Ursolysin

The common medication Ursolizin is often prescribed for diseases of the biliary system – pathologies of the liver and bile ducts.

Indications Ursolysin

Ursolizin may be prescribed for the following therapeutic purposes:

• for softening radiologically negative gallstones of cholesterol origin, the size of which does not exceed 1.5 cm (with a functioning gallbladder);
• for the treatment of inflammatory processes in the stomach associated with the reflux of bile into it;
• to eliminate the symptoms of primary biliary cirrhosis if cirrhosis is in the compensated stage.

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Release form

Ursolizin is produced in the form of capsules for internal use: blister plates contain 10 capsules, and a cardboard box contains two blister plates.

Ursolizin is available in two dosage options:

• Ursolizin 150 mg, which contains 150 mg of the active ingredient ursodeoxycholic acid;
• Ursolizin 300 mg, which contains 300 mg of the active ingredient ursodeoxycholic acid.

The capsules are dense, white, with a white powdery substance inside.

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Pharmacodynamics

The active ingredient of the drug Ursolizin is a bile acid, normally present in human bile secretions in the form of small amounts of cholic or chenodeoxycholic acid.

When taking Ursolizin capsules internally, the drug reduces the cholesterol content in bile, prevents its absorption by the intestinal walls, and reduces the release of cholesterol into the bile environment.

It is generally accepted that gallstones dissolve as a result of the dispersed decomposition of cholesterol and the formation of liquid crystalline structures.

Presumably, the effect of Ursolizin in liver and cholestatic pathologies is associated with the relative replacement of lipophilic toxic bile acids with a protective hydrophilic non-toxic acid. In addition, the producing capacity of liver cells improves, and immunoregulatory processes are normalized.

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Pharmacokinetics

After internal use, Ursolizin is well absorbed in the intestinal cavity, due to passive and active transport. After the absorption processes, the active ingredient Ursolizin is conjugated in the liver with the participation of glycine and taurine, after which it leaves the body as part of the bile.

Primary hepatic passage clearance rates can be as high as 60%.

Under the influence of intestinal microorganisms, incomplete degradation of the active ingredient Ursolizin is observed, with the formation of 7-ketolithocholic and lithocholic acid. The latter is considered toxic to the liver and leads to changes in the liver parenchyma in rodents. However, in humans, a relatively small amount of acid is absorbed, which is sulfated by the liver and deactivated, and then leaves the body with bile secretions and feces.

The biological half-life of the active ingredient Ursolizin can range from 3.5 to 5.8 days.

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Dosing and administration

Ursolizin is prescribed only by a doctor. For patients weighing up to 47 kg, or those who have difficulty swallowing encapsulated drugs, the doctor may prescribe other similar medications in suspension form.

• In the presence of gallstones of cholesterol origin, 10 mg of Ursolizin per kg of the patient's weight is prescribed. The capsules are swallowed whole, daily at night, regularly. The duration of treatment is usually from six months to a year. If after 12 months of treatment there is no positive result, then Ursolizin is discontinued. The quality of treatment should be checked once every six months, using ultrasound and radiography. At the same time, the probability of calcification of stones is assessed. If signs of calcification are detected, therapy is discontinued.
• In case of inflammation in the stomach with reflux of bile, 1 capsule of Ursolizin is prescribed at night for two weeks. The treatment regimen can be changed at the discretion of the doctor.
• In primary biliary cirrhosis, the daily dose of Ursolizin should be 12-16 mg per kg of the patient's weight. During the first three months of therapy, Ursolizin is taken three times a day. After the patient's condition improves, they switch to the usual dose - once a day at night.

The capsules are swallowed whole, with water. It is advisable to take them daily at the same time.

In primary biliary cirrhosis, clinical symptoms may worsen at first, such as itching. If this happens, treatment is continued, limiting the intake of Ursolizin to once a day. After the patient's condition has stabilized, the amount of the drug is gradually increased (one capsule is added weekly until the required dosage is reached).

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Use Ursolysin during pregnancy

At present, there is insufficient information on the use of Ursolizin by pregnant patients. Given this, it is preferable to avoid using this medication during pregnancy.

It is recommended that all patients of childbearing age begin taking contraceptives before starting treatment to avoid negative consequences in case of pregnancy. Contraceptives should be non-hormonal or with a minimum content of estrogens.

Due to the lack of necessary information, it is not recommended to take Ursolizin during breastfeeding.

Contraindications

Ursolizine is not prescribed:

• if you are prone to an allergic reaction to the ingredients of the drug;
• in case of exacerbation of the inflammatory process in the biliary system;
• in case of obstruction of the bile ducts.

You should not choose Ursolizin if you have calcifications in the gallbladder, if you have impaired contractile function of the gallbladder, or if you have frequent hepatic colic.

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Side effects Ursolysin

Treatment with Ursolizin may be accompanied by certain side effects:

• diarrhea, semi-liquid stool;
• pain in the abdomen or in the liver area;
• formation of calcifications;
• transition of biliary cirrhosis of the liver to a transient stage of decompensation;
• allergic reactions in the form of hives.

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Overdose

When taking irrationally large amounts of Ursolizin, diarrhea may develop. Other signs of overdose are unlikely, because with increased intake of Ursolizin into the intestine, its absorption decreases, and the excess of the drug is excreted with feces.

If diarrhea occurs, the dosage of Ursolizin is reviewed and adjusted. If diarrhea persists, Ursolizin is discontinued.

Special measures in case of overdose are not applied. It is recommended to monitor the stability of water-electrolyte balance.

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Interactions with other drugs

Ursolizin should not be taken in combination with drugs such as Cholestyramine, Colestipol, or antacids containing aluminum salts. If the combination of these drugs cannot be avoided, then a 120-minute interval should be maintained between their administrations.

Ursolizine is able to accelerate the absorption of Cyclosporine, which requires additional monitoring of its level in the bloodstream, with possible dosage adjustment.

In some patients, Ursolizin may impair the absorption of Ciprofloxacin.

Estrogen-containing drugs, as well as medications that reduce cholesterol levels in the bloodstream (eg, Clofibrate) can increase the likelihood of gallstone formation and minimize the effect of Ursolizin (if the drug is used to dissolve these stones).

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Storage conditions

Ursolizin can be stored at room temperature – up to +25°C. It is necessary to ensure that children do not have access to places where medicines are stored.

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Shelf life

Ursolizine is suitable for use for three years from the date of manufacture.