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

Excipients: cellulose microcrystalline 23 mg, povidone-K 25-15 mg, crospovidone (type A) 12.5 mg, talc 8.5 mg, magnesium stearate 5 mg, silicon colloidal dioxide 4 mg, polysorbate 80 2 mg, film membrane: hypromellose - 5.7 mg, talc - 1.45 mg, macrogol-6000 - 0.85 mg.

Description:

Biconvex, oblong-shaped tablets, coated with a film coat of white, with a risk on both sides.

Pharmacotherapeutic group:hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Hepatoprotective agent, has a cholagogue effect. Reduces the synthesis of cholesterol in the liver, its absorption in the intestine and concentration in the 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; causes an increase in gastric and pancreatic secretion, increases lipase activity, and 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, the formation of interleukin-2, reduces the number of eosinophils.

Pharmacokinetics:

After oral administration ursodeoxycholic acid quickly 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. About 60-80% is absorbed. After absorption, bile acid is almost completely conjugated in the liver with glycine and taurine and is excreted with 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, a relative decrease in the content of other more lipophilic bile acids is observed.

Under the influence of intestinal bacteria ursodeoxycholic acid partially destroyed with the formation of 7-keto-lithocholic and lithocholic acids. Lithocholic acid is hepatotoxic, in some animal species it causes damage to the liver parenchyma. In man, it is absorbed only in a small amount, sulfated in the liver and, thus, detoxified before excretion into bile and excretion with feces. The half-life of ursodeoxycholic acid is 3.5-5.8 days.

Indications:

Dissolution of gallstones cholesterol stones, 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 (as part of complex therapy), non-alcoholic steatohepatitis, alcoholic liver disease, dyskinesia of biliary excrement ways.

Contraindications:

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

Children under the age of 3 years, as well as patients with difficulty in swallowing tablets, it is recommended to use the drug Ursofalk in suspension.

Pregnancy and lactation:

Sufficient data on the use of ursodeoxycholic acid in the first trimester of pregnancy are absent. The drug should not be used during pregnancy, except in cases of extreme necessity. Women of childbearing age can take the drug only if they use reliable contraceptives.

It is recommended to use non-hormonal contraceptives, or oral contraceptives with a low estrogen content, as hormonal oral contraceptives can enhance gallstone stone formation. Before the start of treatment, a possible pregnancy should be excluded.

It is not established whether it penetrates ursodeoxycholic acid in breast milk. In this regard, you should not take the drug Ursofalk during lactation.If it is necessary to treat the drug, breastfeeding should be discontinued.

Dosing and Administration:

For patients who can not swallow the drug Ursofalk, tablets coated with a film coat of 500 mg, or with a body weight of less than 47 kg, Ursofalk is recommended in capsules or suspensions. Tablets should be taken without chewing, squeezed with liquid. They should be taken regularly.

Dissolution of cholesteric gallstones

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

up to 60 kg	1 tablet
61-80 kg	1¹/₂ pills
81-100 kg	2 tablets
more than 100 kg	2¹/₂ pills

To dissolve gallstones, it usually takes 6-24 months. If after 12 months of treatment the size of the stones does not decrease, then the treatment should be stopped.

The effectiveness of treatment should be evaluated every 6 months with ultrasound or radiography. During the interim survey, it should be assessed whether stone calcification has occurred during the past period. In the case of calcification of stones, treatment should be discontinued.

Treatment of biliary reflux gastritis

For 250 mg (1/2 tablet) daily in the evening before bedtime.

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 varies from 1 to 3 tablets (14 ± 2 mg 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 dose daily dose in the evening.

Body weight (kg)	Daily dose (mg / kg)	Ursofalk®, film-coated tablets, 500 mg
		first 3 months			in the future
		morning	noon	evening	evening (single entry reception)
47-62	12-16	1/2	1/2	1/2	1¹/₂
63-78	13-16	1/2	1/2	1	2
79-93	13-16	1/2	1	1	2¹/₂
94-109	14-16	1	1	1	3
more than 110	-	1	1	11/2	3¹/₂

The use of the drug Ursofalka for the treatment of primary biliary cirrhosis can continue 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, treatment should be continued, taking 1/2 tablet daily, then gradually increase the dose (increasing the daily dose weekly for ½ tablets) until the recommended dosing regimen is again achieved.

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

Primary sclerosing cholangitis - daily dose of 12-15 mg / kg; if necessary, the dose may be increased to 20 mg / kg in 2-3 doses. Duration of therapy is from 6 months to several years (see section: "Special instructions")

Cystic fibrosis (as part of complex therapy) - daily dose of 12-15 mg / kg; if necessary, the dose may be increased to 20 mg / kg in 2-3 doses. The duration of therapy is from 6 months to several years.

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

Alcoholic liver disease - the average daily dose of 10-15 mg / kg in 2-3 doses The duration of therapy is from 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 effects:

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

Very frequent (≥1 / 10)

Frequent (≥1 / 100 - <1/10)

Infrequent (≥1 / 1000 - <1/100)

Rare (≥1 / 10000 - <1/1000)

Very rare (<1/10000).

Disorders from the gastrointestinal tract:

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

In the treatment of primary biliary cirrhosis, very rarely there were acute pains in the right upper abdomen.

Disturbances from the liver and bile ducts:

In very rare cases, against the background of treatment with ursodeoxycholic acid, calcification of gallstones can occur.

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

Disturbances from the skin and subcutaneous tissues:

In very rare cases, there may be allergic reactions, including hives.

If any of the side effects indicated in the manual is aggravated, or if you notice other side effects not listed in the instructions, please inform your doctor.

Overdose:

In case of an overdose, diarrhea may occur. In general, other symptoms of an overdose are unlikely, as with the increase in the dose of ursodeoxycholic acid, its absorption decreases, and excretion with colonic masses increases.

Specific treatment is not required. The consequences of diarrhea are treated symptomatically (restoration of the water-electrolyte balance).

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 prior to taking Ursofalk.

Ursodeoxycholic acid can enhance the absorption of cyclosporine from the intestine. Therefore, in patients who simultaneously take ciclosporin, it is necessary to determine the concentration of cyclosporine in the blood and, if necessary, adjust the dose of cyclosporine.

Ursodeoxycholic acid can reduce the absorption of ciprofloxacin. It is proved that ursodeoxycholic acid reduces the maximum concentration and area under the pharmacokinetic concentration-time curve of the calcium antagonist nitrendipine. In addition, a decrease in the therapeutic effect of dapsone has been reported.

This information, as well as the data received in vitro, suggest that ursodeoxycholic acid can induce isoenzymes CYP3A. Nevertheless, the results of controlled clinical trials indicate that ursodeoxycholic acid does not exert a pronounced induction effect on the isoenzyme CYP3A.

Estrogens, hypolipidemic drugs such as clofibrate, increase bile saturation with cholesterol and can reduce the litholytic effect of ursodeoxycholic acid.

Special instructions:

Ursofalk should be taken under medical supervision. During the first 3 months of treatment, liver function tests (transaminases, alkaline phosphatase and gamma-glutamyltranspeptidase) in the blood serum should be monitored 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 quickly determine if the patient is responding to primary biliary cirrhosis for ongoing treatment.

When used in patients to dissolve cholesterol gallstones:

In order to assess the progress in treatment and for the timely detection of signs of calcification of stones depending on the size of the stones,the gallbladder should be visualized (oral cholecystography) with examination of blackouts in the "standing" and "lying on the back" (ultrasound) 6-10 months after the start of 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, Ursofalk should not be used.

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

Very rarely there were cases of decompensation of liver cirrhosis. After discontinuation of therapy, regression of manifestations of decompensation was noted.

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.

Patients with diarrhea should reduce the dosage of the drug. With persistent diarrhea, treatment should be discontinued.

Women of childbearing age can take the drug only if they use reliable contraceptives. It is recommended to use non-hormonal contraceptives,or oral contraceptives with a low estrogen content, since hormonal oral contraceptives can enhance gallstone stone formation. Before the start of treatment, a possible pregnancy should be excluded.

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

Effects on the ability to drive vehicles and moving mechanisms are not revealed.

Form release / dosage:Tfilm coated abeyes, 500 mg.

Packaging:

For 25 tablets in a contour mesh box made of PVC / PVDC film / aluminum foil (blister).

For 2 or 4 blisters together with instructions for medical use in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003568

Date of registration:14.04.2016

Expiration Date:14.04.2021

The owner of the registration certificate: Dr. Falk Farma GmbH Dr. Falk Farma GmbH Germany

Manufacturer: & nbsp

Dr. FALK PHARMA, GmbH Germany

Representation: & nbspDOCTOR FALK PHARMA GmbH DOCTOR FALK PHARMA GmbH Germany

Information update date: & nbsp17.06.2016

Illustrated instructions

Instructions

Ursofalk (Ursofalk®)