Active substanceSulfasalazineSulfasalazine
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  • Sulfasalazine
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  • Sulfasalazine
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    ATOLL, LLC     Russia
  • Sulfasalazine-native
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    NATIVA, LLC     Russia
  • Dosage form: & nbsptfilm-covered laths
    Composition:On 1 tablet:

    Active substance: sulfasalazine - 500.0 mg.

    Excipients: pregelatinized starch - 115.0 mg, sodium carboxymethyl starch - 29.0 mg, povidone-K25 - 24.0 mg, magnesium stearate - 7.0 mg, silicon dioxide colloid - 5.0 mg.

    Shell composition: hypromellose - 8,4 mg, macrogol-4000 - 2,1 mg, titanium dioxide - 4,1 mg, ferric oxide yellow oxide - 0,4 mg.

    Description:

    Round, biconvex tablets, covered with a film coat from light yellow to brownish-yellow color. On the cross section of the tablet, two layers are visible: a brownish-yellow core and a film membrane.

    Pharmacotherapeutic group:antimicrobial and anti-inflammatory intestinal
    ATX: & nbsp

    J.04.A.A   Aminosalicylic acid and its derivatives

    Pharmacodynamics:

    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.

    Pharmacokinetics:

    About 30% of sulfasalazine in film-coated tablets is absorbed from the small intestine, the remaining 70% are digested with intestinal microflora with the formation of 60-80% sulfiridine and 25% -5-ASA. There are large individual differences in the maximum serum concentrations (CmOh) sulfasalazine and its metabolites; in "slow acetylators" they are higher, which increases the risk of unwanted effects. Sulfasalazine reaches a maximum concentration in 3-12 hours after taking the tablets coated with a film membrane.

    Linkage with plasma proteins 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 (T1/2) sulfasalazine - 5-10 h, sulfapiridine - 6-14 h, 5-ASA - 0.6-1.4 h. Intestine is removed 5% sulfapyridine and 67% 5-ASA, kidneys - 75-91% of the absorbed sulfasalazine (in for 3 days).

    Indications:

    - Ulcerative colitis (treatment of exacerbations and maintenance therapy in the remission phase);

    - Crohn's disease (mild and moderate forms in the phase of exacerbation);

    - rheumatoid arthritis; juvenile rheumatoid arthritis with ineffectiveness of non-steroidal anti-inflammatory drugs (NSAIDs).

    Contraindications:

    - Hypersensitivity to sulfasalazine or other components of the drug, as well as sulfonamides or salicylates;

    - porphyria;

    - granulocytopenia;

    - aplastic anemia;

    - congenital deficiency of glucose-6-phosphate dehydrogenase (risk of jaundice development);

    - hepatic and / or renal insufficiency;

    - children under 10 years of age and / or body weight of 35 kg or less, with chronic inflammatory bowel diseases (for this dosage form and dosage);

    - obstruction of the intestine or urinary tract;

    - Children younger than 6 years with juvenile rheumatoid aarthritis (efficacy and safety not established);

    - the period of breastfeeding.
    Carefully:

    Bronchial asthma, atopic dermatitis, allergic reactions in the anamnesis (allergic reactions to furosemide, thiazide diuretics, sulfonylurea derivatives, carbonic anhydrase inhibitors are possible), systemic forms of juvenile rheumatoid arthritis (risk of developing serum sickness); pregnancy.

    Pregnancy and lactation:

    During pregnancy, prescription of the drug is possible only on 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 stopped (sulfasalazine displaces bilirubin from the connection with plasma proteins, thereby increasing the risk of developing nuclear jaundice and hyperbilirubinemia in newborns - toxic damage to the nerve centers of the brain). In newborns with deficiency of glucose-6-phosphate dehydrogenase, the development of hemolytic anemia is possible.

    Sulfasalazine is normally secreted into mother's milk in very small amounts; in preterm infants and in children at high risk, the risk of developing nuclear jaundice increases. The concentration of sulfapiridine in mother's milk is 40% of the concentrations in the mother's plasma. If it is necessary to use sulfasalazine during lactation, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside, after eating.

    Ulcerative colitis, Crohn's disease

    Adults and children over 16 years of age: in the first day - 500 mg 4 times a day; in the 2 nd - 1 g 4 times a day; in the third and subsequent days - 1,5-2 g 4 times a day.

    After the acute clinical symptoms of ulcerative colitis subsided, adults and adolescents and / or body weight over 65 kg are prescribed a maintenance dose of 500 mg 3-4 times a day for several months.

    Children from 10 to 16 years and / or body weight from 35 to 50 kg - 500 mg 4 times a day.

    Supportive therapy for children and adolescents under 16 and / or body weight less than 65 kg is not recommended.

    The maximum daily intake for adults is 8 g, for dechildren under 16 years old - 2 y.

    Rheumatoid arthritis and juvenile rheumatoid arthritis

    Adults and children over 16 years of age: during the first week - 500 mg once a day, during the second - 500 mg twice a day, third and then - 500 mg 3 times a day.

    The therapeutic dose can be from 1.5 to 3 g / day. The clinical effect is manifested 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 of 20-29 kg: 1 tab. 2 times a day;

    Children from 8 to 12 years of age and / or body weight of 30-39 kg: 1 tab. 2-3 times a day;

    Children from 12 to 16 years of age and / or body weight of 40-50 kg: 1 tab. 3 times a day or 2 tablets. 2 times a day;

    Children over 16 years of age and / or body weight over 50 kg: 2 tab. 2 times a day.

    The maximum daily dose for children is 2 g or 40-50 mg / kg body weight.

    Side effects:

    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, dizziness, sleep disturbance, hallucinations, ataxia, convulsions, depression, aseptic meningitis.

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

    On the part of the organs of hematopoiesis: macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia due to enzymatic disorders - with unstable hemoglobin molecules (Heinz-Ehrlich body), methemoglobinemia, agranulocytosis, thrombocytopenia, aplastic anemia, hypoprothrombinemia.

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

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

    From the sense organs: noise in ears.

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

    Allergic reactions: generalized skin rash, urticaria, erythema, pruritus, exfoliative dermatitis, photosensitivity, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), fever, lymphadenopathy, serum sickness, periorbital edema, eosinophilia, periarteritis nodosa, anaphylactic shock.

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

    Overdose:

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

    Treatment: symptomatic. It is necessary: ​​to provoke vomiting, to wash the stomach, intestines; urine alkalinization, forced diuresis. In anuria and / or renal failure, fluid and electrolyte intake should be limited.

    Interaction:

    Sulfasalazine reduces the absorption of folic acid and digoxin.

    Strengthens the effect of anticoagulants, antiepileptic and oral hypoglycemic agents, as well as side effects of cytostatics, immunosuppressants, hepato- and nephrotoxic agents.

    Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

    Antibacterial agents, in connection with the oppressive effect on the intestinal flora, reduce the effectiveness of sulfasalazine in ulcerative colitis.

    Special instructions:

    During the period of treatment, periodic monitoring of the activity of liver enzymes in the 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 increased amount of liquid.

    Sulfasalazine is recommended with caution to appoint patients with systemic forms of juvenile rheumatoid arthritis, t. there is a risk of unwanted effects, incl. serum sickness (fever, nausea, vomiting, headache, skin rash, impaired liver function).

    Effect on the ability to drive transp. cf. and fur:Care must be taken when driving vehicles and working with complex technical devices in connection with the possibility of dizziness.
    Form release / dosage:

    Tablets, film-coated, 500 mg.

    Packaging:

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    10, 20, 30, 40, 50, 60 or 100 tablets in cans of polyethylene terephthalate for medicinal products sealed with caps screwed on with first opening control or by a "push-turn" system of polypropylene or polyethylene or polypropylene cans for drugs sealed with lids stretched with the control of the first opening of polyethylene or cans of polypropylene for drugs, sealed with lids pulled with the control of the first opening of high-pressure polyethylene.

    One jar or 1, 2, 3, 4, 5, 6 or 10 contour squares, together with the instructions for use, are placed in a cardboard package (bundle).

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003765
    Date of registration:04.08.2016
    Expiration Date:04.08.2021
    The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspOZONE LLC OZONE LLC Russia
    Information update date: & nbsp20.08.2016
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