Sulfasalazine-EH - instructions for use, doses, side effects, contraindications

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Dosage form: & nbsp

Tablets, covered with enteric coating.

Composition:

1 tablet contains:

CORE:

Active substance:

sulfasalazine, coated with povidone (corresponding to 500 mg of sulfasalazine) 535,000 mg

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

SHELL:

Titanium dioxide, iron oxide oxide yellow 10 (E172), talc, triethyl citrate, macrogol-6000, carmellose sodium, methacrylic acid and ethyl acrylate copolymer (1: 1) (dry matter).

Description:Round biconvex tablets with bevelled edge, covered with a coating from yellow to brownish-yellow with a characteristic odor. View at a break: from orange to brownish-orange.

Pharmacotherapeutic group:Antimicrobial and anti-inflammatory intestinal.

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 against diplococci, streptococci, gonococci, E. coli.

Pharmacokinetics:

About 30% of sulfasalazine in enteric coated tablets is absorbed from the small intestine,the remaining 70% are digested with intestinal microflora with the formation of sulfapyridine 60-80% and 25% - 5-ASA. Sulfasalazine reaches a maximum concentration in 3-12 hours after taking the tablets, covered with an enteric coating. 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. Half-life of sulfasalazine is 5-10 hours, sulfapyridine is 6-14 hours, 5-ASA is 0.6-1.4 hours. 5% of sulfapyridine and 67% of 5-ASA are excreted through the intestine, 75-91% of the absorbed kidneys sulfasalazine (within 3 days).

Indications:

- Nonspecific 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.

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 with chronic inflammatory bowel disease; children younger than 6 years with juvenile rheumatoid arthritis (for this dosage form and dosage) (efficacy and safety not proven);

- lactation period.

Carefully:Bronchial asthma, an allergic reaction in the anamnesis (a possible allergic reaction 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.

If it is necessary to prescribe Sulfasalazine-EH during lactation, the question of stopping breastfeeding should be resolved.

Dosing and Administration:

Inside, after eating.

Nonspecific ulcerative colitis, Crohn's disease:

Adults and children over 16 years of age: in 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 with a body weight of more than 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 - 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 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 from 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 and / or with a 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, vertigo, 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), methemoglobinemia, agranulocytosis, thrombocytopenia, aplastic anemia, hypoprothrombinemia.

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, 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, toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema (Stevens-Johnson syndrome), fever, lymphadenopathy, serum sickness, periorbital edema, eosinophilia, nodular polyarteritis, 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.With anuria and / or renal failure: intake of fluid and electrolytes 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, increase the risk of myelosuppression. Antibiotics in connection with the oppressive effect on the intestinal flora reduce the effectiveness of ulcerative colitis.

Special instructions: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 insufficiency), the use of increased amounts liquid. Sulfasalazine It is recommended to appoint patients with caution with systemic forms of juvenile rheumatoid arthritis, there is a risk of unwanted effects, incl. Serum sickness (fever, nausea, vomiting, headache, rash and liver dysfunction).

Effect on the ability to drive transp. cf. and fur:There have been no reports of a significant effect of Sulfasalazine-EH on the ability to drive and other mechanisms.

Form release / dosage:Tablets, coated with enteric coating of 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. Keep out of the reach of children.

Shelf life:

5 years.KRK

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015099 / 01

Date of registration:25.11.2008

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-EH (Sulfasalazin-EN)