Ursodex
Ursodex: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Ursodex
ATX code: A05AA02
Active ingredient: Ursodeoxycholic acid (Ursodeoxycholic acid)
Manufacturer: Sun Pharmaceutical Industries Ltd. (India)
Description and photo update: 2018-24-10
Ursodex is a hepatoprotector that also has immunomodulatory, choleretic, hypolipidemic, cholelitholytic and hypocholesterolemic effects.
Release form and composition
The dosage form of the release of Ursodex is film-coated tablets: brown-red, biconvex, round, on one side of the risk; the color of the kernel on the break is white (10 pcs. in blisters, in a cardboard box 1, 5 or 10 packs).
Composition of 1 tablet:
- active substance: ursodeoxycholic acid - 150 or 300 mg;
- auxiliary components (150/300 mg): purified talc - 6.4 / 20 mg; lactose - 43.5 / 87 mg; starch - 9/18 mg; sodium lauryl sulfate - 3/6 mg; microcrystalline cellulose - 22/44 mg; magnesium stearate - 3/6 mg; povidone K-30 - 10/10 mg; colloidal silicon dioxide - 1.5 / 3 mg; sodium carboxymethyl starch - 13/26 mg;
- film coat (150/300 mg): macrogol-6000 - 0.95 / 1.9 mg; hypromellose E5 - 4.8 / 9.6 mg; titanium dioxide - 0.48 / 0.96 mg; iron oxide red - 0.09 / 0.18 mg; iron oxide yellow - 0.08 / 0.16 mg.
Pharmacological properties
Pharmacodynamics
Ursodex is a hepatoprotector with choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and immunomodulatory properties.
As a result of stabilization of the membranes of cholangiocytes and hepatocytes, ursodeoxycholic acid has a direct cytoprotective effect. Under the influence of the drug on the gastrointestinal circulation of bile acids, the content of hydrophobic acids decreases (they are potentially toxic). It has a hypocholesterolemic effect (due to a decrease in the absorption of cholesterol in the intestine and some other biochemical effects). Suppresses cell death caused by toxic bile acids.
Ursodeoxycholic acid has high polar properties, resulting in the formation of non-toxic mixed micelles with toxic (apolar) bile acids, which leads to a decrease in the ability of gastric refluctate to damage cell membranes in patients with reflux esophagitis and biliary reflux gastritis. In addition, ursodeoxycholic acid forms double molecules that can be incorporated into the composition of cell membranes, stabilizing them and making them immune to the effects of cytotoxic micelles.
Other effects of the substance:
- a decrease in the saturation of bile with cholesterol (due to the inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in secretion into bile);
- an increase in the solubility of cholesterol in bile with the formation of liquid crystals with it;
- decrease in the lithogenic index of bile.
As a result of the use of Ursodex, cholesterol gallstones are dissolved (due to a change in the ratio of bile acids / cholesterol in bile). Taking the drug also prevents the formation of new calculi, which is ensured by a decrease in the content of cholesterol in bile. It induces choleresis rich in bicarbonates, this leads to an increase in the passage of bile and stimulates the excretion of toxic bile acids through the intestine.
The immunomodulatory effect of Ursodex is due to the inhibition of the expression of HLA antigens (human leukocyte antigens - tissue compatibility antigens) on the membranes of cholangiocytes and hepatocytes and the normalization of the natural killer activity of lymphocytes. According to the studies, ursodeoxycholic acid delays the progression of fibrosis in primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis, and reduces the likelihood of esophageal varicose veins.
Pharmacokinetics
Absorption of ursodeoxycholic acid from the jejunum occurs through passive diffusion, from the ileum through active transport. Plasma concentration for oral administration of 500 mg of the substance is 3.8; 5.5 and 3.7 mmol / l (achieved after 30, 60, 90 minutes, respectively).
The distribution of the substance is characterized by a high degree of binding to plasma proteins (from 96 to 99%). Penetrates the placental barrier.
Ursodeoxycholic acid undergoes presystemic elimination with the formation of glycine and taurine conjugates, which are secreted into bile. Approximately 50–70% of the total administered dose is excreted in the bile.
The remainder of the non-absorbed fraction undergoes bacterial cleavage in the colon, where the formation of lithocholic acid, which is partially absorbed from the intestine, is biotransformed in the liver into sulfolitocholyltauric and sulfolitocholylglycine conjugates and then excreted.
Indications for use
- primary biliary cirrhosis in patients with no signs of decompensation (symptomatic treatment);
- biliary reflux gastritis;
- small / medium-sized cholesterol stones in patients with no gallbladder dysfunction (to dissolve).
Contraindications
- high calcium gallstones (X-ray positive);
- non-functioning gallbladder;
- pancreatitis;
- inflammatory diseases of the gallbladder, bile ducts and intestines in acute course;
- severe renal / hepatic impairment;
- liver cirrhosis in the stage of decompensation;
- lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
- weight up to 34 kg;
- pregnancy and lactation;
- individual intolerance to any component of Ursodex.
Instructions for the use of Ursodex: method and dosage
Ursodex is taken orally, without chewing, with a little water, preferably in the evening.
Recommended dosage regimen:
- dissolution of cholesterol gallstones: 10 mg / kg per day, course duration - from 6 to 12 months; after the dissolution of the stones, the continuation of therapy is shown for several more months with a preventive purpose;
- biliary reflux gastritis: once a day, 250 mg, course duration - from 10 days to 6 months, if necessary, it can be longer - up to 2 years;
- primary biliary cirrhosis: 10 to 15 mg / kg per day.
Side effects
- digestive system: abdominal pain, nausea, diarrhea, increased activity of hepatic transaminases, calcification of gallstones; in patients with primary biliary cirrhosis - reversible transient decompensation of liver cirrhosis;
- others: allergic reactions (including hives).
Overdose
There are no data on cases of overdose of Ursodex.
special instructions
In order for the stones to dissolve successfully, several conditions must be met:
- pure cholesterol structure of stones;
- stones up to 1.5–2 cm;
- filling the gallbladder with stones no more than half;
- complete preservation of the function of the biliary tract.
During therapy for dissolving gallstones, patients should be under medical supervision for the following indicators: activity of hepatic transaminases and alkaline phosphatase, gamma-glutamyltransferase, bilirubin concentration. If the increased rates persist, therapy is canceled.
The first 3 months of using Ursodex, cholecystography should be performed once a month, then once every 3 months. At least once every six months, the effectiveness of the therapy should be assessed (using ultrasound). After confirmation of the dissolution of calculi, the drug should be continued for at least 3 months. This will further dissolve small stones that are not detected by ultrasound.
If after 6-12 months of therapy, partial dissolution of calculi has not occurred, the probability of success is considered minimal.
The detection of an unimaged gallbladder during the treatment period is a sign that the calculi have not dissolved and Ursodex must be canceled. Also, the cancellation of treatment is required in the following cases: calcification of gallstones, impaired contractility of the gallbladder, or frequent attacks of biliary colic.
Application during pregnancy and lactation
According to the instructions, Ursodex is contraindicated in pregnant and lactating women.
Pediatric use
The drug is not prescribed for patients weighing up to 34 kg.
With impaired renal function
It is contraindicated to take Ursodex to patients with severe renal insufficiency.
For violations of liver function
Contraindications to taking Ursodex are liver cirrhosis and severe liver failure.
Drug interactions
Possible interactions:
- estrogens, gestagens, neomycin, lipid-lowering drugs: an increase in the saturation of bile with cholesterol, which can cause a decrease in the ability of ursodeoxycholic acid to dissolve cholesterol gallstones;
- antacids containing aluminum and ion-exchange resins: the combination is contraindicated, since combination therapy can lead to impaired absorption of ursodeoxycholic acid;
- cyclosporine: an increase in its absorption from the intestine (its concentration in the blood should be monitored, if necessary, the doctor can adjust its dose).
Analogs
The analogues of Ursodex are: Ursolit, Ursofalk, Urdoksa, Ursosan, Ursoliv, Ursodez.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ursodex
According to reviews, Ursodex is used mainly for dissolving stones, as well as with increased hepatic parameters. In some cases, the therapy is highly effective in both adults and children. However, there are reviews that indicate that the drug had to be abandoned due to the development of side effects or due to insufficient therapeutic effect.
Price for Ursodex in pharmacies
The approximate price for Ursodex (50 or 100 300 mg tablets) is 420 or 1100-1150 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
