Sulfasalazine-EN, pills 500mg, 50pcs

Composition

1 tablet, coated with an enteric coating, contains:

Active ingredient:

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

excipients:

pregelatinized starch,

magnesium stearate,

colloidal silicon dioxide,

anhydrous.

Pharmacological action

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

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, and Escherichia coli.

Pharmacokinetics

About 30% of sulfasalazine in enteric coated tablets is absorbed from the small intestine, while the remaining 70% is broken down by the intestinal microflora to form 60-80% sulfapyridine and 25% 5-ASA. Sulfasalazine reaches its maximum concentration 3-12 hours after ingestion of enteric-coated tablets. Binding to 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-6-14 hours,5-ASA-0.6-1.4 hours. It is excreted through the intestine-5% of sulfapyridine and 67% of 5-ASA, kidneys-75-91% of absorbed sulfasalazine (within 3 days).

Indications

• Non-specific 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.

Use during pregnancy and lactation

During pregnancy, the drug can only be prescribed according to strict indications and in the minimum effective dose. If the course of the disease allows, then in the last trimester of pregnancy, the drug should be discontinued.

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

Contraindications

• 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 insufficiency;
• children under 10 years of age and/or body weight of 35 kg with chronic inflammatory disease of the colon; children under 6 years with juvenile rheumatoid arthritis (for this dosage form and dosage) (effectiveness and safety has not been proven);
• lactation.

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

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.

Central and peripheral nervous system disorders: headache, peripheral neuropathy, vertigo, dizziness, hallucinations, seizures, ataxia, sleep disorders, depression, aseptic meningitis.

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

Hematopoietic disorders: macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia due to enzyme disorders – with unstable hemoglobin molecules (Heinz-Ehrlich corpuscles), methemoglobinemia, agranulocytosis, thrombocytopenia, egoistic 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 side of the senses: tinnitus.

Laboratory data: hyperbilirubinemia, increased activity of alkaline phosphatase, “hepatic” 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 sickness, periorbital edema, eosinophilia, polyarteritis nodosa, anaphylactic shock.

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

Interaction

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

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

Antibiotics in connection with the depressing effect on the intestinal flora reduce the effectiveness of ulcerative colitis.

How to take, course of use and dosage

Inside, after eating.

Non-specific 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 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. Maintenance 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 – 2 g.

Rheumatoid arthritisadults and children over 16 years of age: during the first week,500 mg is 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 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 and / or weighing from 20-29 kg: 1 tablet 2 times a day. Children from 8 to 12 years and / or weighing 30-39 kg: 1 tablet 2-3 times a day. Children from 12 to 16 years of age 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.

Overdose

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

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

Special instructions

During treatment, periodic monitoring of the level 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 a urine test (in case of renal failure), the use of an increased amount of fluid are recommended.

Sulfasalazine should be used with caution in patients with systemic forms of juvenile rheumatoid arthritis, as there is a risk of undesirable effects, including serum sickness (fever, nausea, vomiting, headache, rash, and liver dysfunction).

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

Form of production

Enteric coated tablets

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf life

5 years

Active ingredient

Sulfasalazine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets