Ulcolfry^® (Tablets) Instructions for Use

Marketing Authorization Holder

Dr. Reddy’s Laboratories Ltd. (India)

ATC Code

A07EC02 (Mesalazine)

Active Substance

Mesalazine (Rec.INN registered by WHO)

Dosage Form

Ulcolfry®

Extended-release tablets, enteric-coated, 1.2 g: 60 or 120 pcs.

Dosage Form, Packaging, and Composition

Extended-release tablets, enteric-coated from brown to reddish-brown, biconvex, capsule-shaped; on cross-section – a core from white to almost white.

Excipients: hypromellose – 46 mg, carmellose sodium – 41 mg, microcrystalline cellulose – 26 mg, crospovidone – 22 mg, colloidal silicon dioxide – 22 mg, magnesium stearate – 10 mg.

Enteric coating composition methacrylic acid and methyl methacrylate copolymer [1:1] – 49.72 mg, methacrylic acid and methyl methacrylate copolymer [1:2] – 16.58 mg, talc – 11.88 mg, diacetylated monoglycerides – 9.00 mg, titanium dioxide (E171) – 3.53 mg, macrogol 6000 – 2.09 mg, red iron oxide dye (E172) – 2.20 mg;
polishing materials macrogol 6000 – 3.00 mg.

10 pcs. – blisters (6) – cardboard packs.
10 pcs. – blisters (12) – cardboard packs.

Clinical-Pharmacological Group

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

Pharmacotherapeutic Group

Intestinal antimicrobial and anti-inflammatory agent

Pharmacological Action

An 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, 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.

T_1/2 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.

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

ICD codes

Dosage Regimen

Administer orally or rectally.

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

For oral administration of Ulcolfry^® extended-release tablets, swallow tablets whole with a sufficient amount of liquid; do not crush or chew.

For active ulcerative colitis, the usual adult dose is 2.4-4.8 g of mesalazine per day, administered in divided doses.

For the maintenance of remission of ulcerative colitis, the usual adult dose is 1.2-2.4 g per day.

For active Crohn’s disease affecting the ileum and/or colon, the usual adult dose is up to 4.8 g per day in divided doses.

For rectal administration in distal ulcerative colitis, use appropriate rectal formulations; the oral and rectal routes can be combined for extensive disease.

Monitor patients for treatment response and adjust the dose as necessary to maintain remission.

In patients with renal or hepatic impairment, use with caution and monitor renal function and liver enzymes regularly.

Discontinue treatment if signs of intolerance, worsening colitis, or acute hypersensitivity reactions occur.

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, peptic ulcer of the stomach or duodenum 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 should be discontinued in the last 2-4 weeks of pregnancy.

If use during lactation is necessary, 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

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, as well as 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.