Ursodeoxycholic Acid
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Pharmacological properties
a significant amount of ursodeoxycholic acid was found in human bile.
After oral administration, it reduces the saturation of bile cholesterol, inhibiting its absorption in the intestine and reducing the secretion of cholesterol in bile. Perhaps, due to the dispersion of cholesterol and the formation of liquid crystals, the gallstones gradually dissolve.
According to modern data, the effect of ursodeoxycholic acid in liver diseases and cholestasis is due to the relative replacement of lipophilic, similar to detergents of toxic bile acids, hydrophilic cytoprotective non-toxic ursodeoxycholic acid, an improvement in the secretory ability of hepatocytes and immunoregulatory processes.
Use in children
Cystic fibrosis. The use of ursodeoxycholic acid can reduce proliferation in the bile ducts, stop the progression of histological changes, and even eliminate hepatobiliary changes if therapy is started in the early stages of cystic fibrosis. For greater effectiveness, treatment with ursodeoxycholic acid should be started immediately after clarifying the diagnosis of cystic fibrosis.
Pharmacokinetics When administered orally, ursodeoxycholic acid is rapidly absorbed in the small and upper ileum by passive transport, and in the terminal ileum by active transport. The absorption rate is usually 60–80%. In the liver, bile acid undergoes almost complete conjugation with the amino acids glycine and taurine and is then excreted in the bile. The clearance of the first passage through the liver is up to 60%.
Depending on the daily dose and the underlying disorder or condition of the liver, the more hydrophilic ursodeoxycholic acid accumulates in the bile. At the same time, there is a relative decrease in the amount of other more lipophilic bile acids.
Under the influence of intestinal bacteria, partial degradation to 7-ketolitocholic and lithocholic acids occurs. Litocholic acid is hepatotoxic and causes damage to the liver parenchyma in some animal species. In humans, only a small amount is absorbed, which is sulfated in the liver and thus detoxified before being excreted with bile and, finally, with feces.
Biological T½ ursodeoxycholic acid is 3.5–5.8 days.
Indications
Dissolution of X-ray negative cholesterol gallstones no larger than 15 mm in diameter in patients with a functioning gallbladder, despite the presence of gallstones in it.
Treatment of biliary reflux gastritis.
Symptomatic treatment of primary biliary cirrhosis (PBC) in the absence of decompensated liver cirrhosis.
Treatment of hepatobiliary disorders in cystic fibrosis in children aged 6 to 18 years.
Application
For patients whose body weight is 47 kg or who have difficulty swallowing grinterol capsules, it is necessary to use ursodeoxycholic acid preparations in another dosage form.
For dissolving cholesterol gallstones
Approximately 10 mg of ursodeoxycholic acid / kg body weight (Table 1).
Table 1| Body weight | Number of capsules |
|---|---|
| ≤60 | 2 |
| 61–80 | 3 |
| 81–100 | 4 |
| ≥100 | 5 |
Capsules should be swallowed whole, washed down with water, 1 time per day in the evening before bedtime.
Capsules must be taken regularly.
The time required to dissolve gallstones is usually 6-24 months. If a decrease in gallstone size is not observed after 12 months of admission, treatment should be discontinued.
The success of treatment should be monitored every 6 months using ultrasound or X-ray examination. In addition, it should be checked whether calcification of stones has occurred over time. If this happens, treatment should be discontinued.
For the treatment of biliary reflux gastritis
1 capsule 250 mg 1 time per day with a sufficient amount of liquid in the evening before bedtime.
Usually the course of treatment is 10-14 days. The duration of the course of treatment depends on the condition of the patient, so the doctor must decide on the duration of treatment in each case individually.
For symptomatic treatment of PBC
The daily dose depends on body weight and varies from 3 to 7 capsules (14 ± 2 mg of ursodeoxycholic acid / kg body weight).
In the first 3 months of treatment, 250 mg capsules should be taken throughout the day, distributing the daily dose in 3 divided doses. With an improvement in liver function indicators, the dose can be taken 1 time per day in the evening.
table 2| Body weight | Daily dose
mg / kg body weight |
Capsules | |||
| First 3 months | Further | ||||
| Morning | Day | Evening | Evening (1 time per day) | ||
| 47–62 | 12–16 | 1 | 1 | 1 | 3 |
| 63–78 | 13–16 | 1 | 1 | 2 | 4 |
| 79–93 | 13–16 | 1 | 2 | 2 | 5 |
| 94–109 | 14–16 | 2 | 2 | 2 | 6 |
| ≥110 | 2 | 2 | 3 | 7 | |
Capsules should be swallowed whole with a liquid. It is necessary to observe the regularity of admission.
The duration of 250 mg capsules for PBC can be unlimited.
In patients with PBC, it is rare that clinical symptoms may worsen at the beginning of treatment, for example, itching may intensify. In this case, treatment should be continued, taking 1 capsule of 250 mg / day, and then gradually increase the dose (increasing the daily dose by 1 capsule every week) until the prescribed dosage regimen is reached.
Use in children
For children with cystic fibrosis aged 6–18 years, the dose is 20 mg / kg / day and is divided into 2–3 doses with a subsequent increase to 30 mg / kg / day if necessary.
Table 3| Body weight | Daily dose, mg / kg | Greenterol 250 mg hard capsules | ||
| Morning | Day | Evening | ||
| 20–29 | 17–25 | 1 | ‒ | 1 |
| 30–39 | 19–25 | 1 | 1 | 1 |
| 40–49 | 20–25 | 1 | 1 | 2 |
| 50–59 | 21–25 | 1 | 2 | 2 |
| 60–69 | 22–25 | 2 | 2 | 2 |
| 70–79 | 22–25 | 2 | 2 | 3 |
| 80–89 | 22–25 | 2 | 3 | 3 |
| 90–99 | 23–25 | 3 | 3 | 3 |
| 100–109 | 23–25 | 3 | 3 | 4 |
| ≥110 | 3 | 4 | 4 | |
Children
For the dissolution of cholesterol gallstones, treatment of biliary reflux gastritis and symptomatic treatment of PBC. There are no fundamental age restrictions for the use of the drug Greenterol in children, but if the body weight of the child is 47 kg and / or p
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2020-07-30
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