Instructions for Sulfasalazine
Sulfasalazine , an anti-inflammatory drug used to treat Crohn's disease and NUC, is an intestinal antimicrobial drug.
Sulfasalazine selectively accumulates in the connective tissue of the intestine 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 degraded by the intestinal microflora to form sulfapyridine and 5-ASA, 60-80% and 25%, respectively. There are large individual differences in the maximum serum concentrations (Cmax) of sulfasalazine and its metabolites; in "slow acetylators" they are higher, which increases the risk of undesirable effects. Sulfasalazine reaches Cmax in blood plasma 3-12 hours after taking enteric-coated tablets.
The connection with blood plasma proteins of sulfasalazine - 99%, sulfapyridine - 50%, 5-ASA - 43%. Sulfapyridine is metabolized in the liver by hydroxylation with the formation of 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% of sulfapyridine and 67% of 5-ASA, by the kidneys - 75-91% of the absorbed sulfasalazine (within 3 days).
Sulfasalazine Indications for use:
Ulcerative colitis (treatment of exacerbations and maintenance therapy in remission);
Crohn's disease (mild and moderate forms in the acute phase);
rheumatoid arthritis, juvenile rheumatoid arthritis with ineffectiveness of nonsteroidal anti-inflammatory drugs (NSAIDs).
Mode of application Sulfasalazine:
Inside, after eating.
Ulcerative colitis, Crohn's disease
Adults and children over 16 years old: on the 1st 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 have subsided, adults and children over 16 years of age and / or weighing more than 65 kg are prescribed a maintenance dose of 500 mg 3-4 times a day for several months.
Children aged 10 to 16 years and / or weighing from 35 kg to 50 kg: 500 mg 4 times a day. Supportive therapy for children under 16 years of age and / or weighing less than 65 kg is not recommended.
The maximum daily dose for adults is 8 g, for children under 16 years of age - 2 g.
Rheumatoid arthritis and juvenile rheumatoid arthritis
Adults and children over 16 years old: during the first week, appoint 500 mg 1 time per day, during the second week - 500 mg 2 times a day, during the third week - 500 mg 3 times a day, etc. The therapeutic dose can range 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 old and / or weighing 20-29 kg: 1 tablet 2 times a day.
Children from 8 to 12 years old and / or weighing 30-39 kg: 1 tablet 2-3 times a day.
Children from 12 to 16 years old and / or weighing 40-50 kg: 1 tablet 3 times a day or 2 tablets 2 times a day.
Children over 16 years of age 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 of body weight.
Ulcerative colitis, Crohn's disease:
Adults and children over 16 years of age: on the 1st 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 have subsided, adults and adolescents and / or those weighing 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 old and / or weighing 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 weighing less than 65 kg is not recommended.
The maximum daily dose for adults is 8 g, for children under 16 years of age - 2 g.
Rheumatoid arthritis and juvenile rheumatoid arthritis
Adults and children over 16 years of age: during the first week, appoint 500 mg 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 can range 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 old and / or weighing from 20-29 kg: 1 tablet 2 times a day.
Children from 8 to 12 years old and / or weighing from 30-39 kg: 1 tablet 2-3 times a day.
Children from 12 to 16 years old and / or weighing from 40-50 kg: 1 tablet 3 times a day or 2 tablets 2 times a day.
Children over 16 years of age 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 of body weight.
Side effects Sulfasalazine:
Side effects are related to the degree of plasma concentration of sulfapyridine, especially in people with slow acetylation.
More often, side effects are observed in patients with rheumatoid arthritis.
Disorders from the blood and lymphatic system: macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia due to enzyme disorders - with unstable hemoglobin molecules (Heinz-Ehrlich bodies), methemoglobinemia, agranulocytosis, thrombocytopenia, aprotopenia.
Immune system disorders: generalized skin rash, urticaria, erythema, pruritus, exfoliative dermatitis, photosensitivity, fever, lymphadenopathy, serum sickness, periorbital edema, eosinophilia, periarteritis nodosa, anaphylactic shock.
Mental disorders: hallucinations, depression.
Nervous system disorders: headache, peripheral polyneuropathy, vertigo, dizziness, convulsions, ataxia, sleep disturbance, aseptic meningitis.
Hearing disorders and labyrinthine disorders: tinnitus.
Disturbances from the respiratory system, chest and mediastinal organs: shortness of breath, cough, interstitial pneumonitis, fibrosing alveolitis, infiltrates in the lung tissue.
Digestive system disorders: nausea, vomiting, diarrhea, loss of appetite, pancreatitis, stomatitis, abdominal pain, drug hepatitis.
Skin and subcutaneous tissue disorders: Severe skin adverse reactions: Very rare cases of Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) have been reported.
Renal and urinary tract disorders: proteinuria, hematuria, crystalluria, nephrotic syndrome.
Genital and breast disorders: transient oligospermia and infertility.
Laboratory and instrumental data: hyperbilirubinemia, increased activity of alkaline phosphatase, "hepatic" transaminases in blood plasma.
General disorders and disorders at the injection site: pyrexia, parotitis, yellow-orange staining of urine, skin or soft contact lenses is possible.
