Cansalazine, 500 mg 50 pcs.

Cansalazine is an anti-inflammatory drug with predominant localization of action in the intestine. Mesalazine (5-aminosalicylic acid) inhibits activity of neutrophil lipooxygenase and synthesis of arachidonic acid metabolites (prostaglandins and leukotrienes) which are mediators of inflammation.

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

Pharmacokinetics

Mesalazine is slowly released from the dosage form in the distal small intestine and large intestine after oral administration. Binding to plasma proteins is 43%. It is metabolized in the intestinal mucosa and in the liver to form N-acetyl-5-ASC. T1/2 is 0.5-2 hours. Mesalazine is excreted with urine, mainly in acetylated form.

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

mesalazine 500 mg;

Associates:

calcium hydrophosphate dihydrate,

colloidal silicon dioxide (Aerosil A-300),

copovidone (collidon VA-64 or plasdon ES-630),

sodium alginate (Kelton LVCR),

microcrystalline cellulose,

magnesium stearate.

How to take, the dosage

Long-acting tablets of mesalazine are recommended to be taken whole, without chewing, after meals with plenty of fluids.

Earrheal colitis

Adults: The dose is adjusted individually, usually up to 4 g of mesalazine per day in several doses.
Children: the dose is adjusted individually, usually – 20-30 mg of mesalazine per 1 kg of the patient’s body weight per day in several doses.

Maintenance therapy
Adults: the dose is adjusted individually, usually 2 g of mesalazine per day in several doses.
Children: the dose is adjusted individually, usually 20-30 mg of mesalazine per 1 kg of the patient’s body weight per day in several doses.

Crone’s Disease

The acute stage and maintenance therapy
Adults: the dose is selected individually, usually up to 4 g of mesalazine per day in several doses.
Children: the dose is adjusted individually, usually 20-30 mg of mesalazine per 1 kg of body weight per day in several doses.

Interaction

Special Instructions

Contraindications

Hypersensitivity, blood diseases. gastric and duodenal ulcer, hemorrhagic diathesis, severe renal/liver failure, lactation, the last 2-4 weeks of pregnancy, childhood age (under 12 years), and children with body weight less than 50 kg.

With caution: pregnancy (1st trimester), hepatic and/or renal insufficiency, glucose-6-phosphate dehydrogenase deficiency.

Side effects

Digestive system disorders: nausea, vomiting, heartburn, diarrhea, decreased appetite, abdominal pain, increased activity of “liver” transaminases, hepatitis, pancreatitis.

Cardiovascular system disorders: palpitation, tachycardia, increased or decreased blood pressure, chest pain, shortness of breath.

Nervous system disorders: headache, tinnitus, dizziness, polyneuropathy, tremor, depression.

Urinary system disorders: proteinuria. Hematuria, oliguria. anuria, crystalluria, nephrotic syndrome.

Allergic reactions: skin rash, itching, dermatosis, bronchospasm.

Hematopoietic disorders: anemia (hemolytic, megaloblastic. aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.

Other: weakness, parotitis, photosensitization, lupus-like syndrome, oligospermia, alopecia, decreased tear fluid production.

Overdose

Symptoms: mild to moderate – symptoms of “salicylitis” (nausea, vomiting, tinnitus, visual disturbances, dizziness, severe headache, general malaise, fever – a poor prognostic sign in adults).

Severe – central pulmonary hyperventilation, respiratory alkalosis, metabolic acidosis, confused consciousness, drowsiness, collapse, seizures, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis – shortness of breath, choking, cyanosis, cold clammy sweat; as intoxication increases, respiratory paralysis and dissociation of oxidative phosphorylation increase. causing respiratory acidosis.

In chronic overdose, plasma concentrations determined correlate poorly with the severity of intoxication. The greatest risk of developing chronic intoxication is seen in the elderly when more than 100 mg/kg/day is taken over several days.

In children and elderly patients the initial signs of salicylation are not always visible, so it is advisable to periodically determine the concentration of salicylates in blood: levels above 70 mg% indicate moderate or severe intoxication; above 100 mg% – extremely severe, prognostically unfavorable. If poisoning is of moderate severity the hospitalization is required for 24 hours.

Treatment: provocation of vomiting, administration of activated charcoal and laxatives, constant monitoring of acid-base blood composition (ABBC) and electrolyte balance; depending on the state of metabolism – administration of sodium hydrocarbonate, sodium citrate solution or sodium lactate. Increasing the reserve alkalinity enhances excretion of mesalazine by alkalizing the urine.

Alkalinization of urine is indicated when salicylate levels are above 40 mg% and is provided by intravenous infusion of sodium hydro carbonate (88 mEq in 1 liter of 5% dextrose solution, at a rate of 10-15 ml/h/kg); restoration of circulating blood volume (RBC) and induction of diuresis are achieved by sodium hydro carbonate infusion in the same doses and dilutions, which are repeated 2-3 times.

Caution should be exercised in elderly patients in whom intensive fluid infusion may result in pulmonary edema. The use of acetazolamide to alkalize the urine is not recommended (may cause acidemia and increase the toxic effects of salicylates).

Hemodialysis is indicated for salicylate levels greater than 100-130 mg%. in patients with chronic poisoning-40 mg% or less with indications (refractory acidosis, progressive deterioration, severe CNS damage, pulmonary edema and renal failure). In case of pulmonary edema, artificial lung ventilation (ALV) with an oxygen-enriched mixture.

Pregnancy use

Similarities