Ursodez
Ursodez: 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. In case of impaired 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: Ursodez
ATX code: A05AA02
Active ingredient: Ursodeoxycholic acid (Ursodeoxycholic acid)
Manufacturer: SEVERNAYA ZVEZDA (Russia)
Description and photo update: 2018-22-10
Prices in pharmacies: from 469 rubles.
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Ursodez is a hepatoprotective drug.
Release form and composition
Dosage form Ursodez - capsules: gelatinous, with an opaque solid structure; size no. 0 - white, inside the capsule powder is almost white or white; size No. 00 - white body and orange cap, capsule contents - granules and granular powder of almost white or white color [size No. 0 (0.25 g each): 10 pcs. in a contour acheikova packing, in a cardboard box 4, 5, 6, 9, 10 or 12 packages; 40, 50, 60, 100 or 120 pcs. in a polymer can or a polymer bottle, in a cardboard box 1 can or bottle; size No. 00 (0.5 g each): 10 pcs. in a contour acheikova packing, in a cardboard box 1, 3 or 5 packages; 30 or 50 pcs. in a polymer bottle or polymer can, in a cardboard box 1 bottle or can].
1 capsule contains:
- active substance: ursodeoxycholic acid - 0.25 g or 0.5 g;
- auxiliary components: size No. 0 - starch 1500 (pregelatinized starch), magnesium stearate, aerosil (colloidal silicon dioxide); size No. 00 - croscarmellose sodium (primellose), magnesium stearate, hypromellose (hydroxypropyl methylcellulose);
- shell composition: gelatin, titanium dioxide.
Additionally, in the composition of the cap of capsules No. 00 - sunset yellow dye.
Pharmacological properties
Pharmacodynamics
Ursodeoxycholic acid is a hepatoprotector with choleretic, cholelitholytic and immunomodulatory effects.
The choleretic activity of the drug is due to a decrease in cholesterol synthesis in the liver, its absorption in the intestine and a decrease in the concentration level in bile. By increasing the solubility of cholesterol in the biliary system, ursodeoxycholic acid stimulates the formation and excretion of bile, decreasing its lithogenicity, and increasing the content of bile acids. Promotes increased gastric and pancreatic secretion, increased lipase activity.
Has a hypoglycemic effect.
The drug partially or completely dissolves cholesterol stones, reduces the saturation of bile with cholesterol, which leads to the mobilization of cholesterol from gallstones.
The immunomodulatory activity of the drug is manifested in a decrease in the expression of some antigens on the membrane of hepatocytes, a decrease in the number of eosinophils, the effect of ursodeoxycholic acid on the formation of interleukin-2 and the number of T-lymphocytes.
Pharmacokinetics
Due to passive diffusion from the small intestine, about 90% of ursodeoxycholic acid is absorbed; through active transport, the drug is absorbed from the ileum. The maximum concentration (Cmax) in the blood serum after a single dose of 0.5 g after 0.5, 1 and 1.5 hours is 3.8; 5.5 and 3.7 mmol / L, respectively.
Ursodeoxycholic acid has a high binding to plasma proteins, it reaches 96–99%. Overcomes the placental barrier. When taken systematically, it is 48% of the total amount of bile acids in the blood serum. The therapeutic effect of Ursodez depends on the level of its concentration in bile.
The drug metabolism occurs in the liver. The resulting taurine and glycine conjugates are secreted into bile.
Approximately 50–70% of the drug is excreted from the total dose by bile, a small part of the active substance not absorbed enters the large intestine. There, as a result of breakdown by bacteria (7-dehydroxylation), lithocholic acid is formed, which is absorbed to some extent from the colon. Lithocholic acid is sulfated in the liver, then rapidly excreted in the form of a sulfolitocholyl-tauric or sulfolitocholylglycine conjugate.
Indications for use
- biliary dyskinesia;
- dissolution of cholesterol stones of small and medium fraction with a functioning gallbladder;
- chronic hepatitis of various origins;
- biliary reflux gastritis;
- symptomatic therapy of primary biliary cirrhosis in the absence of signs of decompensation;
- primary sclerosing cholangitis;
- cystic fibrosis (cystic fibrosis);
- alcoholic liver disease;
- non-alcoholic steatohepatitis.
Contraindications
- liver cirrhosis in the stage of decompensation;
- high calcium gallstones (X-ray positive);
- non-functioning gallbladder;
- severe renal and / or liver dysfunction;
- acute stage of inflammatory diseases of the gallbladder, bile ducts, intestines;
- severe functional disorders of the pancreas;
- period of pregnancy;
- breast-feeding;
- age up to 3 years;
- adults and children weighing up to 34 kg;
- hypersensitivity to the components of the drug.
Care should be taken when appointing Ursodez to patients with cholelithiasis, cholestatic liver diseases.
Instructions for the use of Ursodez: method and dosage
Ursodez capsules are taken orally, swallowed whole and washed down with a little water.
The dose and course of treatment is prescribed by the doctor based on clinical indications.
Recommended daily dosage of Ursodez:
- dissolution of cholesterol gallstones: at the rate of 0.01 g of ursodeoxycholic acid per 1 kg of the patient's body weight, 1 time per day (before going to bed in the evening). The duration of treatment is from 6 to 24 months. In the absence of a therapeutic effect (reduction in the size of stones) after 12 months of treatment, further use of the drug should be discontinued. The effectiveness of treatment is assessed every 6 months based on the results of an ultrasound scan (ultrasound) or radiography. During an interim examination, the structure of the stones is assessed. If during the elapsed period the stones have calcified, the treatment should be discontinued. After complete dissolution of the stones, taking the drug should be continued for several months in order to prevent recurrent cholelithiasis;
- biliary reflux gastritis: 0.25 g 1 time per day in the evening before bedtime. The course of treatment is from 0.5 to 6 months, if necessary - up to 24 months;
- symptomatic therapy of primary biliary cirrhosis: at the rate of 0.01-0.015 g per 1 kg of body weight, during the first three months the daily dose is divided into 2-3 doses. After improving liver function indicators, you can switch to a single dose in the evening. The duration of the course of treatment is not limited. If at the beginning of treatment the clinical symptoms worsen (in the form of increased itching), the daily dose should be reduced to 0.25 g and continued treatment, gradually increasing it until the previously recommended dose is reached;
- non-alcoholic steatohepatitis, chronic hepatitis of various origins, alcoholic liver disease: 0.01–0.015 g per 1 kg of body weight in 2–3 doses, treatment is continued for 6–12 months or more;
- primary sclerosing cholangitis: 0.012–0.015 g per 1 kg of body weight in 2-3 doses. If necessary, the dose can be increased to 0.02 g per 1 kg per day. Course duration - from 6 months or more;
- cystic fibrosis: 0.02–0.03 g per 1 kg of body weight in 2-3 doses. Long-term treatment - from 6 months or more;
- dyskinesia of the biliary tract: an average of 0.01 g per 1 kg of body weight, the dose received is divided into 2 doses. The course of treatment is 0.5–2 months. If necessary, a repetition of the course of therapy is indicated.
Since the daily dose of Ursodez is prescribed at the rate of a certain dose per 1 kg of the patient's weight, the result is a number that is not always a multiple of the whole capsule at a dose of 0.25 g. Therefore, it is recommended to round off the result and use the following daily doses of the drug when prescribing:
- 0.01 g per 1 kg of body weight: with a patient weighing 34–35 kg - 0.25 g; 36-60 kg - 0.5 g; 61–85 kg - 0.75 g; 86-110 kg - 1 g;
- 0.012 g per 1 kg of weight: 34-50 kg - 0.5 g; 51–70 kg - 0.75 g; 71–90 kg - 1 g; 91-110 kg - 1.25 g;
- 0.015 g per 1 kg of weight: 34–40 kg - 0.5 g; 41–55 kg - 0.75 g; 56–70 kg - 1 g; 71–90 kg - 1.25 g; 90-105 kg - 1.5 g; 106-110 kg - 1.75 g;
- 0.02 g per 1 kg: 34–40 kg - 0.75 g; 41–55 kg - 1 g; 56–65 kg - 1.25 g; 66-80 kg - 1.5 g; 81-90 kg - 1.75 g; 91-105 kg - 2 g; 106-110 kg - 2.25 g;
- 0.03 g per 1 kg of weight: 34–35 kg - 1 g; 36–45 kg - 1.25 g; 46-50 kg - 1.5 g; 51-60 kg - 1.75 g; 61–70 kg - 2 g; 71-75 kg - 2.25 g; 76–85 kg - 2.5 g; 86–95 kg - 2.75 g; 96-100 kg - 3 g, 101-110 kg - 3.25 g.
For the treatment of children over the age of 3 years, the dosage regimen is prescribed individually; it is recommended to use 0.01–0.02 g per 1 kg per day.
Side effects
- from the digestive system: pain in the right hypochondrium and (or) the epigastric region, diarrhea, nausea, calcification of gallstones, increased activity of hepatic transaminases; possibly (in patients with primary biliary cirrhosis) - transient decompensation of liver cirrhosis (disappears after discontinuation of the drug);
- others: allergic reactions.
Overdose
Overdose symptoms have not been established.
In case of an overdose of Ursodez, symptomatic therapy is indicated.
special instructions
Treatment with Ursodez should be under the supervision of a physician.
Every month, during the first three months of therapy, an examination is carried out for the state of the functional parameters of the liver (transaminases, alkaline phosphatase, gamma-glutamyltransferase) in the blood serum. Further monitoring should be carried out 1 time in 3 months in order to identify abnormal liver function in the early stages. Based on the results of studies in patients with primary biliary cirrhosis, the response to treatment is determined.
To assess the effectiveness of treatment and timely detection of signs of calcification of stones 6–10 months after the start of treatment, it is necessary to conduct a study of the gallbladder using oral cholecystography and ultrasound of opacities in the standing and supine position. If it is impossible to visualize the gallbladder on X-rays, as well as with calcification of stones, frequent attacks of colic, low contractility of the gallbladder, Ursodez should not be used.
In the treatment of late stages of primary biliary cirrhosis, the development of decompensation of liver cirrhosis is possible. After discontinuation of the drug, regression of manifestations of decompensation is noted.
The use of high doses (0.02–0.03 g per 1 kg) of ursodeoxycholic acid for a long time can cause severe side effects in patients with primary sclerosing cholangitis.
In case of development of diarrhea, the dose of the drug should be reduced, with persistent diarrhea - discontinue treatment.
Influence on the ability to drive vehicles and complex mechanisms
The effect of the drug on the patient's ability to drive vehicles and mechanisms has not been established.
Application during pregnancy and lactation
According to the instructions, Ursodez is contraindicated during the period of gestation and breastfeeding.
Pediatric use
Cannot be prescribed under the age of 3 years or children over 3 years of age with a body weight of up to 34 kg.
With impaired renal function
The use of Ursodez is contraindicated in severe renal impairment.
If liver function is impaired
Do not take Ursodez for patients with severe liver dysfunction and liver cirrhosis in the stage of decompensation.
It is recommended to prescribe with caution in cholestatic liver pathologies.
Drug interactions
With the simultaneous use of Ursodez:
- with colestipol, cholestyramine, antacids containing aluminum oxide or aluminum hydroxide: the absorption of the drug in the intestine decreases, its absorption and effectiveness, therefore, if necessary, their combination with ursodeoxycholic acid, it should be taken only 2 hours after taking these funds;
- with lipid-lowering agents (to a greater extent - clofibrate), neomycin, estrogens, progestogens: the saturation of bile with cholesterol increases, which reduces the drug's ability to dissolve cholesterol bile stones;
- with cyclosporine: absorption of cyclosporine from the intestine may increase, control of the level of concentration of cyclosporin in the blood is required, if necessary, its dose is adjusted;
- with ciprofloxacin: absorption of ciprofloxacin may decrease.
Analogs
Ursodez analogs: Livodexa, Ursofalk, Urdoksa, Ursosan, Ursorom Rompharm, Urso, Ursodex, Ursolit, Ursoliv, Ursorom C, Choludeksan, Exhol.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C, protected from moisture and light.
Shelf life: capsules No. 0 (0.25 g each) - 5 years, capsules No. 00 (0.5 g each) - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ursodez
Reviews about Ursodez are mostly positive, even in the early stages of treatment, patients indicate a significant improvement in their condition (a decrease in bilirubin levels, no pain in the right hypochondrium).
Price for Ursodez in pharmacies
The price for Ursodez 0.25 g per package containing 50 capsules is from 623 rubles, 100 capsules - from 1082 rubles, for 30 capsules in a dose of 0.5 g - from 727 rubles.
Ursodez: prices in online pharmacies
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Drug name Price Pharmacy |
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Ursodez 250 mg capsule 40 pcs. 469 r Buy |
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Ursodez 250 mg capsule 50 pcs. 559 r Buy |
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Ursodez 500mg capsules 30 pcs. RUB 611 Buy |
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Ursodez 500 mg capsules 30 pcs. RUB 611 Buy |
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Ursodez 250 mg capsule 100 pcs. 981 RUB Buy |
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Ursodez 250mg capsules 100 pcs. 988 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
