Ursofalk, 500 mg, film-coated tablets, 50 pcs.

Ursofalk, 500 mg, film-coated tablets, 50 pcs.

Inside.

Children and adults weighing less than 47 kg, as well as patients who cannot swallow Ursofalk in the form of film-coated tablets, are recommended to use Ursofalk in the form of a suspension.

Dissolution of Xc gallstones.

The recommended dose is 10 mg/kg/day.

Capsules

Oral suspension

Film-coated tablets

The drug must be taken daily in the evening, before bed (the capsules are not chewed), with a small amount of liquid.

Duration of treatment is 6–24 months. If after 12 months of treatment the size of the stones does not decrease, then treatment should be stopped. To prevent recurrent cholelithiasis, it is recommended to take the drug for several months after the stones have dissolved.

The effectiveness of treatment should be assessed every 6 months with ultrasound or radiography. During the interim examination, it is necessary to assess whether calcification of the stones has occurred during the intervening period. In case of calcification of stones, treatment should be discontinued.

Treatment of biliary reflux gastritis

1 capsule/1 measuring cup/0.5 tablet. (250 mg) of Ursofalk daily in the evening, before bedtime (the capsules are not chewed), washed down with a small amount of water.

The course of treatment is from 10–14 days to 6 months, if necessary – up to 2 years.

Treatment of primary biliary cirrhosis

The daily dose depends on body weight and ranges from 3 to 7 capsules / from 2 to 7 measuring cups / from 1.5 to 3.5 tablets. (from approximately (14±2) mg/kg UDCA).

In the first 3 months of treatment, the use of Ursofalk (capsules, film-coated tablets) should be divided into several doses throughout the day. After improvement of liver parameters, the daily dose of the drug can be taken 1 time in the evening.

The following mode of application is recommended:

Capsules

Oral suspension

Film-coated tablets

Capsules should be taken regularly, without chewing, with a small amount of liquid.

The use of Ursofalk for the treatment of primary biliary cirrhosis can be continued indefinitely.

In patients with primary biliary cirrhosis, in rare cases, clinical symptoms may worsen at the beginning of treatment, for example, itching may become more frequent. In this case, treatment should be continued, taking 1 capsule/0.5 tablet. daily, then gradually increase the dosage (increasing the daily dose weekly by 1 capsule/0.5 tablet) until the recommended dosage regimen is achieved again.

Symptomatic treatment of chronic hepatitis of various origins.

Daily dose: 10–15 mg/kg in 2–3 doses. Duration of treatment is 6–12 months or more.

Primary sclerosing cholangitis.

Daily dose - 12–15 mg/kg; if necessary, the dose can be increased to 20–30 mg/kg in 2–3 doses. The duration of therapy ranges from 6 months to several years (see “Special Instructions”).

Cystic fibrosis (cystic fibrosis).

Daily dose 12–15 mg/kg; if necessary, the dose can be increased to 20–30 mg/kg in 2–3 doses. The duration of therapy ranges from 6 months to several years.

Body weight more than 10 kg: UDCA dosage - 20–25 mg/kg/day. Measuring device - measuring cup.

Conversion table

Children weighing up to 10 kg get sick very rarely. In this case, a disposable syringe should be used.

Single doses for children weighing up to 10 kg should be measured using a syringe as the measuring cup provided is not designed for volumes less than 1.25 ml. Use a disposable 2 ml syringe in 0.1 ml increments. Please note that disposable syringes are not included in the package with the drug, but can be purchased at the pharmacy.

How to measure the required dose using a syringe:

1. Shake the bottle before opening.

2. Pour a small amount of suspension into a measuring cup, which is included in the package with the drug.

3. Fill the syringe with a slightly larger volume of the drug than required.

4. Tap the syringe with your fingers to remove air bubbles from the collected suspension.

5. Make sure that the required volume of suspension is in the syringe; if necessary, gain or release excess volume.

6. Carefully pour the contents of the syringe directly into the child’s mouth.

Do not insert the syringe into the vial. Do not pour unused suspension from the syringe or measuring cup back into the vial.

Body weight up to 10 kg: UDCA dosage - 20 mg/kg/day. The measuring device is a disposable syringe.

Film-coated tablets

Non-alcoholic steatohepatitis.

The average daily dose is 10–15 mg/kg in 2–3 doses. The duration of therapy ranges from 6–12 months or more.

Alcoholic liver disease.

The average daily dose is 10–15 mg/kg in 2–3 doses. The duration of therapy is 6–12 months or more.

Biliary dyskinesia.

The average daily dose is 10 mg/kg in 2 divided doses for 2 weeks to 2 months. If necessary, it is recommended to repeat the course of treatment.

Ursofalk 500 mg 50 pcs. film-coated tablets

pharmachologic effect

Hepatoprotective agent.

Composition and release form Ursofalk 500 mg 50 pcs. film-coated tablets

Tablets - 1 tablet:

• Active substance: Ursodeoxycholic acid - 500.00 mg;
• Excipients: microcrystalline cellulose - 23 mg, povidone K-25 - 15 mg, crospovidone (type A) - 12.5 mg, talc - 8.5 mg, magnesium stearate - 5 mg, colloidal silicon dioxide - 4 mg, polysorbate 80 - 2 mg, film coating: hypromellose - 5.7 mg, talc - 1.45 mg, macrogol-6000 - 0.85 mg

25 tablets per blister pack made of PVC / PVDC film / aluminum foil (blister).

2 blisters along with instructions for medical use in a cardboard box with first opening control.

Description of the dosage form

Biconvex, oblong-shaped tablets, white film-coated, scored on both sides.

Directions for use and doses

For patients who cannot swallow Ursofalk, 500 mg film-coated tablets, or whose body weight is less than 47 kg, it is recommended to use Ursofalk capsules or suspension. The tablets should be taken without chewing, with liquid. They should be taken regularly.

Dissolution of cholesterol gallstones

The recommended dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight per day, which corresponds to:

It usually takes 6-24 months for gallstones to dissolve. If after 12 months of treatment the size of the stones does not decrease, then treatment should be stopped.

The effectiveness of treatment should be assessed every 6 months with ultrasound or radiography. During the interim examination, it is necessary to assess whether calcification of the stones has occurred during the intervening period. In case of calcification of stones, treatment should be discontinued.

Treatment of biliary reflux gastritis

250 mg (½ tablet) daily in the evening before bed.

The course of treatment is from 10-14 days to 6 months, if necessary - up to 2 years.

Treatment of primary biliary cirrhosis

The daily dose depends on body weight and varies from 1½ to 2½ tablets (14 ± 2 mg ursodeoxycholic acid per 1 kg of body weight).

During the first 3 months of treatment, the daily dose should be divided into several doses. After improving the functional parameters of the liver, you can switch to a single daily dose in the evening.

The use of Ursofalk for the treatment of primary biliary cirrhosis can be continued indefinitely.

In patients with primary biliary cirrhosis, in rare cases, clinical symptoms may worsen at the beginning of treatment, for example, itching may become more frequent. In this case, treatment should be continued, taking ½ tablet daily, then the dose should be gradually increased (increasing the daily dose weekly by ½ tablet) until the recommended dosage regimen is achieved again.

Symptomatic treatment of chronic hepatitis of various origins is a daily dose of 10-15 mg/kg in 2-3 doses. Duration of treatment is 6-12 months or more.

Primary sclerosing cholangitis - daily dose 12-15 mg/kg; if necessary, the dose can be increased to 20 mg/kg in 2-3 doses. The duration of therapy ranges from 6 months to several years.

Cystic fibrosis (as part of complex therapy) - daily dose of 20 mg/kg/day in 2-3 divided doses, with a further increase to 30 mg/kg/day if necessary.

Non-alcoholic steatohepatitis - average daily dose of 10-15 mg/kg in 2-3 doses. The duration of therapy ranges from 6-12 months or more.

Alcoholic liver disease - average daily dose of 10-15 mg/kg in 2-3 doses. The duration of therapy ranges from 6-12 months or more.

Biliary dyskinesia - average daily dose of 10 mg/kg in 2 divided doses for 2 weeks to 2 months. If necessary, it is recommended to repeat the course of treatment.

Pharmacodynamics

Hepatoprotective agent, has a choleretic effect. Reduces cholesterol synthesis in the liver, its absorption in the intestines and concentration in bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and secretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids; causes increased gastric and pancreatic secretion, enhances lipase activity, and has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones when administered enterally, reduces the saturation of bile with cholesterol, which promotes the mobilization of cholesterol from gallstones. It has an immunomodulatory effect, affects immunological reactions in the liver: it reduces the expression of certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, the formation of interleukin-2, and reduces the number of eosinophils.

Pediatric population

Cystic fibrosis (cystic fibrosis)

According to clinical reports, there is many years of experience (up to 10 years or more) in treating pediatric patients with cystic fibrosis-associated hepatobiliary disease (CFAHD) with ursodeoxycholic acid. There is evidence that ursodeoxycholic acid therapy can reduce bile duct proliferation, slow the development of lesions detected by histological examination, and even promote the reversal of changes in the hepatobiliary system if therapy is started in the early stages of CFAHD. To optimize treatment efficacy, ursodeoxycholic acid therapy should be initiated as soon as possible after the diagnosis of CFAHD.

Pharmacokinetics

After oral administration, ursodeoxycholic acid is rapidly absorbed in the jejunum and proximal ileum by passive diffusion, and in the distal ileum by active transport. Approximately 60-80% of the dose taken is absorbed. After absorption, ursodeoxycholic acid is almost completely conjugated in the liver with glycine and taurine and excreted in the bile. During the first passage through the liver, up to 60% is metabolized.

Depending on the daily dose, the type of disease and the condition of the liver, more or less amount of ursodeoxycholic acid accumulates in the bile. At the same time, there is a relative decrease in the content of other, more lipophilic bile acids.

Under the influence of intestinal bacteria, ursodeoxycholic acid is partially degraded to form 7-keto-lithocholic and lithocholic acid. Lithocholic acid is hepatotoxic; in some animal species it causes damage to the liver parenchyma. In the human body it is absorbed only in small quantities. During the process of metabolism, it is sulfated in the liver, due to which it is neutralized even before it is excreted into bile and excreted from the body with feces. The half-life of ursodeoxycholic acid is 3.5 to 5.8 days.

Indications for use Ursofalk 500 mg 50 pcs. film-coated tablets

Dissolution of cholesterol gallstones, biliary reflux gastritis, primary biliary cirrhosis in the absence of signs of decompensation, chronic hepatitis of various origins, primary sclerosing cholangitis, cystic fibrosis, non-alcoholic steatohepatitis, alcoholic liver disease, biliary dyskinesia.

Contraindications

X-ray positive (high calcium) gallstones; impaired contractility of the gallbladder, blockage of the bile ducts (blockage of the common bile duct or cystic duct), frequent episodes of biliary colic; acute inflammatory diseases of the gallbladder and bile ducts; liver cirrhosis in the stage of decompensation; severe liver and/or renal failure, hypersensitivity to the components of the drug or other bile acids.

Pediatric population

Unsuccessfully performed portoenterostomy or cases of failure to restore normal bile flow in children with biliary atresia.

Ursodeoxycholic acid has no age restrictions for use, but children under 3 years of age are recommended to use Ursofalk in suspension, as difficulties may arise when swallowing capsules.

Application of Ursofalk 500 mg 50 pcs. film-coated tablets during pregnancy and breastfeeding

According to animal studies, ursodeoxycholic acid has no effect on fertility. There are no data on the effects of ursodeoxycholic acid treatment on fertility in humans.

There are limited or no data on the use of ursodeoxycholic acid in pregnant women. Animal studies have shown reproductive toxicity in early pregnancy. Ursofalk should not be used during pregnancy, unless clearly necessary. The use of the drug by women of childbearing potential is only possible if they use reliable methods of contraception. It is recommended to use non-hormonal contraceptives or oral contraceptives with low estrogen content. However, patients taking Ursofalk to dissolve gallstones should use effective non-hormonal contraceptives, as hormonal oral contraceptives may increase the formation of gallstones. The possibility of pregnancy should be excluded before starting treatment.

Based on several documented case reports, the level of ursodeoxycholic acid in breast milk in women is very low and therefore adverse reactions are not expected in breastfed infants.

special instructions

Ursofalk should be taken under medical supervision.

During the first three months of treatment, liver function parameters should be monitored: transaminases, alkaline phosphatase and gamma-glutamyl transpeptidase in the blood serum every 4 weeks and then every 3 months. Monitoring these parameters makes it possible to identify liver dysfunction in the early stages. This also applies to patients in the later stages of primary biliary cirrhosis. In addition, it can quickly determine whether a patient with primary biliary cirrhosis is responding to treatment.

When used to dissolve cholesterol gallstones:

In order to assess progress in treatment and to promptly detect signs of calcification of stones depending on the size of the stones, the gallbladder should be visualized (oral cholecystography) with examination of opacities in the standing and supine position (ultrasound) 6-10 months after the start of treatment .

If the gallbladder cannot be visualized on x-rays or in cases of calcified stones, poor contractility of the gallbladder or frequent attacks of colic, Ursofalk should not be used.

Patients taking Ursofalk to dissolve gallstones should use effective non-hormonal methods of contraception, as hormonal contraceptives may increase the formation of gallstones.

When treating patients in the later stages of primary biliary cirrhosis:

Cases of decompensation of liver cirrhosis have been reported extremely rarely. After cessation of therapy, a partial reverse development of the manifestations of decompensation was noted.

In patients with primary biliary cirrhosis, in rare cases, at the beginning of treatment, clinical symptoms may increase, for example, itching may increase. In this case, the dose of the drug must be reduced and then gradually increased again, as described in the “Method of administration and dosage” section.

When used in patients with primary sclerosing cholangitis: Long-term therapy with high doses of ursodeoxycholic acid (28-30 mg/kg/day) in patients with this pathology can cause serious side effects.

In patients with diarrhea, the dosage of the drug should be reduced. If diarrhea persists, treatment should be discontinued.

Impact on the ability to drive vehicles and operate machinery

Ursodeoxycholic acid does not affect the ability to drive vehicles and machines, or the effect is minimal.

Overdose

In case of overdose, diarrhea is possible. As a rule, other symptoms of overdose are unlikely, since as the dose increases, the absorption of ursodeoxycholic acid decreases and, accordingly, more of it is excreted in the feces. There is no need to use specific measures in case of overdose. Treatment of the consequences of diarrhea is symptomatic, aimed at replenishing fluid volume and restoring electrolyte balance.

Side effects Ursofalk 500 mg 50 pcs. film-coated tablets

The assessment of adverse events is based on the following classification: Very common (≥ 1/10); Frequent (≥ 1/100 -

Gastrointestinal disorders:

In clinical studies, loose stools or diarrhea were common during treatment with ursodeoxycholic acid.

During the treatment of primary biliary cirrhosis, acute pain in the right upper abdomen was very rarely observed.

Disorders of the liver and biliary tract:

In very rare cases, calcification of gallstones may occur during treatment with ursodeoxycholic acid.

When treating advanced stages of primary biliary cirrhosis, decompensation of liver cirrhosis was observed in very rare cases, which disappears after discontinuation of the drug.

Disorders of the skin and subcutaneous tissues:

In very rare cases, allergic reactions, including urticaria, may occur.

If any of the side effects indicated in the instructions get worse, or you notice other side effects not listed in the instructions, please inform your doctor.

Drug interactions

Cholestyramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce the absorption of ursodeoxycholic acid in the intestine and thus reduce its absorption and effectiveness. If the use of drugs containing at least one of these substances is still necessary, they should be taken at least 2 hours before taking Ursofalk.

Ursodeoxycholic acid may interfere with the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the physician should check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine if necessary.

In some cases, Ursofalk may reduce the absorption of ciprofloxacin.

In a clinical study in healthy volunteers, co-administration of ursodeoxycholic acid (500 mg/day) and rosuvastatin (20 mg/day) resulted in a slight increase in plasma rosuvastatin levels. The clinical significance of this interaction, including with other statins, is unknown.

In healthy volunteers, ursodeoxycholic acid has been shown to reduce peak plasma concentrations (Cmax) and area under the concentration-time curve (AUC) of the slow calcium channel blocker nitrendipine. In case of concomitant use of nitrendipine and ursodeoxycholic acid, careful monitoring is recommended. The dose of nitrendipine may need to be increased. There are also reports of interactions with dapsone, which led to a decrease in the therapeutic effect of the latter. These observations, along with data from in vitro experiments, suggest that ursodeoxycholic acid is capable of inducing enzymes of the cytochrome P450 3A system. However, in a designed interaction study with budesonide, which is a known substrate of cytochrome P450 3A, no induction was noted.

Estrogen hormones and blood cholesterol-lowering drugs such as clofibrate increase cholesterol secretion in the liver and therefore may stimulate the formation of gallstones, which counteracts the effect of ursodeoxycholic acid, which is used to dissolve gallstones.