Mesalazine (5-aminosalicylic acid) inhibits the activity of neutrophil lipoxygenase and the synthesis of metabolites of arachidonic acid (prostaglandins and leukotrienes), which are mediators of inflammation. Inhibits migration, degranulation, phagocytosis of neutrophils, and secretion of immunoglobulins by lymphocytes. Mesalazine has antioxidant properties.
Depending on the method of application of Salofalk the release of mesalazine occurs as a direct and colonic intestine (enemas and suppositories) or in the terminal small intestine and in the colon (tablets). In tablets the active substance is protected by a cover, which is resistant to gastric juice. Dosage form manufactured in such a way that mesalazine is slowly released only in the terminal small intestine and in the colon. It is established that the dissolution of tablets Salofalk starts in the small intestine via 110-170 min after administration, using 165-225 min tablet is completely dissolved. This process is not affected by changes in medium pH caused by food intake or other drugs. In the intestinal mucosa and in the liver mesalazine is metabolised into N-acetyl-5-ASA. Due to the relatively low absorption mesalazine and its rapid conversion to N-acetyl-5-ASA is already in the mucosa of the intestine, the concentration of mesalazine in the blood plasma remains relatively low after a single dose of Salofalk at a dose of 0, 25 g concentration of mesalazine is 0, 5-1, 5 µg/ml. the Binding of mesalazine with blood plasma proteins is 43%, N-acetyl-5-ASA — 75-83%. In breast milk penetrates 0, 1% mesalazine in the form of N-acetyl-5-ASA. The half-life of mesalazine is 0, 5-2 hours (depending on the dose), the clearance is 300 ml/min. The drug is excreted by the kidneys, mainly in the acetylated form.
Ulcerative colitis (prevention and treatment of exacerbations), Crohn’s disease (prevention and treatment of exacerbations).
The choice of formulation depends primarily on the location and extent of the affected area of the intestine. In the treatment of patients with common forms of ulcerative colitis (total, Subtotal) typically use the drug in pill form. In the treatment of patients with distal forms of colitis (proctitis, proktoshigmoidit) is preferably rectal administration of the drug in the form of suppositories and enemas. In patients with left-sided lesions of the colon as a possible local treatment with suppositories and enemas and their combination with tablets. For the treatment of patients with mild and moderate forms of ulcerative colitis and Crohn’s disease is usually prescribed for 0, 5 g 3 times a day, daily dose — 1, 5 g. in severe forms of the disease the daily dose can be increased to 3-4 g. the Drug in high doses are recommended to use no more than 8-12 weeks. Prevention of relapse the drug is prescribed in doses of 1, 5 g/day, if necessary — within a few years.
Taking pills morning, afternoon and evening without chewing, with enough fluid for 1 hour before meals.
Suppositories in the acute phase of the disease is prescribed rectal 500 mg 3 times a day. In particularly severe cases, the dose is doubled. During long-term therapy administered rectally 250 mg 3 times a day. Usually the acute symptoms are removed after 8-12 weeks of treatment.
Suspension for use in enemas administered 60 grams 1 time per day before sleep (pre-clean the intestines).
Granules: for the treatment of acute ulcerative colitis depending on the clinical situation, take contents of 1 packet of granules of Salofalk 500 mg 3 times a day or 1 sachet of granules of Salofalk 1000 mg 3 times a day (equivalent to 1, 5-3 g mesalazine daily).
For maintenance of remission in ulcerative colitis: take contents of 1 packet of granules of Salofalk 500 mg 3 times a day (equivalent to 1, 5 g mesalazine daily).
Granules of Salofalk not administer to children under 6 years, as experience with the drug in this age group is insufficient.
Children older than 6 years and adolescents: in acute conditions, depending on the severity of the disease, granules appoint a rate of 30-50 mg mesalazine/kg body weight per day in 3 divided doses. To maintain remission granules appoint a rate of 15-30 mg mesalazine/kg body weight per day in 2 admission. Children with body weight under 40 kg is recommended to prescribe half the dose for adults with body weight over 40 kg — the usual dose for adults.
Granules salofalk worth us 500 mg salofalk worth us 1000 mg it is impossible to chew. The contents of the sachet with granules of Salofalk 500 mg or 1000 mg Salofalk need to be taken in the morning, afternoon and evening. Granules should be placed on the tongue and swallow without chewing with a sufficient amount of liquid.
Hypersensitivity to salicylates, blood diseases, severe violations of the liver and kidneys, age of 2 years, peptic ulcer of the stomach or duodenal ulcers, haemorrhagic diathesis.
Rarely abdominal pain, diarrhoea, flatulence, nausea and vomiting, headache and dizziness. Possible hypersensitivity reactions — urticaria, pruritus, fever, bronchospasm, peri and myocarditis, acute pancreatitis and interstitial nephritis. In rare cases, when using mesalazine develops allergic alveolitis, pancholi. Some drugs, the chemical structure close to mesalazine, may under certain circumstances cause a syndrome similar to lupus erythematosus. In rare cases, possible myalgia and arthralgia. There is a possibility of development of methemohlobinemia. In some cases after mesalazine use noted changes in the composition of the blood (aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia). Described isolated cases of hepatitis, increased activity of transaminases.
It is recommended to perform blood and urine tests before and 14 days after the start of treatment and then another 2-3 times with 4-week break. In the case of normal results of the control tests carried out 1 time in 3 months. For monitoring of renal function is recommended to determine the level of urea and creatinine in serum and to investigate the urinary sediment.
You should pay attention to the possibility of development of methemohlobinemia.
If a disturbance of lung function, particularly in asthma, the drug should be used with caution.
With the development of hypersensitivity reactions, the drug should be discontinued immediately.
Salofalk worth us potentiates the action of anticoagulants and increases the risk of gastrointestinal bleeding, enhances the negative effects of corticosteroids on the digestive tract, potentiates hypoglycemic effect of sulfonylureas, increases the toxicity of methotrexate, reduces the severity of tuberculostatic action of rifampicin and decreases the uricosuric effect of probenecid/sulfinpirazon, the diuretic effect of spironolactone and furosemide.
At temperatures up to 25 °C.