The instruction for medical use
of Dezursolen Torgovoye medicine a name
Mezhdunarodnoye the unlicensed
name Ursodezoksikholevaya acid
the Dosage form
of the Capsule with the modified release of 450 mg
One capsule contains
active agent – ursodezoksikholevy acid of 450 mg,
excipients: hydroxypropyl cellulose, cellulose microcrystalline,
structure of a cover of the capsule: the titan dioxide (E 171), gelatin
Solid gelatin capsules of 00 in size with the body and a lid of white color. Contents of capsules – round microgranules of white color
Drugs for treatment of diseases of a liver and biliary tract. Drugs for treatment of a gall bladder. Drugs of bile acids. Ursodezoksikholiyevy acid
the ATX A05AA02 Code
After intake ursodezoksikholevy acid is well soaked up from digestive tract. It is metabolized in a liver in taurinovy and glycine conjugates. The formed conjugates cosecrete in bile. The insignificant amount of not soaked up ursodezoksikholiyevy acid comes to a large intestine where is exposed to splitting by bacteria.
Gets through a placental barrier. About 50-70% of a dose are removed with bile, the rest with a stake.
The therapeutic effect depends generally on concentration of ursodezoksikholevy acid in bile, but not in blood serum.
The developed dosage form in the form of capsules with the modified release causes gradual release of active agent and its receipt in intestines at different times, and respectively and longer elimination half-life. It provides bioavailability within about 7-8 hours. This form has advantages due to single dose in day, thereby providing effective concentration of ursodezoksikholevy acid in plasma during 24 h.
Active agent of drug – ursodezoksikholevy acid (UDHK).
Dezursolen renders hepatoprotective, bile-expelling, cholelitholytic, hypolipidemic, gipokholesterinemichesky action.
Drug reduces bile saturation by cholesterol by reduction of synthesis and secretion of cholesterol in a liver and inhibition of its absorption in intestines.
Increases solubility of cholesterol in a bile-excreting system, stimulates education and biliation. Having high polar properties, ursodezoksikholevy acid 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, ursodezoksikholevy acid forms the double molecules capable to be included cellular membranes of hepatocytes, holangiotsit, GIT epithelial cells, to stabilize them and to do irresponsive to action of cytotoxic micelles.
Reducing concentration of bile acids, toxic for hepatocytes, and stimulating a cholepoiesis, ursodezoksikholevy acid promotes permission of an intra hepatic cholestasia.
The therapeutic effectiveness of Dezursolen is caused by his ability to reduce the litogenny index of bile, to dissolve cholesteric gallstones and to prevent formation of new concrements, to eliminate the dispepsichesky symptoms accompanying gepatobiliarny pathologies.
– dissolution of X-ray negative cholesteric stones of a gall bladder and the stones remaining after bile duct surgery
as a part of complex therapy:
– primary biliary cirrhosis in the absence of signs of a decompensation
the Route of administration and doses
select the Dose of drug individually, depending on severity of a disease.
At long-term treatment, for dissolution of gallstones, the average daily dose makes 450 mg. At the patients having obesity, the daily dose can be increased up to 900 mg.
For maintenance of the correct conditions of dissolution of the existing gallstones, duration of treatment is not less than 4-6 months, is more often up to 9 months without interruption, besides treatment has to be continued within 3-4 months after x-ray and ultrasonographies showed lack of bilious concrements.
In primary biliary cirrhosis in the absence of signs of a decompensation the daily dose makes 8-10 mg kg of body weight (1 capsule).
The doctor can make the decision to correct a dose: in particular, if Dezursolen is well had, he can be accepted in much higher doses.
Capsules with the modified release need to be accepted once a day before going to bed, without chewing and washing down with a small amount of water.
The general course of treatment should not exceed 2 years.
Often (& gt, 1/100 and & lt, 1/10)
– a pastopodobny chair, diarrhea
Seldom (& gt, 1/10.000 and & lt, 1/1.000)
nausea, vomiting, a constipation, passing increase in activity of hepatic transaminases
it is Very rare (& lt, 1/10.000)
– abdominal pain with localization in right hypochondrium or in epigastric area (at treatment of primary biliary cirrhosis)
– calcination of bilious concrements
– a decompensation of primary biliary cirrhosis (with partial regression after the treatment termination)
– allergic reactions (urticaria, a skin itching)
of the Contraindication
– hypersensitivity to active agent, bile acids or auxiliary components of drug
– acute inflammatory diseases of a gall bladder, biliary tract or intestines, including an empyema of a gall bladder
– obstruction of biliary tract (general hepatic or vesical channels)
– frequent biliary gripes
– the X-ray positive (calcinated) concrements of a gall bladder
– disorder of motor activity of a gall bladder, a nonfunctioning
gall bladder, bilious fistula, bilious and gastrointestinal fistula
– cirrhosis in a decompensation stage
– a heavy liver or renal failure
– acute pancreatitis
– children’s age up to 18 years
– pregnancy and the period of a lactation
At simultaneous use with other medicines are possible the following interactions:
with Colestyraminum, kolestipoly or the antiacid drugs containing aluminum as these drugs in intestines connect ursodezoksikholevy acid and, thus, inhibit its absorption and reduce efficiency of therapy. If use of the drugs containing one of these substances is necessary, they should be applied in 2 hours prior to or after reception Dezursolen.
with cyclosporine – ursodezoksikholevy acid can increase intestinal absorption of cyclosporine. Therefore when performing such combination therapy it is necessary to control the serumal level of cyclosporine and if necessary to regulate its dose.
with ciprofloxacin – in some cases ursodezoksikholevy acid can reduce ciprofloxacin absorption.
with nitrendipiny – ursodezoksikholevy acid reduces values of the maximum concentration in blood plasma (Cmax) and values of the area under curve (AUC) of the calcic antagonist of a nitrendipin. Proceeding from it and also from the message about interaction with substance dapsone (reduction of therapeutic effect) and from the researches in vitro, it is possible to assume that drug induces activity of enzyme of P450 3A4 cytochrome which is taking part in metabolism of medicines. Therefore, in case of simultaneous use of drugs which are metabolized with participation of this enzyme it is necessary to be careful and consider that dose adjustment can be necessary.
with oral hypoglycemic drugs – strengthening of their action.
with hypolipidemic drugs (Clofibratum, bezafibrat, probutsol), estrogen, hormonal contraceptives – weakening of effect of ursodeoksikholiyevy acid owing to increase in level of cholesterol in bile and, thus, decrease in efficiency of Dezursolen at dissolution of gallstones.
Dezursolen should be accepted under observation of the doctor. For the first 3 months of treatment every 4 week it is necessary to control functional parameters of a liver and to determine activity of aspartate aminotransferase (nuclear heating plant), alaninaminotranspherase (ALT) and gamma glutamiltransferazy (GGT), bilirubin and alkaline phosphatase, further such tests are recommended to be carried out every 3 month.
For assessment of therapeutic effect and early detection of calcification of gallstones it is necessary to check a condition of a gall bladder in a standing position and lying on spin by means of ultrasonography or to the cholecystography there are each 6-10 months.
With signs of calcification of gallstones the treatment should be stopped. It is not necessary to appoint drug at impossibility of carrying out a holetsistogramma, disorder of activity of a gall bladder or frequent biliary gripes.
At use in a late stage of primary biliary cirrhosis cirrhosis decompensation cases which partially regressed after drug withdrawal were very seldom observed.
In case of development of diarrhea it is necessary to lower a drug dose, and in case of persistent diarrhea the treatment should be stopped.
Pregnancy and the period of a lactation
of Sufficient data on use of ursodezoksikholevy acid during pregnancy, especially in the first trimester, it is not received.
Prior to drug treatment it is necessary to exclude pregnancy.
To women of childbearing age, during treatment it is recommended to apply non-hormonal contraceptives or oral hormonal contraceptives with the low content of estrogen.
It is unknown whether ursodezoksikholevy acid gets to breast milk. Therefore, Dezursolen it is not necessary to apply during feeding by a breast. If treatment by ursodezoksikholevy acid is necessary, feeding by a breast has to be stopped.
Features of influence on ability to run the vehicle or potentially dangerous mechanisms
Drug does not influence speed of response at control of motor transport or work with other mechanisms.
Symptoms: in case of overdose of drug the development of diarrhea is possible. In general, development of other symptoms of overdose is improbable since at increase in the accepted dose the absorption of ursodezoksikholevy acid decreases and increases its removal with excrements.
Treatment: at overdose performing specific therapy is not required, consequences of diarrhea it is necessary to treat symptomatic by means of rehydration, substitution of electrolytes and intake of Colestyraminum.
The form of release and packing
On 5 capsules place in blister strip packagings from a film of polyvinylchloride and aluminum foil.
On 4 planimetric packs together with the instruction for medical use in the state and Russian languages place in a cardboard pack.
To Store storage conditions at a temperature not higher than 25 wasps.
To store out of children’s reach!
A period of storage
not to use drug after the expiration date specified on packing.
To Develop prescription status According to the prescription