Sulfasalazine-EN, 500 mg 50 pcs

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

Sulfasalazine selectively accumulates in the intestinal connective tissue with 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 are absorbed from the small intestine, the remaining 70% are cleaved by the intestinal microflora to form 60-80% sulfapyridine and 25% 5-ASC. Sulfasalazine reaches maximum concentration 3-12 hours after intake of enteric coated tablets. Sulfasalazine plasma protein binding is 99%, sulfapyridine – 50%, 5-ASC – 43%.

Sulfapyridine is metabolized in the liver by hydroxylation to form inactive metabolites, 5-ASC – by acetylation. Half-life of sulfasalazine is 5-10 hours, of sulfapyridine – 6-14 hours, of 5-ASC – 0.6-1.4 hours. Excretion through the intestine is 5% of sulfapyridine and 67% of 5-ASC, by the kidneys – 75-91% of the absorbed sulfasalazine (within 3 days).

Indications

Active ingredient

Composition

1 enteric-coated tablet contains:

the active ingredient:

sulfasalazine,

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

excipients:

Pregelatinized starch,

Magnesium stearate,

colloidal silicon dioxide,

anhydrous.

How to take, the dosage

Internal, after meals.

Non-specific ulcerative colitis, Crohn’s disease:
Adults and children over 16 years old: on the 1st day 500 mg 4 times daily; on the 2nd day 1 g 4 times daily; on the 3rd and subsequent days 1.5-2 g 4 times daily. After acute clinical symptoms of ulcerative colitis subside, a maintenance dose of 500 mg 3-4 times daily for several months is prescribed to adults and adolescents and/or those with body weight over 65 kg.
For children aged 10-16 years old and/or with body mass from 35 kg to 50 kg: 500 mg 4 times a day.
Maintenance therapy for children and adolescents under 16 years old and/or with body mass less than 65 kg is not recommended.
Maximal daily dose for adults is 8 g, for children under 16 years old – 2 g.

Rheumatoid arthritis
Adults and children over 16 years: during the first week, 500 mg once a day, during the second – 500 mg 2 times a day, during the third – 500 mg 3 times a day, and so on. The therapeutic dose may be from 1.5 g to 3 g per day. Clinical effect appears after 6-10 weeks of therapy. The course of therapy is 6 months and more.
Children of 6 to 8 years of age and/or body weight of 20-29 kg: 1 tablet 2 times a day.
Children of 8 to 12 years of age and/or body weight of 30-39 kg: 1 tablet 2-3 times a day.
Children aged 12 to 16 years 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 of body weight.

Interaction

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

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

Antibiotics due to their depressing effect on intestinal flora decrease effectiveness in ulcerative colitis.

Special Instructions

A periodic control of plasma “liver” enzymes, general blood count (at the beginning of therapy: 1-2 times a month, then every 3-6 months of treatment) and urinalysis (if renal insufficiency), increased fluid intake is recommended during treatment.

Sulfasalazine is recommended for patients with systemic forms of juvenile rheumatoid arthritis with caution because there is a risk of adverse effects, including serum sickness (fever, nausea, vomiting, headache, rash and liver dysfunction).

Impact on the ability to drive and other mechanical devices: There have been no reports of significant effects of Sulfasalazine-EN on the ability to drive and other mechanisms.

Contraindications

With caution: bronchial asthma, history of allergic reactions (cross-allergic reaction to furosemide, thiazide diuretics, sulfonylurea derivatives, carbohydrate inhibitors is possible), systemic forms of juvenile rheumatoid arthritis (risk of serum disease); pregnancy.

Side effects

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.

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

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

Hematopoietic organs: Macrocytosis, leukopenia, neutropenia, megaloblast anemia, hemolytic anemia, hemolytic anemia due to enzyme disorders – with unstable hemoglobin molecules (Heinz-Ehrlich bodies), methemoglobinemia, agranulocytosis, thrombocytopenia, egoic anemia, hypoprotrombinemia.

Urogenital system disorders: proteinuria, hematuria, crystalluria, nephrotic syndrome, transient oligospermia and infertility.

Respiratory system: dyspnea, cough, interstitial pneumonitis, fibrosing alveolitis, lung tissue infiltrates.

Sensory system disorders: tinnitus.

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

Allergic reactions: Generalized skin rash, urticaria, erythema, skin itching, exfoliative dermatitis, photosensitization, toxic epidermal necrolysis (Lyell syndrome), malignant exudative erythema (Stevens-Johnson syndrome), fever, lymphoadenopathy, serum disease, periorbital edema, eosinophilia, nodular polyarteritis, anaphylactic shock.

Others: hyperthermia, parotitis, possible yellow-orange coloring of urine, skin, or soft contact lenses.

Overdose

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

Treatment: symptomatic. Necessary: provoke vomiting, gastric lavage, bowel washing; conduct alkalinization of urine, forced diuresis. If anuria and/or renal failure: fluid and electrolyte intake should be limited.

Pregnancy use

In pregnancy, the drug may be administered only with strict indications and in the lowest effective dose. The drug should be discontinued in the last trimester of pregnancy if the course of the disease permits.

If it is necessary to prescribe Sulfasalazine-EN during lactation, discontinuation of breastfeeding should be considered.

Similarities