Kansalazine - instructions for use, dose, side effects, contraindications

Composition:1 tablet of prolonged action contains: active substance: mesalazine - 500 mg;
Excipients: calcium hydrophosphate dihydrate 28 mg, silicon dioxide colloid 6 mg, copovidone 37 mg, sodium alginate 42 mg, cellulose microcrystalline 113 mg, magnesium stearate 4 mg.

Description:Tablets are almost white or white with a grayish shade of color, round, biconvex.Small inclusions are allowed.

Pharmacotherapeutic group:Antimicrobial and anti-inflammatory intestinal.

ATX: & nbsp

A.07.E.C.02 Mesalazine

A.07.E.C Aminosalicylic acid and its analogues

Pharmacodynamics:Has a local anti-inflammatory effect due to inhibition of neutrophil lipoxygenase activity and synthesis of prostaglandins and leukotrienes. Slows migration, degranulation, phagocytosis of neutrophils, as well as secretion of immunoglobulins by lymphocytes. Has antibacterial action against Escherichia coli and some cocci (manifested in the large intestine).
Has antioxidant effects (due to the ability to bind to free oxygen radicals and destroy them). It has good tolerability, reduces the risk of recurrence in Crohn's disease, especially in patients with ileitis and a long duration of the disease.

Pharmacokinetics:About 30-50% of the dose is absorbed, mainly in the small intestine. Mesalazine is subjected to acetylation in the intestinal mucosa, in the liver and, to a small extent, enterobacteria, forming N-acetyl-5-aminosalicylic acid.The connection with plasma proteins is 43%, and N-acetyl-5-aminosalicylic acid - 73-83%. Mesalazine and its metabolite does not penetrate the blood-brain barrier, it penetrates into the mother's milk.
Cumulative properties are available in healthy volunteers after taking the drug at a dose of 1500 mg / day. Cumulates in chronic renal failure (CRF). Mesalazine and its metabolites are excreted from the body by the kidneys and intestines.

Indications:Nonspecific ulcerative colitis, Crohn's disease (prevention and treatment of exacerbations).

Contraindications:Hypersensitivity, blood diseases, peptic ulcer of the stomach and duodenum, hemorrhagic diathesis, severe renal / hepatic insufficiency, lactation period, the last 2-4 weeks of pregnancy, children's age (up to 12 years), as well as children weighing less than 50 kg.

Carefully:Pregnancy (I trimester), hepatic and / or renal insufficiency, deficiency of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:It is known that mesalazine penetrates through the placental barrier, however, limited experience of the drug in pregnant women does not allow to evaluate 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 concentration lower than in a woman's blood, whereas a metabolite-acetyl-mesalazine-is found in a similar or higher concentration. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:Mesalazine tablets prolonged action is recommended to take whole, without chewing, after eating, squeezed a lot of liquid.
ULCERATIVE COLITIS
Stage of exacerbation
Adults: the dose is selected individually, usually up to 4 g of mesalazine per day in several doses.
Children: the dose is selected individually, usually 20-30 mg of mesalazine per 1 kg of patient's body weight per day in several doses.
Supportive therapy
Adults: the dose is selected individually, usually 2 g of mesalazine per day in several doses.
Children: the dose is selected individually, usually 20-30 mg of mesalazine per 1 kg of the patient's body weight per day in several doses.
CROHN'S DISEASE
Stage of exacerbation 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 selected individually, usually 20-30 mg of mesalazine per 1 kg of body weight per day in several doses.

Side effects:From the digestive system: nausea, vomiting, heartburn, diarrhea, decreased appetite, abdominal pain, increased activity of "hepatic" transaminases, hepatitis, pancreatitis.
From the cardiovascular system: palpitation, tachycardia, increase or decrease in blood pressure, chest pain, dyspnea.
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, dermatosis, bronchospasm.
From the hematopoiesis: anemia (hemolytic, megaloblastic, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.
Other: weakness, parotitis, photosensitivity, lupus-like syndrome, oligospermia, alopecia, a decrease in the production of tear fluid.

Overdose:A single dose of less than 150 mg / kg - an overdose of mild severity, 150-300 mg / kg - moderate, more than 300 mg / kg - severe.
Symptoms: mild and moderate severity - symptoms of "salicilism" (nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache, general malaise, fever - poor prognostic sign in adults). Heavy-hyperventilation of the lungs of the central genesis, respiratory alkalosis, metabolic acidosis, confused consciousness, drowsiness, collapse, convulsions, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis - dyspnea, choking, cyanosis, cold sticky sweat; with increasing intoxication, paralysis of respiration and dissociation of oxidative phosphorylation, causing respiratory acidosis, increase.
In chronic overdose, the concentration in the plasma is poorly correlated with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly with more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicylism are not always noticeable,therefore 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% - about extremely severe, prognostically unfavorable. With moderate poisoning, hospitalization is necessary for 24 hours.
Treatment: provocation of vomiting, the appointment of activated carbon and laxatives, constant monitoring of acid-base blood composition (CBS) and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate solution or sodium lactate. Increased reserve alkalinity enhances the excretion of mesalazine by alkalinizing urine. Urine alkalization is indicated at a salicylate level above 40 mg% and is provided by intravenous infusion of sodium bicarbonate (88 mEq / in 1 L of 5% dextrose solution, at a rate of 10-15 ml / h / kg); the restoration of the volume of circulating blood (BCC) and the induction of diuresis are achieved by the introduction of sodium bicarbonate in the same doses and dilutions, which are repeated 2-3 times. Caution should be exercised in elderly patients in whom intensive fluid infusion can lead to pulmonary edema.It is not recommended to use acetazolamide for alkalinization of urine (it can cause acidemia and enhance the toxic effect of salicylates). Hemodialysis is indicated at a salicylate level of more than 100-130 mg%, in patients with chronic poisoning -40 mg% and lower in the presence of indications (refractory acidosis, progressive deterioration, severe CNS damage, pulmonary edema and kidney failure). With pulmonary edema - artificial ventilation (IVL) with a mixture enriched with oxygen.

Interaction:Enhances hypoglycemic effect of sulfonylurea derivatives, ulcerogenicity of glucocorticosteroids, toxicity of methotrexate. It reduces the activity of furosemide, spironolactone, sulfonamides, rifampicin. Enhances the effect of anticoagulants. Increases the effectiveness of uricosuric medicines (tubular secretion blockers). Slows the absorption of cyanocobalamin.

Special instructions:It is advisable to regularly conduct a general blood test (before, during, and after treatment) and urine, monitoring the excretory function of the kidneys.
Patients who are "slow acetylators" have an increased risk of side effects.It can be observed staining of urine and tears in yellow-orange color, staining of soft contact lenses.
In case of skipping the drug, the missed dose should be taken at any time or along with the next dose.
If several doses are missed, then, without stopping treatment, see a doctor. If suspected of developing acute intolerance syndrome mesalazine necessary cancel.

Effect on the ability to drive transp. cf. and fur:Patients should avoid driving, as well as performing work that requires a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of prolonged action of 500 mg.

Packaging:For 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
According to 1, 3, 5, 6, 9 or 10 contour cell packs of 10 tablets or 2, 4 or 6 contiguous cell packs of 15 tablets together with the instruction for use are placed in a pack of cardboard.

Storage conditions:In a dry, dark place at a temperature of not more than
25 ° C.

Shelf life:3 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006281/09

Date of registration:10.08.2009 / 12.12.2011

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp2016-09-22

Illustrated instructions

Instructions

Kansalazin® (Kansalazin)