Sulfasalazine - instructions for use, dose, side effects, contraindications

Active substanceSulfasalazineSulfasalazine

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Sulfasalazine

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KRKA, dd, Novo mesto, AO

Sulfasalazine

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ATOLL, LLC Russia

Sulfasalazine-native

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NATIVA, LLC Russia

Dosage form: & nbspFilm-coated tablets.

Composition:

1 tablet contains:

CORE:

Active substance:

Sulfasalazine, coated with povidone *, 535.00 mg (corresponding to 500 mg of sulfasalazine);

Excipients: starch pregelatinized, magnesium stearate, silicon dioxide colloidal, anhydrous;

SHELL: hypromellose, propylene glycol.

* Sulfasalazine, coated with povidone contains: sulfasalazine, povidone 3%, water.

Description:Round, slightly biconcave tablets with a bevel, brownish-yellow color, covered with a transparent, colorless film membrane. Blotches of a lighter color are allowed.

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 to form sulfapyridine 60-80% and 25% -5-ASA. There are large individual differences in the maximum serum concentrations (Ssh) of 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 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. Intestine is 5% sulfapyridine and 67% 5-ASA, kidney 75% 91% of the absorbed sulfasalazine (within 3 days).

Indications:

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

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

- Rheumatoid arthritis; juvenile rheumatoid arthritis with inoperative 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 disease (for this dosage form and dosage);

- obstruction of the intestine or urinary tract;

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

- lactation period.

Carefully:Bronchial asthma, atopic dermatitis, allergic reactions in the anamnesis (possible allergic reactions to furosemide, thiazide diuretics, sulfonylurea derivatives, inhibitors of carbonic anhydrase), 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 bond 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 administer the drug Sulfasalazine During lactation breastfeeding should be discontinued.

Dosing and Administration:

Inside, after taking pshci.

Ulcerative colitis, Crohn's disease:

Adults and children over 16 years: on the first day of 500 mg 4 times a day; on the second day, 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 more 65 kg prescribe 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 and / or body weight less than 65 kg Not recommended.

The maximum daily intake 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, 500 mg once a day, 500 mg twice a day for the second, 500 mg 3 times a day for the third, and so on. The therapeutic dose can 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 of 20-29 kg: 1 tablet 2 times a day.

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

Children from 12 to 16 years of age and / or body weight of 40-50 kg: 1 tablet 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 tablets 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, hallucinations, convulsions, ataxia, sleep disturbance, depression, aseptic meningitis.

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

From the 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 absorption folic acid and digoxin.

Strengthens the action anticoagulants, antiepileptic and oral hypoglycemic funds, as well as side effects cytostatics, immunosuppressants, hepato - and nephrotoxic means.

Medicines that inhibit bone marrow hematopoiesis, increaseck 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 it is recommended with caution that patients with systemic forms of juvenile rheumatoid arthritis should be prescribed. 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:10 tablets per blister. For 5 blisters in a pack of cardboard along with instructions for use.

Storage conditions:At a temperature of no higher than 25 ° C, in the original packaging. Keep out of the reach of children.

Shelf life:

5 years.

Terms of leave from pharmacies:On prescription

Registration number:П N012019 / 01

Date of registration:09.07.2010

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Sulfasalazine (Sulfasalazin)