Ursomik - instructions for use, dose, side effects, contraindications

Composition of gelatin capsule shell: gelatin 134,465 mg, glycerol 62,114 mg, methyl parahydroxybenzoate 0.24 mg, titanium dioxide 0.968 mg, purified water 17.2 mg, dye Sunny Sunset yellow E-110 0.013 mg.

Description:

Capsules soft gelatinous oval with a seam, elastic, opaque, light brown color.

The contents of the capsules are an oil suspension from light yellow to dark yellow with an odorless odor. During storage, it is possible to exfoliate the mixture.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

The active substance providing pharmacological action of the drug Ursomik® - acid ursodeoxycholic.

Has hepatoprotective, choleretic, cholelitholytic, hypocholesterolemic, hypolipidemic and some immunomodulating action.

Fitting into the hepatocyte membrane stabilizes its structure and to protect the hepatocyte from the damaging effect of bile salts, reducing, thus, the cytotoxic effect. When cholestasis activates Ca²⁺-dependent protease and alpha-stimulated exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, lithocholic, deoxycholic et al.) whose concentrations in patients with chronic liver diseases inflated.

With its high polarity, ursodeoxycholic acid forms a non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of the gastric reflyuktata damage cell membranes with biliary reflux gastritis and reflux esophagitis. Furthermore, ursodeoxycholic acid forms double molecules capable included in the composition of cell membranes (hepatocytes, cholangiocytes, epithelial cells of the gastrointestinal tract), to stabilize them and make refractory to the cytotoxic mitselltsitoprotektivny, hepatoprotective effect.

Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in secretion in bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces the lithogenic bile index. The result is the dissolution of cholesterol gallstones (a consequence of the change in the ratio of cholesterol / bile acids to bile) and the prevention of the formation of new concrements (the result of a decrease in the content of bile cholesterol) is the litholytic effect.

It induces choleresis, rich in bicarbonates, which leads to an increase in bile passage and stimulates the excretion of toxic bile acids through the intestine, which contributes to the resolution of intrahepatic cholestasis, an anti-cholestatic effect. Immunomodulatory effect due to oppression of expression HLA-antigens on the membranes of hepatocytes and cholangiocytes, a decrease in the activity of immunocompetent immunoglobulins (in the first place Ig M), the normalization of the natural killer activity of lymphocytes, the effect on the formation of interleukin-2, a decrease in the number of eosinophils,

Reliably delay the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis - antifibrolytic effect.

Ursodeoxycholic acid slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes, etc.) - an antiapoptotic effect.

Pharmacokinetics:

When ingested absorbed in the small intestine (about 90%) due to passive diffusion, and in the ileum through active transport. The maximum concentration (C_m_Oh) in the blood plasma is achieved after 1-3 hours. The association with blood plasma proteins is high (healthy volunteers with proteins are associated with at least 70% of unconjugated ursodeoxycholic acid).

When taken in a single dose of 500 mg, the serum concentration in 30, 60 and 90 minutes is 3.8; 5.5 and 3.7 μmol / L, respectively. With the systematic administration of acid ursodeoxycholic becomes the main bile acid of blood serum (48 % total amount of bile acids).

The therapeutic effect depends on the concentration of acid ursodeoxycholic in bile; on the background of therapy, there is a dose-dependent increase in its share in the bile acid pool to 50-75 % (at daily doses of 10-20 mg / kg).

It is included in the system of gastrointestinal circulation.

In the liver, the ursodeoxycholic acid binds to glycine and taurine; The resulting conjugates are secreted in bile.

Passes through the placental barrier.

Excreted mainly (50-70%) through the intestine, a very small amount (less than 1%) - with urine. A small amount of non-succinic acid ursodeoxycholic in the large intestine undergoes cleavage by bacteria (7-dehydroxylation) to lithocholic acid, which is partially absorbed from the colon, sulfated in the liver and rapidly excreted with feces in the form of sulfotylcholylglycine or sulfotylcholitaurine conjugates. Part of the lithocholic acid in enterohepatic circulation enters the liver and is re-transformed into xeno- and ursodeoxycholic acids.

Indications:Dissolution of small and medium cholesterol stones with a functioning gallbladder. Biliary reflux-gastritis. Primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment). Chronic hepatitis of various genesis. Primary sclerosing cholangitis. Cystic fibrosis. Nonalcoholic steatohepatitis. Alcoholic liver disease. Biliary dyskinesia.

Contraindications:

■ hypersensitivity to the components of the drug;

■ X-ray positive (high in calcium) gallstones;

■ acute inflammatory diseases of the gallbladder, bile ducts and intestines, Crohn's disease;

■ non-functioning gallbladder;

■ complete obstruction of the biliary tract;

■ cirrhosis of the liver in the stage of decompensation;

■ marked violations of the kidneys, liver, pancreas;

■ bile-gastrointestinal fistula;

■ frequent biliary colic;

■ lactation period;

■ Children under 3 years of age (not recommended for use in this dosage form).

Carefully:

Child age from 3 years (possible difficulty in swallowing capsules).

Pregnancy and lactation:

The use of ursodeoxycholic acid in pregnancy is possible only if the expected benefit for the mother exceeds the potential risk to the fetus. Data on the isolation of ursodeoxycholic acid are absent. It is recommended to stop breastfeeding if you need to use the drug during lactation.

Dosing and Administration:

For the various indications for use, the following daily dosing regimens are recommended:

To dissolve cholesteric gallstones approximately 10 mg of ursodeoxycholic acid per 1 kg of human body weight:

up to 60 kg 2 capsules

61-80 kg 3 capsules

81-100 kg 4 capsules

over 100 kg 5 capsules

Capsules should be taken in the evening, before going to bed, without chewing and washing down with a small amount of liquid.

Capsules should be used regularly.

Duration of treatment for dissolution of stones is 6-12 months. If the size of the stones does not decrease after 12 months, treatment should not be continued.

The success of treatment should be monitored by ultrasound or radiology every 6 months. At the subsequent inspection it is necessary to check up, whether there was a calcification of stones in an interval of time. In the event that this occurred, treatment should be discontinued.

For the treatment of biliary reflux gastritis and biliary reflux esophagitis: one capsule, which is taken daily, in the evening, before going to sleep, without chewing and washing down with a small amount of liquid.

The treatment period is 10-14 days. In general, the duration of the application depends on the course of the disease.

For symptomatic treatment of primary biliary cirrhosis (PBC):

The daily dose of the drug depends on the weight of the patient, and varies from 3 to 7 capsules (14 ± 2 mg ursodeoxycholic acid per 1 kg of body weight).

In the first 3 months of treatment with the drug Ursomik®, capsules 250 mg, the drug should be divided throughout the day. After improving the liver, the daily dose of the drug can be taken once, in the evening.

Body weight (kg)	Daily dose (mg / kg)	capsules
		first 3 months			further
		morning	day	evening	evening (1 per day)
47-62	12-16	1	1	1	3
63-78	13-16	1	1	2	4
79-93	13-16	1	2	2	5
94-109	14-16	2	2	2	6
more than 110		2	2	3	7

Capsules should be taken without chewing, squeezed with a small amount of liquid. It is necessary to observe the regularity of reception. The use of Ursomyc® capsules for the treatment of primary biliary cirrhosis can be unlimited in time.

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

Primary sclerosing cholangitis: 12-15 mg / kg / day (up to 20 mg) for 6-24 months (up to several years).

Cystic Fibrosis: up to 20-30 mg / kg / day for 6-24 months or more.

With chronic hepatitis of various genesis (toxic, medicinal, etc.), non-alcoholic steatohepatitis, alcoholic liver disease the average daily dose is 12-15 mg / kg (2-5 capsules) in 2-3 divided doses. The duration of therapy is 6-12 months or more.

With dyskinesia biliary tract an average daily dose of 10 mg / kg in 2 divided doses for 2 weeks to 2 months.

Children over 3 years old the drug is administered individually, based on a calculation of 20 mg / kg / day.

Side effects:

Ursomik ® is well tolerated by patients.

Diarrhea or constipation, nausea, vomiting, pain in the epigastric region and right hypochondrium, calcification of gallstones, increased activity of hepatic transaminases, exacerbation of previously existing psoriasis, allergic reactions (rashes, itching), allergic reactions can occur rarely.

In the treatment of primary biliary cirrhosis, transient decompensation of liver cirrhosis can occur, which disappears after drug withdrawal.

In case of any unusual reactions, stop taking the medication and consult a doctor.

Overdose:

Cases of overdose of ursodeoxycholic acid are not known.

Interaction:

Colestyramine, cholesterol and antacids containing aluminum hydroxide bind ursodeoxycholic acid in the intestine, reduce its absorption and impair its effectiveness. In case of the need for simultaneous treatment with the above mentioned drugs, it is recommended to apply them 2 hours before or after taking Ursomica®. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin, progestins can increase the saturation of bile with cholesterol and reduce the ability of acid ursodeoxycholic to dissolve cholesterol bile stones. Ursodeoxycholic acid can reduce the absorption of ciprofloxacin.

Ursomik® can increase the absorption of cyclosporine in the intestine. Therefore, it is necessary for people taking this medication at the same time to control the level of cyclosporine and adjust its doses.

Special instructions:

In cholelithiasis, treatment effectiveness is monitored every 6 months by X-ray and ultrasound examination of the biliary tract to prevent relapse of cholelithiasis.

Positive results can be obtained only in the presence of purely cholesterol (roentgenogenic) gallstones with a size of not more than 15-20 mm, with the preserved function of the gallbladder and the patency of the vesicle and common bile ducts.

For prolonged (more than 1 month) treatment, a biochemical blood test should be performed monthly to determine the activity of hepatic transaminases, alkaline phosphatase, gamma-glutamyltransferase and bilirubin (especially in the first 3 months of therapy). If the increased indices remain, the drug should be discontinued.

After complete dissolution of the calculus, it is recommended to continue to use for at least 3 months, in order to facilitate the dissolution of stone residues, the sizes of which are too small for their detection.

If within 6-12 months after the beginning of therapy of partial dissolution of concrements did not occur, it is unlikely that the treatment will be effective.

Detection during treatment of a nonvisualizable gallbladder is evidence that no complete dissolution of the calculi has occurred, and treatment should be discontinued.

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

Long-term therapy with high doses of ursodeoxycholic acid (28-30 mg / kg / day) can lead to the development of serious side effects in patients with primary sclerosing cholangitis.

Effect on the ability to drive transp. cf. and fur:

Does not affect the ability to drive vehicles and other mechanisms.

Form release / dosage:Capsules 250 mg.

Packaging:

For 10 capsules in a contour mesh package made of polyvinylchloride film AND aluminum foil.

For 5 contour mesh packages together with instructions for use; in a pack of cardboard.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003387

Date of registration:28.12.2015

Expiration Date:28.12.2020

The owner of the registration certificate:MINSKINTERKAPS, UP MINSKINTERKAPS, UP Republic of Belarus

Manufacturer: & nbsp

MINSKINTERKAPS, UP Republic of Belarus

Representation: & nbspMINSKINTERKAPS MINSKINTERKAPS Republic of Belarus

Information update date: & nbsp14.07.2016

Illustrated instructions

Instructions

Ursomik® (Ursomik)