Ursodeoxycholic acid-Vertex, 250 mg capsules 100 pcs

Pharmacotherapeutic group: Hepatoprotective drug

ATC code: A05A02

Pharmacological properties

Pharmacodynamics

Indications

– dissolution of cholesterol gallstones;

– biliary reflux gastritis;

– primary biliary cirrhosis in the absence of signs of decompensation;

– chronic hepatitis of various genesis;

– primary sclerosing cholangitis;

– cystic fibrosis (cystic fibrosis);

– non-alcoholic steatohepatitis;

– alcoholic liver disease;

– biliary dyskinesia.

Active ingredient

Composition

One capsule contains:

the active substance: ursodeoxycholic acid – 250 mg;

excipients: Corn starch – 63 mg, povidone K-30 – 10 mg, colloidal silica – 5 mg, magnesium stearate – 2 mg;

Solid gelatin capsules: titanium dioxide – 2.0%; gelatin – up to 100%.

How to take, the dosage

Ingestion. Children and adults with body weight less than 47 kg are recommended to use ursodeoxycholic acid in the form of suspension.

Dissolution of cholesterol gallstones

The recommended dose of ursodeoxycholic acid depends on body weight and is 10 mg/kg/day (see Table 1).

Table 1 Calculation of daily number of capsules of the drug as a function of body weight

Table 1table border=”1″ cellspacing=”0″ cellpadding=”0″>

Body weight, kg

Number of capsules, pcs.

up to 60

td>

2

61-80

3

81-100

4

over 100

The drug should be taken daily in the evening before going to bed (capsules should not be chewed), with a small amount of liquid. The treatment period is 6-12 months.

In order to prevent recurrence of cholelithiasis it is recommended to take the drug for several months after the stones have dissolved.

The treatment of biliary reflux gastritis

1 capsule of the drug daily in the evening before going to bed (capsules are not chewed), with a small amount of water.

The course of treatment is from 10-14 days to 6 months, if necessary up to 2 years.

The treatment of primary biliary cirrhosis

The daily dose depends on the body weight and is from 3 to 7 capsules (about 14±2 mg/kg of ursodeoxycholic acid).

In the first 3 months of treatment, the use of the drug should be divided into several doses during the day. After the liver parameters improve, the daily dose can be taken 1 time in the evening.

The following regimen of the drug is recommended (Table 2).

Table 2

Regimen of drug administration depending on body weight

Body weight, (kg)

ursodeoxycholic acid capsules 250 mg

First 3 months of treatment

Afterwards

Morning

Day

Evening

Evening

(1 time per day)

47-62

1

1

1

3

63-78

1

2

4

79-93

1

2

2

5

94-109

2

2

6

Over 110

2

3

7

The capsules should be taken regularly, without chewing, with a small amount of liquid.

The use of the drug for treatment of primary biliary cirrhosis may be continued indefinitely. In patients with primary biliary cirrhosis in rare cases clinical symptoms may worsen at the beginning of treatment, for example, itching may become more frequent. In this case, treatment should be continued by taking 1 capsule daily and then the dose should be gradually increased (increasing the daily dose weekly by 1 capsule) until the recommended dosing regimen is reached again.

Symptomatic treatment of chronic hepatitis of various genesis

The daily dose is 10-15 mg/kg in 2-3 doses. Duration of treatment 6-12 months or more.

Primary sclerosing cholangitis

The daily dose is 12-15 mg/kg. If necessary, the dose may be increased to 20-30 mg/kg in 2-3 doses. The duration of therapy ranges from 6 months to several years (see section “Special Precautions”).

Mucoviscidosis (cystic fibrosis)

The daily dose is 20 mg/kg/day in 2-3 doses, with further increase to 30 mg/kg/day if necessary.

Table 3

Mode of administration of the drug according to body weight

table border=”1″ cellspacing=”0″ cellpadding=”0″>

Body weight (kg)

Daily dose (mg/kg body weight)

ursodeoxycholic acid capsules 250 mg

Morning

Interaction

Colestyramine, colestipol, and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce absorption of ursodeoxycholic acid in the intestine and thus reduce its absorption and effectiveness. If the use of drugs containing at least one of these substances is still necessary, they should be taken at least 2 hours before taking ursodeoxycholic acid.

Ursodeoxycholic acid can affect the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the physician should check the blood concentration of cyclosporine and, if necessary, adjust its dose.

Ursodeoxycholic acid may decrease absorption of ciprofloxacin.

In a clinical study involving healthy volunteers, concomitant use of ursodeoxycholic acid (500 mg/day) and rosuvastatin (20 mg/day) resulted in a slight increase in plasma levels of rosuvastatin. The clinical significance of this interaction, including for other statins, is unknown. In healthy volunteers ursodeoxycholic acid has been shown to decrease the maximum plasma concentration and the area under the pharmacokinetic curve of the slow calcium channel blocker – nitrendipine. In case of concomitant use of nitrendipine and ursodeoxycholic acid, close monitoring is recommended. It may be necessary to increase the dose of nitrendipine.

There have also been reports of interactions with dapsone, which reduced the therapeutic effect of the latter. These observations, along with data from in vitro experiments, suggest that ursodeoxycholic acid is capable of inducing enzymes of the cytochrome P450 3A system. However, in a planned interaction study with budesonide, which is a known cytochrome P450 3A substrate, no induction was noted.

Estrogenic hormones and blood cholesterol-lowering drugs, such as clofibrate, increase cholesterol secretion in the liver and therefore may stimulate gallstone formation, offsetting the effect of ursodeoxycholic acid, which is used to dissolve gallstones.

Special Instructions

The drug should be taken under medical supervision.

In the first 3 months of treatment, functional liver parameters: transaminases, alkaline phosphatase and gamma-glutamyl transpeptidase in blood plasma should be monitored every 4 weeks, and then every 3 months. Monitoring of these parameters allows early detection of liver dysfunction. This also applies to patients in the later stages of primary biliary cirrhosis. In addition, this allows us to quickly determine if a patient with primary biliary cirrhosis is responding to treatment.

When using the drug to dissolve cholesterol gallstones

. In order to evaluate the progress of treatment and for the purpose of timely detection of the signs of gallstones calcinosis depending on their size, the gallbladder should be visualized (oral cholecystography) with observation of darkening in standing and supine position (ultrasound examination) 6-10 months after the start of treatment.

If the gallbladder cannot be visualized on X-rays, as well as in cases of calcification of the stones, poor gallbladder contractility or frequent attacks of colic, the drug should not be used.

Patients taking ursodeoxycholic acid to dissolve gallstones should use effective non-hormonal methods of contraception, because hormonal contraceptives may increase gallstone formation (see sections Interaction with other medicinal products and Use during pregnancy and breast-feeding).

When treating patients in advanced stages of primary biliary cirrhosis

Cases of decompensation of liver cirrhosis were extremely rarely observed. After discontinuation of therapy, a partial reversal of decompensation manifestations was observed.

In patients with primary biliary cirrhosis in rare cases at the beginning of treatment it is possible to increase clinical symptoms, for example, itching may intensify. In this case, the dose of the drug should be reduced, and then gradually increased again, as described in the section “Dosage and administration”.

When used in patients with primary sclerosing cholangitis

Long-term therapy with high doses of ursodeoxycholic acid (28-30 mg/kg/day) in patients with this pathology may cause serious adverse events.

In patients with diarrhea, the drug dose should be reduced. Treatment should be discontinued in patients with persistent diarrhea.

The effect on the ability to drive vehicles, machinery Ursodeoxycholic acid has no or minimal effect on the ability to drive vehicles and mechanisms.

Synopsis

Solid gelatin capsules № 0 of white color. The content of the capsules is a mixture of powder and granules or compacted mass of white or almost white color.

Contraindications

– hypersensitivity to the components of the drug and other bile acids;

– X-ray-positive (with high calcium content) gallstones;

– impaired gallbladder contractility;

– blockage of biliary tract (blockage of common bile duct or vesicular duct);

– frequent episodes of biliary colic;

– acute inflammatory diseases of the gallbladder and bile ducts;

– decompensated cirrhosis of liver;

– expressed hepatic and/or renal failure;

– children under 3 years of age (not recommended for use in this dosage form).

Pediatric population

– unsuccessfully performed portoenterostomy or cases of failure to restore normal bile flow in children with biliary atresia.

Ursodeoxycholic acid has no age restrictions for use, but children under the age of 3 years are recommended to use the drug in the form of suspension, since there may be difficulty in swallowing the capsules.

Cautions for children > 3 years of age (may have difficulty swallowing the capsules).

Side effects

Classification of the frequency of side effects according to the recommendations of the World Health Organization (WHO):

very often ≥ 1/10;

often from ≥ 1/100 to < 1/10; infrequent from ≥ 1/1000 to < 1/100;

rarely from ≥ 1/10000 to < 1/1000;

very rarely < 1/10000, including individual reports;

frequency is unknown – it is not possible to determine the frequency of occurrence from the available data.

Gastrointestinal disorders:

often, loose stools or diarrhea;

very rarely, acute right upper abdominal pain (when treating primary biliary cirrhosis).

Liver and biliary tract disorders:

very rarely – calcification of gallstones, decompensation of liver cirrhosis, which disappears after discontinuation of the drug (in treatment of advanced stages of primary biliary cirrhosis).

Skin and subcutaneous tissue disorders:

very rarely – allergic reactions, including urticaria.

Overdose

In case of overdose, diarrhea is possible. As a rule, other symptoms of overdose are unlikely, since with increasing dose absorption of ursodeoxycholic acid decreases and, accordingly, more of it is excreted through the intestine. There is no need for specific measures in case of overdose. Treatment of the consequences of diarrhea is symptomatic, aimed at replenishing fluid volume and restoring electrolyte balance.

Pregnancy use

Pregnancy

The data on the use of ursodeoxycholic acid during pregnancy are limited or absent. Animal studies have shown reproductive toxicity in early pregnancy.

Ursodeoxycholic acid should not be used during pregnancy unless clearly necessary.

Fertility

According to animal studies, ursodeoxycholic acid has no effect on fertility. There are no data on the effect of treatment with ursodeoxycholic acid on fertility in humans.

The use of the drug by women of childbearing age is possible only if reliable contraception methods are used. It is recommended to use non-hormonal contraceptives, or oral contraceptives with low estrogen content. However, patients taking ursodeoxycholic acid to dissolve gallstones should use effective non-hormonal contraceptives, as hormonal oral contraceptives may increase gallstone formation. Possible pregnancy should be excluded before the beginning of treatment.

Breastfeeding

According to several documented cases, the level of ursodeoxycholic acid in breast milk in women is very low, and therefore adverse reactions in breastfed children are not expected.

Similarities