Urcevel capsules 250mg, No. 100

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

Children and adults weighing less than 47 kg are recommended to use ursodeoxycholic acid in suspension.
Dissolution of cholesterol gallstones The
recommended dose is 10 mg ursodeoxycholic acid per 1 kg of body weight per day, which corresponds to:

Body weight, kg. Number of capsules, pcs:

Up to 60 kg - 2 drops

61-80 kg - 3 drops

81-100 kg - 4 drops

Over 100 kg - 5 drops

The drug must be taken daily in the evening, before bedtime (the capsules are not chewed), with a small amount of liquid.
Duration of treatment is 6-12 months. For the prevention of recurrent cholelithiasis, it is recommended to take the drug for several months after the stones dissolve.
Treatment of biliary reflux gastritis
1 capsule of ursodeoxycholic acid daily in the evening before bedtime, without chewing and drinking a little 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 (approximately 14 ± 2 mg ursodeoxycholic acid per 1 kg of body weight).
In the first 3 months of treatment, the intake of ursodeoxycholic acid should be divided into several doses throughout the day. After improvement of hepatic parameters, the daily dose of the drug can be taken 1 time in the evening.
The following regimen is recommended:
250 mg capsules.

The first 3 months of treatment:

47-62 kg in the morning, afternoon, evening, 1 drop each.

Then 3 cap evenings 1 time.

63-78 kg in the morning, 1 drop in the afternoon, 2 drops in the evening.

Further, 4 drops. in the evening 1 time

79-93 kg in the morning 1 drop, in the afternoon, 2 drops in the evening.

Further, 5 drops. in the evening 1 time.

94-109 kg in the morning, afternoon, evening, 2 drops.

Then 6 drops. in the evening 1 time.

Over 110 kg. in the morning, in the afternoon, 2 drops. in the evening, 3 drops.

Next, 7 drops. in the evening 1 time.

The capsules should be taken regularly, without chewing, with a small amount of liquid.
The use of ursodeoxycholic acid 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 daily, then the dosage should be gradually increased, increasing the daily dose by 1 capsule weekly, until the recommended dosage regimen is reached again.
Symptomatic treatment of chronic hepatitis of various origins - daily vine 10-15 mg / kg in 2-3 doses. The 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 is from 6 months to several years (see section 'Special instructions').
Cystic fibrosis (cystic fibrosis) - a daily dose of 20 mg / kg / day in 2-3 doses, with a further increase to 30 mg / kg / day if necessary.

Non-alcoholic steatohepatitis - an average daily dose of 10-15 mg / kg in 2-3 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 doses. The duration of therapy is 6-12 months or more.
Biliary dyskinesia - an average daily dose of 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.

Active ingredient: ursodeoxycholic acid - 250.0 mg.
Excipients: corn starch, colloidal silicon dioxide (aerosil), magnesium stearate.
Composition of the gelatin capsule: titanium dioxide, gelatin.

X-ray positive (high calcium) gallstones violation of the contractility of the gallbladder, blockage of the biliary tract (blockage of the common bile duct or cystic duct), frequent episodes of biliary colic; acute inflammatory diseases of the gallbladder and bile ducts; cirrhosis of the liver in the stage of decompensation; severe hepatic and / or renal failure, hypersensitivity to drug components or other bile acids.
Pediatric population
Unsuccessful portoenterostomy or failure to restore normal bile flow in children with biliary atresia.
Ursodeoxycholic acid has no age restrictions for use, but for children under 3 years of age, it is recommended to use ursodeoxycholic acid in suspension, as it may be difficult to swallow capsules.

Trade name:

Urtsevel

International non-proprietary name:

ursodeoxycholic acid

Dosage form:

capsules

Composition for one capsule:

Active ingredient: ursodeoxycholic acid - 250.0 mg.
Excipients: corn starch, colloidal silicon dioxide (aerosil), magnesium stearate.
Composition of the gelatin capsule: titanium dioxide, gelatin.

Description:

hard gelatin capsules No. 0 white. The contents of the capsules are white or almost white powder.

Pharmacotherapeutic group:

hepatoprotective agent

Pharmacological properties

Pharmacodynamics
Hepatoprotective agent, has a choleretic effect. Reduces the synthesis of cholesterol in the liver, its absorption in the intestine and concentration in bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and secretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids in it; causes an increase in gastric and pancreatic secretion, enhances lipase activity, has a hypoglycemic effect. It causes partial or complete dissolution of cholesterol stones when administered enterally, 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 some antigens on the membrane of hepatocytes, affects the number of T-lymphocytes, the formation of interleukin-2,reduces the number of eosinophils.
Pediatric population
Cystic fibrosis (cystic fibrosis)
According to clinical reports, there is many years of experience (up to 10 years or more) in treating pediatric patients with cystic fibrosis-associated hepatobiliary disease (CFAHD) with ursodeoxycholic acid. There is evidence that ursodeoxycholic acid therapy can reduce the proliferation of the bile ducts, slow the development of lesions detected by histological examination, and even promote the reversal of changes in the hepatobiliary system if therapy is started in the early stages of CFAHD. In order to optimize the effectiveness of treatment, ursodeoxycholic acid therapy should be started as soon as possible after the diagnosis of CFAHD.

Pharmacokinetics
After oral administration, ursodeoxycholic acid is rapidly absorbed in the jejunum and proximal ileum by passive diffusion, and in the distal ileum by active transport. Approximately 60-80% of the dose taken is absorbed. After absorption, ursodeoxycholic acid is almost completely conjugated in the liver with glycine and taurine and excreted in the bile. During the first passage through the liver, up to 60% is metabolized.
Depending on the daily dose, the type of disease and the condition of the liver, 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 partially decomposes with the formation of 7-kego-lithocholic and lithocholic acid. Lithocholic acid is hepatotoxic; in some animal species, it causes damage to the liver parenchyma. In the human body, it is absorbed only in small quantities. In the process of metabolism, it is sulfated in the liver, due to which it is rendered harmless even before it is excreted into bile, and excreted from the body with feces. The half-life of ursodeoxycholic acid is 3.5 to 5.8 days.

Indications for use

Dissolution of cholesterol gallstones, biliary reflux gastritis, primary biliary cirrhosis in the absence of signs of decompensation, 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) gallstones violation of the contractility of the gallbladder, blockage of the biliary tract (blockage of the common bile duct or cystic duct), frequent episodes of biliary colic; acute inflammatory diseases of the gallbladder and bile ducts; cirrhosis of the liver in the stage of decompensation; severe hepatic and / or renal failure, hypersensitivity to drug components or other bile acids.
Pediatric population
Unsuccessful portoenterostomy or failure to restore normal bile flow in children with biliary atresia.
Ursodeoxycholic acid has no age restrictions for use, but for children under 3 years of age, it is recommended to use ursodeoxycholic acid in suspension, as it may be difficult to swallow capsules.

Application during pregnancy and during breastfeeding

According to animal studies, ursodeoxycholic acid has no effect on fertility. There are no data on the effect of ursodeoxycholic acid treatment on fertility in humans.
Data on the use of ursodeoxycholic acid in pregnant women are limited or absent. Animal studies have shown reproductive toxicity early in pregnancy. During pregnancy, ursodeoxycholic acid should not be used unless clearly necessary. The use of ursodeoxycholic acid in women of childbearing potential is possible only if they use reliable methods of contraception. It is recommended to use non-hormonal contraceptives or low estrogen oral contraceptives. However, patients taking ursodeoxycholic acid to dissolve gallstones should use effective non-hormonal contraceptives.since hormonal oral contraceptives can increase the formation of gallstones. The possibility of pregnancy should be ruled out before starting treatment.
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 with breastfeeding is not expected.

Method of administration and dosage

Children and adults weighing less than 47 kg are recommended to use ursodeoxycholic acid in suspension.
Dissolution of cholesterol gallstones The
recommended dose is 10 mg ursodeoxycholic acid per 1 kg of body weight per day, which corresponds to:

Body weight, kg. Number of capsules, pcs:

Up to 60 kg - 2 drops

61-80 kg - 3 drops

81-100 kg - 4 drops

Over 100 kg - 5 drops

The drug must be taken daily in the evening, before bedtime (the capsules are not chewed), with a small amount of liquid.
Duration of treatment is 6-12 months. For the prevention of recurrent cholelithiasis, it is recommended to take the drug for several months after the stones dissolve.
Treatment of biliary reflux gastritis
1 capsule of ursodeoxycholic acid daily in the evening before bedtime, without chewing and drinking a little 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 (approximately 14 ± 2 mg ursodeoxycholic acid per 1 kg of body weight).
In the first 3 months of treatment, the intake of ursodeoxycholic acid should be divided into several doses throughout the day. After improvement of hepatic parameters, the daily dose of the drug can be taken 1 time in the evening.
The following regimen is recommended:
250 mg capsules.

The first 3 months of treatment:

47-62 kg in the morning, afternoon, evening, 1 drop each.

Then 3 cap evenings 1 time.

63-78 kg in the morning, 1 drop in the afternoon, 2 drops in the evening.

Further, 4 drops. in the evening 1 time

79-93 kg in the morning 1 drop, in the afternoon, 2 drops in the evening.

Further, 5 drops. in the evening 1 time.

94-109 kg in the morning, afternoon, evening, 2 drops.

Then 6 drops. in the evening 1 time.

Over 110 kg. in the morning, in the afternoon, 2 drops. in the evening, 3 drops.

Next, 7 drops. in the evening 1 time.

The capsules should be taken regularly, without chewing, with a small amount of liquid.
The use of ursodeoxycholic acid 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 daily, then the dosage should be gradually increased, increasing the daily dose by 1 capsule weekly, until the recommended dosage regimen is reached again.
Symptomatic treatment of chronic hepatitis of various origins - daily vine 10-15 mg / kg in 2-3 doses. The 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 is from 6 months to several years (see section 'Special instructions').
Cystic fibrosis (cystic fibrosis) - a daily dose of 20 mg / kg / day in 2-3 doses, with a further increase to 30 mg / kg / day if necessary.

Non-alcoholic steatohepatitis - an average daily dose of 10-15 mg / kg in 2-3 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 doses. The duration of therapy is 6-12 months or more.
Biliary dyskinesia - an average daily dose of 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.

Side effect

Classification of the incidence of adverse reactions according to the recommendations of the World Health Organization (WHO): very often? 1/10; often from? 1/100 to <1/10; infrequently from? 1/1000 to <1/100; rarely from? 1/10000 to <1/1000; very rarely <1/10000, including isolated messages; frequency unknown - from the available data, it is not possible to establish the frequency of occurrence.
Disorders from the gastrointestinal tract
In clinical studies during treatment with ursodeoxycholic acid, loose stools or diarrhea were frequent.
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, during treatment with ursodeoxycholic acid, calcification of gallstones may occur.
In the treatment of advanced stages of primary biliary cirrhosis, in very rare cases, decompensation of liver cirrhosis was observed, which disappears after discontinuation of the drug.
Skin and subcutaneous tissue disorders
In very rare cases, allergic reactions, including urticaria, may occur.
If any of the side effects indicated in the instructions are aggravated, or you notice other side effects that are not indicated in the instructions, please inform your doctor .

Overdose

In case of overdose, diarrhea is possible. As a rule, other symptoms of an overdose are unlikely, since with an increase in the dose, the absorption of ursodeoxycholic acid decreases and, accordingly, more of it is excreted in the feces. There is no need to take specific measures for overdose. Treatment of the consequences of diarrhea is symptomatic, aimed at replenishing the volume of fluid and restoring the electrolyte balance.

Interaction with other medicinal products

Cholestyramine, 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 ursodeoxycholic acid.
Ursodeoxycholic acid may interfere with the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the doctor should check the concentration of cyclosporine in the blood and, if necessary, adjust its dose.
In some cases, ursodeoxycholic acid can reduce the absorption of ciprofloxacin.
In a clinical study involving healthy volunteers, the simultaneous use of ursodeoxycholic acid (500 mg / day) and rosuvastatin (20 mg / day) led to a slight increase in the level of rosuvastatin in blood plasma. The clinical significance of this interaction, including with respect to other statins, is unknown.
In healthy volunteers, ursodeoxycholic acid has been shown to reduce peak plasma concentrations (Cmax) and the area under the concentration-time curve (AUC) of the slow calcium channel blocker nitrendipine. In the case of the simultaneous use of nitrendipine and ursodeoxycholic acid, careful monitoring is recommended. An increase in the dose of nitrendipine may be required. There are also reports of interactions with dapsone, which led to a decrease in the therapeutic effect of the latter. These observations, along with data from in vitro experiments,give reason to believe that ursodeoxycholic acid is capable of inducing enzymes of the cytochrome P450 3A system. However, in a planned study of interaction with budesonide, which is a known substrate of cytochrome P450 3A, induction was not observed.
Estrogen hormones and blood cholesterol-lowering drugs such as clofibrate increase the secretion of cholesterol in the liver and therefore can stimulate the formation of gallstones, which negates the effect of ursodeoxycholic acid, which is used to dissolve gallstones.

special instructions

ѕрием урсодезоксихолевой кислоты должен осуществл¤тьс¤ под наблюдением врача.
¬ течение первых 3 мес¤цев лечени¤ следует контролировать функциональные показатели печени: трансаминазы, щелочную фосфатазу и гамма-глютамилтранспептидазу в сыворотке крови каждые 4 недели, а затем каждые 3 мес¤ца.  онтроль указанных параметров позвол¤ет вы¤вить нарушени¤ функции печени на ранних стади¤х. “акже это касаетс¤ пациентов на поздних стади¤х первичного билиарного цирроза.  роме того, так можно быстро определить, реагирует ли пациент с первичным билиарным циррозом на проводимое лечение.
ѕри применении дл¤ растворени¤ холестериновых желчных камней
?л¤ того, чтобы оценить прогресс в лечении и дл¤ своевременного вы¤влени¤ признаков кальциноза камней в зависимости от их размера, желчный пузырь следует визуализировать (пероральна¤ холецистографи¤) с осмотром затемнений в положении сто¤ и лежа на спине (ультразвуковое исследование) через 6-10 мес¤цев после начала лечени¤.
?сли желчный пузырь невозможно визуализировать на рентгеновских снимках или в случа¤х кальциноза камней, слабой сократимости желчного пузыр¤ или частых приступов колик, урсодезоксихолевую кислоту примен¤ть не следует.
ѕациенткам, принимающим урсодезоксихолевую кислоту дл¤ растворени¤ желчных камней, необходимо использовать эффективные негормональные методы контрацепции, так как гормональные контрацептивы могут увеличивать образование желчных камней (см. разделы Ђ¬заимодействие с другими лекарственными средствамиї и Ђѕрименение при беременности и в период грудного вскармливани¤ї).
ѕри лечении пациентов на поздних стади¤х первичного билиарного цирроза
 райне редко отмечались случаи декомпенсации цирроза печени. ѕосле прекращени¤ терапии отмечалось частичное обратное развитие про¤влений декомпенсации.
” пациентов с первичным билиарным циррозом в редких случа¤х в начале лечени¤ возможно усиление клинических симптомов, например, может усилитьс¤ зуд. ¬ этом случае дозу препарата необходимо снизить, а затем постепенно вновь увеличивать, как описано в разделе Ђ—пособ применени¤ и дозыї.
ѕри применении у пациентов с первичным склерозирующим холангитом
?лительна¤ терапи¤ высокими дозами урсодезоксихолевой кислоты (28-30 мг/кг/сут) у пациентов с данной патологией может вызвать серьезные побочные ¤влени¤.
” пациентов с диареей следует уменьшить дозировку урсодезоксихолевой кислоты. ѕри персистирующей диарее следует прекратить лечение.

¬ли¤ние на способность управл¤ть транспортными средствами, механизмами

Ursodeoxycholic acid does not affect the ability to drive vehicles and mechanisms, or this effect is minimal.

Release form

Capsules 250 mg.
5, 6, 10, 15, 20, 25 capsules in a blister strip packaging from a polyvinyl chloride film and printed aluminum foil varnished.
10, 20, 30, 40, 50, 60, 70, 80, 90, 100 capsules in a polymer jar made of polypropylene or low pressure polyethylene.
Each jar, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 blisters with instructions for use are placed in a cardboard box.

Storage conditions

In a dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life

3 years.
Do not use after the expiration date.

Vacation conditions

Dispensed by prescription.