Ursotsid 30s 250 mg capsule

The instruction for medical use
of medicine

the Trade name
of Ursotsid®

the International unlicensed
name Ursodezoksikholevaya acid

the Dosage form
of the Capsule of 250 mg

Structure
One capsule contains
active agent - ursodezoksikholevy acid of 250 mg,
excipients – starch prezhelatinizirovanny, cellulose microcrystalline PH 101, silicon dioxide colloidal (Aerosil 200), magnesium stearate,
structure of a cover of the capsule:
capsule body: gelatin, caramel (E150),
capsule lid: ferrous oxide red (E172), titan dioxide (E 171), gelatin.

The description
Solid gelatin capsules with the transparent light brown body and an opaque lid of red-brown color. Capsule contents – white powder.

Pharmacotherapeutic group
Drugs for treatment of diseases of a liver and biliary tract. Drugs for treatment of a disease of a gall bladder. Drugs of bile acids. Ursodezoksikholevy acid.
The ATX A05AA02 code
the Pharmacological

Pharmacokinetics Later properties of oral administration ursodezoksikholevy acid is absorbed in digestive tract due to passive diffusion (about 90%) in a small intestine, and in an ileal gut at the expense of active transport. Ursodezoksikholevy acid is metabolized mainly in a liver in taurinovy and glycine conjugates and removed in the conjugated form with bile by enterogepatichesky recirculation (50 - 70%) and partially – with excrements.
A pharmacodynamics
of Ursodezoksikholevaya acid is a bile acid which is physiologically produced in intestines of the person from cholic or chenodesoxycholic acids. Ursodezoksikholevy acid reduces cholesterol content in bile due to suppression of its synthesis and secretion by a liver and also inhibits intestinal absorption of cholesterol.
As hepatoprotective means renders also bile-expelling, cholelitholytic, hypolipidemic action.
The therapeutic effectiveness of drug is caused by its ability to normalize holepoetichesky function, to reduce a bile litogennost, to prevent formation of bilious concrements and to promote dissolution of already available cholesteric gallstones.
Ursodezoksikholevy acid eliminates the dispeptic symptoms accompanying gepatobiliarny pathologies and is applied in cholestatic diseases of a liver.

Indications
- for dissolution of X-ray negative gallstones at the functioning gall bladder
- primary biliary cirrhosis, in the absence of signs of a decompensation
- a biliary reflux gastritis

the Route of administration and doses
УРСОЦИД® is accepted inside, washing down with a small amount of water.
Dissolution of gallstones
of the Capsule is accepted before going to bed once in a daily dose from 8 mg/kg to 12 mg/kg of body weight.
The daily dose 10mg/kg body weights corresponds:
To 2 Ursotsida capsules at patients with body weight to 60 kg
to 3 Ursotsida capsules at patients with body weight to 80 kg
to 4 Ursotsida capsules at patients with body weight to 100 kg
to 5 Ursotsida capsules at patients with body weight
Duration of process of dissolution of gallstones at use of drug is over 100 kg from 6 months to 2 years. If in 6 months from the beginning of use the reduction of gallstones is not observed, then it is inexpedient to continue treatment. For prevention of repeated formation of stones the use of drug within 3-4 months after dissolution of stones is recommended.
A biliary reflux - gastritis
to Patients with biliary a reflux gastritis usually appoint drug in a dose of 250 mg of 1 times a day, it is desirable in the evening. Duration of a course of treatment is 10-14 days.
Primary biliary cirrhosis
the Daily dose depends on body weight and makes 14±2 mg/kg/days (from 3 to 7 capsules). For the first 3 months it is recommended to divide a daily dose into 2-3 receptions. At improvement of indicators of function of a liver the daily dose can be accepted once a day (evening).
The dosing mode











the Body weight (kg)

the Daily dose of mg/kg of body weight

Ursotsid of 250 mg of the capsule


the First 3 months

in a consequence evening (1 time a day)


morning

midday

evening




































47-62 16-16 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









110 14-16 2 2 3 7

At patients with primary biliary cirrhosis in rare instances clinical symptoms can worsen in an initiation of treatment, for example, the itching can amplify. In that case therapy has to be continued in a dose 1 capsule a day and increase gradually (weekly on 1 capsule) until again is not, reach the recommended dosing mode. Therapy can be carried out beyond all bounds long.
47 kg and to patients who cannot swallow the capsule ursodezoksikholevy acid in the form of suspension is recommended to children and adults with the body weight & lt.

Side effects
Seldom
- a dorsodynia
- nausea, vomiting, diarrhea, a constipation, pain in epigastric area, the right the hypochondrium, passing increase in activity of 'hepatic' transaminases
- an alopecia, exacerbation of earlier being available psoriasis
- allergic reactions (urticaria, a skin itching)
Is very rare
- calcination of gallstones
- at treatment of primary biliary cirrhosis can be observed a passing decompensation of cirrhosis which disappears after drug withdrawal

of the Contraindication
- hypersensitivity to drug components
- rentgenpolozhitelny gallstones with the high content of calcium
- a nonfunctioning gall bladder, disturbance of sokratitelny activity of a gall bladder
- a full obturation of biliary tract
- zhelche-gastro intestinal fistula
- inflammatory diseases of a small and large intestine
- an acute cholangitis, acute cholecystitis (including
acute infectious diseases of a gall bladder and bile ducts, an empyema of a gall bladder)
- frequent bilious gripes
-
- a heavy liver and/or renal failure
- acute and chronic pancreatitis in an aggravation stage
- children's age up to 12 years (for this dosage form)

Medicinal interactions
УРСОЦИД® it is not necessary to appoint cirrhosis in a decompensation stage along with holestiraminy, kolestipoly or the antiacid drugs containing hydroxide or aluminum oxide as these drugs in intestines connect ursodezoksikholevy acid and, thus, inhibit its absorption and reduce efficiency of therapy. If necessary these drugs need to be taken, at least, with a 2-hour interval to or after reception УРСОЦИД®.
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.
In some cases ursodezoksikholevy acid can reduce ciprofloxacin absorption.
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 and also reduces therapeutic effectiveness of dapsone. These data indicate possible induction by ursodezoksikholevy acid cytochrome of P450-dependent enzymes 3A though it was not confirmed in controlled clinical trials.
Estrogen and some hypolipidemic drugs, such as Clofibratum, can promote formation of bilious concrements and, thus, reduce efficiency of ursodezoksikholevy acid at dissolution of gallstones.

Special instructions
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), further such tests are recommended to be carried 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.
For assessment of therapeutic effect and early detection of possible calcination of concrements in 6 months after an initiation of treatment, depending on the size of stones, it is necessary to conduct a research of a general view of a gall bladder (oral cholecystography) and diagnostics of possible occlusion of bile ducts in a standing position and lying on spin (ultrasonic inspection). After full dissolution of stones it is recommended to continue use of drug within 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.
УРСОЦИД® it is not necessary to appoint at impossibility of receiving 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.
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.
Pregnancy and a lactation
of Sufficient data on use of ursodezoksikholevy acid during pregnancy, especially in the first trimester, it is not received. Researches on animals testify teratogenic action at an early stage of pregnancy. Урсоцид® it should not be used during pregnancy. Prior to drug treatment it is necessary to exclude pregnancy. Women of childbearing age can appoint drug only at the condition of application of reliable means of contraception – use of the non-hormonal or containing low doses estrogen of contraceptives is recommended. However, at dissolution of gallstones the patients should use effective non-hormonal methods of contraception as oral hormonal contraceptives can promote formation of concrements.
Data on discharge of ursodezoksikholevy acid breast milk are absent now. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.
The feature of influence on ability to run the vehicle or potentially dangerous mechanisms
does not influence.

Overdose
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 and substitution of electrolytes.

The form of release and packing
On 5, 15 or 10 capsules place in blister strip packaging from a white opaque film of PVH/PE/PVDH and printing aluminum foil.
On 2 (for 5 and 15 capsules) or on 5 or 10 (for 10 capsules) planimetric packings together with the instruction for medical use in the state and Russian languages place in a pack cardboard with the hologram of manufacturing firm.


To Store storage conditions at a temperature not over 25 of 0C, in the dry, protected from light place.
To store out of children's reach!


2 years
not to apply a period of storage after the expiration date specified on packing.

Prescription status
According to the prescription



Republic of Kazakhstan JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Producer
Almaty, Shevchenko St. 162 E.


The owner of the registration certificate
of JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika
the Republic of Kazakhstan
to Develop