Ekskhol

General characteristics. Structure:

Active agent ursodezoksikholevy acid of 250 mg; excipients: silicon dioxide colloid (A-200 or A-300 aerosil), hydrophosphate calcium dihydrate, magnesium stearate, povidone (пласдон K-90 or коллидон 90 F), lactoses monohydrate (sugar milk);
structure of a gelatinous solid capsule: the case - titanium dioxide, gelatin; a lid - titanium dioxide, gelatin, indigo carmine.

Description:

capsules of 250 mg No. 10, 50 and 100 of white color with a lid of blue color. Contents of capsules - mix of granules and powder from white till almost white color.

Pharmacological properties:

Hepatoprotective means, has cholagogue effect. Reduces synthesis of cholesterol in a liver, its absorption in intestines and concentration in bile, increases solubility of cholesterol in bile-excreting system, stimulates education and biliation. Reduces a bile litogennost, increases in it the content of bile acids; causes strengthening of gastric and pancreatic secretion, increases activity of a lipase, has hypoglycemic effect. Causes partial or full dissolution of cholesteric stones at enteral use, reduces a bile saturation cholesterol that promotes mobilization of cholesterol from gallstones. Has immunomodulatory effect, influences immunological reactions in a liver: reduces an expression of some antigens on a membrane of hepatocytes, influences quantity of T lymphocytes, formation of Interlaken-2, reduces quantity of eosinophils.

Pharmacokinetics. Absorption from a small bowel - high (about 90%). Gets through a placental barrier. The maximum concentration (Cmax) at intake of 50 mg in 30, 60, 90 min. - 3.8, 5.5, 3.7 mmol/l respectively. Time of achievement of the maximum concentration (TCmax) - 1-3 h. Communication with proteins of plasma - high.
It is metabolized in a liver (clearance at "primary passing" through a liver) in taurinovy and glycine conjugates. The formed conjugates cosecrete in bile. It is brought to 50-70% through intestines. The insignificant amount of not soaked up ursodezoksikholevy acid comes to a large intestine where is exposed to splitting by bacteria (7 dehydroxylation); the formed lithocholic acid partially is soaked up from a large intestine, but sulphated in a liver and quickly removed in the form of a sulfolitokholilglitsinovy or sulfolitokholiltaurinovy conjugate.

Indications to use:

Primary biliary cirrhosis in the absence of decompensation signs (symptomatic therapy), dissolution of small and average cholesteric stones at the functioning gall bladder, a biliary reflux - gastritis.

Route of administration and doses:

Inside.

For dissolution of cholesteric gallstones an average daily dose - 10 mg/kg. A course of treatment - 6-12 months. For prevention of repeated formation of stones administration of drug within several more months after dissolution of stones is recommended.
At biliary a reflux gastritis the dose makes 250 mg once a day. A course of treatment - from 10 - 14 days to 6 months, if necessary - up to 2 years.
Symptomatic therapy of primary biliary cirrhosis: a daily dose - 10-15 mg/kg. Capsules accept in the evening, without chewing, washing down with a small amount of water. Less than 34 kg are recommended to patients with body weight administration of drug in the form of suspension.

Features of use:

It is necessary for successful dissolution that stones were purely cholesteric, no more than 15-20 mm in size, the gall bladder is filled with stones no more than on a half and biliary tract completely kept the function.
At appointment for the purpose of dissolution of gallstones control of activity of "hepatic" transaminases and the alkaline phosphatase (AP), gamma glutaminetransferase (GGT), concentration of bilirubin is necessary. The cholecystography it is necessary to spend each 4 weeks to the first 3 months of treatment, further - each 3 months. Control of efficiency of treatment to spend each 6 months during ultrasonography within the first year of therapy.
At preservation of the raised indicators drug should be cancelled. After full dissolution of concrements it is recommended to continue use within at least 3 months to promote dissolution of the remains of concrements which sizes are too small for their detection. If within 6-12 months after the beginning of therapy of partial dissolution of concrements did not occur, it is improbable that treatment will be effective.
Detection during treatment of not visualized gall bladder is the certificate that full dissolution of concrements did not happen, and treatment should be stopped.

Side effects:

Dorsodynia, diarrhea (can be dozozavisimy), abdominal pain, it is rare - calcination of gallstones, increase in activity of "hepatic" transaminases, an alopecia, locks, dizziness, nausea, an exacerbation of earlier being available psoriasis, vomiting, allergic reactions.

Interaction with other medicines:

The antacids containing Al3 + and ion-exchange resins (Colestyraminum), reduce absorption.
Hypolipidemic medicines (especially Clofibratum), are oestrogenic, Neomycinum or progestins increase bile saturation by cholesterol and can reduce ability to dissolve cholesteric bilious concrements.

Contraindications:

Hypersensitivity, rentgenpolozhitelny (with the high content of Sa2+) gallstones, a nonfunctioning gall bladder, желче - gastrointestinal fistula, chronic hepatitis, inflammatory diseases of a small and large intestine, acute cholecystitis, an acute cholangitis, cirrhosis in a decompensation stage, a liver and/or renal failure, pancreatitis, obturation of biliary tract, acute infectious diseases of a gall bladder and bilious channels, an empyema of a gall bladder, pregnancy, the lactation period, children's age.

Overdose:

Cases of overdose are not revealed. In case of overdose carry out a symptomatic treatment.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Capsules on 250 mg.
On 10 or 15 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 1, 3, 5, 10 blister strip packagings on 10 capsules or on 2, 4, 6 blister strip packagings on 15 capsules with the application instruction in a pack from a cardboard.