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Kansalazine® (Tablets, Suppositories) Instructions for Use

ATC Code

A07EC02 (Mesalazine)

Active Substance

Mesalazine (Rec.INN WHO registered)

Clinical-Pharmacological Group

Drug with anti-inflammatory action used for the treatment of Crohn’s disease and UC

Pharmacotherapeutic Group

Antidiarrheals, intestinal anti-inflammatory/antimicrobial agents; intestinal anti-inflammatory agents; aminosalicylic acid and similar agents

Pharmacological Action

Anti-inflammatory agent with a predominant localization of action in the intestine. Mesalazine (5-aminosalicylic acid) inhibits the activity of neutrophil lipoxygenase and the synthesis of arachidonic acid metabolites (prostaglandins and leukotrienes), which are mediators of inflammation.

It inhibits the migration, degranulation, phagocytosis of neutrophils, as well as immunoglobulin secretion by lymphocytes. Mesalazine has antioxidant properties by binding to free oxygen radicals.

Pharmacokinetics

After oral administration, Mesalazine is slowly released from the dosage form in the distal part of the small intestine and in the large intestine.

Plasma protein binding is 43%. It is metabolized in the intestinal mucosa and in the liver to form N-acetyl-5-ASA. T1/2 is 0.5-2 hours. Mesalazine is excreted in the urine, mainly in the acetylated form.

Indications

For oral administration: treatment of exacerbations and prevention of relapses in ulcerative colitis and Crohn’s disease.

Rectally: treatment of ulcerative colitis involving the distal parts of the rectum.

ICD codes

ICD-10 code Indication
K50 Crohn’s disease [regional enteritis]
K51 Ulcerative colitis
ICD-11 code Indication
DD70.Z Crohn’s disease, unspecified location
DD71.Z Ulcerative colitis, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Determine the dosage and route of administration (oral or rectal) based on the disease indication, its severity, and localization.

For oral administration with tablets, swallow whole with a sufficient amount of water. Do not crush or chew the tablets.

For the treatment of acute exacerbations of ulcerative colitis, administer a total daily dose of 3-4 grams of mesalazine, divided into 3-4 equal doses.

For the maintenance of remission in ulcerative colitis, administer a total daily dose of 1.5-2 grams, divided into 2-3 doses.

For the treatment of Crohn’s disease, follow the dosage prescribed for ulcerative colitis exacerbations.

For rectal administration with suppositories, use for proctitis or inflammation limited to the rectum.

Insert one 500 mg suppository into the rectum 2-3 times per day. Administer after bowel evacuation.

For maintenance therapy with suppositories, use one 500 mg suppository 2 times per day.

Adjust the dosage for pediatric patients aged 3 years and older based on body weight, typically 20-30 mg/kg/day in divided doses.

For geriatric patients or those with mild to moderate renal or hepatic impairment, use the standard dose with increased monitoring. Do not use in severe impairment.

Regularly assess patient response and tolerance. Perform blood tests and monitor renal function before treatment and periodically during therapy.

Adverse Reactions

From the digestive system diarrhea, nausea, vomiting, heartburn, abdominal pain, loss of appetite, dry mouth, stomatitis, increased activity of liver enzymes.

From the nervous system headache, depression, dizziness, sleep disorders, paresthesia, tremor, tinnitus.

Allergic reactions skin rash, itching, erythema.

From the cardiovascular system palpitations, tachycardia, arterial hypertension or hypotension, chest pain, shortness of breath.

From the urinary system proteinuria, hematuria, crystalluria, oliguria, anuria.

From the hematopoietic system anemia, leukopenia, agranulocytosis, thrombocytopenia; hypoprothrombinemia.

Other alopecia, decreased production of tear fluid.

Contraindications

Hypersensitivity to salicylates; blood diseases, severe liver and/or kidney dysfunction, gastric or duodenal ulcer in the acute phase, blood clotting disorders.

Contraindicated in children under 3 years of age; in children and adolescents from 3 to 18 years of age, use is contraindicated depending on the dosage form used.

With caution

Liver and kidney diseases, glucose-6-phosphate dehydrogenase deficiency, allergic diseases and predisposition to them; diseases predisposing to the development of myo- and pericarditis; atopic dermatitis, atopic eczema.

Use in Pregnancy and Lactation

In the first trimester of pregnancy, use is possible only for strict indications. If the individual course of the disease allows, mesalazine intake should be discontinued in the last 2-4 weeks of pregnancy.

If it is necessary to use during lactation, the issue of stopping breastfeeding should be decided, due to the lack of sufficient clinical experience with the use of mesalazine in this category of patients.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction.

Use with caution in liver diseases.

Use in Renal Impairment

Contraindicated in severe renal dysfunction.

Use with caution in kidney diseases.

Pediatric Use

Contraindicated in children under 3 years of age; in children and adolescents from 3 to 18 years of age, use is contraindicated depending on the dosage form used.

Geriatric Use

Dose adjustment is not required.

Special Precautions

Before starting treatment, and then monthly during the first 3 months of treatment, peripheral blood count, liver function, and blood urea and creatinine concentrations should be monitored. In patients who are “slow acetylators”, the risk of side effects is increased.

Organic or functional obstruction of the upper gastrointestinal tract may contribute to a delayed action of mesalazine when taken orally.

Drug Interactions

With simultaneous use of mesalazine with azathioprine, mercaptopurine, the toxicity of azathioprine and mercaptopurine increases; with warfarin – a case of decreased effectiveness of warfarin has been described.

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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Kronopharm, LLC (Russia)

Manufactured By

Altpharm LLC (Russia)

Dosage Form

Bottle Rx Icon Kansalazine® Rectal suppositories 500 mg: 10 or 30 pcs.

Dosage Form, Packaging, and Composition

Rectal suppositories torpedo-shaped, from almost white to light gray in color, with a possible light pink tint.

1 supp.
Mesalazine 500 mg

Excipients : Hard fat Witepsol H-15 – 1680 mg, docusate sodium – 2 mg, cetyl alcohol – 18 mg.

5 pcs. – contour cell packaging (2) – cardboard boxes.
5 pcs. – contour cell packaging (6) – cardboard boxes.

Marketing Authorization Holder

Kronopharm, LLC (Russia)

Manufactured By

Canonpharma Production, CJS (Russia)

Dosage Form

Bottle Rx Icon Kansalazine® Prolonged-release tablets 500 mg: 30, 50, 60, 90 or 100 pcs.

Dosage Form, Packaging, and Composition

Prolonged-release tablets round, biconvex, from almost white with a grayish tint to light brown in color with inclusions.

1 tab.
Mesalazine 500 mg

Excipients : calcium hydrogen phosphate dihydrate – 28 mg, copovidone – 37 mg, colloidal silicon dioxide – 6 mg, magnesium stearate – 4 mg, sodium alginate – 42 mg, microcrystalline cellulose – 113 mg.

10 pcs. – contour cell packaging (5) – cardboard boxes.
10 pcs. – contour cell packaging (10) – cardboard boxes.
15 pcs. – contour cell packaging (2) – cardboard boxes.
15 pcs. – contour cell packaging (4) – cardboard boxes.
15 pcs. – contour cell packaging (6) – cardboard boxes.

Marketing Authorization Holder

Kronopharm, LLC (Russia)

Manufactured By

Canonpharma Production, CJS (Russia)

Dosage Form

Bottle Rx Icon Kansalazine® Enteric-coated film-coated tablets, 500 mg: 50 or 100 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets yellow, oval, biconvex; on the cross section – from almost white with a grayish tint to light brown in color with inclusions.

1 tab.
Mesalazine 500 mg

Excipients : glycine – 10 mg, hypromellose (hydroxypropyl methylcellulose) – 2 mg, colloidal silicon dioxide – 5 mg, croscarmellose sodium – 10 mg, magnesium stearate – 5 mg, anhydrous sodium carbonate – 80 mg, povidone K30 – 20 mg, microcrystalline cellulose – 83 mg.

Film coating composition: Acryl-Eze Yellow (93O220009) – 93.818 mg, including: methacrylic acid and ethyl acrylate copolymer [1:1] – 37.5272 mg, yellow iron oxide dye – 2.8182 mg, colloidal silicon dioxide – 1.1712 mg, sodium bicarbonate – 1.1224 mg, sodium lauryl sulfate – 0.4758 mg, talc – 34.953 mg, titanium dioxide – 11.2606 mg, triethyl citrate – 4.5018 mg, methacrylic acid and ethyl acrylate copolymer [1:1] (Kollicoat MAE100P) – 28.182 mg.

10 pcs. – contour cell packaging (5) – cardboard boxes.
10 pcs. – contour cell packaging (10) – cardboard boxes.

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