Укрлив

General characteristics. Structure:

Active ingredient: ursodeoxycholic acid; 5 ml of suspension contain ursodeoksikholiyevy acid 250 mg.

Excipients: cellulose microcrystallic, benzoic acid (E 210),
xylitol, glycerin, saccharin of sodium, sodium chloride, citric acid, monohydrate; sodium citrate,
flavoring additive a lemon, the water purified.

Pharmacological properties:

Pharmacodynamics. A small amount of ursodeoksikholiyevy acid usually contains in human bile.
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 gallstones.
According to modern representations consider that ursodeoksikholiyevy acid at diseases of a liver and cholestatic diseases causes effect due 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 excreted with bile. The clearance of the first passing through a liver makes up to 60%.
Under the influence of colibacilli partial degradation to 7-ketolithocholic and lithocholic acids 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 with excrements.
Biological half-life of ursodeoksikholiyevy acid makes 3,5-5,8 days.

Indications to use:

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

Route of administration and doses:

At various indications recommend the following daily doses.

For dissolution of cholesteric gallstones
About 10 mg on 1 kg of body weight every day that corresponds:

Body weight                            Measured spoons *                      Equivalent, ml
From 5 to 7 kg                                 ¼                                               1,25
From 8 to 12 kg                               ½                                               2,50
From 13 to 18 kg                             ¾ (=¼ + ½)                              3,75
From 19 to 25 kg                                                                            1 5,00
From 26 to 35 kg                             1 ½                                            7,50
From 36 to 50 kg                                                                            2 10,00
From 51 to 65 kg                             2 ½                                           12,50
From 66 to 80 kg                                                                            3 15,00
From 81 to 100 kg                                                                          4 20,00
It is more than 100 kg                                                                          of 5 25,00

* 1 measured spoon (= 5 ml of suspension) contains 250 mg of ursodeoksikholiyevy acid.
For measurement of doses it is possible to use the plastic one-time syringe without needle.

Suspension should be accepted in the evening, before going to bed. It needs to be applied regularly.
Time necessary for dissolution of gallstones, usually makes from 6 to 24 months.
If reduction of the sizes of gallstones is not observed after 12 months, treatment should be stopped.
Success of treatment needs to be checked by means of ultrasonography or the cholecystography through everyone
6 months. It is necessary to conduct additional researches for identification of possible calcification of stones.
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 makes about 14 ± 2 mg of ursodeoksikholiyevy acid/kg of body weight.

In the first 3 months of treatment Ukrliv® suspension needs to be accepted during the day, having distributed a daily dose on
several receptions. At improvement of indicators of function of a liver the daily dose can be accepted once a day, in the evening.

 

* 1 measured spoon (= 5 ml of suspension) contains 250 mg of ursodeoksikholiyevy acid.

For measurement of doses it is possible to use the plastic one-time syringe without needle.

Suspension should be accepted regularly, according to the scheme of the dosage which is stated above. Use with
uspenziya of Ukrliv® at primary biliary cirrhosis can be continued without restrictions in time.

In some cases at patients with primary biliary cirrhosis in an initiation of treatment clinical can worsen
symptoms, for example, the itch can amplify. If it occurred, therapy should be continued using
lower daily dose of Ukrliv® suspension, and then gradually to increase it (once a week)
before achievement of the dosage specified in the scheme.

Features of use:

Ukrliv® suspension should be accepted under observation of the doctor.
Within the first three months of treatment it is necessary to check parameters of function of a liver (nuclear heating plant (SGOT), ALT (SGPT) and g-GT) every 4 week, and then - every 3 month.
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.
The benzoic acid which is contained in suspension can cause in sensitive patients hypersensitivity reaction in the form of irritation of skin, eyes and mucous membranes. Newborns have the increased risk of jaundice.

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 and 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 owes baht is 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.
The dosage should be carried out according to body weight.

Side effects:

Assessment of side reactions is based on such data on their frequency:

Very much to a chastye:ta which are observed more than at 1 patient from 10 which are treated Chastye:te which are observed more than at 1 patient from 100 which are treated Nechastye:te which are observed more than at 1 patient from 1000 which are treated Rare: those which are observed more than at 1 patient from 10 000 which are treated Very rare: those which are observed in 1 case from 10 000 patients who are treated, or not numerous, including separate cases Disturbances from digestive tract During clinical tests messages on a liquid chair or diarrhea were frequent during therapy by ursodeoksikholiyevy acid. Very seldom at treatment of primary biliary cirrhosis noted the expressed pain in the right upper part of an abdominal cavity. Disturbances from a liver and a gall bladder At treatment by ursodeoksikholiyevy acid calcification of gallstones very seldom can be observed. At therapy of the developed stages of primary bilious cirrhosis the decompensation seldom or never was observed hepatic cirrhosis which partially regressed after the treatment termination. Hypersensitivity reactions. Very seldom rashes (urticaria) can be observed.

Interaction with other medicines:

Ukrliv® suspension cannot be applied along with Colestyraminum, kolestipoly or antiacid drugs (the substances connecting gastric acid) containing aluminum hydroxide and (or) smectite (aluminum oxide) as these drugs connect ursodeoksikholiyevy acid in intestines and thus reduce its absorption and efficiency. 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 Ukrliv® suspension reception.
Drug can strengthen absorption of cyclosporine from intestines. Therefore, at the patients receiving cyclosporine, the doctor has to check concentration of cyclosporine in blood and correct a cyclosporine dose in case of need.
In some cases Ukrliv® suspension can reduce ciprofloxacin absorption.
Ursodeoksikholiyevy acid reduces the maximum concentration in plasma (Cmax) and the area under curve (AUC) of the calcic antagonist of a nitrendipin. Proceeding from it, and also from the uniform message on interaction with dapsone (reduction of therapeutic effect) and from the researches in vitro, it is possible to assume that ursodeoksikholiyevy acid induces activity of P450 3A4 cytochrome which metabolizes drug.
Therefore, at simultaneous use of the means which are metabolized with participation of this enzyme it is necessary to be careful as there can be a need for dose adjustment.

Contraindications:

- hypersensitivity to any substance which is a part of medicine;
- acute inflammation of a gall bladder or biliary tract;
- impassability of bilious channels (general bilious channel or channel of a bubble);
- dekompensirovanny cirrhosis.
It is impossible to appoint Ukrliv® suspension the patient with a gall bladder which is not visualized by radiological
by methods, with calcific stones, the broken contractility of a gall bladder or that who has frequent bilious gripes.

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 function of a liver. In case of diarrhea a dose it is necessary
to reduce and if diarrhea proceeds, it is necessary to stop drug use.
No specific counter-measures are required, 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 the place, unavailable to children. After the first opening of a bottle to store drug no more than 4 months.

Issue conditions:

According to the recipe

Packaging:

On 200 ml of suspension in bottles, each bottle in cardboard packaging together with a measured spoon.