Sulfasalazin 500 mg, 50 pcs.

1 enteric-coated tablet contains:

active substance:

sulfasalazine

povidone coated (equivalent to 500 mg sulfasalazine) 535,000 mg

Excipients:

pregelatinized starch

magnesium stearate,

silica colloidal

anhydrous.

Sulfasalazin-EN is an antimicrobial and anti-inflammatory intestinal agent.

Sulfasalazine selectively accumulates in the intestinal connective tissue with the release of 5-aminosalicylic acid (5-ASA), which has anti-inflammatory activity, and sulfapyridine, which has antimicrobial bacteriostatic activity against diplococci, streptococci, gonococci, Escherichia coli.

Pharmacokinetics

About 30% of sulfasalazine in enteric-coated tablets are absorbed from the small intestine, the remaining 70% are digested by intestinal microflora to form 60-80% sulfapyridine and 25% 5-ASA. Sulfasalazine reaches its maximum concentration 3-12 hours after taking enteric-coated tablets. Communication with plasma proteins of sulfasalazine - 99%, sulfapyridine - 50%, 5-ASA - 43%.

Sulfapyridine is metabolized in the liver by hydroxylation to form inactive metabolites, 5-ASA by acetylation. The half-life of sulfasalazine is 5-10 hours, sulfapyridine is 6-14 hours, 5-ASA is 0.6-1.4 hours. It is excreted through the intestines - 5% sulfapyridine and 67% 5-ASA, kidneys - 75-91% absorbed sulfasalazine (within 3 days).

• Nonspecific ulcerative colitis (treatment of exacerbations and maintenance therapy in the remission phase);
• Crohn's disease (mild and moderate forms in the acute phase);
• Rheumatoid arthritis; juvenile rheumatoid arthritis.

During pregnancy, the appointment of the drug is possible only according to strict indications and in a minimally effective dose. If the course of the disease allows, then in the last trimester of pregnancy, the drug should be discontinued.

If necessary, the appointment of sulfasalazine-EN during lactation should decide on the termination of breastfeeding.

• Hypersensitivity to sulfasalazine or other components of the drug sulfasalazine-EN, as well as sulfonamides or salicylates;
• porphyria;
• granulocytopenia;
• aplastic anemia;
• congenital deficiency of glucose-6-phosphate dehydrogenase (risk of jaundice);
• hepatic and / or renal failure;
• children under 10 years old and / or weighing 35 kg with a chronic inflammatory bowel disease; children under 6 years of age with juvenile rheumatoid arthritis (for a given dosage form and dosage) (efficacy and safety not proven);
• lactation period.

With caution: bronchial asthma, an allergic reaction in history (a cross-allergic reaction to furosemide, thiazide diuretics, sulfonylurea derivatives, carbonic anhydrase inhibitors is possible), systemic forms of juvenile rheumatoid arthritis (risk of developing serum sickness); pregnancy.

Side effects are associated with the degree of plasma concentration of sulfapyridine, especially in people with slow acetylation. More often side effects are observed in patients with rheumatoid arthritis.

From the central and peripheral nervous system: headache, peripheral neuropathy, vertigo, dizziness, hallucinations, cramps, ataxia, sleep disturbance, depression, aseptic meningitis.

From the gastrointestinal tract: nausea, vomiting, diarrhea, decreased appetite, pancreatitis, stomatitis, abdominal pain, drug hepatitis.

From the hemopoietic organs: macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia due to enzymatic disorders - with unstable hemoglobin molecules (Heinz-Erlich bodies), methemoglobinemia, agranulocytosis, thrombocytopenia.

From the genitourinary system: proteinuria, hematuria, crystalluria, nephrotic syndrome, transient oligospermia and infertility.

From the respiratory system: shortness of breath, cough, interstitial pneumonitis, fibrosing alveolitis, lung tissue infiltrates.
From the sensory organs: tinnitus.

Laboratory data: hyperbilirubinemia, increased activity of alkaline phosphatase, "liver" transaminases.

Allergic reactions: generalized skin rash, urticaria, erythema, pruritus, exfoliative dermatitis, photosensitization, toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema (Stevens-Johnson syndrome), fever, lymphadenopathy, serum otorrhiza, periomatosis, periomatosis, periomatosis, periomatosis polyarteritis, anaphylactic shock.

Other: hyperthermia, mumps, possibly staining of urine, skin or soft contact lenses in yellow-orange color.

Sulfasalazine reduces the absorption of folic acid and digoxin. Enhances the effect of anticoagulants, antiepileptic and oral hypoglycemic agents, as well as side effects of cytostatics, immunosuppressants, hepato- and nephrotoxic agents.

Medicines that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

Antibiotics due to the inhibitory effect on the intestinal flora reduce the effectiveness of ulcerative colitis.

Inside, after a meal.

Nonspecific ulcerative colitis, Crohn's disease:
Adults and children over 16 years of age: on the first day, 500 mg 4 times a day; on the 2nd day, 1 g 4 times a day; on the 3rd and subsequent days, 1.5-2 g 4 times a day. After the acute clinical symptoms of ulcerative colitis subside, adults and adolescents and / or with a body weight of more than 65 kg are prescribed a maintenance dose of 500 mg 3-4 times a day for several months.
Children from 10 years to 16 years and / or body weight from 35 kg to 50 kg: 500 mg 4 times a day.
Supportive therapy for children and adolescents under 16 years of age and / or body weight less than 65 kg is not recommended.
The maximum daily dose for adults is 8 g, for children under 16 years - 2 g.

Rheumatoid arthritis
Adults and children over 16 years of age: during the first week, 500 mg are prescribed once a day, during the second - 500 mg 2 times a day, during the third - 500 mg 3 times a day, etc. The therapeutic dose may be from 1.5 g to 3 g per day. The clinical effect appears after 6-10 weeks of therapy. The course of treatment is 6 months or more.
Children from 6 to 8 years and / or body weight from 20-29 kg: 1 tablet 2 times a day.
Children from 8 to 12 years old and / or body weight from 30-39 kg: 1 tablet 2-3 times a day.
Children from 12 to 16 years old and / or body weight from 40-50 kg: 1 tablet 3 times a day or 2 tablets 2 times a day.
Children over 16 years old and / or weighing more than 50 kg: 2 tablets 2 times a day. The maximum daily dose for children is 2 g or 40-50 mg / kg body weight.

Symptoms: nausea, vomiting, abdominal pain, dizziness. When using very high doses, the following can occur: anuria, crystalluria, hematuria, symptoms of toxic damage to the central nervous system (convulsions).

Treatment: symptomatic. Necessary: ​​provoke vomiting, rinse the stomach, intestines; alkalize urine, forced diuresis. For anuria and / or kidney failure: fluid and electrolyte intake should be limited.

During the treatment period, periodic monitoring of the level of “liver” enzymes in blood plasma, a general blood test (at the beginning of therapy: 1-2 times a month, then every 3-6 months of treatment) and urinalysis (with renal failure), the use of an increased amount is recommended liquids.

Sulfasalazine is recommended for patients with caution with systemic forms of juvenile rheumatoid arthritis, as there is a risk of developing unwanted effects, including serum sickness (fever, nausea, vomiting, headache, rash and impaired liver function).

Influence on the ability to drive a car and other mechanical means: there were no reports of a significant effect of Sulfasalazin-EN on the ability to drive a car and other mechanisms.

Enteric Coated Tablets