infringement or liver condition are more hydrophilic ursodeoxycholic acid cumulates in the bile. At the same time, there is a relative decrease of other more lipophilic bile acids.
Under the influence of intestinal bacteria partial degradation to 7-katolickiego and litojoleva acids. Litojoleva acid is hepatotoxic and causes damage to the liver parenchyma in some animal species. In humans, only a small amount of it is absorbed, which in the liver is sulfated and thus detoxified, before being excreted with bile and, finally, with feces.
The biological half-life of ursodeoxycholic acid is 3.5-5.8 days.
To dissolve x-ray cholesterine gallstones of size no more than 15 mm in diameter in patients with functioning gallbladder, despite the presence of bile (new) stone in it.
For the treatment of biliary reflux gastritis.
For the symptomatic treatment of primary biliary cirrhosis (PBC) in absence of decompensated liver cirrhosis.
For the treatment of hepatobiliary disorders in cystic fibrosis in children aged 6 to 18 years.
Hypersensitivity to any substance that is part of the drug.
Acute inflammation of the gallbladder or bile ducts.
Obstruction of the bile ducts (blockage of the common bile duct or duct).
Frequent episodes of hepatic colic.
Radio-opaque calcified gallstones.
Violation of contractility of the gallbladder.
An unsuccessful result of portoenterostomy or lack of adequate bile outflow in children with biliary atresia.
Interaction with other medicinal products and other forms of interaction.
Ursofalk 250 mg should not be used in conjunction with cholesterol, colestipol or antacids containing aluminium hydroxide and/or smectitis, since these drugs bind ursodesoxycholic acid in the intestine and thus prevent its absorption and reduce efficiency. If the use of drugs containing one of these substances, it is necessary, they should be taken at least 2:00 or 2:00 after ingestion of capsules of 250 mg. Ursofalk
Ursofalk 250 mg can increase the absorption of ciclosporin from the intestine. In patients taking cyclosporine, the doctor should check the concentration of this substance in the blood and, if necessary, adjust the dose of cyclosporine.
In some cases, capsules of Ursofalk 250 mg can reduce the absorption of ciprofloxacin.
In a clinical study in healthy volunteers, the combined use of ursodesoxycholic acid (500 mg/day) and rosuvastatin (20 mg/day) led to some increase in the concentration of rosuvastatin in plasma. The clinical significance of this interaction, as well as the significance in other statins, is unknown.
Ursodesoxycholic acid has been shown to reduce peak plasma concentrations (C max ) and the area under the nitrendipine calcium antagonist (AUC) curve in healthy volunteers. It is recommended that careful observation of the result of the combined application of nifedipine and ursodeoxycholic acid. You may need to increase the dose of nifedipine.
In addition, the therapeutic effects of Dapsone were reported to have decreased.
The information and data obtained in vitro , suggest that ursodeoxycholic acid could potentially cause the induction of enzymes of cytochrome P450 3A. But well-designed study of the interaction budesonida that is a proven substrate of cytochrome P450 3A, a similar effect was not observed.
Estrogenic hormones, and drugs to reduce the concentration of cholesterol in the blood can increase the secretion of cholesterol by the liver and thus contribute to stone formation in the gallbladder, is the opposite effect to ursodeoxycholic acid used for dissolution.
Taking The drug Ursofalk 250 mg capsules should be under the supervision of a doctor.
During the first three months of treatment the functional indices of liver function (AST, ALT and GGT) should be monitored every 4 weeks and later once in three months. This makes it possible to determine the presence or absence of a response to treatment in patients with PBTs, as well as timely identify potential liver disorders, especially in patients with PBTs at late stages.
Application for dissolution of cholesterol gallstones
In order to assess the progress in the treatment, as well as for the timely detection of any signs of calcification of stones, depending on the size of the stones, it is necessary to visualize the gallbladder (oral cholecystography) with an examination of eclipses in the patient's standing and lying on his back (under ultrasound control) 6-10 months after the start of treatment.
Ursofalk 250 mg capsules should not be used if the gallbladder cannot be visualized on x-rays or in the case of calcification of stones, violation of the contractile gallbladder or frequent hepatic colic.
Women taking Ursofalk 250 mg capsules for dissolution of gallstones should use an effective nonhormonal method of contraception, since hormonal contraceptives may increase the formation of stones in the gallbladder.
Treatment of patients with PBC at a later stage
Very rarely reported decompensation of cirrhosis, which may partially regress after discontinuation of therapy.
In patients with PBTs, very rarely can symptoms increase at the beginning of treatment, for example, itching may increase. In such cases, the dose of Ursofalk 250 mg capsules should be reduced to one capsule of Ursofalk 250 mg per day then the dose can be increased, as described in the section "Method of administration and doses".
When diarrhea occurs, the dosage should be reduced; if diarrhea does not stop, it should be stopped.
Application during pregnancy and lactation
Studies in animals have not shown the effect of ursodesoxycholic acid on fertility. Data on the impact on fertility in humans are not available.
Data on the use of ursodeoxycholic acid for pregnant women is insufficient. The results of animal studies indicate the presence of reproductive toxicity in the early stages of pregnancy. Ursofalk 250 mg capsules should not be used during pregnancy, except in cases of extreme necessity. Women of childbearing age can take the drug only if they use reliable contraception.
It is recommended to use non-hormonal contraceptives or oral contraceptives with low estrogen content. Patients who get Ursofalk 250 mg capsules for dissolution of gallstones should use an effective non-hormonal contraceptives, as hormonal oral contraceptives may increase stone formation in the gallbladder. Before treatment should rule out the possibility of pregnancy.
According to several recorded cases of use of the drug during breastfeeding, the content of ursodesoxycholic acid in milk was extremely low, so do not expect the development of any adverse events in children receiving such milk.
The ability to influence the reaction rate when driving motor transport or operating other mechanisms
Effects on ability to drive and use machinery has not been observed.
Way applications and doses
For patients, body weight less than 47 kg or who have difficulty swallowing capsules of Ursofalk available another pharmaceutical form of Ursofalk - suspension.
For dissolution of cholesterol gallstones
Approximately 10 mg of ursodeoxycholic acid per kg of body weight (see Table.One)
body mass capsules
up to 60 kg
more than 100 kg
Capsules should be swallowed whole, with water, 1 time a day in the evening before going to bed.
Capsules should be taken regularly.
It is necessary for dissolution of gallstones time usually makes 6-24 months. If reducing the size of gall stone is not observed after 12 months of treatment to continue therapy should not be.
The success of treatment should be checked every 6 months using ultrasound or x-ray studies. Additional research needs to be checked, over time calcification of stones didn't take place. If this happens, treatment should be stopped.
For the treatment of biliary reflux gastritis
1 capsule of Ursofalk 250 mg once daily with some liquid in the evening before bed.
Usually for treatment of gastritis with bile reflux Ursofalk capsules of 250 mg taken for 10-14 days. The duration of treatment depends on the patient's condition. The doctor must decide on the duration of treatment in each case individually.
For the symptomatic treatment of primary biliary cirrhosis (PBC)
The daily dose depends on body weight and varies from 3 to 7 capsules (14 ± 2 mg of ursodeoxycholic acid/kg body weight).
In the first 3 months of treatment Ursofalk capsules of 250 mg should be taken in the course of a day, dividing the daily dose into 3 doses. When improving liver function dose can be taken once a day in the evening.
Body weight (kg)daily dose
(Mg/kg body weight)capsules
the first 3 mesyatsev further
(1 times a day)
more than 110 2237
Capsules need to be swallowed whole, liquid squeezed. It is necessary to observe regularity of reception.
The use of capsules of Ursofalk 250 mg with primary biliary cirrhosis may be unlimited in time.
In patients with primary biliary cirrhosis rarely at the beginning of treatment may worsen clinical symptoms, for example, itching may increase. In this case, treatment should continue, taking 1 capsule of Ursofalk 250 mg daily, then gradually increase the dose (increasing each week, the daily dose in 1 capsule) to achieve the assigned dosing regimen.
the use of children
For children with cystic fibrosis aged 6 to 18 years, the dosage is 20 mg/kg/day and is divided into 2-3 admission, followed by an increase in the dose to 30 mg/kg/day if necessary.
Ursofalk, capsules of 250 mg
20 - 2917-251-
30 - 3919-25111
40 - 4920-25112
50 - 5921-25122
60 - 6922-25222
70 - 7922-25223
80 - 8922-25233
90 - 9923-25333
100 - 10923-25334
> 110 344
For dissolution of cholesterol gallstones, treatment of biliary reflux gastritis and symptomatic treatment of PBC:
There are no principal age limits for the use of Ursofalk children but if the child weighs less than 47 kg and/or if the child has difficulty swallowing, it is recommended to apply Ursofalk in suspension.
For the treatment of hepatobiliary disorders in cystic fibrosis:
Apply to children aged 6 to 18 years.
In cases of overdose, diarrhea is possible. Other symptoms of overdose are unlikely, since the absorption of ursodeoxycholic acid decreases with increasing doses and therefore most of its amount is excreted with feces.
In case of diarrhea dose should be reduced, and if the diarrhea is constant, therapy should be stopped.
There is no need for specific events. The effects of diarrhea should be treated symptomatically, with the restoration of the balance of fluid and electrolytes.
Additional information on specific groups of patients
Long-term therapy with high doses of ursodesoxycholic acid (28-30 mg/kg/day) in patients with primary sclerosing cholangitis (use for unregistered indications) was associated with a higher frequency of serious adverse events.
The assessment of the frequency of adverse reactions is based on the following data:
Very often > 1/10.
Often > 1/100 and <1/10.
Infrequently > 1/10 00 and <1/100.
Rarely > 1/10 000 and <1/1 000.
Very rarely <1/10 000, including individual cases.
The gastro-intestinal tract
In clinical studies, there have been frequent reports of pasty stools or diarrhea throughout the treatment with ursodeoxycholic acid.
Very rarely for the treatment of primary biliary cirrhosis were characterized by a strong abdominal pain localized in the right hypochondrium.
From the liver and gallbladder
Very rarely in the treatment of ursodesoxycholic acid possible calcification of gallstones.
During the treatment of advanced stages of primary biliary cirrhosis very rarely observed decompensation of cirrhosis, which partially regressed after treatment.
Very rarely possible allergic reactions, including rash, urticaria.
The drug can not be used after the expiration date indicated on the package.
Does not require special storage conditions. Keep out of reach of children.
10 capsules in a blister, 1 blister in a cardboard box.
At 25 capsules per blister, 2 or 4 blisters in a carton made of cardboard.
Category home away from home
Dr. Falk Pharma GmbH.
Manufacturer's location and address of the place of business
D-79108 Freiburg, Germany.
CAPSULES 250MG URSOSAN NUMBER 50
Ursosan capsules 250 mg № 50-hepatoprotector, which is assigned to the primary biliary cirrhosis and reflux gastritis. Also, the tool is used for sclerosing cholangitis, hepatitis, cholelithiasis and other diseases of the biliary tract.
The drug is prescribed by the doctor after the examination. The medicine is used orally before meals. Capsules should be swallowed without chewing, drinking water. Typically, the daily dose upotreblyaetsya in 1 reception. It is best to use capsules before going to bed. Long-term therapeutic result is observed with regular admission Ursosan.
Recommendations for the treatment of cholesterol gallstones:
Calculation of the daily dosage: 10 mg per 1 kg of weight.
The duration of admission-6 months-2 years.
Every six months held ultrasound and x-ray study of the rocks.
The first months of use requires systematic monitoring of liver enzymes.
If calcined concrements are detected, the drug is stopped.
Gastritis with bile reflux may be treated with the use of one capsule 1 time a day course of 10-14 days. According to the indications, the course of therapy is prolonged.
For the treatment of primary biliary cirrhosis daily dose is calculated: 14 mg per 1 kg of body weight. The norm is divided into 3 doses. Rarely at the beginning of use of the drug, the patient's condition may worsen. To eliminate the symptoms, the daily rate is reduced to 250 mg.