Samezil (Tablets, Suppositories, Suspension) Instructions for Use

ATC Code

A07EC02 (Mesalazine)

Active Substance

Mesalazine (Rec.INN registered by WHO)

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

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. T_1/2 is 0.5-2 h. 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

Dosage Regimen

Determine the dosage and route of administration based on the indication, disease activity, and dosage form.

For oral administration (tablets, suspension), take the dose in its entirety. Do not crush or chew the tablets.

For the treatment of acute exacerbations of ulcerative colitis, administer up to 3-4 grams of mesalazine per day, divided into 2-4 doses.

For the maintenance of remission of ulcerative colitis, administer a dose of 1.5-2 grams per day, divided into 2 doses.

For the treatment of Crohn’s disease, administer up to 3-4 grams per day, divided into multiple doses.

For rectal administration (suppositories), use for the treatment of ulcerative colitis affecting the rectum.

Administer one 500 mg suppository rectally, 1 to 3 times per day, as directed. The total daily rectal dose typically does not exceed 1.5 grams.

Adjust the final dosage and duration of therapy individually based on clinical response and tolerability.

Adhere strictly to the prescribed regimen. Do not exceed the recommended daily dose.

Monitor blood counts, renal function (serum creatinine, urea), and liver enzymes before treatment initiation and periodically during therapy.

Discontinue use immediately and consult a physician if severe abdominal cramps, acute abdominal pain, bloody diarrhea, fever, or severe headache occurs.

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 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, then in the last 2-4 weeks of pregnancy, the intake of mesalazine should be discontinued.

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 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 levels 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 30°C (86°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.