The instruction for medical use
of URSOSAN medicine
A trade name
Mezhdunarodnoye the unlicensed
name Ursodezoksikholevaya acid
the Dosage form
of the Capsule of 250 mg
One capsule contains
active agent – acid of ursodezoksikholevy 250 mg,
excipients: starch corn, starch corn pregelated, silicon dioxide colloidal, magnesium stearate,
Structure of a gelatin capsule: titan dioxide (E 171), gelatin.
Solid gelatin capsules of white color, size 0.
Contents of capsules white or almost white powder, either white or almost white powder with weight pieces, or the white or almost white powder pressed by a column and which is breaking up when pressing.
Drugs for treatment of diseases of a liver and biliary tract.
Drugs of bile acids. Ursodezoksikholevy acid
the ATX A05AA02 Code
Pharmacokinetics of Ursodezoksikholevaya properties acid is absorbed in a jejunum due to passive diffusion (about 90%), and in an ileal gut by means of active transport. The maximum concentration in blood serum (Cmax) at intake of 500 mg in 30, 60, 90 min. makes 3.8 mmol/l, 5.5 mmol/l and 3.7 mmol/l respectively. Cmax is reached in 1-3 h. Communication with proteins of blood plasma high – up to 96-99%. Gets through a gematoplatsentarny barrier. At systematic reception of Ursosan, ursodezoksikholevy acid makes about 48% of total amount of all bile acids in blood serum that corresponds to 40-60% of concentration of ursodezoksikholevy acid as a part of bile (at a dosage of 10-14 mg/kg of body weight). The therapeutic effect of drug depends on concentration of ursodezoksikholevy acid in bile much more, than in blood serum.
It is metabolized in a liver (clearance at primary passing through a liver) in taurinovy and glycine conjugates. The formed conjugates cosecrete in bile. About 50-70% of the general dose of drug are removed with bile. The insignificant amount of not soaked up ursodezoksikholevy acid comes to a large intestine where is exposed to splitting by bacteria (7 dehydroxylation), the formed lithocholic acid partially is soaked up from a large intestine, but sulphated in a liver and quickly removed in the form of a sulfolitokholilglitsinovy or sulfolitokholiltaurinovy conjugate.
Ursosan’s pharmacodynamics – hepatoprotective means, renders bile-expelling, cholelitholytic, hypolipidemic, gipokholesterinemichesky and some immunomodulatory action.
Having the high polarizing properties, Ursosan 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. Ursosan forms the double molecules capable to be included cellular membranes (hepatocytes, holangiotsit, digestive tract epithelial cells), to stabilize them and to do irresponsive to action of cytotoxic micelles. Reducing concentration of bile acids, toxic for a hepatic cell, and stimulating the cholepoiesis rich with bicarbonates, ursodezoksikholevy acid effectively promotes permission of an intra hepatic cholestasia. Reduces bile saturation cholesterol due to oppression of its absorption in intestines, suppression of synthesis in a liver and lowerings of secretion in bile, increases solubility of cholesterol in bile, forming with it 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-1 antigens on membranes of hepatocytes and HLA-2 on holangiotsita, normalization of natural killerny lymphocyte activity. Ursosan slows down processes of senilism and death of cells of a liver (apoptosis of hepatocytes, holangiotsit, etc.) and also prevents development of fibrosis in patients with primary biliary cirrhosis, a mucoviscidosis and an alcoholic steatogepatit, i.e. possesses anti-apoptotic, antifibrotichesky action.
– a syndrome of a biliary sladzh (cholestasia), dissolution of cholesteric gallstones at the functioning gall bladder and impossibility of removing calculus surgical or endoscopic by methods
– acute and chronic hepatitis
– toxic (including medicinal) damages of a liver
– the alcoholic liver disease
– not alcoholic steatogepatit
– primary biliary cirrhosis in compensation stage
– primary sclerosing cholangitis
– cystous fibrosis of a liver in a mucoviscidosis
– the postoperative period concerning an atresia of intra hepatic bilious ways
– dyskinesia of biliary tract
– a biliary reflux gastritis, a reflux esophagitis
– prevention of a recurrence of a lithogenesis after cholecystectomia
– prevention of damages of a liver at use of hormonal contraceptives and tsitostatik
the Route of administration and doses
Ursosan accept inside, without chewing and washing down with enough water.
In diffusion diseases of a liver the daily dose of Ursosan is divided into 2-3 receptions, capsules accept together with food.
In acute and chronic hepatitises appoint in a daily dose 10 mg/kg which is accepted 2-3 times a day together with food for a long time (from several months to several years).
In cholelithiasis (dissolution of cholesteric gallstones and biliary sladzh), dyskinesia of biliary tract the daily dose makes 15 mg/kg and is accepted once for the night. The course of treatment for dissolution of stones proceeds before full dissolution with the subsequent reception within 3 months for prevention of a recurrence of a lithogenesis. In dyskinesia of biliary tract the course of treatment is established by the doctor.
At biliary a reflux gastritis and a reflux esophagitis – on 250 mg
(1 capsule) a day, before going to bed. A course of treatment – from 10-14 days to 6 months, if necessary – up to 2 years.
After cholecystectomia for prevention of a repeated cholelithiasis – 250 mg 2 times a day within several months.
For prevention of damages of a liver at use of hormonal contraceptives and tsitostatik – 250 mg 2 times a day within several months.
At toxic, medicinal damages of a liver, an alcoholic liver disease – 10-15 mg/kg/days in 2-3 receptions. Duration of therapy is 6-12 months and more.
In primary biliary cirrhosis: 10-15 mg/kg/days (if necessary – up to 20 mg/kg) in 2-3 receptions. Duration of therapy is from 6 months to several years.
In primary sclerosing cholangitis – 12-15 mg/kg/days (up to 20 mg/kg) in 2-3 receptions. Duration of therapy is from 6 months to several years.
At not alcoholic steatogepatit – 13-15 mg/kg/days in 2-3 receptions. Duration of therapy is from 6 months to several years.
In a mucoviscidosis to children 6 years are more senior, with body weight it is more than 34 kg, appoint in a dose 20-40 mg/kg/days in 2-3 receptions. Duration of therapy is from 6 months to several years. Less than 34 kg (is more often in 6-13 years) are recommended to children with body weight a daily dose of 10 mg/kg of weight.
During the postoperative period concerning an atresia of intra hepatic bilious ways – 10-15 mg/kg/days in 2-3 receptions. Duration of therapy is 6-12 months and more.
– pain in right hypochondrium
– nausea, vomiting, diarrhea (can be dose-dependent), constipations, passing (tranzitorny) increase in activity of hepatic transaminases
– allergic reactions (a small tortoiseshell, usually in an initiation of treatment)
– exacerbation of earlier being available psoriasis, an alopecia
– calcination of gallstones
of the Contraindication
– hypersensitivity to active agent and other components of drug
– existence rentgenpolozhitelny (with the high content of calcium) gallstones
– a nonfunctioning gall bladder
– bilious, gastro, intestinal fistula
– acute cholecystitis
– an acute cholangitis
– cirrhosis in a decompensation stage
– a liver and/or renal failure
– an obturation of biliary tract
– acute infectious diseases of a gall bladder and bile ducts
– an empyema of a gall bladder
– the I trimester of pregnancy and the period of a lactation
– children’s age up to 6 years
the Antacids containing aluminum and ion-exchange resins (holestiramin) reduce absorption. Hypolipidemic medicines (especially Clofibratum), are oestrogenic, Neomycinum or progestins increase bile saturation by cholesterol and can reduce ability to dissolve cholesteric bilious concrements. Ursodezoksikholevy acid can increase absorption of cyclosporine in intestines.
At administration of drug for the purpose of dissolution of gallstones the observance of the following conditions is necessary: stones have to be cholesteric (X-ray negative), their size should not exceed 15-20 mm, the gall bladder has to remain functional and has to be filled with stones no more than on a half, the passability of a vesical and general bile duct has to be kept. At long (more than 1 month) administration of drug, each 4 weeks in the first 3 months of treatment, further – each 3 months to carry out biochemical analysis of blood for determination of activity of hepatic transaminases. Control of efficiency of treatment it is necessary to spend each 6 months according to ultrasound examination of biliary tract. After full dissolution of stones it is recommended to continue Ursosan’s use within, at least, 3 months to promote dissolution of the remains of stones which sizes are too small for their detection and for prevention of a recurrence of a lithogenesis. If in 6 months from the beginning of use the reduction of the sizes of gallstones is not observed, then it is inexpedient to continue treatment.
Use of ursodeoksikholevy acid during II and III trimester of pregnancy it is possible to appoint pregnancy and the period of a lactation after careful assessment of the expected advantage for mother and risk for a fruit from drug use.
Features of influence of drug on ability to run the vehicle or potentially dangerous mechanisms
Use of drug does not influence ability to run motor transport or potentially dangerous mechanisms.
overdose Cases are not known for ursodeoksikholevy acid
the Form of release and packing
On 10 capsules place in blister strip packagings from a film of polyvinylchloride and aluminum foil.
On 1, 5 or 10 planimetric packs together with the instruction for medical use in the state and Russian languages place in a cardboard box.
To Store storage conditions in the dry place protected from light at a temperature of 15-25 With!
To store out of children’s reach!
not to apply a period of storage after an expiration date!
According to the prescription
missile defense Producer. MED. TsS Prague and. the lake
of Telchsk 1, 140 00 Prague 4
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of goods
of PROM LLP.
Physician.KAZ G. Almaty, Dostyk Ave. 132, office 9, ph. 8 (727) 260-89-36
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