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

Hepatoprotective agent, has choleretic, cholelitholitic, hypolipidemic, hypocholesterolemic and some immunomodulating action. Reduces the synthesis of cholesterol in the liver, concentration in the bile, increases the solubility of cholesterol in the bile excretory system, stimulates the formation and excretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids. Causes partial or complete dissolution of cholesterol stones when ingested, 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: reduces the expression of certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, the formation of interleukin-2, reduces the number of eosinophils.

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 connection with plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With systematic admission ursodeoxycholic acid becomes the main bile acid in the serum and accounts for about 48% of the total amount of bile acids in the blood. The therapeutic effect of the drug depends on the concentration of ursodeoxycholic acid in the bile.

Metabolised in the liver in taurine and glycine conjugates. The resulting conjugates are secreted in bile.

About 50-70% of the total dose of the drug is excreted with bile. A very small amount (less than 1%) is in the urine. A small amount of non-absorbed ursodeoxycholic acid enters the large intestine, where it undergoes cleavage by bacteria.The resulting lithocholic acid is partially absorbed from the colon, sulphated in the liver and is excreted as a sulfolithocholylglycine or sulfolitocholyltaurine conjugate.

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 (cystic fibrosis).

Nonalcoholic steatohepatitis. Alcoholic liver disease. Biliary dyskinesia.

Contraindications:

X-rays are positive (high in calcium) gallstones. Non-functioning gallbladder.

Acute inflammatory diseases of the gallbladder, bile duct and intestine. Cirrhosis in the stage of decompensation.

Expressed violations of the kidneys, liver, pancreas.

Hypersensitivity to the components of the drug.

Age to 3 years (not recommended for use in this dosage form).

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

Pregnancy and lactation:

Pregnancy

The drug can be used during pregnancy only in those cases when the potential benefit of its use for the mother exceeds the possible risk to the fetus.

Breastfeeding period

Data on the isolation of ursodeoxycholic acid with breast milk are absent. It is recommended to stop breastfeeding if you need to use the drug during this period.

Dosing and Administration:

Children and adults weighing less than 47 kg are advised to use the drug in suspensions of other manufacturers.

Dissolution of cholesteric gallstones

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

Body mass	Number of capsules
Up to 60 kg	2
61-80 kg	3
81-100 kg	4
more than 100 kg	5

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

Duration of treatment is 6-12 months. For the prevention of repeated cholelithiasis, the use of the drug is recommended for several months after the dissolution of the stones.

Treatment of biliary reflux gastritis

1 capsule (250 mg) daily in the evening before bedtime, without chewing and washing 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.

Symptomatic treatment of primary biliary cirrhosis

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

In the first 3 months of treatment, the drug should be divided into several doses during the day. After improving liver function, the daily dose of the drug can be taken once, in the evening.

The following dosing regimen is recommended:

Body mass	Daily dose	morning	afternoon	evening
47-62 kg	750 mg (3 capsules)	1 capsule	1 capsule	1 capsule
63-78 kg	1000 mg (4 capsules)	1 capsule	1 capsule	2 capsules
79-93 kg	1250 mg (5 capsules)	1 capsule	2 capsules	2 capsules
94-109 kg	1500 mg (6 capsules)	2 capsules	2 capsules	2 capsules
more than 110 kg	1750 mg (7 capsules)	2 capsules	2 capsules	3 capsules

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

The use of the drug for the treatment of primary biliary cirrhosis can be continued for an unlimited time.

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

Symptomatic treatment of chronic hepatitis of different genesis

The daily dose is 10-15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 divided doses. The duration of therapy is 6-12 months or more.

Primary sclerosing cholangitis

The daily dose is 12-15 mg ursodeoxycholic acid per 1 kg of body weight, if necessary, the daily 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 (cystic fibrosis)

The daily dose is 12-15 mg of ursodeoxycholic acid per 1 kg of body weight, if necessary, the daily dose can be increased to 20-30 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 doses. The duration of therapy is from 6 months to several years.

Non-alcoholic steatohepatitis

The average daily dose is 10-15 mg ursodeoxycholic acid per 1 kg of body weight 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 ursodeoxycholic acid per 1 kg of body weight in 2-3 divided doses. The duration of therapy is from 6-12 months or more.

Biliary dyskinesia

The average daily dose is 10 mg ursodeoxycholic acid per 1 kg of body weight in 2 divided doses. The duration of therapy is from 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.

Side effects:

The incidence of adverse reactions is as follows: very often (≥1 / 10 cases), often (≥1 / 100 and <1/10 cases) infrequently (≥1 / 1000 and <1/100 cases), rarely (≥1 / 10000 and <1/1000 cases) and very rarely (<1/10000 cases).

From the gastrointestinal tract:

In clinical studies against the backdrop of treatment of ursodeoxycholic acid, an unformed stool or diarrhea was often observed.

In the treatment of primary biliary cirrhosis of the liver, acute pains in the right hypochondrium and epigastric region were very rarely observed.

From the liver and bile ducts:

Very rarely, against the background of treatment with ursodeoxycholic acid, calcification of gallstones can occur.

In the treatment of advanced stages of primary biliary cirrhosis, decompensation of liver cirrhosis, which disappeared when the drug was withdrawn, was very rarely observed.

From the skin:

Very rarely there may be hives.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

Cases of an overdose have not been revealed. In case of an overdose, symptomatic treatment is performed.

Interaction:

Colestramine, 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 efficacy. If the use of drugs containing at least one of these substances is nevertheless necessary, they should be taken at least 2 hours before the reception of ursodeoxycholic acid. Ursodeoxycholic acid can enhance the absorption of cyclosporine from the intestine. Therefore, in patients receiving ciclosporin, the doctor should check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine, if necessary.

In some cases ursodeoxycholic acid can reduce the absorption of ciprofloxacin.

Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase bile saturation with cholesterol and may decrease the ability to dissolve cholesterol bile stones.

Special instructions:

The drug should be administered under the supervision of a doctor.

During the first three months of treatment, it is necessary to monitor the activity of "hepatic" transaminases, alkaline phosphatase and gamma-glutamyltranspeptidase in the blood serum every 4 weeks, and then every 3 months. Control of these parameters allows us to identify violations of liver function in the early stages. This also applies to patients in the late stages of primary biliary cirrhosis. In addition, it is possible to determine whether the patient reacts with primary biliary cirrhosis of the liver for ongoing treatment.

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.

When used to dissolve cholesterol gallstones

In order to evaluate the progress in treatment and to detect signs of calcification of stones in time, depending on the size of the stones, the gallbladder should be visualized (oral cholecystography) with examination of blackouts in the standing and lying position on the back (ultrasound examination) 6-10 months after the beginning treatment.

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

In the treatment of patients with advanced stages of primary biliary cirrhosis

Very rarely there were cases of decompensation of liver cirrhosis. After the cessation of therapy, a partial reverse development of manifestations of decompensation was noted.

In patients with diarrhea, the dosage of the drug should be reduced. With persistent diarrhea, treatment should be discontinued.

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

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

Form release / dosage:

Capsules 250 mg.

Packaging:

5, 10, 20, 25 capsules in a contour cell box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 4, 5 contour squares 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002585

Date of registration:15.08.2014 / 14.03.2016

Expiration Date:15.08.2019

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp12.07.2016

Illustrated instructions

Instructions

Ursoprim (Ursoprim)