Kansalazin^® Prolong (Tablets) Instructions for Use

Marketing Authorization Holder

Kronopharm, LLC (Russia)

Manufactured By

Canonpharma Production, CJS (Russia)

Or

PharmVILAR NPO, LLC (Russia)

ATC Code

A07EC02 (Mesalazine)

Active Substance

Mesalazine (Rec.INN registered by WHO)

Dosage Form

Kansalazin® Prolong

Prolonged-release tablets 500 mg

Dosage Form, Packaging, and Composition

Prolonged-release tablets

10 pcs. – blister packs (10 pcs.) – cardboard packs (100 pcs.) – By prescription
10 pcs. – blister packs (5 pcs.) – cardboard packs (50 pcs.) – By prescription
15 pcs. – blister packs (2 pcs.) – cardboard packs (30 pcs.) – By prescription
15 pcs. – blister packs (4 pcs.) – cardboard packs (60 pcs.) – By prescription
15 pcs. – blister packs (6 pcs.) – cardboard packs (90 pcs.) – By prescription

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 site 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, and phagocytosis of neutrophils, as well as immunoglobulin secretion by lymphocytes. Mesalazine possesses 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. T_1/2 is 0.5-2 h. Mesalazine is excreted in the urine, predominantly in the acetylated form.

Indications

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

For rectal administration: treatment of ulcerative colitis involving the distal parts of the rectum.

ICD codes

Dosage Regimen

Administer orally or rectally as directed by a physician.

Establish the dose and treatment regimen individually based on indication, disease activity, and patient age.

For adult patients with ulcerative colitis, the typical oral dosage for acute exacerbations is 1.5 to 3 grams of mesalazine per day, divided into two or three doses.

For maintenance of remission in ulcerative colitis, administer 1.5 grams per day in divided doses.

For adult patients with Crohn’s disease (ileocolitis), the typical oral dosage is 3 to 4 grams per day in divided doses.

Do not exceed a maximum daily dose of 4 grams.

Swallow the prolonged-release tablets whole with a sufficient amount of liquid; do not crush or chew.

Take tablets with meals to reduce potential gastrointestinal adverse effects.

For rectal administration in distal ulcerative colitis, use the appropriate rectal formulation as prescribed; dosage depends on the extent of mucosal involvement.

Adjust the dosage with caution in patients with renal or hepatic impairment; contraindicated in severe impairment.

Monitor blood counts, renal function, and liver enzymes before and 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 tear production.

Contraindications

Hypersensitivity to salicylates; blood diseases, severe impairment of liver and/or kidney function, 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 discontinuing breastfeeding should be considered, 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 impairment.

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

Dosage 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 levels should be monitored. In patients who are “slow acetylators,” the risk of adverse 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.