Cholestenorm (Tablets) Instructions for Use

Marketing Authorization Holder

Natur Produkt France (France)

ATC Code

C10AB02 (Bezafibrate)

Active Substance

Bezafibrate

Dosage Form

Cholestenorm

Tablets 200 mg: 50 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – blister packs (5) – cartons.

Clinical-Pharmacological Group

Hypolipidemic agent

Pharmacotherapeutic Group

Hypolipidemic agent – fibrate

Pharmacological Action

Hypolipidemic agent. It suppresses the synthesis of cholesterol and promotes the physiological breakdown of atherogenic cholesterol and LDL, and suppresses the synthesis of triglycerides.

By activating hepatic and extrahepatic lipoprotein lipase, it accelerates the process of breakdown of triglyceride-rich lipoproteins and their removal from plasma.

It increases glucose utilization, improves blood flow, and by acting on the thrombogenic factor, reduces the risk of thrombosis.

It reduces elevated fibrinogen levels, decreases platelet aggregation and blood viscosity.

Pharmacokinetics

After oral administration, Bezafibrate is well absorbed from the gastrointestinal tract. Plasma protein binding is 95%.

The plasma T_1/2 is about 1-2 hours. The majority of the dose is excreted in the urine, about 50% as unchanged substance, the rest as metabolites, including 20% glucuronides.

It is detected in small amounts in feces. Excretion may be enhanced by forced diuresis. It is not subject to dialysis.

In patients with renal failure, an increase in the T_1/2 of bezafibrate is possible.

Indications

Hyperlipoproteinemias types III, IV, and V that are not corrected by special diet and physical exercise, including in obesity, diabetes mellitus.

ICD codes

Dosage Regimen

Administer the tablets orally.

The standard adult dosage is 200 mg three times daily.

Take tablets with a sufficient amount of water during or after a meal.

This is a long-term treatment; adhere to the prescribed regimen consistently.

After achieving the desired therapeutic lipid level, the maintenance dose may be reduced to 400 mg per day, administered as 200 mg twice daily.

Do not adjust the dosage without medical supervision.

In patients with renal impairment, dosage adjustment is necessary; the maximum dose is 400 mg per day.

For severe renal impairment (creatinine clearance below 15 mL/min), this medication is contraindicated.

Regularly monitor serum lipid levels, liver function tests, and complete blood count during therapy.

If a treatment course is interrupted, a repeat course may be initiated under a physician’s guidance based on clinical indicators.

Adverse Reactions

From the digestive system: nausea, anorexia, feeling of heaviness in the epigastrium are possible; rarely – increased activity of liver transaminases, increased lithogenic index of bile.

From the hematopoietic system: anemia, leukopenia.

From the musculoskeletal system: myalgia, myopathy with rigidity of large muscle groups, rhabdomyolysis.

Other: allergic reactions.

Contraindications

Liver diseases (except for fatty degeneration), gallbladder diseases, severe renal impairment, pregnancy, lactation.

Use in Pregnancy and Lactation

Contraindicated: pregnancy, lactation.

Use in Hepatic Impairment

Contraindicated: liver diseases (except for fatty degeneration).

Use in Renal Impairment

Contraindicated: severe renal impairment.

Pediatric Use

Bezafibrate should be used with caution during the growth period.

Special Precautions

Bezafibrate should be used with caution during the growth period, as well as in patients with a history of erosive-ulcerative lesions of the gastrointestinal tract.

During treatment, it is necessary to strictly adhere to a diet; the composition of blood lipoproteins, functions of the gallbladder, liver, pancreas, and peripheral blood picture should be regularly monitored.

Drug Interactions

With simultaneous use, Bezafibrate enhances the effects of indirect anticoagulants.

With simultaneous use with HMG-CoA reductase inhibitors, the risk of developing rhabdomyolysis increases.

With simultaneous use with cyclosporine, the plasma concentration of the latter increases and the risk of nephrotoxicity increases.

Fibrates are capable of displacing a number of drugs from their plasma protein binding sites, including hypoglycemic agents – sulfonylurea derivatives (including tolbutamide), phenytoin; in patients with hypoalbuminemia – furosemide.

The interaction with hypoglycemic agents is complex: Bezafibrate impairs glucose tolerance in patients with diabetes mellitus. Against the background of bezafibrate therapy, dose adjustment of the hypoglycemic drug is required.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.