Exhol capsules 250mg, 100pcs

Composition

1 capsule contains:

Active ingredient:

ursodeoxycholic acid 250 mg;

excipients:

colloidal silicon dioxide (aerosil A -200 or A -300),

calcium hydrophosphate dihydrate,

magnesium stearate,

povidone (plasdon K-90 or collidone 90 F),

lactose monohydrate (milk sugar);

composition of solid gelatin capsule:

body – titanium dioxide,

gelatin;

lid-titanium dioxide,

gelatin,

indigo carmine.

Pharmacological action

Pharmaceutical group:

hepatoprotective agent.

Pharmaceutical action:

 Exhol is a hepatoprotective agent that has a choleretic effect.

Reduces the synthesis of cholesterol in the liver, its absorption in the intestines and concentration in bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and excretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids in it; causes increased gastric and pancreatic secretion, increases the activity of lipase, has a hypoglycemic effect.

Causes partial or complete dissolution of cholesterol stones with enteral application, reduces the saturation of bile with cholesterol, which contributes to the mobilization of cholesterol from gallstones.

It has an immunomodulatory effect, affects immunological reactions in the liver: it reduces the expression of certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, the formation of interleukin -2, and reduces the number of eosinophils.

Pharmacokinetics:

Absorption from the small intestine is high (about 90%). Penetrates the placental barrier. The maximum concentration (Cmax) when taking 50 mg orally after 30,60, and 90 minutes is 3.8,5.5, and 3.7 mmol/l, respectively. The time to reach the maximum concentration (TMAX) is 1-3 hours. The connection with plasma proteins is high.

It is metabolized in the liver (clearance during “primary passage” through the liver) to taurine and glycine conjugates. The resulting conjugates are secreted into the bile. It is excreted by 50-70% through the intestines. A small amount of unabsorbed ursodeoxycholic acid enters the large intestine, where it is broken down by bacteria (7-dehydroxylation); the resulting litocholic acid is partially absorbed from the colon, but is sulfated in the liver and is quickly excreted as a sulfolitocholylglycine or sulfolitocholyltaurine conjugate.

Indications

Primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy), dissolution of small and medium cholesterol stones with a functioning gallbladder, biliary reflux gastritis.

Contraindications

• Hypersensitivity,
• roentgenologically (with a high content of CA 2+) gall stones,
• non-functioning gall bladder,
• bile, gastrointestinal fistula,
• chronic hepatitis,
• inflammatory diseases of the small and large intestine,
• acute cholangitis,
• liver and/or kidney failure,
• pancreatitis,
• obstruction of the biliary tract,
• acute infectious diseases of the gallbladder and bile ducts,
• empyema of the gall bladder,
• pregnancy,
• lactation,
• children’s age.

Side effects

• Back pain,
• diarrhea (may be dose-dependent),
• abdominal pain,
• calcification of gallstones,
• increased activity of “liver” transaminases,
• alopecia,
• constipation,
• dizziness,
• nausea,
• exacerbation of previously existing psoriasis,
• vomiting,
• allergic reactions.

Interaction

Antacids containing Al3+ and ion exchange resins (colestyramine) reduce absorption.

Lipid-lowering medications (especially clofibrate), estrogens, neomycin, or progestins increase bile saturation with cholesterol and may reduce the ability to dissolve cholesterol bile stones.

How to take, course of use and dosage

Exhol is taken orally.

To dissolve cholesterol gallstones, the average daily dose is 10 mg / kg. The course of treatment is 6-12 months. To prevent the re-formation of stones, it is recommended to take the drug for several more months after the dissolution of the stones.

For biliary reflux gastritis, the dose is 250 mg once a day. The course of treatment is from 10-14 days to 6 months, if necessary-up to 2 years.

Symptomatic treatment of primary biliary cirrhosis: daily dose – 10-15 mg / kg. Capsules are taken in the evening, without chewing, with a small amount of water. Patients with a body weight of less than 34 kg are recommended to take the drug in suspension.

Overdose

No cases of overdose were detected.

In case of overdose, symptomatic treatment is performed.

Special instructions

For successful dissolution, it is necessary that the stones are pure cholesterol, no more than 15-20 mm in size, the gallbladder is filled with stones no more than half, and the biliary tract completely retains its function. When prescribing for the purpose of dissolving gallstones, it is necessary to monitor the activity of “hepatic” transaminases and alkaline phosphatase( ALP), gamma-glutamine transferase (GGT), and bilirubin concentration. Cholecystography should be performed every 4 weeks in the first 3 months of treatment, and then every 3 months. Monitoring the effectiveness of treatment should be performed every 6 months during ultrasound during the first year of therapy.

If elevated indicators persist, the drug should be discontinued. After the calculus is completely dissolved, it is recommended to continue the application for at least 3 months, in order to promote the dissolution of calculus residues, the size of which is too small to detect.

If there is no partial dissolution of the calculus within 6-12 months after the start of therapy, it is unlikely that the treatment will be effective.

Detection of an unvisualized gallbladder during treatment is an indication that the calculus has not completely dissolved and treatment should be discontinued.

Composition

Capsule Form of production

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Description

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

for Reflux esophagitis, Liver damage, Alcoholism, Hepatitis, Cirrhosis of the liver, Biliary Dyskinesia, Cholelithiasis