Sulfasalazine - EN 500mg 50 tablets — Made in Slovenia — Free Delivery

Pharmacological properties

Pharmacodynamics. Sulfasalazine is anti-inflammatory. has an immunosuppressive effect, especially in the connective tissue, intestinal wall and serous fluid, where its concentration is highest. thanks to the intestinal flora, salazosulfapyridine decomposes to sulfapyridine and 5-aminosalicylic acid. sulfapyridine inhibits the proliferation of killer cells and the transformation of lymphocytes.

Sulfasalazine-EH - in the form of enteric tablets, accumulates in the connective tissue of the intestine with the release of 5-aminosalicylic acid, which has an anti-inflammatory effect, and sulfapyridine, which has an antimicrobial effect against diplococci, streptococci, gonococci, Escherichia coli.

The preparation exhibits an immunosuppressive effect, especially in the connective tissue, intestinal wall and serous fluid, where its concentration is highest. Sulfapyridine reduces systemic inflammation and has an antibacterial effect, inhibits the action of natural cell killers and the transformation of leukocytes.

The anti-inflammatory effect of 5-aminosalicylic acid (mesalazine) is most pronounced in the treatment of inflammatory bowel diseases. Basically, 5-aminosalicylic acid locally inhibits COX and lipoxygenase in the intestinal wall and thus prevents the formation of prostaglandins, leukotrienes and other inflammatory mediators. Due to its low absorption, it reduces inflammation in the large intestine.

Pharmacokinetics. About 30% of the dose of sulfasalazine taken is absorbed in the small intestine, and 70% is metabolized by intestinal bacteria in the large intestine to sulfapyridine and 5-aminosalicylic acid. Cmax of sulfasalazine and its metabolites in blood plasma is quite different in different patients - with a low level of acetylation, they are much higher and are associated with frequent cases of side effects. Cmax of sulfasalazine in blood plasma is achieved 3–12 hours after ingestion of enteric tablets and 12–24 hours after taking coated tablets. It binds to blood plasma proteins and penetrates well into connective tissue. The main part of the absorbed amount of sulfasalazine returns with bile to the intestine; a small amount is excreted unchanged in the urine. T1 / 2 sulfasalazine - 5-10 hours

It is metabolized in the liver (by acetylation, hydroxylation and conjugation with glucuronic acid), excreted by the kidneys. T½ - 6-14 hours, depending on the rate of acetylation. Only 30% of 5-aminosalicylic acid is absorbed, acetylated in the liver and excreted in the urine, 70% - unchanged in the feces.

Indications

Sulfasalazine: acute attack or exacerbation of Crohn's disease, ulcerative colitis; to support the period of remission in ulcerative colitis.

Sulfasalazine can be combined with GCS and metronidazole.

Sulfasalazine-EH: inflammatory bowel disease (eg, Crohn's disease, ulcerative colitis);

rheumatoid arthritis in adults, juvenile rheumatoid arthritis (as part of auxiliary therapy).

Application

The dose should be selected individually, taking into account the severity of the disease and the possibility of side effects.

Patients should take the tablets with meals. The tablets must be swallowed whole with a glass of liquid.

If the next dose of the preparation is not taken in a timely manner, you need to take it as soon as possible. If the time for the next dose is approaching, the recommended treatment schedule should be continued (without doubling the dose).

Sulfasalazine

Worsening or worsening of ulcerative colitis and Crohn's disease

Adults are prescribed 2-4 tablets (1-2 g) 4 times a day. After improvement of the condition, the dose should be gradually reduced.

Maintaining the period of remission of ulcerative colitis

The duration of treatment is unlimited. Adults are prescribed 1 tablet (500 mg) 4 times a day.

Sulfasalazine-EH

Inflammatory bowel disease

Acute treatment:

The initial dose for adults is 2-4 tablets (1-2 g) per day. The daily dose must be divided into at least 3 doses. The dose is gradually increased to 3–8 g.

Patients who have not previously taken Sulfasalazine-EH are advised to increase the dose gradually over 9 days.

Children over the age of 6 are recommended to use 40–150 mg / kg of body weight per day. The daily dose must be divided into at least 3 doses.

Maintaining the period of remission

The recommended maintenance dose for adults is 4-6 tablets (2-3 g) per day. The daily dose must be divided into at least 3 doses.

In children over the age of 6 years, use 20–75 mg / kg of body weight per day. The daily dose must be divided into at least 3 doses.

Rheumatoid arthritis and juvenile polyarthritis

The recommended dose for adults is 2 g per day. Patients should start treatment with 1 tablet (500 mg) of sulfasalazine per day. It is necessary to increase the dose of sulfasalazine gradually, at weekly intervals, until a dose of 2 g / day is reached (the daily dose must be divided into 2–4 doses). In some patients, a pronounced clinical effect can be achieved after 12 weeks of treatment. If the clinical effect after 12 weeks of use is insufficient, the daily dose may be increased to 3 g.

In the case of a dose above 2 g / day, it is necessary to constantly monitor the patient's condition.

For children over the age of 6 years, the dose of the preparation is determined by the doctor at the rate of 30–75 mg of sulfasalazine per 1 kg of body weight per day in 2–3 doses. Children tolerate the preparation better if the initial dose is 3-4 times lower than the recommended dose and is gradually increased over the course of a month until the maintenance dose is reached. Children are prescribed no more than 4 tablets (2 g) per day.

Contraindications

Hypersensitivity to sulfasalazine, sulfonamides and salicylates, porphyria, granulocytopenia. childhood. for sulfasalazine-ene - age up to 6 years.

Side effects

Most of the side effects of sulfasalazine are minor and are mainly associated with the degree of concentration of sulfapyridine in the blood plasma, especially in persons with delayed excretion (delayed acetylation). side effects develop mainly in patients with rheumatoid arthritis.

General

Hyperthermia, yellow-orange staining of urine, skin or soft contact lenses.

On the part of the cardiovascular system

Pericarditis.

From the gastrointestinal tract

Often: nausea, vomiting, diarrhea, and loss of appetite.

Rarely: hepatitis, pancreatitis, stomatitis and mumps.

Hematological disorders

Often: macrocytosis (9%), leukopenia (3.7%) and neutropenia (2%).

Rarely: megaloblastic anemia, hemolytic anemia, methemoglobinemia, anemia, agranulocytosis, thrombocytopenia, aplastic anemia, and hypoprothrombinemia.

From the side of the central nervous system

Very often: headache (30%).

Rare: peripheral neuropathy, dizziness, tinnitus, ataxia, insomnia, hallucinations, convulsions, and aseptic meningitis; encephalopathy - for Sulfasalazine-EH.

Mental disorders: depression - for Sulfasalazine-EN.

From the senses

Violation of taste, smell, ringing in the ears.

From the genitourinary system

Proteinuria, hematuria, crystalluria, nephrotic syndrome, oligospermia and male infertility are reversible. In patients with porphyria, an exacerbation of seizures is possible.

Allergic reactions

Very rare: Skin rash, urticaria, erythema, pruritus, exfoliative dermatitis, photosensitive reactions, exanthema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, Sjogren's syndrome, systemic lupus erythematosus, serum sickness, fever, lymphadenopathy, periorbital edema, conjunctival edema scleral polyarteritis nodosa and eosinophilia.

From the respiratory system

Rarely: shortness of breath, cough, pulmonary infiltrates and fibrous alveolitis.

From the musculoskeletal system

Rarely: arthralgia.

Change in laboratory parameters

During treatment with sulfasalazine, levels of amylase, bilirubin, alkaline phosphatase and liver transaminase activity may increase.

Special instructions

It is recommended to conduct a general blood test (at the beginning of treatment - 1-2 times a month, then - every 3-6 months) and urinalysis before starting treatment, as well as periodically during treatment in patients with renal failure. use should be discontinued immediately in case of suspicion or laboratory confirmation of serious hematological disorders.

It is required to monitor liver function on a monthly basis during the first 3 months of using the preparation. Patients with impaired liver function are prescribed sulfasalazine with caution.

Monitoring of the state of renal function should be carried out at the beginning of treatment and during preparation therapy. In patients with glucose-6-phosphate dehydrogenase deficiency, the preparation is used with caution, since sulfasalazine can cause hemolytic anemia.

During the treatment period, it is recommended to drink plenty of fluids.

Changes in laboratory blood parameters (macrocytosis, pancytopenia) due to folic acid deficiency can be normalized by taking folic or folinic acids.

Special observation during treatment with sulfasalazine is necessary for patients with renal or hepatic insufficiency, asthma and allergies (cross-hypersensitivity to furosemide, thiazide diuretics, sulfonylurea derivatives, carbonic anhydrase inhibitors is possible). In case of allergies or other side effects, the use of sulfasalazine must be stopped immediately. For mild forms of sulfasalazine allergy, desensitization is possible.

Use during pregnancy and lactation. The negative effect of sulfasalazine is not completely excluded, therefore the preparation is used in pregnant women only under strict indications. During treatment, breastfeeding should be discontinued.

Children. Sulfsalazine in coated tablets is not used in children. Sulfasalazine-EH is used in children over the age of 6 years.

The ability to influence the reaction rate when driving or working with other mechanisms. During treatment, it is necessary to refrain from driving vehicles and working with other mechanisms.

Interactions

Sulfasalazine reduces the absorption of folic acid and digoxin. drinking enough fluids and avoiding acylation of urine (for example, due to concomitant intake of hexamethylenetetramine) can reduce the manifestations of crystalluria and the formation of stones.

Sulfonamides are similar to some oral hypoglycemic agents. Therefore, some patients who take sulfonamides may experience hypoglycemia. Patients who use sulfasalazine and hypoglycemic agents in parallel should be under medical supervision.

When used simultaneously with anticoagulants and hypoglycemic agents - sulfonylurea derivatives - enhances their effect. In connection with the inhibition of the enzyme thiopurine methyltransferase by sulfasalazine with the simultaneous use of sulfasalazine and thiopurine-6-mercaptopurine or azathiopurine, bone marrow suppression and leukopenia may occur.

The use of sulfasalazine and methotrexate in patients with rheumatoid arthritis does not affect the pharmacokinetics of the preparation. However, an increased incidence of gastrointestinal side effects, in particular nausea, has been reported. Antibiotics can reduce the effectiveness of Sulfasalazine and Sulfasalazine-EH.

Overdose

Patients with impaired renal function are at a higher risk of severe overdose. high doses of sulfasalazine cause nausea, vomiting, and abdominal pain. in case of an overdose, anuria, crystalluria, hematuria and symptoms of toxic damage to the central nervous system (convulsions) are possible. toxicity is proportional to the concentration of sulfapyridine in the blood.

Careful monitoring of the patient's condition is necessary, since in some cases methemoglobinemia or sulfhaemoglobinemia may occur, which requires appropriate treatment.

When symptoms of an overdose appear, it is necessary to lavage the stomach, cleanse the intestines, alkalize urine, and forced diuresis. In case of anuria and / or renal failure, fluid and electrolyte intake should be limited. The effectiveness of measures is assessed by the level of concentration of sulfapyridine in blood plasma. There is no specific antidote.

Storage conditions

At temperatures up to 25 ° c.