Ursonost 150mg 20 capsules — Made in Italy — Free Delivery

(Ursonost 150mg )
Ursonost 150mg 20 capsules — Made in Italy — Free Delivery
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Francia Farmaceutici Industria Brand: Francia Farmaceutici Industria

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Description Ursonost 150mg 20 capsules — Made in Italy — Free Delivery

Pharmacological properties

Pharmacodynamics. Ursodeoxycholic acid (udc) is a 7β-epimer of chenodeoxycholic acid and bile acid, which is physiologically present in human bile in insignificant concentration compared to the total amount of bile acids.

UDCA inhibits hepatic synthesis and secretion of cholesterol, as well as absorption of cholesterol in the intestine. It probably has a weak inhibitory effect on the synthesis and secretion of endogenous bile acids into bile and does not affect the release of phospholipids into bile.

With constant administration of the preparation, the concentration of UDCA in bile reaches its maximum value after about 3 weeks. Despite its insolubility in an aqueous medium, CS can be solubilized in at least two different ways in the presence of dihydroxy bile acids. In addition to solubilizing CS in micelles, UDCA has a unique effect that causes the dissolution of CS in the form of liquid crystals in an aqueous medium. Thus, despite the fact that the administration of high doses (for example, 15–18 mg / kg / day) does not lead to a concentration of UDCA, which exceeds 60% of the total amount of the pool of bile acids, bile enriched with UDCA effectively dissolves CS. The general effect of UDCA is to increase the concentration of bile, at which it is saturated with cholesterol.

Various mechanisms of action of UDCA are aimed at reducing the level of calculus-forming cholesterol, which is secreted into bile, as well as solubilizing it, which helps dissolve cholesterol gallstones.

After stopping the intake of UDCA, the concentration of bile acid in bile decreases exponentially, decreasing to about 5-10% of its normal level after about 1 week.

Pharmacokinetics. About 90% of the therapeutic dose of UDCA is absorbed in the small intestine after oral administration. After absorption, UDCA enters the liver through the portal vein and undergoes primary metabolism (that is, there is a pronounced first pass effect), where it is conjugated with glycine or taurine and then secreted into the hepatic bile ducts. UDCA in bile is concentrated in the gallbladder and is released into the duodenum from the gallbladder through the common duct due to contraction of the gallbladder, which is a physiological response to food. Only trace amounts of UDCA appear in the systemic circulation, a very small amount of it is excreted in the urine. The area of ​​therapeutic effects of the preparation is in the liver, bile and intestinal lumen.

Apart from conjugation, UDCA is not metabolized by the liver or intestinal mucosa. A small amount of the preparation undergoes bacterial degradation with each cycle of the hepatic circulation. UDCA can be either oxidized or reduced on 7-carbon, which gives, respectively, 7-ketolithocholic acid (7-CLA) or lithocholic acid (LCA). In addition, there is a bacterial catalytic deconjugation of glyco- and taurousodeoxycholic acid in the small intestine. Free UDCA, 7-CLA, and LCA are insoluble in the aqueous medium, and large amounts of these compounds are excreted from the distal intestine with feces. Reabsorbed free UDCA is restored by the liver. 80% of LCA formed in the small intestine is excreted in the feces, but 20%, which are absorbed, are sulfated at the 3-hydroxyl group in the liver to relatively insoluble lithocholil conjugates, which are excreted in the bile and dissolve in the feces. The absorbed 7-CLX is stereospecifically cleaved in the liver to chenodiol.

LCA is formed by 7-dehydroxylation of dihydroxy bile acids (UDCA and chenodiol) in the intestinal lumen. The reaction of 7-dehydroxylation is alpha-specific, that is, henodiol lends itself more effectively to 7-dehydroxylation than UDCA, and for equimolar doses of UDCA and chenodiol, the levels of LCA present in bile do not change. During experiments on animals, it was recorded that the accumulation of LCA leads to liver damage due to insufficient activity of LCA sulfation. A person has the ability to sulfate LCA. In some patients, liver damage was noted in the course of studies, but it was not associated with UDCA therapy. This is because some people may have a reduced ability to sulfate, but this phenomenon has not been studied.

Indications

Ursonost is prescribed for patients with X-ray negative, uncalcified gallbladder stones of 20 mm in the largest diameter, for whom an optional cholecystectomy can be performed, including patients with a high surgical risk due to systemic disease, elderly patients, individuals with individual intolerance to general anesthesia or patients who refuse from the operation.

Ursonost is prescribed to prevent the formation of gallstones in obese patients who plan to rapidly reduce body weight.

Application

Udhk should be used under medical supervision.

The capsules must be swallowed whole with a liquid. It is required to observe the regularity of admission.

For patients whose body weight is less than 47 kg or who have difficulty swallowing capsules, it is recommended to use the preparation in a different dosage form (for example, suspension).

Dissolution of gallstones. The recommended dose of Ursonost for treatment of radiopaque gallbladder stones is 8-10 mg / kg / day in two or three doses.

Control ultrasound of the gallbladder should be performed every 6 months during the first year of preparation therapy. If gallstones dissolve, use of the preparation should be continued and an ultrasound scan should be performed every 1–3 months. In most patients who ultimately experienced complete dissolution of the stones, partial or complete dissolution of the stones was noted at the first evaluation of treatment. If partial dissolution of stones is not observed after 12 months of therapy with Ursonost, the probability of success is significantly reduced.

Prevention of stone formation. The recommended dose for the prevention of gallstones in patients planning a rapid decrease in body weight is 600 mg / day (300 mg 2 times a day).

Contraindications

Patients with calcified cholesterol stones or radiopaque stones.

Patients with urgent indications for cholecystectomy, including nonremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or patients with biliary fistulas.

Allergy to bile acids.

Side effects

When conducting studies, the nature and frequency of adverse reactions were the same in all groups. the following are the side reactions and conditions noted most often:

General disorders: flu-like symptoms, allergies.

From the digestive tract: abdominal pain, dyspepsia, constipation, diarrhea, nausea, vomiting, cholecystitis.

From the respiratory system: bronchitis, cough, pharyngitis, upper respiratory tract infections.

From the musculoskeletal system: arthralgia, arthritis, back pain.

From the nervous system: dizziness, headache.

On the part of the skin and appendages: hair loss.

From the genitourinary system: urinary tract infections.

Hypersensitivity Reactions: Very rarely, allergic reactions, including rash, urticaria, are possible.

Special instructions

Dissolution of gallbladder calculi with ursonost requires long-term therapy. complete dissolution does not occur in all patients, and recurrence of calculi within 5 years is observed in 50% of patients treated with udhk. the conditions of udxc therapy must be carefully observed, and alternative therapies should be considered. the safety of using ursonosta for more than 24 months has not been established.

The ability to control the composition of bile to check for a decrease in the content of cholesterol in bile is an important element of a favorable prognosis of treatment results.

Patients with frequent biliary colic, biliary tract infections, severe pancreatic disorders, or those with bowel disease that may affect the gastro-hepatic circulation of bile acids (jejunoileal resection or stomosis, regional ileitis) should be used with caution.

For patients taking Ursonost to dissolve gallstones, it is advisable to undergo ultrasound or cholecystography every 6 months to check the effectiveness of the preparation. One of the indicators of progressive treatment can be monitoring the composition of bile in order to control the decrease in the content of cholesterol.

Women using a gallstone dissolving preparation should use an effective non-hormonal contraceptive method, as hormonal contraceptives can increase gallstone formation.

Ultrasound or cholecystography is recommended to be repeated every 6 months in patients using Ursonost to dissolve gallstones.

During the first 3 months of treatment, every 4 weeks, the doctor needs to monitor liver function by sampling for AST, ALT and GGT and every 3 months with further treatment. Control studies make it possible to determine whether the patient's body is responding to the treatment of primary biliary cirrhosis, and such monitoring also provides an opportunity for early detection of potential impairments in hepatic function.

Dissolution of cholesterol gallstones. For a correct assessment of the therapeutic effect and for the timely detection of calcified gallstones, their size and condition, it is necessary to visualize the gallbladder (oral cholecystography): a general image and occlusions in the patient's standing position, lying on his back (ultrasound) 6-10 months after the start of treatment taking into account the size of the calculi.

It is inappropriate to use UDCA if the gallbladder cannot be visualized by x-ray in case of calcified gallstones, impaired contraction of the gallbladder, or with frequent biliary colic.

Use in the elderly. In clinical studies, about 4% of patients were 65 years of age or older (about 3% were over 75 years old). No age-related differences in safety and efficacy were identified. Other reported clinical trials have not found differences between elderly and younger patients. However, small differences in the effectiveness and greater sensitivity of some elderly people taking Ursonost cannot be ruled out. Therefore, it is recommended to individually select the dose for patients of this age category.

Use during pregnancy and lactation. There is insufficient data on the use of the preparation during pregnancy, especially in the first trimester. Animal studies indicate teratogenic effects in the early stages of pregnancy.

UDCA should not be used during pregnancy unless it is strictly necessary. Women of reproductive age can use Ursonost only if they use proven contraceptives. Non-hormonal contraceptives or low-estrogen oral contraceptives are recommended. If patients are taking UDCA to dissolve gallstones, only effective non-hormonal contraceptives should be used, as hormonal contraception can contribute to the formation of gallstones. Before starting treatment, it is necessary to exclude the possibility of pregnancy.

There is no information about the penetration of Ursonost into breast milk. Therefore, you should not use the preparation during breastfeeding. If UDCA treatment is mandatory, then breastfeeding should be discontinued.

Children. There is not enough experience with the use of the preparation in children.

The ability to influence the reaction rate when driving or working with other mechanisms. There was no effect on the ability to drive vehicles or operate machinery.

Interactions

Bile acid sequestrants such as cholestyramine and colestipol may interfere with the action of udxa, decreasing its absorption. it has been shown that aluminum-based antacids adsorb bile acids in vitro, therefore, they can reduce the absorption of udxa. estrogens, oral contraceptives and clofibrate (as well as other preparations that lower lipid levels) increase the secretion of hepatic cholesterol and may reduce the effectiveness of udxa.

Ursonost can enhance intestinal absorption of cyclosporine. Therefore, in patients taking cyclosporine, it is necessary to control the concentration of this substance in the blood and, if necessary, change the dose.

In some cases, UDCA can reduce the absorption of ciprofloxacin.

There was a decrease in the maximum concentration (Cmax) of the calcium antagonist nitrendipine in the blood plasma and the area under the curve (AUC) while using it with UDCA. When interacting with dapsone, a decrease in the severity of the therapeutic effect of UDCA was noted.

These observations and the results of in vitro studies indicate the potential of UDCA to induce enzymes such as cytochrome P450 3A. But controlled clinical studies have shown that UDCA does not have a significant inductive effect on enzymes such as cytochrome P450 3A.

Estrogenic hormones and agents that reduce the concentration of cholesterol in the blood, such as clofibrate, can promote the formation of gallstones, have an effect opposite to that of UDCA, which is used to dissolve gallstones.

Overdose

In case of overdose, diarrhea is possible. other symptoms of overdose are unlikely, since the absorption of udxa decreases with increasing dose, so most of its amount is excreted in the feces.

If diarrhea occurs, the dose should be reduced, and if the diarrhea is persistent, the therapy should be discontinued.

There is no need for specific measures. Treatment for diarrhea is symptomatic, aimed at restoring fluid and electrolyte balance.

There are known cases of UDCA overdose when using the preparation at a dose of up to 4 g / day, but this dose did not have significant consequences.

If a high dose of UDCA is accidentally taken, it is recommended to take the usual measures, as for intoxication, or to prescribe cholestyramine to bind bile acids.

Additional information on special patient groups. Long-term therapy with high doses of UDCA (28–30 mg / kg / day) in patients with primary sclerosing cholangitis (use for unregistered indications) was associated with a higher incidence of serious adverse events.

Storage conditions

At a temperature not higher than 25 ° C.

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