the Trade name
Mezhdunarodnoye the unlicensed
name Ursodezoksikholevaya acid
the Dosage form
of the Structure One Capsule Capsule contains
active agent – acids of ursodezoksikholevy 250 mg,
excipients – silicon dioxide colloidal, hydrophosphate calcium a dihydrate, magnesium stearate, povidone, lactoses monohydrate (sugar milk),
structure of the body of a gelatin capsule: titan E171 dioxide, gelatin,
structure of a lid of a gelatin capsule: E132 indigo carmine, titan E171 dioxide, gelatin.
Solid gelatin capsules No. 0, with the body of white color and a lid of blue color. Contents of capsules – mix of granules and powder from white till almost white color.
Drugs for treatment of diseases of a liver and biliary tract. Drugs of bile acids. Ursodezoksikholevy acid.
ATX A05AA02 code
Pharmacokinetics Is Absorbed properties from a small intestine due to passive diffusion (about 90%), and
in an ileal gut by means of active transport. The maximum concentration (Cmax) at intake of 50 mg in 30, 60, 90 min. – 3.8, 5.5, 3.7 mmol/l respectively. Time of achievement of the maximum concentration (TCmax) – 1-3 h. Communication with proteins of plasma high – up to 96-99%. Gets through a placental barrier. At system administration of drug becomes the main bile acid 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 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.
Hepatoprotective means, renders bile-expelling, cholelitholytic, hypolipidemic, gipokholesterinemichesky and some immunomodulatory action.
Having high polar properties, ursodezoksikholevy acid (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 refluxezofagita. Besides, UDHK 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, UDHK 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. Immunopromoting effect 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, 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. UDHK slows down processes of senilism and death of cells (hepatocytes, holangiotsit, etc.).
Primary biliary cirrhosis in the absence of signs of a decompensation (symptomatic therapy), dissolution of small and average cholesteric stones at the functioning gall bladder, a biliary reflux gastritis.
Route of administration and doses
For dissolution of cholesteric gallstones an average daily dose – 10 mg/kg. A course of treatment – 6-12 months. For prevention of repeated formation of stones the administration of drug within several more months after dissolution of stones is recommended. At biliary a reflux gastritis the dose makes 250 mg once a day. A course of treatment – from 10-14 days to 6 months, if necessary – up to 2 years.
Symptomatic therapy of primary biliary cirrhosis: a daily dose – 10-15 mg/kg.
Capsules accept in the evening, without chewing, washing down with a small amount of water. Less than 34 kg are recommended to patients with body weight administration of drug in the form of suspension.
the Frequency of the side reactions given below was defined according to the following scheme:
– very often ≥1/10
– it is frequent ≥1/100, & lt, 1/10
– is not frequent ≥1/1000, & lt, 1/100
– is rare ≥1/10000, & lt, 1/1000
– is very rare also lt, 1/10000, including separate messages
– a dorsodynia
– diarrhea (can be dose-dependent), abdominal pain
– nausea, vomiting, calcination of gallstones, constipations, increase in activity of hepatic transaminases
– an alopecia, exacerbation of earlier being available psoriasis
– allergic reactions (a small tortoiseshell, usually in an initiation of treatment, a skin itching)
– hypersensitivity to drug components
– rentgenpolozhitelny (with the high content of Ca2+) gallstones
– a nonfunctioning gall bladder (including an empyema of a gall bladder)
– zhelche-gastrointestinal fistula
– inflammatory diseases of a small and large intestine
– acute cholecystitis, an acute cholangitis
– cirrhosis in a decompensation stage
– a liver and/or renal failure
– acute and chronic pancreatitis in an aggravation stage
– an obturation of biliary tract
– acute infectious diseases of a gall bladder and bile ducts
– pregnancy and the period of a lactation
– children’s and teenage age up to 18 years
the Antacids containing Al3 + and ion-exchange resins (Colestyraminum), 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.
At a concomitant use with cyclosporine acid ursodezoksikholevy can increase absorption of the last in intestines.
Acid ursodezoksikholevy increases effect of oral hypoglycemic drugs.
it is necessary For successful dissolution that stones were purely cholesteric, no more than 15-20 mm in size, the gall bladder is filled with stones no more than on a half and biliary tract completely kept the function.
When assigning for the purpose of dissolution of gallstones the control of activity of hepatic transaminases and the alkaline phosphatase (AP), gamma glutaminetransferase (GGT), concentration of bilirubin is necessary. The cholecystography it is necessary to spend each 4 weeks in the first 3 months of treatment, further – each 3 months. Control of efficiency of treatment to spend each 6 months during ultrasonography within the first year of therapy.
At preservation of the raised indicators, drug should be cancelled. After full dissolution of concrements it is recommended to continue use within, at least, 3 months to promote dissolution of the remains of concrements which sizes are too small for their detection.
If within 6-12 months after the beginning of therapy of partial dissolution of concrements did not occur, it is improbable that treatment will be effective.
Detection during treatment of not visualized gall bladder is the certificate that full dissolution of concrements did not happen, and treatment should be stopped.
There Is no feature of influence of medicine on ability to run the vehicle or other potentially dangerous mechanisms data.
Cases of overdose are not described. In case of overdose carry out symptomatic therapy.
A form of release and packing
of the Capsule on 250 mg.
On 10 capsules place in blister strip packaging from a film of the polyvinylchloride and printing aluminum foil varnished.
On 1, 5, 10 blister strip packagings together with the instruction for medical use in the state and Russian languages place in a pack from cardboard.
To Store storage conditions in the dry, protected from light place at a temperature not above 25 °C.
To store out of children’s reach!
not to use a period of storage after an expiration date.
According to the prescription
CJSC Kanonfarm production Producer, Russia