Sulfasalazin-EH (sulfasalazine) enteric tablets 500 mg. №50

Description

Sulfasalazin-EH (sulfasalazine) enteric tablets 500 mg. №50

Composition

active substance: sulfasalazine;

1 tablet contains 500 mg of sulfasalazine;

Excipients: povidone, pregelatinized starch, magnesium stearate, colloidal anhydrous silica, titanium dioxide (E 171), iron oxide yellow (E 172), talc, triethyl citrate, macrogol 6000, sodium carboxymethylcellulose (methyl cellulose), metallurgy.

Dosage form

Intestinal soluble tablets.

Main physical and chemical properties: round, light brown, slightly biconvex tablets, film-coated.

Pharmacotherapeutic group

Anti-inflammatory drugs used in intestinal diseases. Aminosalicylic acid and similar agents. Sulfasalazine.
ATX code A07E C01.

Pharmacological properties

It is an anti-inflammatory agent used for bowel diseases. It has an immunosuppressive effect – it suppresses the proliferation of killer cells, the transformation of lymphocytes. Locally inhibits cyclooxygenase, lipoxygenase in the intestinal wall, preventing the formation of leukotrienes, prostaglandins, and other inflammatory mediators.

Indications

Sulfasalazin-EH tablets shown:

• for the induction and maintenance of remission in ulcerative colitis;
• for the treatment of active Crohn’s disease;
• for the treatment of rheumatoid arthritis in case of insufficient effectiveness of NSAIDs;
• for the treatment of juvenile polyarticular / oligosarticular rheumatoid arthritis.

Contraindications

The drug Sulfasalazin-EH tablets is not used:

• with intolerance to the components;
• with intestinal obstruction;
• with obstruction of the urinary tract;
• with porphyria;
• with severe renal dysfunction (GFR less than 30 ml / minute / 1.7 Zm2);
• with severe liver dysfunction;
• in the presence of severe asthma attacks, urticaria, rhinitis, and other manifestations of allergy caused by the intake of acetylsalicylic acid, other NSAIDs in history;
• children under 6 years old.

Application during pregnancy and lactation

There is no data on the risk of teratogenic effects. The likelihood of negative effects on the fetus during pregnancy is low.
Since the harmful effect is not completely excluded, the drug is used during pregnancy if absolutely necessary.
Sulfasalazine passes into breast milk.

Method of administration and dosage

The dose should be selected individually, taking into account the severity of the disease and tolerability of the drug.

Patients should take the tablets with a meal. The tablets should be swallowed whole, do not break or crush, drink 1 glass of liquid.

If the patient misses the next dose, it should be taken as soon as possible. If the next dose is approaching, the recommended treatment schedule should be extended (without doubling the dose).

Ulcerative colitis

Initial therapy

Adults: 3-4 g per day in evenly divided doses with intervals between doses of not more than 8 hours. It is recommended to start therapy with lower doses, such as 1-2 g per day, to reduce possible intolerance of the gastrointestinal tract. If a daily dose of more than 4 g is required to achieve the desired therapeutic effect, the increased risk of toxic reactions should be considered.

Children over 6 years of age: dose 40-60 mg / kg body weight for each 24-hour period, divided into 3-6 doses. The drug is not recommended for children for whom a single dose, calculated based on their body weight, is less than 1 tablet (500 mg).

Supportive therapy

Adults: 2 g per day.

Children over 6 years of age: dose of 30 mg / kg body weight for each 24-hour period, divided into 4 doses. The drug is not recommended for children for whom a single dose, calculated based on their body weight, is less than 1 tablet (500 mg).

The efficacy of Sulfasalazin-EH tablets in acute ulcerative colitis can be assessed by clinical criteria, including fever, changes in body weight and the degree and frequency of diarrhea and bleeding, and by sigmoscopy and evaluation of biopsy specimens. It is often necessary to continue taking the drug, even if clinical symptoms, including diarrhea, have been controlled. If the endoscopic examination confirms a satisfactory degree of improvement, the dose of Sulfasalazin-EH should be reduced to maintenance. If diarrhea occurs again, the dose should be increased to the previous effective dose.

Sulfasalazin-EH tablets, in particular, is indicated for patients who cannot take sulfasalazine tablets without a shell due to gastrointestinal intolerance (eg loss of appetite, nausea). If symptoms of gastric intolerance (loss of appetite, nausea, vomiting, etc.) are observed with the first few doses of Sulfasalazin-EH, they are probably due to increased total levels of sulfapyridine in serum and may be reduced by reducing the daily dose of Sulfasalazin-EH doubled, followed by its gradual increase over several days. If gastric intolerance persists, the drug should be discontinued for 5-7 days and then restarted at lower daily doses.

Rheumatoid arthritis in adults

2 g per day in two equal doses. It is recommended to start therapy with lower doses of the drug Sulfasalazin-EH tablets, such as 0.5-1 g per day to reduce possible intolerance of the gastrointestinal tract. The recommended dosing regimen is given below.

In rheumatoid arthritis, the effect of the drug Sulfasalazin-EH tablets can be assessed by the degree of improvement, the number of joints with active inflammation and its severity. Therapeutic efficacy is observed as early as 4 weeks after starting treatment with the drug, but some patients may require treatment for 12 weeks before clinical benefits are identified. The possibility of increasing the daily dose to 3 g may be considered if clinical efficacy after 12 weeks is insufficient. Careful monitoring of the patient at a dose of more than 2 g per day is recommended.

Recommended dosage regimen for rheumatoid arthritis in adults:

Juvenile rheumatoid arthritis with polyarthritis syndrome

The drug Sulfasalazin-EH tablets is not recommended for children for whom a single dose is calculated based on their body weight, is less than 1 tablet (500 mg).

Children over 6 years of age: 30-50 mg / kg body weight per day, divided into 2 dose levels. Usually the maximum dose is 2 g per day. To reduce possible gastrointestinal intolerance, start with a quarter or a third of the planned maintenance dose and increase it every week until the maintenance dose is reached after 1 month.

Some patients may be sensitive to sulfasalazine treatment. Various desensitization regimens have been reported to be effective in 34 of 53 patients, 7 of 8 patients, and 19 of 20 patients. These regimens suggest that you should start with an initial total daily dose of 50-250 mg of sulfasalazine with doubling the dose every 4-7 days to obtain the desired therapeutic level. If symptoms of sensitivity occur, treatment with the drug should be discontinued. Desensitization should not be performed in patients with a history of agranulocytosis or in patients who have experienced an anaphylactoid reaction to a previous dose of sulfasalazine.

Children

The safety and efficacy of the drug in patients under 2 years of age with ulcerative colitis have not been established.

The safety and efficacy of the drug in the treatment of signs and symptoms of juvenile rheumatoid arthritis with polyarthritis syndrome in patients aged 6 to 16 years have been confirmed by appropriate well-controlled studies in adult patients with rheumatoid arthritis. Extrapolation of data from adult patients with rheumatoid arthritis to children with juvenile rheumatoid arthritis with polyarthritis syndrome is based on the similarity of the disease and the effectiveness of therapy in these two groups of patients. Published research confirms the possibility of extrapolating data on the safety and efficacy of sulfasalazine in juvenile rheumatoid arthritis with polyarthritis syndrome.

A high incidence of adverse events has been reported in patients with systemic juvenile arthritis. The use of the drug in children with systemic juvenile rheumatoid arthritis often resulted in a serum-like reaction. This reaction was often severe and manifested by fever, nausea, vomiting, headache, rash, and abnormal liver function tests. Treatment with sulfasalazine in the systemic course of juvenile rheumatoid arthritis is not recommended.

Overdose

Symptoms: vomiting, abdominal pain, drowsiness, convulsions, kidney dysfunction, methemoglobinemia, sulfhemoglobinemia.
In case of an overdose, gastric lavage (or stimulation of vomiting) is performed, laxatives and infusion therapy are prescribed.

Side effects:

• Hematological disorders: macrocytosis, pancytopenia, agranulocytosis, aplastic anemia, megaloblastic anemia, hypoprothrombinemia, purpura, methemoglobinemia, congenital neutropenia, myelodysplastic syndrome.
• Immune disorders: epidermal necrolysis, anaphylaxis, erythema multiforme, interstitial lung disease, exfoliative dermatitis, drug rash with eosinophilia, DRESS syndrome, serum sickness, pneumonitis with / without eosinophilia, fibrosing alveolitis, vasculitis, pleuriditis without tamponade, periarteritis nodosa, hepatitis, liver necrosis with / without immune complexes, lupus-like syndrome, fulminant hepatitis, Much-Habermann syndrome, photosensitivity, rhabdomyolysis, arthralgia, alopecia, periorbital edema, hypersensitivity reactions.
• Gastrointestinal disorders: hepatitis, pancreatitis, liver failure, impaired absorption of folic acid, bloody diarrhea, stomatitis, impaired absorption of digoxin, diarrhea, neutropenic enterocolitis, abdominal pain, exacerbation of ulcerative colitis.
• Mental Disorders: Depressive Syndrome.
• Neurological disorders: dysgeusia, seizures, transverse myelitis, transverse lesion of the posterior cord of the spinal cord, meningitis, cauda equina syndrome, encephalopathy, Guillain-Barré syndrome, peripheral neuropathy, dizziness, depression of mental functions, hearing loss, dysosmia, insomnia, hallucinations, tinnitus, drowsiness.
• Genitourinary disorders: nephrotic syndrome, toxic nephropathy with anuria / oliguria, nephritis, hematuria, urinary tract infections, crystalluria, hemolytic uremic syndrome, proteinuria, interstitial nephritis.
• Others: discoloration of the skin, alopecia, erythema, facial edema, discoloration of urine, pseudomonucleosis.