Composition
1 tablet contains:
Active ingredient: Â
mesalazine 500 mg;
Auxiliary substances:
calcium hydrophosphate dihydrate,
colloidal silicon dioxide (aerosil A-300),
copovidone (collidone VA-64 or plasdon Es-630),
sodium alginate (Kelton LVCR),
microcrystalline cellulose,
magnesium stearate.
Pharmacological action
Cansalazine is an anti-inflammatory agent with a predominant localization of action in the intestine. Mesalazine (5-aminosalicylic acid) inhibits the activity of neutrophilic lipoxygenase and the synthesis of arachidonic acid metabolites (prostaglandins and leukotrienes), which are mediators of inflammation.
It inhibits migration, degranulation, neutrophil phagocytosis, and the secretion of immunoglobulins by lymphocytes. Mesalazine has antioxidant properties by binding to free oxygen radicals.
Pharmacokinetics
After oral use, mesalazine is slowly released from the dosage form in the distal part of the small intestine and in the large intestine. Binding to plasma proteins 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 h. Mesalazine is excreted in the urine, mainly in acetylated form.
Indications
Non-specific ulcerative colitis, Crohn’s disease (prevention and treatment of exacerbations).
Use during pregnancy and lactation
It is known that mesalazine penetrates the placental barrier, however, limited experience of using the drug in pregnant women does not allow us to assess possible side effects. Use in pregnant women is possible only if the intended benefit to the mother exceeds the possible risk to the fetus. Mesalazine is excreted in breast milk at a lower concentration than in the blood of a woman, while the metabolite – acetyl-mesalazine-is found in a similar or higher concentration. If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be decided.
Contraindications
Hypersensitivity, blood diseases. peptic ulcer of the stomach and duodenum, hemorrhagic diathesis, severe renal / hepatic insufficiency, lactation, the last 2-4 weeks of pregnancy, children (up to 12 years), as well as children with a body weight of less than 50 kg.
With caution:  pregnancy (I trimester), hepatic and / or renal failure, glucose–6-phosphate dehydrogenase deficiency.
Side effects
From the digestive system: Â nausea, vomiting, heartburn, diarrhea, decreased appetite, abdominal pain, increased activity of “liver” transaminases, hepatitis, pancreatitis.
From the cardiovascular system: Â palpitations, tachycardia, high or low blood pressure, pain behind the sternum, shortness of breath.
Nervous system disorders: Â headache, tinnitus, dizziness, polyneuropathy, tremor, depression.
From the urinary system: Â proteinuria. hematuria, oliguria. anuria, crystalluria, nephrotic syndrome.
Allergic reactions: Â skin rash, pruritus, dermatoses, bronchospasm.
From the side of hematopoietic organs: Â anemia (hemolytic, megaloblastic. aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.
Other services: Â weakness, mumps, photosensitivity, lupus-like syndrome, oligospermia, alopecia, decreased production of tear fluid.
Interaction
Increases the hypoglycemic effect of sulfonylurea derivatives. ulcerogenicity of glucocorticosteroids. toxicity of methotrexate. Weakens the activity of furosemide, spironolactone, sulfonamides, rifampicin. Enhances the effect of anticoagulants. Increases the effectiveness of uricosuric drugs (tubular secretion blockers). Slows down the absorption of cyanocobal amine.
How to take, course of use and dosage
Long-acting mesalazine tablets are recommended to be taken whole, without chewing, after meals, washed down with a large amount of liquid.
ULCERATIVE COLITIS
Stage of exacerbati Onadults: Â the dose is selected individually, usually up to 4 g of mesalazine per day in several doses. Children: Â the dose is selected individually, usually 20-30 mg of mesalazine per 1 kg of body weight of the patient per day in several doses.
Supportive therapyadults: Â the dose is selected individually, usually 2 g of mesalazine per day in several doses. Children: Â the dose is selected individually, usually 20-30 mg of mesalazine per 1 kg of body weight of the patient per day in several doses.
CROHN’S DISEASE
Acute stage and maintenance therapyadults: Â the dose is selected individually, usually up to 4 g of mesalazine per day in several doses. Children: Â the dose is selected individually, usually 20-30 mg of mesalazine per 1 kg of body weight per day in several doses.
Overdose
Symptoms:  mild to moderate symptoms of “salicylism” (nausea, vomiting, tinnitus, visual disturbances, dizziness, severe headache, general malaise, fever — a poor prognostic sign in adults).
Severe -hyperventilation of the lungs of central origin, respiratory alkalosis, metabolic acidosis, confusion, drowsiness, collapse, convulsions, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis — shortness of breath, suffocation, cyanosis, cold sticky sweat; with increased intoxication, respiratory paralysis and dissociation of oxidative phosphorylation increases. causing respiratory acidosis.
In chronic overdose, the concentration determined in plasma does not correlate well with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly when taking more than 100 mg/kg/day for several days.
In children and elderly patients, the initial signs of salicylism are not always noticeable, so it is advisable to periodically determine the concentration of salicylates in the blood: a level above 70 mg% indicates moderate or severe poisoning; above 100 mg% — extremely severe, prognostically unfavorable. In case of moderate poisoning, hospitalization for 24 hours is required.
Treatment:  provocation of vomiting, use of activated charcoal and laxatives, constant monitoring of the acid-base composition of the blood (CBS) and electrolyte balance; depending on the state of metabolism — the introduction of sodium bicarbonate, sodium citrate solution or sodium lactate. An increase in reserve alkalinity increases the excretion of mesalazine by alkalizing the urine.
Urine alkalinization is indicated at salicylate levels above 40 mg% and is provided by intravenous infusion of sodium hydrocarbonate (88 mEq in 1 liter of 5% dextrose solution, at a rate of 10-15 ml/h / kg); restoration of circulating blood volume (BCC) and induction of diuresis are achieved by use of sodium bicarbonate in the same doses and dilution, which is repeated 2-3 times.
Caution should be exercised in elderly patients in whom intensive fluid infusion may lead to pulmonary edema. It is not recommended to use acetazolamide for alkalinization of urine (it can cause acidemia and increase the toxic effect of salicylates).
Hemodialysis is indicated for salicylate levels greater than 100-130 mg%. in patients with chronic poisoning–40 mg% or lower if indicated (refractory acidosis, progressive deterioration of the condition, severe CNS damage, pulmonary edema and renal failure). In case of pulmonary edema-artificial ventilation of the lungs with a mixture enriched with oxygen.
Special instructions
It is advisable to regularly conduct a general blood test (before, during, and after treatment) and urine, and monitor the excretory function of the kidneys. Patients who are “slow acetylators”. they have an increased risk of side effects. There may be staining of urine and tears in yellow-orange color, staining of soft contact lenses. If you miss taking the drug, the missed dose should be taken at any time or together with the next dose. If you miss several doses, then, without stopping treatment, consult a doctor. If the development of acute intolerance syndrome is suspected, mesalazine should be discontinued. Patients should avoid driving a car, as well as performing work that requires increased concentration of attention and speed of psychomotor reactions.
Storage conditions
Store in a dry place protected from light at a temperature not exceeding 25 °C.
Shelf life
3 years
Active ingredient
Mesalazine
Conditions of release from pharmacies
By prescription
Dosage form
long-acting tablets
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