Index of drugs

Rheumatoid arthritis resistant to treatment with NLZP. Inflammatory bowel diseases (eg ulcerative colitis, Crohn's disease).

1 tabl contains 500 mg of sulfasalazine.

Sulfasalazine exerts anti-inflammatory, immunosuppressive and antibacterial effects. It is used to inhibit inflammatory conditions, especially the intestinal mucosa and to treat active rheumatoid arthritis. Mechanism of action in inflammatory bowel diseases: the main action of sulfasalazine is the anti-inflammatory action of the nascent mesalazine. In addition, immunosuppressive activity was detected as a result of suppression of lymphocyte and granulocyte metabolism and inhibition of various enzyme systems by all three compounds (sulfasalazine, sulfapyridine, mesalazine). The bacteriostatic effect of sulphapiridine formed locally in the colon may also have clinical significance. The drug affects both aerobic and anaerobic bacterial flora. The mechanism of action in rheumatoid arthritis has not been established. After oral administration, the drug is partially absorbed (in about 20% of the administered dose) in the small intestine and then undergoes enterohepatic circulation. The maximum plasma concentration is reached after 3-6 h, and the degree of binding to proteins is about 99%. There are significant differences in the serum concentration of the drug. There is a moderate tendency to accumulation of sulfasalazine in the body. A small percentage of the dose is excreted in the urine. Sulfasalazine is broken down by bacteria in the lumen of the colon into two major metabolites: sulfapyridine and mesalazine (5-aminosalicylic acid). Sulfapyridine is rapidly absorbed, partially metabolized in the liver to inactive acetylsulfapyridine and excreted primarily in unchanged form in the urine. The non-acetylated sulfapyridine is partially bound to serum proteins and the maximum serum concentration is reached after 12 hours. Sulphapyridine has a tendency to accumulate; it stops to be detected in the serum only after 3 days of discontinuation of the drug. The degree of sulfapyridine acetylation is genetically determined. Patients with free acetylation have higher serum concentrations of free sulfapyridine and, therefore, have a greater tendency to side effects. Mesalazine is absorbed to a lesser extent. 15% of the dose is excreted in the urine. The major part of the administered dose, 75%, remains in the lumen of the colon and is excreted in the stool as 5-aminosalicylic acid.

Hypersensitivity to sulfasalazine or other components of the preparation. Hypersensitivity to sulfonamides and salicylates. Intermittent porphyria, mixed porphyria. Obstruction of the urinary tract or intestines. Do not use in children under the age of 2 years.

Caution should be used in patients with severe allergies and bronchial asthma, with G-6-PD deficiency (risk of haemolytic anemia). Sulfasalazine should not be used in patients with impaired renal or hepatic function or poor blood composition, unless the potential benefits outweigh the risks. For patients with mild hypersensitivity desensitization should be considered. In case of severe hypersensitivity reactions, the drug should be discontinued. At a dose of 70 mg / kg / day, the blood concentration may reach levels considered to be a toxic threshold (50 μg / ml). There have been reports of severe skin reactions (in some cases leading to death) during the use of sulfasalazine, such as exfoliative dermatitis, Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). Patients should be informed about the signs and symptoms, and closely monitored for skin reactions; the greatest risk of exfoliative dermatitis, Stevens-Johnson syndrome or toxic epidermal necrolysis exists at an early stage of treatment, in most cases in the first month of treatment.If signs or symptoms of exfoliative dermatitis, Stevens-Johnson syndrome or toxic epidermal necrolysis (eg skin rash, mucosal lesions or any signs of hypersensitivity) occur, discontinue sulfasalazine therapy and never take it again. Severe, life-threatening systemic hypersensitivity reactions have also been observed, such as drug eruptions with eosinophilia and general symptoms. You should be aware of the early signs of hypersensitivity (fever, lymphadenopathy, with or without rash) and possibly stop the treatment.

The drug can be used during pregnancy only if absolutely necessary. Sulfasalazine given orally inhibits the absorption and metabolism of folic acid, which may cause its deficiency. Cases of neural tube defects have been reported in infants whose mothers took sulfasalazine during pregnancy, but there is no direct relationship between exposure to sulfasalazine and the occurrence of these defects. Sulfasalazine passes into breast milk, but the amount of the drug present in breast milk should not pose a threat to a healthy child. In premature infants and newborn babies with physiological jaundice, caution is advisable. Blood stools or diarrhea have been reported in breast-fed infants by sulphasalazine-treated mothers who have resolved after mothers discontinued sulphasalazine.

Very common: stomach problems, nausea. Common: leukopenia, loss of appetite, dizziness, headache, disturbed taste, tinnitus, cough, abdominal pain, diarrhea, bloating, vomiting, pruritus, joint pain, proteinuria, fever. Uncommon: thrombocytopenia, depression, shortness of breath, alopecia, urticaria, facial edema, increased liver enzymes. Rare: jaundice, changes in the nail area. Very rare: serious side effects on the skin: Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome). Frequency unknown: aseptic meningitis, pseudomembranous colitis, agranulocytosis, aplastic anemia, hemolytic anemia, macrocytosis, megaloblastic anemia, pancytopenia, anaphylactic shock, serum sickness, encephalopathy, peripheral neuropathy, olfactory disorders, pericarditis, cyanosis, fibrosing alveolitis , interstitial lung disease, eosinophil infiltrates, exacerbation of symptoms in ulcerative colitis, pancreatitis, hepatic failure, fulminant hepatitis, hepatitis, drug erosions with eosinophilia and general symptoms, angioneurotic edema, toxic, pustular dermatitis, erythema, rash, exfoliative dermatitis, lichen planus, hypersensitivity to light, systemic lupus erythematosus, Sjogren's syndrome, nephrotic syndrome, interstitial nephritis, crystalluria, haematuria, transient oligospermia, yellow coloration of the skin and body fluids, induction of autoantibodies. If severe side effects occur, treatment should be discontinued.

Orally.Rheumatoid arthritis. Adults and the elderly: dosage should be adjusted individually. The recommended dosage is 1-3 g per day. The most frequently used dose is 2 tablets. 2 times a day. It is recommended to start treatment with smaller doses and gradually increase them according to the scheme: day 1 - 4: 1 tabl. in the morning, 2 tabl. in the evening; day 5.-8 .: 1 tabl. in the morning, 2 tabls in the evening; day 9 and following: 2 tablets in the morning, 2 tabl. in the evening. If the patient's response to treatment is unsatisfactory for 2-3 months, the daily dose of sulfasalazine may be increased to a maximum of 3 g. In patients with adverse reactions, the dose may be temporarily reduced.Inflammatory bowel disease - an acute form of the disease. Adults and the elderly: severe exacerbations of the disease: 2-4 tabl. 3-4 times a day. Mild and moderate throws: 2 tabl. 3-4 times a day. Children: 40-60 mg / kg / day in 3-6 divided doses.Inflammatory bowel diseases - supportive treatment. Adults and the elderly: 2 tabl. 2-3 times a day. Treatment with this dose should not be interrupted and should be continued for a prolonged period of time if side effects do not occur. In the event of exacerbation of the disease, the dose is increased to 2-4 tabl. 3-4 times a day. Children: 20-30 mg / kg / day in 3-6 divided doses.Dosing should be adjusted individually depending on the clinical condition, the patient's tolerance of the medicine and the response to treatment. It is recommended that patients who have never been treated with sulfasalazine should increase their dose gradually over several weeks. The daily dose should be evenly distributed into divided doses.Way of giving. The tablets should be taken with meals, with a glass of water; swallow whole, do not crush or break.