Ursodeks 100s 250 mg capsule
- $94.60
The instruction for medical use
of URSODEKS® medicine
the Trade name
of Ursodeks®
the International unlicensed
name Ursodezoksikholevaya acid
the Dosage form
of the Capsule, 250 mg
Structure
One capsule contains
active agent - acid of ursodeoksikholevy (ursodezoksikholevy)
250 mg,
excipients: prezhelatinizirovanny starch, kopovidon, calcium stearate,
structure of a gelatin capsule: gelatin, methylparahydroxybenzoate, propilparagidroksibenzoat, titan dioxide (E 171).
Description
Solid gelatin capsules 0 of No. in size, white color. Contents of capsules – powder of white or almost white color.
Pharmacotherapeutic group
Drugs for treatment of diseases of a liver and biliary tract. Drugs of bile acids. Ursodezoksikholiyevy acid.
The ATX A05A A02 code
the Pharmacological
Pharmacokinetics of Ursodezoksikholevaya properties acid (UDHK) is soaked up in a jejunum due to passive diffusion (about 90%), and in an ileal gut - by means of active transport. The maximum concentration of UDHK in plasma is reached in 1-3 hours after intake. At systematic reception, ursodezoksikholevy acid becomes the main bile acid in serum, making about 48% of total amount of bile acids in blood. Linking with proteins of plasma - about 96-99%. The therapeutic effect depends generally on concentration of ursodezoksikholevy acid in bile, but not in blood serum. Concentration in bile depends on a dose: at increase in a daily dose the content of ursodezoksikholevy acid in bile respectively increases. The maximum concentration in bile is noted at a daily dose 10-15 mg/kg. UDHK gets through a placental barrier. Ursodezoksikholevy acid is metabolized in a liver in taurinovy and glycine conjugates. Elimination half-life 3.5 - 5.8 days. Very small quantity is removed with bile about 50-70% of a dose, - with urine.
The pharmacodynamics
of Ursodex - hepatoprotective means, renders bile-expelling, cholelitholytic, hypolipidemic, gipokholesterinemichesky and some immunomodulatory action.
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.
Indications
- for dissolution of the cholesteric X-ray-negative stones of a gall bladder which are not exceeding 15 mm in the diameter at the functioning gall bladder
- for treatment biliary a reflux gastritis
- for treatment of primary biliary cirrhosis in the absence of signs of a decompensation as a part of complex therapy
the Route of administration and doses
patients can use Drug inside with body weight more than 47 kg. For patients who have body weight less than 47 kg or who have difficulties when swallowing capsules it is possible to use drug in the form of suspension.
For dissolution of cholesteric gallstones
the Dose of drug is selected individually. Usually daily dose of drug makes 10 mg/kg of body weight. Capsules are recommended to be accepted once a day before going to bed, without chewing and washing down with a small amount of water.
Treatment duration for dissolution of the available concrements has to be from 6 to 12 months. Each 6 months it is necessary to control efficiency of therapy by means of ultrasonic or X-ray inspection. If after 6 months of treatment of reduction of the sizes of gallstones it is not observed, then further continuation of therapy is inexpedient. For prevention of a recurrence of cholelithiasis it is recommended to continue administration of drug for 3-4 months after dissolution of the available concrements.
For treatment biliary the reflux gastritis
is Appointed on 250 mg (1 capsule) 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 symptomatic treatment of primary biliary cirrhosis
the Daily dose of drug is selected the doctor individually and usually makes 10-15 mg/kg of body weight.
The body weight (kg)
the Daily dose
(body weight mg/kg)
of the Capsule
the first 3 months
further
put morning
evening
evening (1 time a day)
47-62 12-16 1 1 1 3 63-78 13-16 1 1 2 4 79-93 13-16 1 2 2
5 94-109 14-16 2 2 2 6
more than 110 2 2 3 7
for the first months of treatment is recommended to divide a daily dose into 2-3 receptions. After improvement of indicators of a liver it is possible to accept a daily dose of drug once, in the evening. Duration of therapy is from 6 months to several years.
At patients with primary biliary cirrhosis in an initiation of treatment the deterioration in clinical symptoms, for example, strengthening of an itching is possible. In this case therapy should be continued on 1 capsule a day, it is gradually possible to raise a dose (increasing a daily dose by 1 capsule every week) to achievement of the recommended dose.
Side effects
- a pastopodobny chair or diarrhea (at treatment of primary biliary cirrhosis)
- abdominal pain with localization in right hypochondrium
- calcination of gallstones (at therapy of the developed stages of primary biliary cirrhosis)
- a decompensation of primary biliary cirrhosis (with partial regression after the treatment termination)
- allergic reactions (urticaria)
of the Contraindication
- hypersensitivity to drug components
- acute inflammatory bowel diseases, a gall bladder and
biliary tract (acute cholecystitis, an acute cholangitis,
an empyema of a gall bladder, a cholelithiasis attack)
- full obstruction of biliary tract
- cirrhosis in a decompensation stage
- acute and chronic pancreatitis in an aggravation stage
- the calcinated gallstones (with the high content of calcium,
X-ray - positive)
- disturbance of sokratitelny function of a gall bladder
- the profound renal failures, a liver, a pancreas
- bilious and gastrointestinal fistula
- frequent episodes of hepatic gripes
Medicinal interactions
of Ursodezoksikholevaya acid should not be applied along with the following medicines:
The antiacid drugs containing aluminum (holestiramin, holestipol)
These drugs reduce binding of ursodezoksikholevy acid in a small intestine, inhibiting its absorption therefore it is not necessary to apply these medicines at the same time. If use of the drugs containing one of these substances is necessary, then they should be applied, at least, in 2 hours prior to or after reception of the Ursodeksa capsules,
Cyclosporines
Cyclosporine increases absorption of ursodezoksikholevy acid in a small intestine therefore it is necessary to control periodically cyclosporine level in blood and in case of need – to adjust its doses),
Ciprofloxacin
In some cases ursodezoksikholevy acid can reduce ciprofloxacin absorption,
Oral hypoglycemic drugs
of Ursodezoksikholevaya acid can strengthen their actions,
Hypolipidemic drugs (Clofibratum, bezafibrat, probutsol), estrogen
These drugs can reduce effect of ursodezoksikholiyevy acid, owing to increase in level of cholesterol in bile.
Ursodezoksikholevy acid reduces the maximum concentration (Cmax) in blood plasma and the area under curve (AUC) for the calcic antagonist of a nitrendipin. Proceeding from it and also from the only 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 need of dose adjustment.
The special
instructions Drug to apply only 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 define activity of aspartate aminotransferase (nuclear heating plant), alaninaminotranspherases (ALT) and gamma glutamiltransferazy (GGT), further such tests it is recommended to carry out every 3 month. Such monitoring allows to establish the patients with primary biliary cirrhosis responding to performing therapy and also to carry out early identification of possible deterioration in hepatic function, especially patients with primary biliary cirrhosis in an advanced stage have diseases.
Урсодекс® it is not necessary to appoint at impossibility of carrying out a holetsistogramma of a gall bladder, in the presence of the calcinated concrements, in disorders of motor activity of a gall bladder or frequent biliary gripes.
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.
At use of ursodezoksikholevy acid for treatment of primary biliary cirrhosis in an advanced stage of a disease cirrhosis decompensation cases which partially regressed after drug withdrawal very seldom were 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.
Children
Are not present basic age restrictions for drug use to children, but capsules should not be used to children with body weight less than 47 kg. If the child experiences difficulties with swallowing and/or its body weight less than 47 kg it is recommended to use drug in the form of suspension.
Pregnancy and the period of a lactation
of Sufficient data on safety of use of ursodezoksikholevy acid, in particular in Ι a pregnancy trimester, no. Drug should not be used during pregnancy.
Before an initiation of treatment to exclude pregnancy. To women of reproductive age to appoint drug only on condition of reliable contraception.
Due to the lack of reliable data about ability of ursodezoksikholevy acid to get into breast milk, drug should not be used during feeding by a breast. In need of drug use the feeding by a breast should be stopped.
To women of childbearing age, during treatment of Ursodeksom® it is recommended to apply non-hormonal contraceptives or oral hormonal contraceptives with the low content of estrogen.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
the Overdose
At overdose does not influence there can be diarrhea. Other symptoms of overdose are improbable as absorption of ursodezoksikholevy acid decreases at increase in its dose, and according to its bigger quantity is excreted with excrements.
Treatment: reduction of a dose of drug, and in case of constant diarrhea – drug withdrawal, the symptomatic therapy directed to recovery of balance of liquid and electrolytes.
A form of release and packing
On 10 capsules in blister strip packaging from a film of polyvinylchloride and aluminum foil.
On 1, 5 or 10 blister strip packagings together with the approved instruction for medical use in the state and Russian languages place in a pack from cardboard.
Packs place in boxes of cardboard for a retail container or corrugated fibreboard.
The text from the approved instruction for medical use in the state and Russian languages is allowed to apply on a pack.
To Store storage conditions in dry, protected from light, the place, at a temperature not above 30 °C.
To store out of children's reach!
3 years
not to use a period of storage after an expiration date.
Prescription status
According to the prescription
JSC Khimfarm Producer, the Republic of Kazakhstan
the Owner of the registration certificate
of JSC Khimfarm, the Republic of Kazakhstan
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods) of JSC Khimfarm, Shymkent, Republic of Kazakhstan, 160019 Rashidov St., 81 Phone number 7252 (561342) Fax number 7252 (561342)
to Develop the E-mail address of infomed@santo.kz
of URSODEKS® medicine
the Trade name
of Ursodeks®
the International unlicensed
name Ursodezoksikholevaya acid
the Dosage form
of the Capsule, 250 mg
Structure
One capsule contains
active agent - acid of ursodeoksikholevy (ursodezoksikholevy)
250 mg,
excipients: prezhelatinizirovanny starch, kopovidon, calcium stearate,
structure of a gelatin capsule: gelatin, methylparahydroxybenzoate, propilparagidroksibenzoat, titan dioxide (E 171).
Description
Solid gelatin capsules 0 of No. in size, white color. Contents of capsules – powder of white or almost white color.
Pharmacotherapeutic group
Drugs for treatment of diseases of a liver and biliary tract. Drugs of bile acids. Ursodezoksikholiyevy acid.
The ATX A05A A02 code
the Pharmacological
Pharmacokinetics of Ursodezoksikholevaya properties acid (UDHK) is soaked up in a jejunum due to passive diffusion (about 90%), and in an ileal gut - by means of active transport. The maximum concentration of UDHK in plasma is reached in 1-3 hours after intake. At systematic reception, ursodezoksikholevy acid becomes the main bile acid in serum, making about 48% of total amount of bile acids in blood. Linking with proteins of plasma - about 96-99%. The therapeutic effect depends generally on concentration of ursodezoksikholevy acid in bile, but not in blood serum. Concentration in bile depends on a dose: at increase in a daily dose the content of ursodezoksikholevy acid in bile respectively increases. The maximum concentration in bile is noted at a daily dose 10-15 mg/kg. UDHK gets through a placental barrier. Ursodezoksikholevy acid is metabolized in a liver in taurinovy and glycine conjugates. Elimination half-life 3.5 - 5.8 days. Very small quantity is removed with bile about 50-70% of a dose, - with urine.
The pharmacodynamics
of Ursodex - hepatoprotective means, renders bile-expelling, cholelitholytic, hypolipidemic, gipokholesterinemichesky and some immunomodulatory action.
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.
Indications
- for dissolution of the cholesteric X-ray-negative stones of a gall bladder which are not exceeding 15 mm in the diameter at the functioning gall bladder
- for treatment biliary a reflux gastritis
- for treatment of primary biliary cirrhosis in the absence of signs of a decompensation as a part of complex therapy
the Route of administration and doses
patients can use Drug inside with body weight more than 47 kg. For patients who have body weight less than 47 kg or who have difficulties when swallowing capsules it is possible to use drug in the form of suspension.
For dissolution of cholesteric gallstones
the Dose of drug is selected individually. Usually daily dose of drug makes 10 mg/kg of body weight. Capsules are recommended to be accepted once a day before going to bed, without chewing and washing down with a small amount of water.
Treatment duration for dissolution of the available concrements has to be from 6 to 12 months. Each 6 months it is necessary to control efficiency of therapy by means of ultrasonic or X-ray inspection. If after 6 months of treatment of reduction of the sizes of gallstones it is not observed, then further continuation of therapy is inexpedient. For prevention of a recurrence of cholelithiasis it is recommended to continue administration of drug for 3-4 months after dissolution of the available concrements.
For treatment biliary the reflux gastritis
is Appointed on 250 mg (1 capsule) 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 symptomatic treatment of primary biliary cirrhosis
the Daily dose of drug is selected the doctor individually and usually makes 10-15 mg/kg of body weight.
The body weight (kg)
the Daily dose
(body weight mg/kg)
of the Capsule
the first 3 months
further
put morning
evening
evening (1 time a day)
47-62 12-16 1 1 1 3 63-78 13-16 1 1 2 4 79-93 13-16 1 2 2
5 94-109 14-16 2 2 2 6
more than 110 2 2 3 7
for the first months of treatment is recommended to divide a daily dose into 2-3 receptions. After improvement of indicators of a liver it is possible to accept a daily dose of drug once, in the evening. Duration of therapy is from 6 months to several years.
At patients with primary biliary cirrhosis in an initiation of treatment the deterioration in clinical symptoms, for example, strengthening of an itching is possible. In this case therapy should be continued on 1 capsule a day, it is gradually possible to raise a dose (increasing a daily dose by 1 capsule every week) to achievement of the recommended dose.
Side effects
- a pastopodobny chair or diarrhea (at treatment of primary biliary cirrhosis)
- abdominal pain with localization in right hypochondrium
- calcination of gallstones (at therapy of the developed stages of primary biliary cirrhosis)
- a decompensation of primary biliary cirrhosis (with partial regression after the treatment termination)
- allergic reactions (urticaria)
of the Contraindication
- hypersensitivity to drug components
- acute inflammatory bowel diseases, a gall bladder and
biliary tract (acute cholecystitis, an acute cholangitis,
an empyema of a gall bladder, a cholelithiasis attack)
- full obstruction of biliary tract
- cirrhosis in a decompensation stage
- acute and chronic pancreatitis in an aggravation stage
- the calcinated gallstones (with the high content of calcium,
X-ray - positive)
- disturbance of sokratitelny function of a gall bladder
- the profound renal failures, a liver, a pancreas
- bilious and gastrointestinal fistula
- frequent episodes of hepatic gripes
Medicinal interactions
of Ursodezoksikholevaya acid should not be applied along with the following medicines:
The antiacid drugs containing aluminum (holestiramin, holestipol)
These drugs reduce binding of ursodezoksikholevy acid in a small intestine, inhibiting its absorption therefore it is not necessary to apply these medicines at the same time. If use of the drugs containing one of these substances is necessary, then they should be applied, at least, in 2 hours prior to or after reception of the Ursodeksa capsules,
Cyclosporines
Cyclosporine increases absorption of ursodezoksikholevy acid in a small intestine therefore it is necessary to control periodically cyclosporine level in blood and in case of need – to adjust its doses),
Ciprofloxacin
In some cases ursodezoksikholevy acid can reduce ciprofloxacin absorption,
Oral hypoglycemic drugs
of Ursodezoksikholevaya acid can strengthen their actions,
Hypolipidemic drugs (Clofibratum, bezafibrat, probutsol), estrogen
These drugs can reduce effect of ursodezoksikholiyevy acid, owing to increase in level of cholesterol in bile.
Ursodezoksikholevy acid reduces the maximum concentration (Cmax) in blood plasma and the area under curve (AUC) for the calcic antagonist of a nitrendipin. Proceeding from it and also from the only 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 need of dose adjustment.
The special
instructions Drug to apply only 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 define activity of aspartate aminotransferase (nuclear heating plant), alaninaminotranspherases (ALT) and gamma glutamiltransferazy (GGT), further such tests it is recommended to carry out every 3 month. Such monitoring allows to establish the patients with primary biliary cirrhosis responding to performing therapy and also to carry out early identification of possible deterioration in hepatic function, especially patients with primary biliary cirrhosis in an advanced stage have diseases.
Урсодекс® it is not necessary to appoint at impossibility of carrying out a holetsistogramma of a gall bladder, in the presence of the calcinated concrements, in disorders of motor activity of a gall bladder or frequent biliary gripes.
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.
At use of ursodezoksikholevy acid for treatment of primary biliary cirrhosis in an advanced stage of a disease cirrhosis decompensation cases which partially regressed after drug withdrawal very seldom were 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.
Children
Are not present basic age restrictions for drug use to children, but capsules should not be used to children with body weight less than 47 kg. If the child experiences difficulties with swallowing and/or its body weight less than 47 kg it is recommended to use drug in the form of suspension.
Pregnancy and the period of a lactation
of Sufficient data on safety of use of ursodezoksikholevy acid, in particular in Ι a pregnancy trimester, no. Drug should not be used during pregnancy.
Before an initiation of treatment to exclude pregnancy. To women of reproductive age to appoint drug only on condition of reliable contraception.
Due to the lack of reliable data about ability of ursodezoksikholevy acid to get into breast milk, drug should not be used during feeding by a breast. In need of drug use the feeding by a breast should be stopped.
To women of childbearing age, during treatment of Ursodeksom® it is recommended to apply non-hormonal contraceptives or oral hormonal contraceptives with the low content of estrogen.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
the Overdose
At overdose does not influence there can be diarrhea. Other symptoms of overdose are improbable as absorption of ursodezoksikholevy acid decreases at increase in its dose, and according to its bigger quantity is excreted with excrements.
Treatment: reduction of a dose of drug, and in case of constant diarrhea – drug withdrawal, the symptomatic therapy directed to recovery of balance of liquid and electrolytes.
A form of release and packing
On 10 capsules in blister strip packaging from a film of polyvinylchloride and aluminum foil.
On 1, 5 or 10 blister strip packagings together with the approved instruction for medical use in the state and Russian languages place in a pack from cardboard.
Packs place in boxes of cardboard for a retail container or corrugated fibreboard.
The text from the approved instruction for medical use in the state and Russian languages is allowed to apply on a pack.
To Store storage conditions in dry, protected from light, the place, at a temperature not above 30 °C.
To store out of children's reach!
3 years
not to use a period of storage after an expiration date.
Prescription status
According to the prescription
JSC Khimfarm Producer, the Republic of Kazakhstan
the Owner of the registration certificate
of JSC Khimfarm, the Republic of Kazakhstan
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods) of JSC Khimfarm, Shymkent, Republic of Kazakhstan, 160019 Rashidov St., 81 Phone number 7252 (561342) Fax number 7252 (561342)
to Develop the E-mail address of infomed@santo.kz
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