Ursofalk capsules 250 mg No. 50
Compound
Active substance: ursodeoxycholic acid - 250 mg. Excipients: corn starch - 73 mg, colloidal silicon dioxide - 5 mg, magnesium stearate - 2 mg, titanium dioxide - 1.94 mg, gelatin - 80.51 mg, sodium lauryl sulfate - 0.2 mg, purified water - 14.55 mg.
Pharmacokinetics
Absorbed in the jejunum due to passive diffusion, in the ileum - due to active transport. When taken orally in a single dose of 500 mg, the concentration in the blood serum after 30, 60 and 90 minutes is 3.8, 5.5 and 3.7 µmol/l, respectively.
When taken systematically, ursodeoxycholic acid (UDCA) becomes the main bile acid in the blood serum (48% of the total bile acid content). Included in the enterohepatic circulation system. The therapeutic effectiveness of the drug depends on the concentration of UDCA in bile. During therapy, there is a dose-dependent increase in the proportion of UDCA in the bile acid pool to 50-75% (at daily doses of 10-20 mg/kg). Penetrates through the placental barrier.
Indications for use
- dissolution of cholesterol gallstones;
- biliary reflux gastritis;
- primary biliary cirrhosis of the liver in the absence of signs of decompensation (symptomatic treatment);
- chronic hepatitis of various origins;
- primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis);
- non-alcoholic steatohepatitis;
- alcoholic liver disease;
- biliary dyskinesia.
Contraindications
- X-ray positive (high calcium content) gallstones; non-functioning gallbladder;
- acute inflammatory diseases of the gallbladder, bile ducts and intestines;
- liver cirrhosis in the stage of decompensation;
- severe dysfunction of the kidneys, liver, pancreas;
- hypersensitivity to the components of the drug.
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.
Directions for use and doses
Dissolution of cholesterol gallstones
Approximately 10 mg per 1 kg of body weight daily, which corresponds to:
- 2 capsules (2 measuring spoons) Ursofalk in patients weighing up to 60 kg;
- 3 capsules (3 measuring spoons) Ursofalk in patients weighing up to 80 kg;
- 4 capsules (4 measuring spoons) Ursofalk for patients weighing up to 100 kg.
Capsules should be taken in the evening, before going to bed, without chewing and with a small amount of liquid. Duration of treatment is 6-12 months. To prevent recurrent cholelithiasis, it is recommended to take the drug for several months after the stones have dissolved.
Treatment of biliary reflux gastritis
1 capsule (1 scoop) Ursofalk daily. The course of treatment is from 10-14 days to 6 months, if necessary - up to 2 years.
Symptomatic treatment of primary biliary cirrhosis
The daily dose depends on body weight and ranges from 2 to 6 capsules (measuring spoons) (approximately 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight).
The following mode of application is recommended:
- Body weight 34-50 kg: 2 capsules (measuring spoons, daily dose); in the morning - 1, in the afternoon - -, in the evening - 1.
- Body weight 51-65 kg: 3 capsules (measuring spoons, daily dose); in the morning - 1, in the afternoon - 1, in the evening - 1.
- Body weight 66-85 kg: 4 capsules (measuring spoons, daily dose); in the morning - 1, in the afternoon - 1, in the evening - 2.
- Body weight 86-110 kg: 5 capsules (measuring spoons, daily dose); in the morning - 1, in the afternoon - 2, in the evening - 2.
- Body weight over 110 kg: 6 capsules (measuring spoons, daily dose); in the morning - 2, in the afternoon - 2, in the evening - 2.
Storage conditions
Store out of the reach of children at a temperature not exceeding 25 °C.
Best before date
5 years. Do not use after the expiration date stated on the package.
special instructions
For successful litholysis with ursodeoxycholic acid, the following conditions must be met: the stones must be purely cholesterol, i.e. do not give a shadow on the radiograph; the size of the stones should not exceed 15-20 mm; the gallbladder must fully maintain its function; the gallbladder should be no more than half filled with stones; patency of the cystic duct should be maintained; The common bile duct should be free of stones.
When using ursodeoxycholic acid to dissolve gallstones in the first 3 months of treatment, it is necessary to determine the activity of liver transaminases every 4 weeks. In the future, these studies can be carried out at intervals of 3 months.
To monitor the effectiveness of treatment, it is recommended to conduct x-ray and ultrasound examination of the biliary tract every 6 months.
To prevent relapses of cholelithiasis, treatment must be continued for several months after the gallstones have dissolved.
Description
Hepatoprotective agent.
Dosage form
Hard gelatin capsules, size No. 0, opaque, white; the contents of the capsules are white powder or granules.
Use in children
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.
Action
Hepatoprotector. Ursodeoxycholic acid is a bile acid. Reduces cholesterol content in bile mainly by dispersing cholesterol and forming a liquid crystalline phase. It affects the enterohepatic circulation of bile salts, reducing the reabsorption in the intestine of endogenous, more hydrophobic and potentially toxic compounds.
In vitro studies have shown that ursodeoxycholic acid has a direct hepatoprotective effect and reduces the hepatotoxicity of hydrophobic bile salts.
It influences immunological reactions, reducing the pathological expression of class I HLA antigens on hepatocytes and suppressing the production of cytokines and interleukins.
Ursodeoxycholic acid reduces the lithogenic index of bile, increasing the content of bile acids in it. Promotes partial or complete dissolution of cholesterol gallstones when administered orally. Has a choleretic effect.
Side effects
Gastrointestinal disorders:
In clinical studies, loose stools or diarrhea were frequently observed 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, in very rare cases, decompensation of liver cirrhosis was observed, which disappears after discontinuation of the drug.
Disorders of the skin and subcutaneous tissues:
In very rare cases, 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.
Use during pregnancy and breastfeeding
Ursodeoxycholic acid should not be used during pregnancy.
Women of childbearing age during treatment with ursodeoxycholic acid are recommended to use non-hormonal contraceptives or contraceptives with low estrogen content.
It is not known whether ursodeoxycholic acid is excreted in breast milk.
Interaction
When used simultaneously with cyclosporine, absorption increases unpredictably and the concentration of cyclosporine in the blood plasma increases.
A case of a decrease in the concentration of ciprofloxacin in the blood plasma in a patient receiving ursodeoxycholic acid is described.
Overdose
No cases of overdose have been identified. In case of overdose, symptomatic treatment is carried out.
Impact on the ability to drive vehicles and operate machinery
There was no effect on the ability to drive vehicles and moving machinery.
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
| Body weight, kg | Number of capsules, pcs. |
| up to 60 | 2 |
| 61–80 | 3 |
| 81–100 | 4 |
| Over 100 | 5 |
Oral suspension
| Body weight, kg | Number of measuring spoons | Corresponding quantity, ml |
| 5–7 | 0,25 | 1,25 |
| 8–12 | 0,5 | 2,5 |
| 13–18 | 0,75 | 3,75 |
| 19–25 | 1 | 5 |
| 26–35 | 1,5 | 7,5 |
| 36–50 | 2 | 10 |
| 51–65 | 2,5 | 12,5 |
| 66–80 | 3 | 15 |
| 81–100 | 4 | 20 |
| Over 100 | 5 | 25 |
Film-coated tablets
| Body weight, kg | Number of film-coated tablets, pcs. |
| up to 60 | 1 |
| 61–80 | 1,5 |
| 81–100 | 2 |
| more than 100 | 2,5 |
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
| Body weight, kg | Daily dose (capsules, pcs.) | In the morning | During the day | In the evening |
| 47–62 | 3 | 1 | 1 | 1 |
| 63–78 | 4 | 1 | 1 | 2 |
| 79–93 | 5 | 1 | 2 | 2 |
| 94–109 | 6 | 2 | 2 | 2 |
| Over 110 | 7 | 2 | 2 | 3 |
Oral suspension
| Body weight, kg | Measuring cups Ursofalk, oral suspension 250 mg/5 ml | |||
| first 3 months | in the future | |||
| morning | day | evening | evening (single dose) | |
| 8–11 | — | 0,25 | 0,25 | 0,5 |
| 12–15 | 0,25 | 0,25 | 0,25 | 0,75 |
| 16–19 | 0,5 | — | 0,5 | 1 |
| 20–23 | 0,25 | 0,5 | 0,5 | 1,25 |
| 24–27 | 0,5 | 0,5 | 0,5 | 1,5 |
| 28–31 | 0,25 | 0,5 | 1 | 1,75 |
| 32–39 | 0,5 | 0,5 | 1 | 2 |
| 40–47 | 0,5 | 1 | 1 | 2,5 |
| 48–62 | 1 | 1 | 1 | 3 |
| 63–80 | 1 | 1 | 2 | 4 |
| 81–95 | 1 | 2 | 2 | 5 |
| 96–115 | 2 | 2 | 2 | 6 |
| More than 115 kg | 2 | 2 | 3 | 7 |
Film-coated tablets
| Body weight, kg | Daily dose, mg/kg | Ursofalk, film-coated tablets, 500 mg | |||
| first 3 months | in the future | ||||
| morning | noon | evening | evening (single dose) | ||
| 47–62 | 12–16 | 0,5 | 0,5 | 0,5 | 1,5 |
| 63–78 | 13–16 | 0,5 | 0,5 | 1 | 2 |
| 79–93 | 13–16 | 0,5 | 1 | 1 | 2,5 |
| 94–109 | 14–16 | 1 | 1 | 1 | 3 |
| more than 110 | — | 1 | 1 | 1,5 | 3,5 |
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.
| Body weight, kg | Daily dose of UDCA, mg/kg | Number of measuring cups of Ursofalk suspension 250 mg/5 ml | |
| Morning | Evening | ||
| 11–12 | 21–23 | 0,5 | 0,5 |
| 13–15 | 21–24 | 0,5 | 0,75 |
| 16–18 | 21–23 | 0,75 | 0,75 |
| 19–21 | 21–23 | 0,75 | 1 |
| 22–23 | 22–23 | 1 | 1 |
| 24–26 | 22–23 | 1 | 1,25 |
| 27–29 | 22–23 | 1,25 | 1,25 |
| 30–32 | 21–23 | 1,25 | 1,5 |
| 33–35 | 21–23 | 1,5 | 1,5 |
| 36–38 | 21–23 | 1,5 | 1,75 |
| 39–41 | 21–22 | 1,75 | 1,75 |
| 42–47 | 20–22 | 1,75 | 2 |
| 48–56 | 20–23 | 2,25 | 2,25 |
| 57–68 | 20–24 | 2,75 | 2,75 |
| 69–81 | 20–24 | 3,25 | 3,25 |
| 82–100 | 20–24 | 4 | 4 |
| >100 | 4,5 | 4,5 | |
Conversion table
| Number of measuring cups | Oral suspension, ml | UDCA, mg |
| 1 | 5 | 250 |
| 0,75 | 3,75 | 187,5 |
| 0,5 | 2,5 | 125 |
| 0,25 | 1,25 | 62,5 |
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.
| Body weight, kg | Ursofalk suspension dose 250 mg/5 ml, ml | |
| Morning | Evening | |
| 4 | 0,8 | 0,8 |
| 4,5 | 0,9 | 0,9 |
| 5 | 1 | 1 |
| 5,5 | 1,1 | 1,1 |
| 6 | 1,2 | 1,2 |
| 6,5 | 1,3 | 1,3 |
| 7 | 1,4 | 1,4 |
| 7,5 | 1,5 | 1,5 |
| 8 | 1,6 | 1,6 |
| 8,5 | 1,7 | 1,7 |
| 9 | 1,8 | 1,8 |
| 9,5 | 1,9 | 1,9 |
| 10 | 2 | 2 |
Film-coated tablets
| Body weight, kg | Daily dose, mg/kg | Ursofalk, film-coated tablets, 500 mg | ||
| morning | noon | evening | ||
| 20–29 | 17–25 | 0,5 | — | 0,5 |
| 30–39 | 19–25 | 0,5 | 0,5 | 0,5 |
| 40–49 | 20–25 | 0,5 | 0,5 | 1 |
| 50–59 | 21–25 | 0,5 | 1 | 1 |
| 60–69 | 22–25 | 1 | 1 | 1 |
| 70–79 | 22–25 | 1 | 1 | 1,5 |
| 80–89 | 22–25 | 1 | 1,5 | 1,5 |
| 90–99 | 23–25 | 1,5 | 1,5 | 1,5 |
| 100–109 | 23–25 | 1,5 | 1,5 | 2 |
| >110 | 1,5 | 2 | 2 | |
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.
