Укрлив tablets

General characteristics. Structure:

Active ingredient: ursodexycholic acid; 1 tablet contains 250 mg of ursodeoksikholiyevy acid.

Excipients: cellulose microcrystallic, sodium krakhmalglikolit (type A),
K-30 povidone, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. A small amount of ursodeoksikholiyevy acid usually contains in bile of the person. After oral administration it reduces a bile saturation cholesterol, slowing down absorption of cholesterol in a small intestine and reducing secretion of cholesterol in bile. Obviously as a result of dispersion of cholesterol and formation of liquid crystals there is a partial dissolution of cholelithic cholesterol.
According to modern representations it is considered that ursodeoksikholiyevy acid at diseases of a liver and cholestatic diseases causes effect thanks to relative replacement lipophilic, similar to detergents of toxic bile acids on hydrophilic cytoprotective non-toxic ursodeoksikholiyevy acid, and also owing to improvement of secretory ability of hepatocytes and immunoregulatory processes.

Pharmacokinetics. At oral administration ursodeoksikholiyevy acid is quickly soaked up in a small bowel and an upper part of an ileal gut by passive transfer and in final department of an ileal gut by active transfer. Extent of absorption usually makes 60-80%. After absorption bile acid is exposed to almost full hepatic konjyugirovaniye with amino acids glycine and taurine then it is removed with bile. The clearance of primary passing through a liver makes about 60%.
Under the influence of colibacilli partial degradation to 7-ketolithocholic acid and a litokholevoykislota is carried out. Lithocholic acid is hepatotoxic and causes damage of a hepatic parenchyma in some animal species. At the person only an insignificant part which is sulphated in a liver is absorbed and thus it is detoxified before being removed with bile and finally - with excrements. Biological half-life of ursodeoksikholiyevy acid makes 3,5-5,8 days.

Indications to use:

•   For dissolution of rentgennegativny cholesteric gallstones no more than 15 mm in the diameter at patients with the functioning gall bladder, despite existence in it of a bilious stone (it).
•   For a symptomatic treatment of the primary biliary cirrhosis (PBC) under conditions of absence of dekompensirovanny cirrhosis.

Route of administration and doses:

There are no age restrictions of use of the tablets Ukrliv®. For patients with body weight less than 47 kg or which have difficulties when swallowing tablets are possible use of the drug Ukrliv® in other dosage form (suspension).
At various indications the following daily doses are recommended.
For dissolution of cholesteric gallstones
About 10 mg of ursodeoksikholiyevy acid on kilogram of body weight a day that is equivalent:
47 - 60 kg               2 tablets
61–80 kg               3 tablets
81–100 kg             4 tablets
It is more than 100 kg    of 5 tablets
It is necessary to take a pill 1 time a day, swallowing of whole and washing down with a small amount of liquid, in the evening before going to bed.
Tablets need to be applied regularly.
Time, necessary for dissolution of gallstones, usually makes 6-24 months. If reduction of the sizes of gallstones is not observed after 12 months of reception, it is not necessary to continue therapy.
It is necessary to check success of treatment each 6 months by means of ultrasonic or X-ray inspection. Additional researches it is necessary to check whether there was no calcification of stones to time. If it occurred, treatment should be stopped.

For a symptomatic treatment of the primary biliary cirrhosis (PBC)
The daily dose depends on body weight and varies from 3 to 7 tablets (14±2 mg of ursodeoksikholiyevy acid on kilogram of body weight).
In the first 3 months of treatment of the tablet Ukrliv® it is necessary to accept during the day, having distributed a daily dose on several receptions. At improvement of indicators of function of a liver it is possible to accept a daily dose 1 time a day, in the evening.

It is necessary to swallow of tablets without chewing, washing down with liquid. Drug needs to be used regularly.
Use of the tablets Ukrliv® at primary biliary cirrhosis is possible throughout the long period.
At patients with primary biliary cirrhosis in rare instances in an initiation of treatment clinical symptoms can worsen, for example, the itch can amplify. If it happened, therapy should be continued, accepting a half of the tablet Ukrliv® in days then gradually to raise a dose (increasing every week a daily dose by a half of the tablet Ukrliv® before achievement of the shown dosage mode).

Features of use:

The pill Укрлив® 250 of mg needs to be taken under observation of the doctor.
Within the first 3 months of therapy the doctor has to carry out monitoring of parameters of function of a liver of nuclear heating plant (SGOT), ALT (SGPT) and (-GT) each 4 weeks, further - each 3 months.
To estimate progress in treatment and to reveal beforehand any calcification of gallstones, depending on the size of a stone it is necessary to conduct a research of a habit view of a gall bladder (the oral cholecystography) and possible impassability in a standing position and lying on spin (ultrasonic control) in 6 - 10 months from an initiation of treatment.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
Influence on ability to drive the car and to use mechanisms was not observed.

Use during pregnancy or feeding by a breast.
Women of reproductive age can accept drug only on condition of use of reliable contraceptives. Before an initiation of treatment pregnancy has to be excluded. For safety treatment cannot be carried out during the first trimester of pregnancy, except for cases when, according to the doctor, the advantage exceeds risk.   
There are no clinical data on safe use of ursodeoksikholiyevy acid to the women nursing. Therefore patients of this group are not recommended to use drug.

Children.
There are no basic age restrictions for drug Ukrliv® use to children, but tablets do not appoint to children with body weight less than 47 kg. If the child weighs less than 47 kg and/or if the child experiences difficulties with swallowing, it is recommended to apply Ukrliv® in the form of suspension.

Side effects:

Assessment of side reactions is based on the following data on their frequency:

Very frequent: Bol than at 1 of 10 patients receiving treatment	Frequent: Bol than at 1 of 100 patients receiving treatment
Infrequent: Bol than at 1 of 1000 patients receiving treatment	Rare: Bol than at 1 of 10000 patients receiving treatment
Very rare: at 1 of 10000 patients receiving treatment or is more rare, including separate cases

Disturbances from digestive tract
During clinical trials messages on a liquid chair or diarrhea throughout treatment by ursodeoksikholiyevy acid were frequent.
Very seldom at treatment of primary bilious cirrhosis there was severe abdominal pain to localization in right hypochondrium.
Disturbances from a liver and a gall bladder
Seldom or never at treatment calcification of gallstones can be observed by ursodeoksikholiyevy acid.
Throughout therapy of the developed stages of primary biliary cirrhosis the cirrhosis decompensation which partially regressed after the treatment termination seldom or never is observed.
Hypersensitivity reactions
Very seldom rashes (urticaria) can be observed.

Interaction with other medicines:

Such drugs as холестирамин, and some antacids containing aluminum hydroxide and (or) smectite (aluminum oxide), contact in vitro bile acid and can suppress absorption of ursodeoksikholiyevy acid. If use of the drugs containing one of these substances nevertheless is necessary, it is necessary to accept them a minimum in 2 hours prior to or after reception of the tablets Ukrliv®.
At some patients accepting ursodeoksikholiyevy acid and cyclosporine at the same time increase in level of cyclosporine in blood serum is possible.
It is recommended not to appoint at the same time the drugs increasing removal of cholesterol in bile such as the oestrogenic hormones, oral contraceptives and some drugs reducing cholesterol level in blood, such as Clofibratum.
In some cases the tablets Ukrliv® can reduce ciprofloxacin absorption.
Ursodeoksikholiyevy acid reduces the maximum concentration (Cmax) in a blood plasma and the area under curve (AUC) for the calcic antagonist of a nitrendipin. Proceeding from it, and also from the message on one case of interaction with dapsone (reduction of therapeutic effect) and the researches in vitro, it is possible to draw a conclusion that ursodeoksikholiyevy acid induces enzyme of P450 3A cytochrome which metabolizes medicines. Thus, in cases of combined use of the medicines which are metabolized with participation of this enzyme it is necessary to be especially careful and to mean that in case of need it is necessary to adjust a dose.

Contraindications:

•   Hypersensitivity to any substance which is a part of medicine.
•   Acute inflammation of a gall bladder or bilious channels.
•   Blockage of a bilious channel (blockage of the general bilious channel or channel of a bubble).
•   The tablet Ukrliv® is not appointed the patient with the gall bladder which is not visualized by radiological methods with calcific stones, the broken contractility of a gall bladder or it which have frequent bilious gripes.
•   Cirrhosis in a decompensation stage.

Overdose:

It is improbable that the overdose can result in serious side effects. There can be diarrhea therefore it is recommended to carry out monitoring of indicators of functions of a liver. In case of diarrhea the dose needs to be reduced and if diarrhea proceeds, it is necessary to stop drug Ukrliv® use.
No specific counter-measures are necessary, effects of diarrhea it is necessary to treat symptomatic with preservation of balance of liquid and electrolytes.
Ion-exchange resin can be useful to binding of bile acid in intestines.

Storage conditions:

To store at a temperature not above 25 °C in dry, protected from light and the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 3 or 10 blisters in cardboard packaging.