The instruction for medical use
of URSOFALK medicine
the Trade name
Mezhdunarodnoye the unlicensed
name Ursodezoksikholevaya acid
the Dosage form
of the Capsule of 250 mg
One capsule contains
active agent – ursodezoksikholevy acid of 250 mg
excipients: corn starch, silicon dioxide colloidal anhydrous, magnesium stearate, the titan dioxide (E 171), gelatin, water purified sodium lauryl sulfate.
the White opaque solid gelatin capsules, the 0 size containing the white pressed powder or granules
Drugs for treatment of diseases of a liver and biliary tract. Drugs for treatment of diseases of biliary tract. Drugs of bile acids. Ursodezoksikholevy acid.
The ATX A05AA02 code
Pharmacokinetics Later properties of intake ursodezoksikholevy acid is quickly soaked up in a small intestine and at the beginning of an ileal gut by means of passive transport and in the termination of an ileal gut by means of active transport. Absorption speed, as a rule, is 60-80%. After absorption, bile acid is exposed to almost complete pairing in a liver with amino acids taurine and glycine, and then is removed with bile. The first clearance through a liver reaches 60%.
Depending on a daily dose and the available disturbance or a condition of a liver, in bile more and more hydrophilic ursodezoksikholevy acid collects. At the same time, relative reduction of content of other, more lipophilic bile acids is observed.
Under the influence of colibacilli there is a partial splitting of drug on 7-keto-lithocholic acid and lithocholic acid. Lithocholic acid of a gepatotoksichn can also cause parenchymatous damages of a liver at some animal species. At people very small amount which is sulphated in a liver is soaked up and thus it detoksitsirutsya before excretion with bile or, finally, with a stake.
Biological elimination half-life of ursodezoksikholevy acid makes 3.5-5.8 days.
Ursofalk – a gepatoprotektor has bile-expelling effect. Reduces synthesis of cholesterol in a liver, its absorption in intestines and concentration in bile, increases solubility of cholesterol in a bile-excreting system, stimulates education and removal of bile. Having high polar properties, UDHK forms the non-toxic mixed micelles with non-polar (toxic) bile acids that reduces ability of the gastric reflyuktat to damage cellular membranes at biliary a reflux gastritis and a reflux esophagitis. Besides UDHK forms the double molecules capable to be included cellular membranes, to stabilize them and to do irresponsive to action of cytotoxic micelles. Reduces bile saturation cholesterol due to oppression of its absorption in intestines, suppression of synthesis in a liver and lowering of secretion in bile, increases solubility of cholesterol in bile, forming with them liquid crystals, reduces the litogenny index of bile. Dissolution of cholesteric gallstones and prevention of formation of new concrements is result. Immunomodulatory action is caused by oppression of an expression of HLA-of antigens on membranes of hepatocytes and holangiotsit, normalization of natural killerny lymphocyte activity, etc. Authentically delays progressing of fibrosis at patients with primary biliary cirrhosis, mucoviscidosis and an alcoholic steatogepatit, reduces risk of developing a varicosity of a gullet.
Within clinical trials the experience of use of ursodezoksikholevy acid within 10 years and more in pediatric population of patients with the gepatobiliarny disease connected with a mucoviscidosis (CFAHD) is got. There are data that use of ursodezoksikholevy acid reduces proliferation of bile ducts, slows down the damages revealed at a histologic research and even contributes to involution of changes of a gepatobiliarny system in case therapy begins at early stages of CFAHD. Therapy by ursodezoksikholevy acid should be begun after establishment of the diagnosis of CFAHD for optimization of efficiency of treatment as soon as possible.
– for dissolution of cholesteric stones of a gall bladder. Cholesteric stones should not look as blackout on the roentgenogram and should not exceed 15 mm in the diameter (despite existence of stones, function of a gall bladder should not be broken)
– for treatment biliary a reflux gastritis
– for treatment of the gepato-biliary disturbances connected with a mucoviscidosis at children from 6 to 18 years.
As a part of complex therapy:
– primary biliary cirrhosis in the absence of signs of a decompensation
the Route of administration and doses
Age restrictions for use of the Ursofalka capsules in a dosage of 250 mg are absent. For patients whose body weight less than 47 kg or patients, it is difficult for them to swallow of the Ursofalka capsules in a dosage
of 250 mg, suspensions are available to intake of 250 mg / 5мл.
Before use of the Ursofalka capsules, consult with your attending physician.
For various indications the following daily modes of dosing are recommended:
For dissolution of cholesteric gallstones
In a daily dose of 10 mg/kg of body weight daily that corresponds:
2 Ursofalka capsules at patients with body weight to 60 kg
to 3 Ursofalka capsules at patients with body weight to 80 kg
to 4 Ursofalka capsules at patients with body weight to 100 kg
to 5 Ursofalka capsules at patients with body weight
need to accept over 100 kg of the Capsule once a day before going to bed, without chewing and washing down with a small amount of liquid. To apply regularly.
Duration of treatment of 6-24 months. If the size of stones after 12 months is not reduced, treatment should not be continued. Control of efficiency of treatment is exercised by an ultrasonic method of a research or by means of X-ray analyses each 6 months. At the subsequent survey it is necessary to check whether there was no calcification of stones. In case it occurred, treatment has to be stopped.
For treatment biliary a reflux gastritis:
Appoint on one capsule, Ursofalka daily, without chewing and washing down with a small amount of liquid in the evening or before going to bed.
The course of treatment makes 10-14 days. In general, duration of use depends on the course of the disease.
For treatment of the primary biliary cirrhosis (PBC):
The daily dose of drug depends on the body weight of the patient, and varies from 3 to 7 capsules (14±2 mg of ursodezoksikholevy acid on 1 kg of body weight).
In the first 3 months of treatment the reception drug should be divided for day. After improvement of indicators of a liver it is possible to accept a daily dose of drug some times, in the evening.
Ursofalk, capsules of 250 mg
the First three months
In the evenings (1r/put)
47-62 1 1 1 3 63-78 1 1 2 4 79-93
1 2 2 5 94-109 2 2 2 6
Over 100 2 2 3 7
Capsules should be accepted, without chewing, washing down with a small amount of liquid. Capsules on 250 mg should be accepted regularly. Use of the Ursofalka capsules in a dosage of 250 mg for treatment of primary biliary cirrhosis can be continued during unlimited time.
At patients with primary biliary cirrhosis in rare instances clinical symptoms can worsen in an initiation of treatment, for example, the itching can become more frequent. In this case treatment should be continued, accepting on one Ursofalka capsule daily, further it is necessary to raise gradually a dosage (increasing a daily dose weekly by one capsule) until again the recommended dosing mode is not reached.
Children at the age of 6-18 years
the Dose: With further increase up to 30 mg/kg/days, if necessary
the Body weight (kg)
the Daily dose (mg/kg)
Ursofalk Solid capsules of 250 mg
Put 20 mg/kg/days
20 – 29 17-25 1
1 30 – 39 19-25 1 1 1 40 –
49 20-25 1 1 2 50 – 59 21-25 1 2 2 60 –
69 22-25 2 2 2 70 – 79 22-25 2 2 3 80 –
89 22-25 2 3 3 90 – 99 23-25 3 3
3 100 – 109 23-25 3 3 4
110 3 4 4
Often (≥1/100, but & lt, 1/10 people):
– a pasty chair
Very seldom (& lt, 1/10ˈ000 people):
– severe pains in a stomach, on the right side during treatment of primary biliary cirrhosis
– calcination of gallstones.
– a cirrhosis decompensation, at treatment of late stages of primary biliary cirrhosis which regresses partially after drug withdrawal.
– small tortoiseshell.
– acute inflammatory diseases of a gall bladder or bile ducts, an empyema of a gall bladder
– impassability of bile ducts (the general bile ducts or vesical channels)
– frequent episodes of hepatic gripes
– X-ray positive (with the high content of calcium) gallstones
– disturbances of contractility of a gall bladder
– hypersensitivity to components of drug or bile acids
– children up to 6 years
– children with an atresia of biliary tract: unsuccessful porto-enterostomy, normal current of bile is not restored.
Holestiramin, holestipol and the antacids containing aluminum hydroxide or smectite (aluminum oxide), reduce absorption of ursodezoksikholevy acid in intestines and thus reduce its absorption and efficiency. If use of the drugs containing at least one of these substances nevertheless is necessary, it is necessary to take them a minimum for 2 h to or after Ursofalk’s reception.
Ursodezoksikholevy acid can influence absorption of cyclosporine from intestines. Therefore at the patients accepting cyclosporine, the doctor has to check concentration of cyclosporine in blood and correct a cyclosporine dose in case of need.
In clinical trial at healthy volunteers the simultaneous use of ursodezoksikholevy acid (500 mg/day) and rosuvastatin (20 mg/day) led to slightly increased level in rosuvastatin plasma. The clinical importance of this interaction together with other statines is unknown.
In some cases Ursofalk can reduce ciprofloxacin absorption.
It is proved that ursodezoksikholevy acid reduces peak plasma concentration (Smakh) and the area under a pharmacokinetic curve – a curve “concentration time” (AUC) of a nitrendipin, the antagonist of calcium at healthy volunteers. Careful monitoring of results of simultaneous use of a nitrendipin and ursodezoksikholevy acid is recommended. Increase in a dose of a nitrendipin can be necessary. Besides, it was reported about weakening of therapeutic effect of dapsone.
On the basis of the provided data and also results of the researches in vitro, it is possible to assume that ursodezoksikholevy acid, induces enzymes 3A of P450 cytochrome, nevertheless, according to adequate clinical trial of medicinal interactions, ursodez-oxycholic acid does not cause the significant induction of a budesonid who belongs to substrates of P450 3A cytochrome.
The estrogenic hormones and agents reducing cholesterol level in blood, such as Clofibratum increase hepatic secretion of cholesterol and, therefore, can stimulate formation of gallstones that is countereffect of the ursodezoksikholevy acid used for dissolution of stones in a gall bladder.
Functional indicators of a liver of nuclear heating plant (SGOT), ALT (SGPT) and gamma GT it is necessary to control special instructions Within the first three months of treatment each 4 weeks, and then each 3 months. Monitoring of the specified parameters allows to reveal abnormal liver functions at early stages, in particular – at patients at late stages of primary biliary cirrhosis, besides, thus it is possible to define quickly whether the patient with primary biliary cirrhosis reacts to the carried-out treatment.
At use for dissolution of cholesteric gallstones:
For assessment of progress in treatment and early detection of symptoms of calcification of stones depending on the size of stones, the gall bladder should be visualized (the oral cholecystography) with survey of blackouts in a standing position and lying on spin (ultrasonography) in 6-10 months after an initiation of treatment.
If the gall bladder cannot be visualized on x-rays or in cases of calcification of stones, weak contractility of a gall bladder or frequent attacks of gripes, the Ursofalk capsules of 250 mg should not be used.
Women when using the Ursofalk capsules of 250 mg for dissolution of cholesteric gallstones have to use an effective non-hormonal method of contraception as hormonal contraceptives can increase formation of gallstones.
At treatment of patients at late stages of primary biliary cirrhosis:
Cirrhosis decompensation cases which partially regressed after the treatment termination were extremely seldom noted.
At patients with primary biliary cirrhosis in rare instances clinical symptoms can worsen in an initiation of treatment, for example, the itching can increase. In such cases the dose of the Ursofalk capsules of 250 mg has to be reduced to one Ursofalk capsule of 250 mg a day, and then gradually again is increased.
In case of diarrhea, the dose has to be reduced, in case of persistent diarrhea, treatment has to be stopped.
Pregnancy and the period of a lactation
of the Research on animals did not show influence of UDHK on fertility. Researches in public about influence on birth rate after treatment of UDHK are absent.
Data on use of ursodezoksikholevy acid for pregnant patients are absent, or are limited. Researches on animals demonstrate existence of teratogenic action during an early phase of pregnancy. It is not necessary to use the Ursofalka capsules during pregnancy without obvious need. Women of childbearing age have to take the drug, only against the background of use of reliable means of contraception.
It is recommended to use non-hormonal methods of contraception, or with the low content of estrogen. At the patients receiving Ursofalk capsules of 250 mg for destruction of stones of a gall bladder it is necessary to use non-hormonal methods of contraception as hormonal contraceptives can promote formation of stones. The possibility of pregnancy, has to be excluded prior to treatment.
According to several confirmed cases, concentration of ursodezoksikholevy acid in milk of the feeding women it is small, emergence of undesirable reactions at children against the background of feeding by a breast is improbable.
The feature of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
does not influence.
At overdose can be diarrhea. Other symptoms of overdose are improbable as absorption of ursodezoksikholevy acid decreases with increase in a dose and, therefore, is more allocated with excrements.
Treatment: diarrheas symptomatic with completion of volume of liquid and electrolytic balance.
Long-term treatment by high doses is (not for the intended purpose) connected by ursodezoksikholevy acid (28-30 mg/kg/day) at patients with primary sclerosing cholangitis with higher rates of serious side effects.
The form of release and packing
On 25 capsules place in blister strip packagings from a film of polyvinylchloride and aluminum foil.
On 1 and 2 planimetric packs together with the instruction for medical use in the state and Russian languages place in a cardboard box.
To Store storage conditions at a temperature not above 25 °C, in the place protected from light.
To store out of children’s reach!
Not to apply a period of storage of 5 years after an expiration date!
According to the prescription
the Producer / Organization-upakovshchik of medicine
Lozan Farma GmbH Otto Khan Strasse 13 79395 Noyenburg, Germany
the Owner of the registration certificate
of Dr. Falk Pharm GmbH
79108 Freiburg, Germany
the Esklyuzivny representative
of Alpen Pharm AG, Bern, Switzerland
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods)
of Alpen Pharm LLP
of Almaty, mdt. Zhetysu-2, 80, quarter 54
Ph./fax + 7 727 2265306
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