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

Nonspecific ulcerative colitis, Crohn’s disease (prevention and treatment of exacerbations).

Pharmacological effect

Cansalazine is an anti-inflammatory drug with a predominant localization of action in the intestines. 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.

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

After oral administration, mesalazine is slowly released from the dosage form in the distal small intestine and colon. Plasma protein binding is 43%. Metabolized in the intestinal mucosa and in the liver with the formation of N-acetyl-5-ASA. T1/2 is 0.5-2 hours. Mesalazine is excreted in the urine, mainly in acetylated form.

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.” have an increased risk of side effects. You may experience yellow-orange discoloration of urine and tears and staining of soft contact lenses.

If you miss a dose, the missed dose should be taken at any time or with the next dose.
If several doses are missed, 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 and speed of psychomotor reactions.

Active ingredient

Mesalazine

Composition

1 tablet contains:

Active substance:

mesalazine 500 mg;

Excipients:

calcium hydrogen phosphate dihydrate,

colloidal silicon dioxide (Aerosil A-300),

copovidon (kollidon VA-64 or plasdon Es-630),

sodium alginate (Kelton LVCR),

microcrystalline cellulose,

magnesium stearate.

Pregnancy

It is known that mesalazine penetrates the placental barrier, however, limited experience with the drug in pregnant women does not allow us to evaluate possible side effects. Use in pregnant women is possible only if the expected benefit to the mother outweighs the possible risk to the fetus.

Mesalazine is excreted in breast milk in concentrations lower than in a woman’s blood, while the metabolite, acetyl mesalazine, is found in similar or higher concentrations. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

Contraindications

Hypersensitivity, blood diseases. peptic ulcer of the stomach and duodenum, hemorrhagic diathesis, severe renal/liver failure, lactation period, last 2–4 weeks of pregnancy, children (up to 12 years), as well as children weighing less than 50 kg.

With caution: pregnancy (first trimester), liver and/or kidney failure, glucose-6-phosphate dehydrogenase deficiency.

Side Effects

From the digestive system: nausea, vomiting, heartburn, diarrhea, loss of appetite, abdominal pain, increased activity of liver transaminases, hepatitis, pancreatitis.

From the cardiovascular system: palpitations, tachycardia, increased or decreased blood pressure, chest pain, shortness of breath.

From the nervous system: headache, tinnitus, dizziness, polyneuropathy, tremor, depression.

From the urinary system: proteinuria. hematuria, oliguria. anuria, crystalluria, nephrotic syndrome.

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

From the hematopoietic organs: anemia (hemolytic, megaloblastic, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.

Other: weakness, mumps, photosensitivity, lupus-like syndrome, oligospermia, alopecia, decreased production of tear fluid.

Interaction

Strengthens the hypoglycemic effect of sulfonylurea derivatives. ulcerogenicity of glucocorticosteroids. toxicity of methotrexate. Weakens the activity of furosemide, spironolactone, sulfonamides, rifampicin. Strengthens the effect of anticoagulants. Increases the effectiveness of uricosuric drugs (tubular secretion blockers). Slows down the absorption of cyanocobal amine.

Overdose

Symptoms: mild to moderate severity – symptoms of “salicylicism” (nausea, vomiting, tinnitus, blurred vision, 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 increasing intoxication, respiratory paralysis and uncoupling of oxidative phosphorylation increase. 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 elderly people when taking more than 100 mg/kg/day for several days.

In children and elderly patients, the initial signs of salicylicism 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. Moderate poisoning requires hospitalization for 24 hours.

Treatment: provocation of vomiting, administration of activated carbon and laxatives, constant monitoring of the acid-base composition of the blood (ABC) and electrolyte balance; depending on the metabolic state – administration of sodium bicarbonate, sodium citrate solution or sodium lactate. Increasing reserve alkalinity enhances the excretion of mesalazine due to alkalinization of urine.

Alkalinization of urine is indicated when salicylate levels are above 40 mg% and is provided by intravenous infusion of sodium bicarbonate (88 mEq in 1 liter of 5% dextrose solution, at a rate of 10–15 ml/h/kg); restoration of circulating blood volume (CBV) and induction of diuresis are achieved by administering 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. The use of acetazolamide for alkalinization of urine is not recommended (it can cause acidemia and enhance the toxic effect of salicylates).

Hemodialysis is indicated for salicylate levels greater than 100–130 mg%. in patients with chronic poisoning – 40 mg% and lower if indicated (refractory acidosis, progressive deterioration, severe central nervous system damage, pulmonary edema and renal failure). For pulmonary edema – artificial pulmonary ventilation (ALV) with an oxygen-enriched mixture.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Shelf life

3 years

Manufacturer

Kanonpharma production CJSC, Russia