Ursofalk

General characteristics. Structure:

Capsules - 1 капс.

Active agent: ursodezoksikholevy acid - 250 mg.

Excipients: starch corn — 73 mg; silicon dioxide colloid — 5 mg; magnesium stearate — 2 mg; sodium lauryl sulfate — 0,2 mg; titanium dioxide — 1,94 mg; gelatin — 80,51 mg; the water purified — 14,55 mg.

Suspension for intake - 5 ml.

Active agent: ursodezoksikholevy acid - 250 mg.

Excipients: the benzoic acid — 7,5 mg; the water purified — 2875,5 mg; ксилитол — 1600 mg; глицерол — 500 mg; MKTs — 100 mg; propylene glycol — 50 mg; sodium citrate — 25 mg; sodium cyclomate — 25 mg; anhydrous citric acid — 12,5 mg; sodium chloride — 3 mg; fragrance lemon (Givaudan PHL-134488) — 1,5 mg.

Tablets - 1 table.

Active agent: ursodezoksikholevy acid - 250 mg.

Excipients: cellulose microcrystallic, K 25 povidone, кросповидон type A, talc, magnesium stearate, silicon dioxide colloid anhydrous, polysorbate 80, gipromeloz, macrogoal 6000.

Pharmacological properties:

Pharmacological action. 

Gepatoprotektivny, cholelitholytic and antilitogenny, cholagogue, immunomodulatory, antifibrotichesky, gipokholesterinemichesky, antineoplastic (onkoprofilaktichesky), prebiotichesky. 

Has direct cytoprotective effect on membranes of hepatocytes and holangiotsit (membrane stabilizing action). Under the influence of drug in a bullet of bile acids the content of hydrophobic (potentially toxic) acids decreases. Due to reduction of absorption of cholesterol in intestines and other biochemical effects has gipokholesterinemichesky effect. Suppresses the death of cells (apoptosis) caused by toxic bile acids (anti-apoptotic action). Slows down growth of tumor cells (antineoplastic action concerning a cholangiocarcinoma, a dysplasia and a colon cancer), including way a ligand - independent activation of glucocorticosteroid receptors and suppression of an expression with - a Myc-protein.

Pharmacokinetics. 

It is absorbed in a jejunum due to passive diffusion, in an ileal gut – at the expense of active transport. At intake in a single dose (500 mg) concentration in blood serum in 30, 60 and 90 min. makes 3,8, 5,5 and 3,7 µmol/l respectively. At systematic reception ursodeoksikholevy acid (UDHK) becomes the main bile acid of blood serum (48% of the general contents of bile acids). Joins in system of gastrointestinal circulation. The therapeutic effectiveness of drug depends on concentration of UDHK in bile. Against the background of therapy there is a dozozavisimy increase in a share of UDHK in a bullet of bile acids up to 50–75% (at daily doses of 10-20 mg/kg of body weight). Passes through a placental barrier. 

Pharmacodynamics. 

Having high polar properties, UDHK forms the non-toxic mixed micelles with non-polar (toxic) bile acids that reduces ability of a 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 unreceptive to action of cytotoxic micelles. Stimulates various proteins of holeretichesky transport by activation of intracellular alarm molecules. Reduces a bile saturation cholesterol due to oppression of its absorption in intestines, suppression of synthesis in a liver and decreases in secretion in bile; increases solubility of cholesterol in bile, forming with it liquid crystals; reduces a litogenny index of bile. Dissolution of cholesteric gallstones and the prevention of formation of new concrements is result. Immunomodulatory action is caused by oppression of an expression of HLA antigens on membranes of hepatocytes and holangiotsit, normalization of a natural killerny lymphocyte activity, etc. Authentically progressing of fibrosis at patients with primary biliary cirrhosis, a mucoviscidosis and alcoholic steatogepatit detains, reduces risk of development of a varicosity of a gullet. 

Indications to use:

- dissolution of cholesteric gallstones in a gall bladder;

- biliary reflux gastritis;

- primary biliary cirrhosis in the absence of signs of a decompensation (symptomatic treatment);

- chronic hepatitises of various genesis;

- primary sclerosing cholangitis, cystous fibrosis (mucoviscidosis);

- not alcoholic steatogepatit;

- alcoholic liver disease;

- dyskinesia of biliary tract.

Route of administration and doses:

Inside. To children and adults with body weight Ursofalk in the form of suspension is recommended to apply less than 34 kg.

Dissolution of cholesteric gallstones. The recommended dose makes 10 mg/kg/days that corresponds:

Body weight, kg	Number of capsules, piece.
to 60	2
61–80	3
81–100	4
Over 100	5

at reception of suspension for intake

Body weight, kg	Number of measured spoons	Corresponding quantity, ml
5–7	1/4	1,25
8–12	1/2	2,5
13–18	3/4 (= 1/4 + 1/2)	3,75
19–25	1	5,0
26–35	1,5	7,5
36–50	2	10,0
51–65	2,5	12,5
66–80	3	15,0
81–100	4	20,0
Over 100	5	25,0

Drug needs to be accepted daily in the evening, before going to bed (the capsule is not chewed), washing down with a small amount of liquid.

Treatment duration — 6–12 months. For prevention of a repeated cholelithiasis administration of drug within several months after dissolution of stones is recommended.

Treatment biliary reflux gastritis.

1 капс. (1 measured glass) daily in the evening, before going to bed (the capsule is not chewed), washing down Ursofalk with a small amount of water.

Course of treatment — from 10–14 days to 6 months, if necessary — up to 2 years.

Symptomatic treatment of primary biliary cirrhosis. The daily dose depends on body weight and makes from 3 to 7 капс. or 2–7 measured glasses (approximately from 14±2 mg/kg of ursodezoksikholevy acid).

In the first 3 months of treatment drug use Ursofalk (capsules, 250 mg) should be divided into several receptions during the day. After improvement of hepatic indicators it is possible to accept a daily dose of drug 1 time in the evening.

The following mode of use is recommended:

Capsules on 250 mg.

Body weight, kg	Daily dose (capsules, piece)	In the morning	In the afternoon	In the evening
47–62	3	1	1	1
63–78	4	1	1	2
79–93	5	1	2	2
94–109	6	2	2	2
Over 110	7	2	2	3

at reception of suspension for intake

Body weight, kg	Daily dose		In the morning, measured spoons	In the afternoon, measured spoons	In the evening, measured spoons
	number of measured spoons	corresponding quantity, ml
5–7	1/4	1,25	-	-	1/4
8–12	1/2	2,5	-	1/4	1/4
13–18	3/4	3,75	1/4	1/4	1/4
19–25	1	5,0	1/2	-	1/2
26–35	1,5	7,5	1/2	1/2	1/2
36–50	2	10,0	1	-	1
51–65	3	15,0	1	1	1
66–80	4	20,0	1	1	2
81–100	5	25,0	1	2	2
Over 100 kg	6	30,0	2	2	2

Capsules should be accepted regularly, without chewing, washing down with a small amount of liquid.

Ursofalk's use for treatment of primary biliary cirrhosis can be continued during unlimited time.

At patients with primary biliary cirrhosis in rare instances clinical symptoms can worsen in an initiation of treatment, for example the itch can become frequent. In this case treatment should be continued, accepting on 1 капс. daily, further it is necessary to raise a dosage gradually (increasing a daily dose weekly on 1 капс.) until again the recommended dosing mode is not reached.

Symptomatic treatment of chronic hepatitises of various genesis. A daily dose — 10–15 mg/kg in 2–3 receptions. Treatment duration — 6–12 months and more.

Primary sclerosing cholangitis. A daily dose — 12–15 mg/kg; if necessary the dose can be increased to 20–30 mg/kg in 2–3 receptions. Duration of therapy makes from 6 months to several years.

Kistochny fibrosis (mucoviscidosis). Daily dose of 12-15 mg/kg; if necessary the dose can be increased to 20–30 mg/kg in 2–3 receptions. Duration of therapy makes from 6 months to several years.

Not alcoholic steatogepatit. An average daily dose — 10–15 mg/kg in 2–3 receptions. Duration of therapy makes of 6–12 months and more.

Alcoholic liver disease. An average daily dose — 10–15 mg/kg in 2–3 receptions. Duration of therapy makes 6–12 months and more.

Dyskinesia of biliary tract. An average daily dose of 10 mg/kg in 2 receptions during of 2 weeks up to 2 months. If necessary the course of treatment is recommended to be repeated.

Features of use:

Administration of drug Ursofalk has to be carried out under observation of the doctor.

Within the first 3 months of treatment it is necessary to control functional trials of a liver (level of transaminases, GGTP and ShchF in blood serum) each 4 weeks, and then each 3 months. Control of the specified parameters allows to reveal abnormal liver functions at early stages. Also it concerns patients at late stages of primary biliary cirrhosis. Besides, it is so possible to define quickly whether the patient with primary biliary cirrhosis reacts to the carried-out treatment.

At use of drug for dissolution of cholesteric gallstones:

- to estimate progress in treatment and for early detection of signs of calcification of stones depending on their size, the gall bladder should be visualized (the peroral cholecystography) with survey of blackouts in a standing position and lying on spin (ultrasonography) in 6–10 months after an initiation of treatment;

- if the gall bladder cannot be visualized on x-ray films or in cases of calcification of stones, weak contractility of a gall bladder or frequent attacks of gripes, drug Ursofalk should not be used.

At treatment of patients at late stages of primary biliary cirrhosis:

- cirrhosis decompensation cases were extremely seldom noted. After the termination of therapy partial involution of manifestations of a decompensation was noted;

- at patients with diarrhea it is necessary to reduce a drug dosage. At persistent diarrhea it is necessary to stop treatment.

One measured glass (5 ml are equivalent) suspensions Ursofalk for intake of 250 mg / 5 contains ml 0,5 mmol (11,39 mg) of sodium. The patients controlling sodium consumption should consider this fact.

Influence on ability to manage vehicles and moving mechanisms. Influence on ability to manage vehicles and moving mechanisms was not revealed.

Side effects:

Assessment of the undesirable phenomena is based on the following classification: very frequent (≥1/10); frequent (≥1/100 — <1/10); infrequent (≥1/1000 — <1/100); rare (≥1/10000 — <1/1000); very rare (<1/10000).

From a GIT: often — not properly executed chair or diarrhea; at treatment of primary biliary cirrhosis very seldom — acute pains in the right upper part of a stomach.

From a liver and biliary tract: very seldom — calcination of gallstones.

At treatment of the developed stages of primary biliary cirrhosis very seldom — a cirrhosis decompensation which disappears after drug withdrawal.

From skin and hypodermic fabrics: very seldom — a small tortoiseshell.

If any of the side effects specified in the present description is aggravated or the patient noticed other side effects which are not specified in the description, it is necessary to report about it to the doctor.

Interaction with other medicines:

Holestiramin, колестипол and the antacids containing aluminum hydroxide connect ursodeoksikholevy acid in intestines, interfere with its absorption and weaken efficiency (the concomitant use is inexpedient). 

Contraindications:

- hypersensitivity to drug components;

- X-ray positive (with the high content of calcium) gallstones;

- nonfunctioning gall bladder;

- acute inflammatory diseases of a gall bladder, bilious channels and intestines;

- cirrhosis in a decompensation stage;

- the expressed renal failures, a liver, a pancreas.

Ursodezoksikholevy acid has no age restrictions in use, but to children under 3 years Ursofalk in the form of suspension since there can be difficulties at a proglatyvaniye of capsules is recommended to apply.

 

Overdose:

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

Storage conditions:

At a temperature not above 25 °C.

To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules, 250 mg. On 10 капс. in the aluminum/PVC blister, on 1 blister in a pack cardboard.

On 25 капс. in the aluminum/PVC blister, on 2 or 4 blisters in a pack cardboard.

Suspension for intake, 250 mg / 5 ml. On 250 ml in a bottle of dark glass with the screwing-up cover with control of the first opening; on 1 фл. together with a measured glass place in a pack cardboard.