Ursofalk (ursodeoxycholic acid) coated tablets 500 mg. №25

Description

Ursofalk (ursodeoxycholic acid) coated tablets 500 mg. №25

Composition

active substance: ursodeoxycholic acid;

1 film-coated tablet contains 500 mg of ursodeoxycholic acid;

Excipients: microcrystalline cellulose, povidone K 25, crospovidone type A, talc, magnesium stearate, colloidal anhydrous silica, polysorbate 80, hypromellose, macrogol 6000.

Dosage form

Film-coated tablets.

Main physical and chemical properties: white or almost white oblong tablets with a notch on both sides.

Pharmacotherapeutic group

Drugs used to treat the liver and biliary tract. Means used in biliary pathology.

ATX code A05A A02.

Drugs used in case of liver disease, lipotropic substances.

ATX code A05B.

Pharmacological properties

A small amount of ursodeoxycholic acid was found in human bile. After oral administration, ursodeoxycholic acid reduces the saturation of bile with cholesterol, inhibiting its absorption in the intestine and reducing the secretion of cholesterol in bile. It is possible that due to the dispersion of cholesterol and the formation of liquid crystals there is a gradual dissolution of gallstones.

According to current knowledge, it is believed that the effect of ursodeoxycholic acid in liver disease and cholestasis is due to the relative replacement of lipophilic, detergent-like toxic bile acids with hydrophilic cytoprotective non-toxic ursodeoxycholic acid, improving the secretory capacity of hepatocytes.

Application for children

Cystic fibrosis

Information is available from clinical reports on the long-term use of ursodeoxycholic acid (for up to 10 years) in the treatment of children with hepatobiliary disorders associated with cystic fibrosis. There is evidence that the use of ursodeoxycholic acid can reduce proliferation in the bile ducts, stop the progression of histological changes and even eliminate hepatobiliary changes, provided that treatment is started in the early stages of cystic fibrosis. For better effectiveness, treatment with ursodeoxycholic acid should be started immediately after the diagnosis of cystic fibrosis.

Indication:

• for the dissolution of X-ray-negative cholesterol gallstones with a diameter of not more than 15 mm in patients with a functioning gallbladder, despite the presence of gallstone (s);
• for symptomatic treatment of primary biliary cirrhosis (PBC) in the absence of decompensated liver cirrhosis;
• for the treatment of hepatobiliary disorders in cystic fibrosis in children aged 6 to 18 years.

Contraindication:

• hypersensitivity to any substance that is part of the drug;
• acute inflammation of the gallbladder or bile ducts;
• obstruction of the bile duct (obstruction of the common bile duct or bladder duct);
• frequent episodes of hepatic colic;
• X-ray contrast calcified gallstones;
• violation of the contractility of the gallbladder;
• cirrhosis of the liver in the stage of decompensation;
• unsuccessful result of portoenterostomy or lack of adequate bile outflow in children with atresia of the bile ducts.

Use during pregnancy or breastfeeding

Animal studies have not shown effects of ursodeoxycholic acid on fertility. There are no data on the effect on human fertility.

There are insufficient data on the use of ursodeoxycholic acid in pregnant women. Animal studies indicate reproductive toxicity in early pregnancy. Ursofalk 500 mg film-coated tablets should not be used during pregnancy unless clearly necessary. Women of childbearing potential should take the drug only in the case of reliable contraception.

Method of application and dosage

There are no age restrictions on the use of Ursofalk tablets.

Ursofalk coated tablets in another dosage form (capsules or suspension) can be used in patients weighing less than 47 kg or who have difficulty swallowing tablets.

To dissolve cholesterol gallstones

Approximately 10 mg of ursodeoxycholic acid per 1 kg of body weight per day.

• up to 60 kg per 1 tablet;
• 61–80 kg per 1 ½ tablet;
• 81–100 kg of 2 tablets;
• more than 100 kg of 2 ½ tablets.

The Ursofalk coated tablets should be swallowed without chewing, drinking a small amount of liquid in the evening before bedtime.

The tablets should be taken regularly.

The time required to dissolve gallstones is usually 6-24 months. If the reduction in the size of gallstones is not observed after 12 months of reception, therapy should not be continued.

The success of the treatment should be checked every 6 months by ultrasound or X-ray examination. Additional research is needed to verify that calcification of the stones has not occurred over time. If this happens, treatment should be stopped.

For the symptomatic treatment of primary biliary cirrhosis (PBC)

The daily dose depends on body weight and varies from 1½ to 3½ tablets (14 ± 2 mg of ursodeoxycholic acid per kilogram of body weight).

In the first 3 months of treatment, Ursofalk coated tablets should be taken during the day, dividing the daily dose into several doses. When liver function improves, the daily dose can be taken once a day in the evening.

• body weight (kg) 47–62 – the first 3 months ½ tablets per day, then 1 (tablets 1 time per day in the evening;
• body weight (kg) 63-78 – the first 3 months ½ tablets in the morning and at lunch, 1 tablet in the evening, then 2 tablets 1 time per day in the evening;
• body weight (kg) 79-93 – the first 3 months ½ tablets in the morning and 1 tablet at lunch and in the evening, then 2 (tablets 1 time per day in the evening;
• body weight (kg) 94–109 – for the first 3 months 1 tablet per day, then 3 tablets once a day in the evening;
• body weight (kg) more than 110 – the first 3 months 1 tablet in the morning and at lunch, 1 (tablet in the evening, then 3 ½ tablets 1 time a day in the evening.

The tablets should be swallowed without chewing, washed down with liquid. The drug should be used regularly.

The use of Ursofalk coated tablets in primary biliary cirrhosis is possible for a long period.

In patients with primary biliary cirrhosis, worsening of clinical symptoms is rare at the beginning of treatment, for example, itching may worsen. In this case, therapy should be continued by taking half a tablet of Ursofalk per day, then gradually increase the dose (increasing the daily dose by half a tablet of Ursofalk until the indicated dosing regimen).

Application for children

Children with cystic fibrosis aged 6 to 18 years

The dose is 20 mg / kg / day and is divided into 2-3 doses, followed by increasing the dose to 30 mg / kg / day if necessary.

Children

For the dissolution of cholesterol gallstones and symptomatic treatment of PBC

There are no general age limits for the use of Ursofalk in children, but children weighing less than 47 kg and / or children who have difficulty swallowing, it is recommended to use Ursofalk as a suspension.

For the treatment of hepatobiliary disorders in cystic fibrosis

Used for children aged 6 to 18 years.

Overdose

In case of overdose, diarrhea is possible. Other symptoms of overdose are unlikely because the uptake of ursodeoxycholic acid decreases with increasing dose and therefore most of the dose is excreted in the faeces.

In case of diarrhea, the dose should be reduced, and if diarrhea is persistent, therapy should be discontinued.

Treatment is symptomatic and involves restoring fluid and electrolyte balance.

Side effects:

• from the gastrointestinal tract: pasty stools or diarrhea have often been reported in clinical trials during treatment with ursodeoxycholic acid;
• from the liver and gallbladder: very rarely in the treatment of ursodeoxycholic acid may calcify gallstones;
• hypersensitivity reactions: very rarely allergic reactions, including rash, urticaria.