active substance: ursodeoxycholic acid;
1 capsule contains 250 mg of ursodeoxycholic acid;
excipients: starch maize, silica colloidal anhydrous, magnesium stearate, titanium dioxide (E 171), gelatin, purified water, sodium lauryl sulfate.
Dosage form. Capsules.
Basic physical and chemical properties: white, opaque hard gelatin capsules size "0" containing a white compressed powder or granules.
Drugs used to treat liver and biliary tract. Agents used in biliary pathology.
ATC code A02 А05А.
Remedies used for liver diseases, lipotropic agents.
Code ATX А05В.
A small amount of ursodeoxycholic acid found in human bile.
After oral administration it reduces the saturation of bile with cholesterol by inhibiting its absorption in the intestine and shigeyuki secretion of cholesterol in bile. Perhaps due to the dispersion of cholesterol and formation of liquid crystals is a gradual dissolution of gallstones.
In accordance with modern knowledge I think that the effect of ursodeoxycholic acid in liver disease and cholestas due to the relative replacement of lipophilic, detergent-like, toxic bile acids are cytoprotective hydrophilic non-toxic ursodeoxycholic acid, to improve the secretory capacity of hepatocytes and mucoregulatory processes.
The use of children
Available information from clinical reports regarding the long-ursodeoxycholic acid (within a period of 10 years) in the treatment of children with hepatobiliary disorders associated with cystic fibrosis. There is evidence in favor of the fact that the use of ursodeoxycholic acid can reduce proliferation in bile ducts, stopping the progression of histological changes and even eliminate hepatobiliary changes, provided they are treated 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 the bile acid undergoes in the liver almost complete conjugation with the amino acids glycine and taurine and then excreted in the bile. Clearance of the first passage through the liver is 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-katolickiej and lithocholic acids. Litojolevu acid is hepatotoxic and causes damage to the liver parenchyma in some animal species. In humans, absorbed only a small quantity of it, which sulfatides in the liver and thus detoxifierea, before being deduced with bile and finally in the feces.
The biological half-life of ursodeoxycholic acid is 3.5-5.8 days.
Rentgenonegativee for dissolution of cholesterol gall stones not larger than 15 mm in diameter in patients with functioning gallbladder, despite presence of gall(s) a stone(NIV).
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 hepatobiliary disorders in cystic fibrosis in children aged 6 to 18 years.
Hypersensitivity to any substance included in the composition of the drug.
Acute inflammation of the gallbladder or bile ducts.
Obstruction of the bile duct (blockage of the common bile duct, or duct of the bladder).
Frequent episodes of hepatic colic.
Calcifur radiopaque stones gallbladder.
Violations of the contractility of the gallbladder.
Bad result portoenterostomy or lack of adequate biliary outflow in children with atresia of the biliary tract.
Interaction with other medicinal products and other forms of interaction.
Ursofalk capsules of 250 mg do not use simultaneously with kolestiraminom, kolestipola or antacids containing aluminium hydroxide and/or smectite, as these drugs bind ursodezoksiholeva acid in the intestine and, thus, prevent its absorption and reduce effectiveness. If the use of drugs containing one of these substances, it is necessary, they should be taken at least 2 hours before or 2 hours after taking the capsules of Ursofalk 250 mg.
Ursofalk capsules of 250 mg may enhance the absorption of cyclosporin from the gut. In patients taking cyclosporine, your doctor should check the concentration of this substance in the blood and if necessary to 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 ursodeoxycholic acid (500 mg/day) and rosuvastatin (20 mg/day) resulted in a slight increase the concentration of rosuvastatin in plasma. The clinical significance of this interaction and the importance relative to other statins, is unknown.
It is proven that ursodeoxycholic acid reduces peak plasma concentration (Cmax) and area under the curve (AUC) of the calcium antagonist nitrendipine in healthy volunteers. It is recommended that careful observation of the result of the combined application of nifedipine and ursodeoxycholic acid. It may be necessary to increase the dose of nifedipine.
In addition, it was reported the weakening of therapeutic action of the Dapsone.
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 interaction with budesonide 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, which is the opposite effect to ursodeoxycholic acid used for dissolution.
The drug Ursofalk 250 mg capsules should be administered under the supervision of a physician.
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 gives the ability to determine the presence or absence of response to treatment in patients with PBTs, and timely detect potential violations of the liver, especially in patients with PBTs in the later stages.
Application for dissolution of cholesterol gallstones
In order to assess the progress in the treatment and for timely detection of any signs of calcification of the stones depending on stone size should be the visualization of the gallbladder (oral cholecystography) with a tour of the blackouts with the patient standing and supine positions (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 the stones, the violation of the contractility of the gall bladder or common 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
Rarely reported decompensation of liver cirrhosis which partially may regress after cessation of therapy.
In patients with PBC is very rare may increase symptoms in the beginning of treatment, for example, itching can be intensified. 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 diarrhoea should reduce the dosage; if the diarrhea does not stop, should stop treatment.
Use during pregnancy or breastfeeding
Studies in animals have not shown an effect ursodeoxycholic acid on fertility. Data on the effect on fertility in humans.
Data regarding the use of ursodeoxycholic acid for pregnant women is insufficient. 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. 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 documented cases of using the drug in women who breastfeed, the content of ursodeoxycholic acid in milk was very low, so you should not expect the development of any adverse events among children who receive 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.
Shelf life. 5 years. The drug should not be used after the expiry date stated on the package.
Storage conditions. Does not require special storage conditions. Keep out of reach of children.
10 capsules per blister; 1 blister in a carton made of cardboard.
25 capsules in a blister, 2 or 4 blisters in a carton made of cardboard.