Choludexan-Reb capsules 300mg №10×6

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Choludexan-Reb caps. 300mg per cont. cell pack. No. 10×6
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Capsules hard gelatinous with a pink body and a red-brown cap. The main active ingredient Ursodeoxycholic acid Release form Capsules Dosage 300 mg Pharmacological properties Pharmacodynamics A small amount of ursodeoxycholic acid is found in human bile. After oral administration, the drug reduces the saturation of bile with cholesterol by inhibiting the absorption of cholesterol in the intestine and by reducing the secretion of cholesterol into bile. Presumably, as a result of the dispersion of cholesterol and the formation of liquid crystals, there is a gradual dissolution of cholesterol stones. According to generally accepted data, the effect of ursodeoxycholic acid on liver diseases and cholestatic diseases is achieved by an equal exchange of lipophilic, detergent-like toxic bile acids for hydrophilic, cytoprotective, non-toxic ursodeoxycholic acid, which leads to an improvement in the secretory ability of hepatocytes and to immunoregulatory processes. Ursodeoxycholic acid has a direct cytoprotective membrane-stabilizing effect on hepatocytes, cholangiocytes and epithelial cells of the gastrointestinal tract. It forms double molecules that interact with lipophilic membrane structures, integrate into cell membranes and stabilize them. Protects liver cells and bile duct cells from damaging factors, makes them immune to the action of cytotoxic micelles. It has immunomodulatory activity, reduces the severity of immunopathological reactions in the liver by reducing the expression of histocompatibility antigens HLA-1 on hepatocytes and HLA-2 on bile duct cells and reducing the impact of immunoglobulins (primarily IgM). Reduces the formation of cytotoxic T-lymphocytes. Stimulating exocytosis in hepatocytes during cholestasis by activating Ca2+-dependent α-protein kinase, ursodeoxycholic acid reduces the concentration of bile acids toxic to hepatocytes, induces choleresis with a high content of bicarbonates, which leads to an increase in the passage of bile. By reducing the synthesis of cholesterol in the liver, as well as its absorption in the intestine, ursodeoxycholic acid reduces the lithogenicity of bile, lowers the cholate-cholesterol index, promotes the dissolution of cholesterol calculi and prevents the formation of new ones. For the successful dissolution of gallstones, it is necessary that the stones be purely cholesterol, their size does not exceed 15-20 mm, and the gallbladder (no more than half filled with stones) and the bile ducts fully retain their function. Ursodeoxycholic acid significantly delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis, and alcoholic steatohepatitis. Reduces the risk of developing esophageal varicose veins. Regulates the processes of apoptosis (aging and cell death) disturbed in the pathology of the liver and other organs. The use of ursodeoxycholic acid inhibits the growth of colon cancer cells. Pharmacokinetics After oral administration, ursodeoxycholic acid is absorbed in the small intestine by passive diffusion, and in the ileum by active transport. The maximum plasma concentration is reached within 30-60 minutes after ingestion, the level of adsorption is 60-80%. With regular use of the drug, ursodeoxycholic acid becomes the main bile acid in blood plasma, accounting for about 48% of the total amount of bile acids in the blood. Protein binding – 96-99%. The therapeutic effect of the drug depends mainly on the concentration of ursodeoxycholic acid in bile, and not in blood plasma. The maximum concentration of ursodeoxycholic acid in bile is noted at a daily dose of the drug 10-14 mg/kg of body weight. With a further increase in the dose, the concentration of ursodeoxycholic acid in bile does not increase. Ursodeoxycholic acid crosses the placental barrier. Approximately 60% of an ingested dose of a drug undergoes a “first pass effect” through the liver. In the liver, ursodeoxycholic acid is conjugated with glycine or taurine and then secreted into the bile. Ursodeoxycholic acid conjugates are absorbed in the small intestine through passive and active mechanisms. A small amount of non-absorbed ursodeoxycholic acid is cleaved by bacteria (7-dehydroxylation) to lithocholic acid, which is partially absorbed from the colon, sulfated in the liver and rapidly excreted in the form of sulfotylocholylglycine or sulfotylcholyltaurine conjugates. Ursodeoxycholic acid is excreted mainly with feces. When used in large doses, the level of excretion of ursodeoxycholic acid in the urine increases, although this value remains insignificant (less than 1%), except in cases of severe cholestatic liver damage. The half-life of ursodeoxycholic acid is 3.5-5.8 days. Indications for use Dissolution of cholesterol gallstones. Cholesterol stones should not appear as opacities on radiographs and should not exceed 15 mm in diameter. Despite the presence of stones, gallbladder function should not be impaired; treatment of gastritis with bile reflux; symptomatic treatment of primary biliary cirrhosis (PBC) in the absence of signs of decompensation. Dosage and administration The capsule is swallowed whole, without chewing, with a sufficient amount of liquid (it is possible with food or a light snack). There are no age restrictions for taking Choludexan-Reb 300 mg capsules, but patients weighing less than 47 kg or who find it difficult to swallow capsules are recommended to prescribe ursodeoxycholic acid in the form of an oral suspension. To dissolve cholesterol gallstones – approximately 10 mg ursodeoxycholic acid / kg body weight. Capsules should be swallowed whole with water, 1 time per day in the evening before bedtime. Capsules should be taken regularly. The time required for gallstones to dissolve is usually 6-24 months. If a decrease in the size of gallstones is not observed after 12 months of administration, therapy should not be continued. The success of the treatment should be checked every 6 months by ultrasound or X-ray. With the help of additional studies, it is necessary to check whether stones have calcified over time. If this happens, treatment should be discontinued. Gastritis with bile reflux – 300 mg of the drug is prescribed at bedtime. The course of treatment is usually 10-14 days. The duration of treatment depends on the condition of the patient. The doctor must decide on the duration of treatment in each case individually. In the symptomatic treatment of primary biliary cirrhosis of the liver (PBC), the daily dose depends on body weight and is determined at the rate of 14 ± 2 mg of ursodeoxycholic acid per kg of body weight. In the first 3 months of treatment, Choludexan-Reb should be taken by dividing the daily dose into 3 doses (morning, noon, evening). With improvement in liver function, the daily dose can be taken 1 time in the evening. It is necessary to control the regularity of admission. The use of the drug Choludexan-Reb in PBC can be unlimited in time. In rare cases, in patients with this disease, clinical symptoms may worsen at the beginning of treatment, for example, itching may increase. In this case, it is recommended to continue treatment by taking 1 capsule per day, gradually increasing the dose (by 1 capsule weekly) until the recommended dosage regimen is reached. Use in the elderly: There are no data on the need for dose adjustment in people of this age group. However, precautions must be taken during treatment. Children: despite the fact that there are no fundamental age restrictions for the use of ursodeoxycholic acid, capsules are not recommended for children weighing less than 47 kg and / or under 6 years of age due to possible swallowing difficulties. If the child weighs less than 47 kg or has difficulty swallowing, it is recommended to use ursodeoxycholic acid in the form of a suspension. Use during pregnancy and lactation The drug is contraindicated in the first trimester of pregnancy. Use in the II and III trimesters of pregnancy is possible only if the benefit to the mother outweighs the potential risk to the fetus (adequate, strictly controlled studies of the use of ursodeoxycholic acid in pregnant women have not been conducted). There are currently no data on the excretion of ursodeoxycholic acid in breast milk. If it is necessary to prescribe a drug during lactation, the issue of stopping breastfeeding should be resolved. The decision to use Choludexan-Reb is made by the doctor. Precautions Before starting treatment, females should ensure that they are not pregnant. Choludexan-Reb should be taken under medical supervision. During the first three months of treatment, liver function tests for ACT (SGOT), ALT (SGPT), and y-GT should be monitored every 4 weeks and then every 3 months. When used to dissolve cholesterol gallstones In order to evaluate progress in treatment and to timely detect signs of calcification of stones, depending on the size of the stones, the gallbladder should be visualized (oral cholecystography) with examination of opacities in the standing position and lying on the back (ultrasound) through 6-10 months after the start of treatment. If the gallbladder cannot be visualized on x-rays or in cases of calcification of stones, weak contractility of the gallbladder or frequent bouts of colic, Choludexan-Reb should not be used. Patients taking Choludexan-Reb to dissolve stones are advised to use non-hormonal methods of contraception, as hormonal contraceptives increase the likelihood of gallstones. In the treatment of primary biliary cirrhosis In very rare cases, decompensation of liver cirrhosis was observed, which partially regressed after discontinuation of treatment. In rare cases, worsening of clinical symptoms at the beginning of treatment, for example, increased itching, is possible. In this case, the dose adjustment described in the section “Method of application and dosage” should be carried out. In the event of diarrhea, the dose of the drug should be reduced, with persistent diarrhea, treatment should be discontinued. Use in pediatrics Due to the fact that Choludexan-Reb is available in the form of 300 mg capsules, the drug is not used in children under the age of 6 years (less than 20 kg of weight). Influence on the ability to drive vehicles and work with mechanisms Choludexan-Reb does not affect the ability to drive a car and perform work that requires a high speed of psychomotor reactions. Interaction with other drugs Ursodeoxycholic acid reduces the maximum plasma concentration (Cmax) and the area under the curve (AUC) of the calcium antagonist nitrendipine. Based on this, as well as the only reported interaction with the substance dapsone (reduced therapeutic effect) and from in vitro studies, it can be assumed that ursodeoxycholic acid induces the activity of cytochrome P4503A4, which metabolizes the drug. With the simultaneous use of drugs that are metabolized with the participation of this enzyme, care must be taken and it should be borne in mind that dose adjustment may be required. Antacids containing aluminum ions and ion exchange resins (cholestyramine) reduce drug absorption. If it is necessary to use a medicinal product containing one of these substances, then it must be taken at least 2 hours before or after taking Choludexan-Reb capsules. The drug Choludexan-Reb may increase the absorption of ciclosporin from the intestines. In patients receiving cyclosporine therapy, blood concentrations of this substance should be monitored by a physician, and the dose of cyclosporine should be adjusted. In some cases, the drug Choludexan-Reb may reduce the absorption of ciprofloxacin. Lipid-lowering agents (especially clofibrate), estrogens, neomycin, or progestins increase bile saturation with cholesterol and may decrease the drug’s ability to dissolve cholesterol gallstones. Contraindications hypersensitivity to the active substance or other ingredients that make up this medicinal product; X-ray positive (high in calcium) gallstones; non-functioning gallbladder; obstruction of the bile ducts, frequent biliary colic; acute inflammatory diseases of the gallbladder, bile ducts and intestines; cirrhosis of the liver in the stage of decompensation; severe hepatic and / or renal failure; pancreatitis; first trimester of pregnancy; children’s age up to 6 years. CompositionCapsule contains: Active substance: ursodeoxycholic acid 300 mg. Excipients: corn starch, anhydrous colloidal silicon dioxide, magnesium stearate, purified water. The composition of the capsule shell: titanium dioxide (E171), iron oxide red (E172), gelatin. Overdose In case of overdose, diarrhea may occur. In general, overdose is unlikely because the absorption of ursodeoxycholic acid decreases with increasing dose, and it is mainly excreted in the feces. If diarrhea occurs, the dose should be reduced, and if diarrhea persists, the use of ursodeoxycholic acid should be discontinued. The effects of diarrhea should be treated symptomatically while maintaining fluid and electrolyte balance. Side effects The side effect frequency parameters used below are defined as follows: very often (? 1/10), often (from ? 1/100 to < 1/10), infrequently (from ? 1/1000 to < 1/100), rarely ( from ? 1/10000 to < 1/1000), very rarely (< 1/10000). Gastrointestinal Disorders: Reports of pasty stools or diarrhea are very common in clinical studies. Very rarely, during the treatment of primary biliary cirrhosis, severe pain occurred in the abdomen, on the right side. Liver and biliary tract disorders: Calcification of stones may very rarely occur during treatment with ursodeoxycholic acid. During the treatment of advanced stages of primary biliary cirrhosis, decompensation of cirrhosis of the liver was very rarely observed, which disappears after discontinuation of the drug. Hypersensitivity reactions: in very rare cases, an allergic rash (urticaria) may occur. Storage conditionsStore at a temperature not exceeding 25°C. Keep out of the reach of children! Buy Choludexan-Reb capsules 300mg №10x6 Price for Choludexan-Reb capsules 300mg №10x6