Kansalazin

General characteristics. Structure:

Active agent: mesalazina of 500 mg;
excipients: calcium hydrophosphate a dihydrate - 28 mg, silicon dioxide colloid - 6 mg, коповидон - 37 mg, sodium alginate - 42 mg, cellulose microcrystallic - 113 mg, magnesium stearate - 4 mg.

Description: tablets of color, almost white or white with a grayish shade, round, biconvex form. Insignificant impregnations are allowed.

Pharmacological properties:

Pharmacodynamics. Possesses the local antiinflammatory action caused by inhibition of activity of a neutrophylic lipoxygenase and synthesis of prostaglandins and leukotrienes. Slows down migration, degranulation, phagocytosis of neutrophils, and also secretion of immunoglobulins lymphocytes. Possesses antibacterial action concerning colibacillus and some cocci (it is shown in a large intestine).
Has antioxidant effect (due to ability to contact free oxygen radicals and to destroy them). Differs in good tolerance, reduces risk of a recurrence at a disease Krone, especially at patients with an ileitis and big duration of a disease.

Pharmacokinetics. About 30-50% of the accepted dose are absorbed, mainly, in a small bowel. Mesalazin is exposed to acetylation in a mucous membrane of intestines, in a liver and, in small degree, - enterobakteriya, forming N-acetyl-5-aminosalicylic acid. Communication with proteins of plasma - 43%, and N-acetyl-5-aminosalicylic acid – 73-83%. Mesalazin and his metabolite do not get through a blood-brain barrier, get into maternal milk.
Cumulative properties are available for healthy volunteers after administration of drug in a dose of 1500 mg/day. Kumuliruyet at the chronic renal failure (CRF).
Mesalazin and his metabolites are brought out of an organism by kidneys and intestines.

Indications to use:

Nonspecific ulcer colitis, disease Krone (prevention and treatment of aggravations).

Route of administration and doses:

Pill of a mesalazin of the prolonged action is recommended to be taken entirely, without chewing, after food, washing down with a large amount of liquid.
ULCER COLITIS
Aggravation stage
Adults: the dose is selected individually, usually - to 4 g of a mesalazin a day in stages.
Children: the dose is selected individually, usually - 20-30 mg of a mesalazin on 1 kg of body weight of the patient a day in stages.
Maintenance therapy
Adults: the dose is selected individually, usually 2 g of a mesalazin a day in stages.
Children: the dose is selected individually, usually 20-30 mg of a mesalazin on 1 kg of body weight of the patient a day in stages.
DISEASE KRONE
Stage of an aggravation and maintenance therapy
Adults: the dose is selected individually, usually - to 4 g of a mesalazin a day in stages.
Children: the dose is selected individually, usually 20-30 mg of a mesalazin on 1 kg of body weight a day in stages.

Features of use:

Reasonablly regular performing the general blood test (before the beginning, in time, and also after treatment) and urine, control of secretory function of kidneys.
Patients, being "slow acetylizers", have the increased risk of development of side effects. Coloring of urine and tears in yellow-orange color, a prokrashivaniye of soft contact lenses can be observed.
In case of the admission of administration of drug the passed dose should be accepted at any time or together with the following dose.
If several doses are passed, then, without stopping treatment, to see a doctor. At suspicion on development of a syndrome of acute intolerance месалазин it is necessary to cancel.
Patients should avoid driving, and also the performance of work demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: nausea, vomiting, heartburn, diarrhea, loss of appetite, abdominal pain, increase in activity of "hepatic" transaminases, hepatitis, pancreatitis.
From cardiovascular system: heartbeat, tachycardia, increase or lowering of arterial pressure, pains behind a breast, an asthma.

From a nervous system: headache, sonitus, dizziness, polyneuropathy, tremor, depression.
From an urinary system: proteinuria, hamaturia, oliguria, anury, crystalluria, nephrotic syndrome.
Allergic reactions: skin rash, itch, dermatosis, bronchospasm.
From bodies of a hemopoiesis: anemia (hemolitic, megaloblastny, aplastic), leukopenia, agranulocytosis, thrombocytopenia, prothrombinopenia.
Others: weakness, parotitis, photosensitization, volchanochnopodobny syndrome, oligospermatism, alopecia, reduction of products of the lacrimal liquid.

Interaction with other medicines:

Strengthens hypoglycemic action of derivatives of sulphonylurea, an ultserogennost of glucocorticosteroids, toxicity of a methotrexate. Weakens activity of furosemide, Spironolactonum, streptocides, rifampicin. Strengthens effect of anticoagulants. Increases efficiency of uricosuric medicines (blockers of canalicular secretion). Slows down cyanocobalamine absorption.

Contraindications:

Hypersensitivity, blood diseases, a peptic ulcer of a stomach and duodenum, hemorrhagic diathesis, a heavy renal/liver failure, the lactation period, the last 2-4 weeks of pregnancy, children's age (up to 12 years), and also to children with body weight less than 50 kg.

With care:
Pregnancy (I trimester), liver and/or renal failure, deficit glyukozo-6-fosfatdegidrogenazy.

Use at pregnancy and a lactation:
It is known what месалазин gets through a placental barrier, however, limited experience of use of drug for pregnant women does not allow to estimate possible side effects. Use for pregnant women is possible, only if the estimated advantage for mother exceeds possible risk for a fruit.
Mesalazin is excreted with breast milk in concentration below, than in the woman's blood whereas the metabolite – acetyl-mesalazin - is found in similar or higher concentration. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

Single dose less than 150 mg/kg - overdose of easy severity, 150-300 mg/kg - moderate, more than 300 mg/kg - heavy.
Symptoms: easy and moderately severe - symptoms of "salitsilizm" (nausea, vomiting, a sonitus, a vision disorder, dizziness, a severe headache, a febricula, fever - a bad predictive sign at adults). Heavy - a hyperventilation of lungs of the central genesis, a respiratory alkalosis, a metabolic acidosis, the confused consciousness, drowsiness, a collapse, spasms, an anury, bleedings. Originally central hyperventilation of lungs leads to a respiratory alkalosis - short wind, suffocation, cyanosis, a cold clammy sweat; with strengthening of intoxication the paralysis of breath and dissociation of oxidizing phosphorylation causing respiratory acidosis accrues.
At chronic overdose the concentration defined in plasma badly correlates with severity of intoxication. The greatest risk of development of chronic intoxication is noted at elderly people at reception within several days more than 100 mg/kg/days. At children and patients of advanced age initial signs of a salitsilizm are not always noticeable therefore it is reasonable to define periodically concentration of salicylates in blood: level over 70 mg of % testifies to a moderate or serious poisoning; higher than 100 mg % extremely heavy, predictively adverse. At moderately severe poisoning hospitalization on 24 h is necessary.
Treatment: provocation of vomiting, purpose of absorbent carbon and laxatives, constant control behind acid-base composition of blood (BRAIDS) and electrolytic balance; depending on a condition of a metabolism - introduction of Natrii hydrocarbonas, solution of sodium of citrate or sodium of a lactate. Increase in reserve alkalinity strengthens removal of a mesalazin due to urine alkalization. Alkalization of urine is shown at the level of salicylates higher than 40 mg of % and is provided in/in infusion of Natrii hydrocarbonas (88 мЭкв in 1 l of 5% of solution of a dextrose, with a speed of 10-15 ml/h/kg); recovery of the volume of the circulating blood (VCB) and induction of a diuresis are reached by introduction of Natrii hydrocarbonas in the same doses and cultivation which is repeated by 2-3 times. It is necessary to be careful at elderly patients at whom intensive infusion of liquid can lead to a fluid lungs. Use of acetazoleamide for urine alkalization is not recommended (can cause an acidemia and strengthen toxic effect of salicylates). The hemodialysis is shown at the level of salicylates more than 100-130 mg of %, patients with chronic poisoning have 40 mg of % and below in the presence of indications (refractory acidosis, the progressing aggravation of symptoms, severe defeat TsNS, a fluid lungs and a renal failure). At a fluid lungs - the artificial ventilation of the lungs (AVL) by the mix enriched with oxygen.

Storage conditions:

Period of validity: 3 years. Not to apply after a period of validity. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of the prolonged action on 500 mg. On 10 or 15 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 1, 3, 5, 6, 9 or 10 blister strip packagings on 10 tablets or on 2, 4 or 6 blister strip packagings on 15 tablets together with the application instruction place in a pack from a cardboard.