Urdoxa 500 pills 500mg, 50pcs

Composition

1 tablet contains:

Active ingredient: ursodeoxycholic acid 500 mg;

excipients: microcrystalline cellulose, colloidal silicon dioxide (aerosil), povidone K-30, polysorbate 80 (tween 80), crospovidone, talc, magnesium stearate;

excipients for the shell: hypromellose (hydroxypropylmethyl cellulose), macrogol 6000 (polyethylene glycol 6000), talc.

Pharmacological action

Hepatoprotective agent.

ATX code: A05AA02

Pharmacological properties

Pharmacodynamics

Hepatoprotective agent, has a choleretic effect. Reduces the synthesis of cholesterol 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 excretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids in it; causes increased gastric and pancreatic secretion, increases the activity of lipase, has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones with enteral application, reduces the saturation of bile with cholesterol, which contributes to the mobilization of cholesterol from gallstones. It has an immunomodulatory effect, affects immunological reactions in the liver: reduces the expression of certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, interleukin-2 formation, reduces the number of eosinophils.

Cystic fibrosis (cystic fibrosis)

According to clinical reports, there is a long-term experience (up to 10 years or more) in the treatment of ursodeoxycholic acid in children with hepatobiliary disease associated with cystic fibrosis. There is evidence that ursodeoxycholic acid therapy can reduce the proliferation of bile ducts, slow the development of lesions detected by histological examination, and even contribute to the reverse development of changes in the hepatobiliary system if therapy begins in the early stages of cystic fibrosis. In order to optimize the effectiveness of treatment, ursodeoxycholic acid therapy should be initiated as early as possible after the diagnosis of cystic fibrosis.

Pharmacokinetics

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

Depending on the daily dose, type of disease, or liver condition, more or less 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 action of intestinal bacteria, ursodeoxycholic acid is partially destroyed to form 7-keto-litocholic and litocholic acids. Litocholic acid is hepatotoxic, and in some animal species it causes damage to the liver parenchyma. In humans, it is absorbed only in small amounts, sulfated in the liver, and thus detoxified before excretion in the bile and excretion through the intestine. The elimination half-life of ursodeoxycholic acid is 3.5-5.8 days.

Indications

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

Use during pregnancy and lactation

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

Pregnancy

Data on the use of ursodeoxycholic acid in pregnant women are limited or absent. Animal studies have shown the presence of reproductive toxicity at an early stage of pregnancy. Urdoxa 500 should not be used during pregnancy unless it is clearly necessary.

Fertility

The use of the drug by women with childbearing potential is possible only if they use reliable methods of contraception.

It is recommended to use non-hormonal contraceptives or oral contraceptives with a low estrogen content, since hormonal oral contraceptives can increase the formation of gallstones in the gallbladder. Possible pregnancy should be ruled out before starting treatment.

Breast-feeding

According to several documented cases, the level of ursodeoxycholic acid in breast milk in women is very low and therefore the occurrence of adverse reactions in children during breastfeeding is not expected.

Contraindications

X-ray positive (high calcium content) gallstones; impaired contractility of the gallbladder; acute inflammatory diseases of the gallbladder and bile ducts; biliary tract occlusion (occlusion of the common bile or cystic ducts), frequent episodes of biliary colic, hypersensitivity to the components of the drug or bile acids, children under 3 years of age (for this dosage form), liver cirrhosis in the decompensation stage and severe liver and/ or renal failure.

Pediatric population

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

Children under 3 years of age, as well as patients with difficulty swallowing tablets, are recommended to use ursodeoxycholic acid in suspension.

Side effects

The assessment of adverse events is based on the following classification: :

Very frequent (≥1/10)

Frequent (≥1/100 – <1/10)

Infrequent (≥1/1000 –

Rare (≥1/10000 –

Very rare (

Disorders of the gastrointestinal tract:

In clinical studies, unformed stools or diarrhea were often observed during treatment with ursodeoxycholic acid.

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

Liver and biliary tract disorders:

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

In the treatment of advanced stages of primary biliary cirrhosis, in very rare cases, decompensation of liver cirrhosis was observed, which regresses after discontinuation of the drug.

Skin and subcutaneous tissue disorders:

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

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

Interaction

Colestyramine, 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 Urdoxa ® 500.

Ursodeoxycholic acid may increase the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine concomitantly, it is necessary to determine the concentration of cyclosporine in the blood and, if necessary, adjust the dose of cyclosporine.

Ursodeoxycholic acid may reduce the absorption of ciprofloxacin.

In a clinical study involving healthy volunteers, concomitant use of ursodeoxycholic acid (500 mg / day) and rosuvastatin (20 mg/day) resulted in a slight increase in rosuvastatin plasma concentrations. The clinical significance of this interaction, including in relation to other statins, is unknown.

Ursodeoxycholic acid has been shown to reduce the maximum concentration and area under the concentration-time pharmacokinetic curve of the calcium antagonist nitrendipine. In addition, a decrease in the therapeutic effect of dapsone has been reported.

These data, as well as data obtained in vitro, suggest that ursodeoxycholic acid can induce CYP3A isoenzymes. However, the results of controlled clinical trials indicate that ursodeoxycholic acid does not have a pronounced inducing effect on the CYP3A isoenzyme.

Estrogens, lipid-lowering drugs such as clofibrate, increase the saturation of bile with cholesterol and may reduce the litholitic effect of ursodeoxycholic acid.

How to take it, course of use and dosage

For patients who cannot swallow Urdoxa 500, film-coated tablets 500 mg, or with a body weight of less than 47 kg, it is recommended to use ursodeoxycholic acid in capsules or suspensions.

Tablets should be taken without chewing, washed down with liquid. They should be taken regularly.

Dissolving 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 the size of the stones does not decrease after 12 months of treatment, then the treatment should be discontinued.

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

Treatment of biliary reflux gastritis

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

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 varies from 11/2 to 31/2 tablets(14 ± 2 mg of 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 Urdoxa ® 500 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, pruritus may become more frequent. In this case, treatment should be continued by taking ½ tablet daily, then gradually increasing the dose (increasing the daily dose weekly by ½ tablet) until the recommended dosage regimen is reached again.

Symptomatic treatment of chronic hepatitis of various origins

The daily dose is 10-15 mg / kg in 2-3 divided doses. The duration of treatment is 6-12 months or more.

Primary sclerosing cholangitis

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

Cystic fibrosis (as part of complex therapy) 

The daily dose is 20 mg / kg / day in 2-3 divided doses, with a further increase to 30 mg/kg/day if necessary.

Non-alcoholic steatohepatitis

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

Alcoholic liver disease

The average daily dose is 10-15 mg / kg in 2-3 divided 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, the course of treatment is recommended to be repeated.

Overdose

In case of overdose, diarrhea is possible. In general, other symptoms of overdose are unlikely, since with an increase in the dose of ursodeoxycholic acid, its absorption decreases, and excretion with feces increases.

No specific treatment is required. The consequences of diarrhea are treated symptomatically (restoration of water and electrolyte balance).

Description

Oblong shape with rounded ends biconvex tablets, covered with a film-coated white or almost white color, with a risk. On a cross-section, the core is white or almost white in color.

Special instructions

Urdoxa 500 should be administered under medical supervision. During the first 3 months of treatment, liver function parameters (transaminases, alkaline phosphatase and gammaglutamyltranspeptidase) in the blood serum should be monitored every 4 weeks, and then every 3 months. Monitoring of these parameters allows detecting liver function disorders in the early stages. This also applies to patients in the late stages of primary biliary cirrhosis. In addition, it can quickly determine whether a patient with primary biliary cirrhosis is responding to treatment.

When used in patients to dissolve cholesterol gallstones:

In order to assess progress in treatment and to timely detect signs of calcification of stones, depending on the size of the stones, the gallbladder should be visualized (oral cholecystography) with examination of darkening in the “standing” and “lying on your back” positions (ultrasound) 6-10 months after the start of treatment.

If the gallbladder cannot be visualized on X-rays or in cases of calcification of stones, weak contractility of the gallbladder or frequent attacks of colic, Urdoxa® 500 should not be used.

In the treatment of patients in the late stages of primary biliary cirrhosis:

Cases of decompensation of cirrhosis of the liver were extremely rare. After discontinuation of therapy, there was a regression of decompensation symptoms.

In patients with primary biliary cirrhosis, in rare cases, clinical symptoms may increase at the beginning of treatment, for example, pruritus may increase. In this case, the dose of ursodeoxycholic acid should be reduced, and then gradually increased again.

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 persistent diarrhea occurs, treatment should be discontinued.

Women of childbearing age can only take the drug if they use reliable contraceptive methods. It is recommended to use non-hormonal contraceptives or oral contraceptives with a low estrogen content, since hormonal oral contraceptives can increase the formation of gallstones in the gallbladder. Possible pregnancy should be ruled out before starting treatment.

Influence on the ability to drive vehicles and mechanisms No effect on the ability to drive vehicles and moving mechanisms was found.

Form of production

Film-coated tablets,500 mg.

10 or 20 tablets in a contour cell package made of polyvinyl chloride film and aluminum foil printed varnished.

1,3,5 contour cell packs of 10 tablets or 5 contour cell packs of 20 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions

At a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date.

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Tablets