Ursosan Forte tabs 500mg #50

Instruction for Ursosan Forte

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Ursosan Forte is a hepatoprotective agent.

Release form and composition

Dosage form - film-coated tablets: oblong, convex on both sides, with a dividing line on one side and a notch on the other, almost white or white (in a cardboard box, instructions for the use of Ursosan Forte and 1, 5 or 10 cell contour packs containing 10 tablets).
Composition of 1 tablet:
    active substance: ursodeoxycholic acid - 500 mg;
    auxiliary components: sodium carboxymethyl starch (type A), magnesium stearate, colloidal silicon dioxide, corn starch (including pregelatinized);
    film casing: Opadrai white 03В28796 (titanium dioxide, hypromellose 6, macrogol 400).

Pharmacodynamics

Ursodeoxycholic acid (UDCA) is a hepatoprotective active substance with cholelitholytic, choleretic, hypocholesterolemic and immunomodulatory effects.
UDCA has high polar properties, due to which it is able to integrate into the membrane of epithelial cells, hepatocytes and cholangiocytes of the gastrointestinal tract. As a result, it stabilizes the structure of the membrane and protects against the damaging effects of toxic bile salts, thereby reducing their cytotoxic effect.
UDCA forms non-toxic mixed micelles with toxic lipophilic bile acids. As a result, with biliary reflux gastritis and cholestatic liver diseases, it reduces the damaging effect of gastric refluctate on cell membranes.
In cholestasis, Ursosan Forte activates Ca2 + -dependent alpha-protease and exocytosis. In patients with chronic liver disease, it reduces the increased concentration of toxic bile acids (including deoxycholic, lithocholic and chenodeoxycholic). By reducing the content of these acids and stimulating choleresis rich in bicarbonates, the drug helps to eliminate intrahepatic cholestasis.
UDCA competitively reduces the absorption of lipophilic bile acids in the intestine, and increases their fractional turnover during enterohepatic circulation. Stimulates choleresis, bile passage and intestinal excretion of toxic bile acids.
Ursosan Forte inhibits the absorption of cholesterol in the intestine, reduces its synthesis and secretion into bile, thereby reducing the concentration in bile. The drug reduces the lithogenic index of bile and increases the content of bile acids in it, removes cholesterol from gallstones. As a result of these properties, under the influence of UDCA, there is a gradual breakdown of cholesterol gallstones.
The substance enhances lipase activity, gastric and pancreatic secretion, has a hypoglycemic effect.
The immunomodulatory effect of UDCA is due to the following properties:
    inhibition of the expression of histocompatibility antigens (HLA-1 on hepatocyte membranes and HLA-2 on cholangiocytes);
    normalization of natural killer activity of T-lymphocytes;
    the formation of interleukin-2;
    suppression of immunocompetent immunoglobulins (Ig), especially IgM;
    decrease in the number of eosinophils;
    regulation of apoptosis of epithelial cells and hepatocytes in the gastrointestinal tract.
Ursosan Forte inhibits the progression of fibrosis. It is a participant in the regulation of the processes of apoptosis of epithelial cells, hepatocytes and cholangiocytes of the gastrointestinal tract.

The use of UDCA in the treatment of cystic fibrosis in children

There is more than 10 years of experience in the use of UDCA in children with hepatobiliary disease due to cystic fibrosis (CFAHD).
According to clinical reports, the drug lowers the proliferation of bile ducts, slows down the development of lesions diagnosed during histological examination. If treatment is started early in CFAHD, UDCA also reverses changes in the hepatobiliary system.

Pharmacokinetics

When taken orally, UDCA is rapidly absorbed through passive diffusion in the jejunum and the proximal ileum, due to active transport in the distal ileum. About 60-80% of the dose taken is absorbed.
Regular intake contributes to the fact that UDCA becomes the main bile acid in the blood serum. The accumulation of acid depends on the type of disease, the state of the patient's liver and the dose of Ursosan Forte taken. At the same time, the amount of other lipophilic bile acids decreases slightly.
UDCA undergoes metabolism in the liver (during the initial passage, the clearance can reach 60%) with the formation of glycine and taurine conjugates - they are secreted into bile, through which from 50 to 70% of the drug dose is excreted.
A small amount of UDCA, not absorbed in the small intestine, enters the large intestine and is broken down there by bacteria (7-dehydroxylation process), resulting in the formation of lithocholic and 7-keto-lithocholic acids.
Lithocholic acid has a toxic effect on the liver. In some animals in the study, it caused damage to the hepatic parenchyma. In the human body, it is absorbed in a small amount, and then metabolized by sulfation to sulfolitocholyltaurin or sulfolitocholylglycine conjugate in the liver, due to which it is detoxified before being excreted into bile. It is excreted in the feces.
The half-life (T1 / 2) from the human body is 3.5-5.8 days.

Indications for use

    non-alcoholic fatty liver disease, including steatohepatitis;
    cholestatic liver diseases of various origins, including cystic fibrosis (cystic fibrosis), primary sclerosing cholangitis and primary biliary cirrhosis (without signs of decompensation);
    chronic hepatitis of various origins (medicinal, toxic, etc.);
    alcoholic liver disease;
    biliary reflux gastritis;
    uncomplicated gallstone disease: cholesterol gallstones with a functioning gallbladder, biliary sludge;
    biliary dyskinesia.

Contraindications

    severe liver failure;
    decompensated cirrhosis of the liver;
    frequent bouts of biliary colic;
    violation of the contractility of the gallbladder;
    occlusion of the bile duct (cystic or common bile duct);
    acute inflammatory diseases of the bile ducts and gallbladder;
    X-ray positive gallstones (high in calcium)
    severe renal failure;
    children under 3 years old;
    Difficulty swallowing tablets (due to solid dosage form) in children over 3 years of age
    unsuccessful portoenterostomy in pediatric patients as a result of atresia of the biliary tract, in cases where it was not possible to restore the normal flow of bile;
    pregnancy;
    hypersensitivity to any component of Ursosan Forte.

Ursosan Forte, instructions for use: method and dosage

Ursosan Forte tablets should be taken orally during or after a meal, swallowed whole with sufficient water. If necessary, the tablet can be broken at the prescribed risk. Broken segments should not be accepted.
For dissolving cholesterol gallstones, the recommended daily dose of Ursosan Forte is 10 mg / kg. Correspondence of the dose to the tablets, depending on the patient's weight:
    <60 kg - 1 tablet;
    61–80 kg - 1½ tablets;
    81-100 kg - 2 tablets;
    > 100 kg - 2½ tablets.
During the first 3 months of therapy, the daily dose should be divided into several doses. The course of treatment can be from 6 to 24 months. If, after 12 months of treatment, there is no decrease in the size of the stones, further administration of Ursosan Forte is inappropriate.
The effectiveness of therapy is assessed every 6 months by means of radiography or ultrasound examination. In intermediate examinations, it is necessary to establish the condition of the stones, whether they have calcified. If this happens, the drug is canceled.
To avoid relapse, Ursosan Forte should be continued for several months after the stones dissolve.
For cholestatic liver diseases, the recommended dose is 12–15 mg / kg / day. In the first 3 months, the daily dose should be divided into several doses, after improvement of liver function tests, a single dose of Ursosan Forte is allowed in the evening. Recommended daily doses depending on the patient's body weight:
    47–62 kg - 12–16 mg / kg: during the first 3 months - ½ tablet in the morning, afternoon and evening, then - 1½ tablets once a day, in the evening;
    63–78 kg - 13–16 mg / kg: the first 3 months - ½ tablet in the morning and in the afternoon, 1 tablet in the evening, then - 2 tablets in the evening;
    79–93 kg: 13–16 mg / kg: for the first 3 months - ½ tablet in the morning, 1 tablet in the afternoon and in the evening, then 2½ tablets in the evening;
    94-109 kg: 14-16 mg / kg: the first 3 months - 1 tablet in the morning, afternoon and evening; then - 3 tablets in the evening;
    110 kg: for the first 3 months - 1 tablet in the morning and in the afternoon, 1½ tablets in the evening, then 3½ tablets in the evening.
In primary biliary cirrhosis, treatment can be continued indefinitely. In rare cases, at the beginning of therapy, it is possible to increase the clinical symptoms of the disease, for example, increased itching. Under these circumstances, ½ tablet of Ursosan Forte should be taken daily and gradually increased (by ½ tablet every week) until the therapeutic dose prescribed by the doctor is reached.
In primary sclerosing cholangitis, 12-15 mg / kg is prescribed per day, in some cases the dose is increased to 20 mg / kg. The daily dose should be divided into 2-3 doses. The course of therapy is from 6 months to several years.
Ursosan Forte with cystic fibrosis is used as part of complex therapy. The recommended daily dose is 20 mg in 2 or 3 divided doses, if necessary, it is further increased to 30 mg / kg.
The recommended dosage regimen of Ursosan Forte, depending on the patient's weight:
    20-29 kg - 17-25 mg / kg: ½ tablet in the morning and in the evening;
    30–39 kg - 19–25 mg / kg: ½ tablet in the morning, afternoon and evening;
    40–49 kg - 20–25 mg / kg: ½ tablet in the morning and in the afternoon, 1 tablet in the evening;
    50-59 kg - 21-25 mg / kg: ½ tablet in the morning, 1 tablet in the afternoon and evening;
    60–69 kg - 22–25 mg / kg: 1 tablet 3 times a day;
    70–79 kg - 22–25 mg / kg: 1 tablet in the morning and in the afternoon, 1½ tablets in the evening;
    80–89 kg - 22–25 mg / kg: 1 tablet in the morning, 1½ tablets in the afternoon and evening;
    90–99 kg - 23–25 mg / kg: 1½ tablets 3 times a day;
    100-109 kg - 23-25 ​​mg / kg: 1½ tablets in the morning and in the afternoon, 2 tablets in the evening;
    > 110 kg: 1½ tablets in the morning, 2 tablets in the afternoon and evening.
For chronic hepatitis, non-alcoholic fatty disease and alcoholic liver disease, Ursosan Forte is prescribed at 10-15 mg / kg / day. The dose is divided into 2-3 doses. The course of therapy is 6–12 months. In some cases, longer treatment may be required.
Dyskinesia of the biliary tract is treated at 10 mg / kg. The dose is divided into 2 doses. The duration of treatment is 0.5–2 months. If necessary, repeat the course.
The daily dose for biliary reflux gastritis averages 250 mg (½ tablet). Ursosan Forte should be taken once a day, in the evening. The therapy can last from 10 days to 6 months. In some cases, it lasts for 2 years.

Calculation of the daily number of tablets

The daily number of Ursosan Forte tablets depending on the patient's body weight when prescribing a dose of 10 mg / kg / day:
    19–35 kg - ½ tablet;
    36-60 kg - 1 tablet;
    61–85 kg - 1½ tablets;
    86-110 kg - 2 tablets.
The daily number of tablets when prescribing a dose of 12 mg / kg / day:
    19-30 kg - ½ tablet;
    31-50 kg - 1 tablet;
    51–70 kg - 1½ tablets;
    71–90 kg - 2 tablets;
    91-110 kg - 2½ tablets.
The daily number of tablets when prescribing a dose of 15 mg / kg / day:
    19-40 kg - 1 tablet;
    41–55 kg - 1½ tablets;
    56–70 kg - 2 tablets;
    71–90 kg - 2½ tablets;
    91-105 kg - 3 tablets;
    106-110 kg - 3½ tablets.
The daily number of tablets when prescribing a dose of 20 mg / kg / day:
    19-30 kg - 1 tablet;
    31-40 kg - 1½ tablets;
    41–55 kg - 2 tablets;
    56–65 kg - 2½ tablets;
    66–80 kg - 3 tablets;
    81–90 kg - 3½ tablets;
    91-105 kg - 4 tablets;
    106-110 kg - 4½ tablets.
The daily number of tablets when prescribing a dose of 30 mg / kg / day:
    19-30 kg - 1½ tablets;
    31–35 kg - 2 tablets;
    36–45 kg - 2½ tablets;
    45-50 kg - 3 tablets;
    51-60 kg - 3½ tablets;
    61–70 kg - 4 tablets;
    71–75 kg - 4½ tablets;
    76–85 kg - 5 tablets;
    86–95 kg - 5½ tablets;
    96-100 kg - 6 tablets;
    101-110 kg - 6½ tablets.

Side effects

    from the gastrointestinal tract: often (≥ 1/100 to <1/10) - diarrhea, loose stools;
    from the liver and biliary tract: very rarely (<1/10 000) - calcification of gallstones; with primary biliary cirrhosis, acute pain in the right upper abdomen; in the late stages of primary biliary cirrhosis, decompensation of liver cirrhosis, regressing after discontinuation of Ursosan Forte;
    from the skin and subcutaneous tissues: very rarely - allergic reactions (including urticaria).

Overdose

An overdose of Ursosan Forte is fraught with diarrhea. If there is prolonged diarrhea, the drug should be discontinued and symptomatic treatment should be carried out (restoration of water-electrolyte balance).
With an increase in the dose, the resorption of UDCA worsens and its excretion with feces increases, so the development of other symptoms of an overdose is unlikely.

Special instructions

In the presence of stones in the gallbladder, the appointment of Ursosan Forte is possible only in the following cases:
    stones are cholesterol (X-ray negative), their size does not exceed 15-20 cm;
    the gallbladder is filled with stones no more than half, its function is preserved;
    the cystic and common bile ducts are not blocked.
With long-term use of Ursosan Forte to dissolve gallstones, a biochemical blood test should be done regularly to determine the activity of microsomal liver enzymes (alkaline phosphatase, transaminase, gamma-glutamyl transpeptidase): in the first 3 months of therapy - every 4 weeks, then - once every 3 months. Monitoring of these parameters allows early detection of possible liver dysfunction. Similar recommendations apply to patients receiving treatment for advanced primary biliary cirrhosis, and these tests can be used to check how the patient is responding to treatment.
In cholesterol gallstones, to assess progress and timely detect signs of calcification, the gallbladder should be visualized (using oral cholecystography) 6–10 months after the start of treatment with an examination of the dark areas in the supine position and standing. Ursosan Forte should be canceled in case of calcification of stones, inability to visualize the gallbladder on X-ray images, weak contractility of the gallbladder, frequent attacks of colic.
Long-term use of high doses of UDCA (28–30 mg / kg per day) in patients with primary sclerosing cholangitis may cause serious side effects.
Women of childbearing age should use reliable methods of contraception during treatment. It is recommended that you choose non-hormonal contraceptives or oral medications that are low in estrogen. Hormonal agents can increase the formation of gallstones. You can start taking Ursosan Forte only after pregnancy has been ruled out.
Treatment with the drug should be carried out under the close supervision of a physician.

Influence on the ability to drive vehicles and complex mechanisms

Ursosan Forte does not have a negative effect on the cognitive and psychophysical functions of a person.

Application during pregnancy and lactation

Adequate and controlled studies on the effect of UDCA on the course of pregnancy in humans have not been conducted. In animal studies, it has been found that the drug exhibits reproductive toxicity in the early stages of pregnancy. As a result, the use of Ursosan Forte during gestation is possible only in extreme cases, when the expected benefit to the woman is definitely higher than the potential risks to the fetus.
UDCA can pass into breast milk in very low concentrations, therefore, side effects are not expected in infants whose mothers took the drug during lactation.

Childhood use

Due to the solid dosage form, Ursosan Forte 500 mg tablets are not prescribed for children under 3 years of age. Also, the tablets should not be given to children who have difficulty swallowing.
It is contraindicated to prescribe the drug to pediatric patients with biliary atresia in case of an unsuccessful portoenterostomy and the absence of a normal bile flow.

With impaired renal function

Ursosan Forte should not be prescribed for severe renal failure.

For violations of liver function

Ursosan Forte is prohibited for use in severe liver failure.

Drug interactions

UDCA can enhance the absorption of cyclosporine from the intestine, therefore, its concentration in the blood plasma should be monitored and the dose adjusted if necessary.
In some cases, the drug can reduce the absorption of ciprofloxacin.
Ursosan Forte should not be used in conjunction with antacids containing ion exchange resins, smectite or aluminum hydroxide, since they reduce the absorption of UDCA in the intestine and, as a result, its effectiveness. If the use of these drugs is necessary, at least 2-hour intervals should be observed between doses.
Some drugs, such as hormonal contraceptives, clofibrate and neomycin, can increase cholelithiasis, resulting in the opposite effect of UDCA in dissolving cholesterol gallstones.
Ursosan Forte reduces the therapeutic effect of dapsone.
In a clinical study, healthy volunteers simultaneously took UDCA (in a daily dose of 500 mg) and rosuvastatin (in a daily dose of 20 mg). A slight increase in the plasma concentration of rosuvastatin was noted. The clinical significance of this phenomenon has not been established, including with the use of other statins.
UDCA reduces the Cmax (maximum concentration) and AUC (area under the concentration-time curve) of nitrendipine. When they are used together, the concentration of the latter in the blood plasma should be carefully monitored and, if necessary, the dose should be increased.
Information on pharmacological interactions and data obtained under in vitro conditions suggest that UDCA is capable of inducing CYP3A isoenzymes. However, the results of controlled clinical trials show that the drug does not have a pronounced inducing activity against the CYP3A isoenzyme.

Terms and conditions of storage

Store at a temperature of 15-25 ° C, protected from light, out of reach of children.
The shelf life is 5 years.

Reviews about Ursosan Forte

According to reviews, Ursosan Forte is an effective drug that dissolves stones in the gallbladder well, protects the liver, lowers blood cholesterol, and improves bile passage. It can be used for a long time, practically does not cause side effects.
In rare negative reviews, patients complain that the drug did not help them dissolve gallstones or caused the development of undesirable reactions not specified in the instructions, such as constipation, hair loss, increased hepatic transaminases, discomfort and pain in the stomach.

Terms of sell

You don't need a prescription to buy Ursosan Forte.