Ursodez®
Inside.
Dissolution of cholesterol gallstones
The recommended (approximate) dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight per day. The drug must be taken daily in the evening, before bed (the capsules are not chewed), with a small amount of liquid. Duration of treatment is 6-12 months. To prevent recurrent cholelithiasis, it is recommended to take the drug for several months after the stones have dissolved.
Treatment of biliary reflux gastritis
1 capsule of Ursodez® daily in the evening before bed, with a small amount of water.
The course of treatment is 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 ranges from 2 to 6 capsules (approximately 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight) in 2-3 doses.
For chronic hepatitis of various origins, non-alcoholic steatohepatitis and alcoholic liver disease
The average daily dose is from 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 doses. The duration of therapy is 6-12 months or more.
For primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)
The average daily dose is from 12 to 15 mg of ursodeoxycholic acid per 1 kg of body weight; if necessary, the average daily dose can be increased to 20-30 mg per 1 kg of body weight in 2-3 doses. The duration of therapy ranges from 6 months to several years.
For biliary dyskinesia
The average daily dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment must be repeated.
Calculation of the daily number of capsules depending on the patient’s body weight and the recommended dose of the drug per 1 kg of body weight
Weight | 10 | 12 | 15 | 20 | 30 |
body, kg | mg/kg/day | mg/kg/day | mg/kg/day | mg/kg/day | mg/kg/day |
34-35 | 1 caps | 2 caps | 2 caps | 3 caps | 4 caps |
36-40 | 2 caps | 2 caps | 2 caps | 3 caps | 5 caps |
41 -45 | 2 caps | 2 caps | 3 caps | 4 caps | 5 caps |
45-50 | 2 caps | 2 caps | 3 caps | 4 caps | 6 caps |
51-55 | 2 caps | 3 caps | 3 caps | 4 caps | 7 caps |
56-60 | 2 caps | 3 caps | 4 caps | 5 caps | 7 caps |
61 -65 | 3 caps | 3 caps | 4 caps | 5 caps | 8 caps |
66-70 | 3 caps | 3 caps | 4 caps | 6 caps | 8 caps |
71-75 | 3 caps | 4 caps | 5 caps | 6 caps | 9 caps |
76-80 | 3 caps | 4 caps | 5 caps | 6 caps | 10 caps |
81-85 | 3 caps | 4 caps | 5 caps | 7 caps | 10 caps |
86-90 | 4 caps | 4 caps | 5 caps | 7 caps | 11 caps |
91 -95 | 4 caps | 5 caps | 6 caps | 8 caps | 11 caps |
96-100 | 4 caps | 5 caps | 6 caps | 8 caps | 12 caps |
101 — 105 | 4 caps | 5 caps | 6 caps | 8 caps | 13 caps |
105-110 | 4 caps | 5 caps | 7 caps | 9 caps | 13 caps |
Contraindications
Like all medications based on chemical compounds, Ursosan has contraindications. First of all, people who have increased sensitivity to the components of this hepatoprotector (allergy) are at risk.
In addition, it is contraindicated in patients who:
- inflammatory process in the acute stage in the gallbladder and bile ducts;
- poor contractility of the gallbladder;
- biliary colic;
- calcified stones were found;
- the gallbladder cannot be determined using radiological methods;
- kidney problems;
- severe liver pathologies.
This remedy for the treatment of the liver and gall bladder is also used in pediatric therapy. But there are age restrictions: it should not be taken by children under 5 years old. But, despite this, there is evidence that if increased bilirubin occurs in newborn babies (newborn jaundice), in especially severe cases, the baby is given ¼ capsule along with breast milk. This is rather an exception to the rule.
The restrictions also apply to other categories of patients.
This drug should be used with caution by those who:
- stomach and duodenal ulcers;
- cirrhosis of the liver;
- a decrease in bile flow was detected (hepatic cholestasis);
- intestinal pathologies associated with inflammatory processes.
The issue of using Ursosan by pregnant women deserves special attention. It is forbidden to take it in the first trimester, but in the second and third trimesters, for health reasons, it is prescribed to women.
Since the first months of bearing a child are especially important for its development, before prescribing the drug, all women of childbearing age are asked to undergo an examination to exclude pregnancy. Treatment with this drug takes months, so women must be protected from pregnancy for the entire duration of therapy.
During lactation, Ursosan is prohibited. Therefore, if there are vital indications for its use, then breastfeeding is stopped.
Ursosan has side effects. They are indicated in the description. Therefore, before taking it, you should know which systems of the human body may be affected by its action.
People often react to the action of Ursosan:
- digestive tract (in the form of diarrhea or pain in the upper abdomen);
- liver (in the form of calcification of existing stones);
- skin (in the form of small rashes).
Side effects are temporary and go away on their own. But if the symptoms manifest themselves with severe pain, you should consult a doctor who will adjust further therapy.
Comparison of drugs Exchol and Ursosan
Interaction
Colestipol, cholestyramine , and antacids containing aluminum hydroxide or aluminum oxide impair the intestinal absorption of ursodeoxycholic acid and, as a result, reduce its effectiveness. It is recommended to take a two-hour break between taking Ursodez and similar drugs.
Ursodeoxycholic acid stimulates the absorption of Cyclosporine from the digestive system.
In some cases, Ursodez reduces the absorption of Ciprofloxacin .
Lipid-lowering drugs, estrogens, gestagens and Neomycin increase the cholesterol content in bile and may weaken the ability of the drug to dissolve cholesterol-type gallstones.
Release form and composition
The dosage form of Ursodez is capsules: gelatin, with an opaque solid structure; size No. 0 - white, inside the capsule the powder is almost white or white; size No. 00 - white body and orange cap, capsule contents - granules and granulated powder of almost white or white color [size No. 0 (0.25 g each): 10 pcs. in a blister pack, in a cardboard pack of 4, 5, 6, 9, 10 or 12 packs; 40, 50, 60, 100 or 120 pcs.
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in a polymer jar or polymer bottle, in a cardboard pack 1 jar or bottle; size No. 00 (0.5 g each): 10 pcs. in a blister pack, in a cardboard box 1, 3 or 5 packages;
30 or 50 pcs . in a polymer bottle or polymer jar, 1 bottle or jar in a cardboard box].
1 capsule contains:
- active ingredient: ursodeoxycholic acid – 0.25 g or 0.5 g;
- auxiliary components: size No. 0 – starch 2020 (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, the cap of capsules No. 00 contains sunset yellow dye.
Indications for use
Due to its wide area of influence and high therapeutic indicators, Ursodez is prescribed for the treatment of various pathologies, which include:
- Cholesterol deposits in the biliary tract. Ursodesis promotes the independent destruction of medium and small formations with subsequent removal from the body.
- Biliary reflux gastritis. At the initial stage of taking the medicine, relief of the inflammatory process localized on the gastric mucosa is noted; with long-term treatment, complete recovery from the disease is noted.
- Primary cirrhosis of the liver. The therapeutic effect is noticeable in small areas of fibrotic liver damage; advanced stages of the disease require potent aggressive medications.
- Chronic stages of hepatitis. Treatment is prescribed on an individual basis, depending on the severity and type of pathology; consultation with a specialist is necessary.
- Kidney diseases that develop as a result of systematic exposure to alcohol. The therapeutic effect is to activate the restoration processes in the gland.
Analogs
In a situation where taking capsules is not possible due to individual sensitivity or the need for a more affordable substitute, doctors prescribe medications with similar pharmacological effects. The pharmacy network is replete with all kinds of medications that have hepatoprotective and choleretic effects. The following drugs analogues of Ursodeza capsules are used in medical practice:
- Urdoxa is a drug that has a hepatoprotective effect. Protects liver cells from the damaging effects of bile salts, thereby reducing the cytotoxic effect of the latter.
- Livodexa is a drug that stabilizes the membranes of cholangiocytes and hepatocytes, reduces the secretion of hydrophobic acids, and has a hypocholesterolemic effect.
- Ursofalk - the drug has a choleretic effect. Reduces cholesterol production in the liver. Helps reduce its concentration in bile. The product increases the solubility of cholesterol.
- Urso is a drug that stimulates pancreatic and gastric secretions and increases lipase activity.
- Ursoliv is a medication that has a direct protective effect on hepatocytes and reduces the toxicity of hydrophobic bile salts.
- Ursolite - helps reduce the concentration of cholesterol in bile mainly through dispersion and the formation of a liquid crystalline phase.
- Ursorom C - the active substance of the drug forms double molecules that have the ability to penetrate into the composition of cell membranes (cholangiocytes, hepatocytes of gastrointestinal epithelial cells) and make them immune to the influence of cytotoxic micelles.
- Choludexan is a drug that reduces the ability of gastric refluxate to have a damaging effect on cell membranes in reflux esophagitis and biliary reflux gastritis. The drug helps eliminate intrahepatic cholestasis.
- Ursosan - reduces the absorption of lipophilic bile acids in the intestine, induces choleresis.
- Exchol - the drug helps reduce the saturation of bile with cholesterol by inhibiting its absorption in the intestine. The drug has a cytoprotective effect and stabilizes the cell membrane of hepatocytes. The drug helps dissolve cholesterol stones.
- Ursor Rompharm - reliably delays the process of connective tissue proliferation in patients with primary alcoholic steatohepatitis, biliary cirrhosis, and cystic fibrosis.
Experts warn that drugs containing ursodeoxycholic acid have a number of serious contraindications and have an immunomodulatory effect, which is why taking them without a doctor’s prescription is dangerous. For this reason, only a doctor should select an analogue, taking into account the severity of the condition and the patient’s weight. Uncontrolled use of ursoxycholic acid drugs can worsen the clinical picture of the disease.
Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Ursodez is a drug with pronounced hepatoprotective . Has a choleretic effect. Reduces the biosynthesis of cholesterol in the liver, its absorption in the intestines and content in bile, increases the solubility of cholesterol in the hepatobiliary system, enhances the excretion and formation of bile. Weakens the lithogenicity of bile, increases the content of bile acids in it. Improves pancreatic and gastric secretion, stimulates lipase . It also has a hypoglycemic effect.
Helps remove cholesterol from gallstones.
It has an immunomodulatory effect: it reduces the expression of antigens on the wall of hepatocytes, affects the content of T-lymphocytes , the production of interleukin-2 , and reduces the content of eosinophils .
Pharmacokinetics
Ursodeoxycholic acid is absorbed from the small intestine as a result of passive diffusion and active transport. The highest concentration in the blood occurs after one hour. Plasma protein binding reaches 97-99%. Penetrates the placenta barrier. The therapeutic effect of the drug depends on the content of the active substance in the bile.
It is transformed into conjugates that are secreted into bile. 50-70% of the dose taken is excreted in bile.