Salazopyrin-EN-tabs 500mg 100 tablets — Made in Sweden — Free Delivery

Pharmacological properties

Pharmacodynamics. In general, the preparation and its metabolites exhibit immunomodulatory properties, have an antibacterial effect, affect the arachidonic acid cascade and change the activity of certain enzymes. the final clinical result is a decrease in the activity of the inflammatory process in the intestine. in rheumatoid arthritis, the modification of the course of the disease is observed after 1–3 months with a characteristic decrease in the level of cp and the values ​​of other indicators of inflammation. mesalazine (me) is not considered to be the cause of this effect.

Radiographic studies have shown a significant slowdown in the progression of the disease (according to the Larsen or Sharp index) in patients in the early stages of the disease when using sulfasalazine for 2 years compared with placebo or hydroxychloroquine. When the preparation is discontinued, the positive effect is reliably preserved.

Pharmacokinetics

Approximately 90% of the dose reaches the colon, where the preparation is broken down by bacteria into sulfapyridine (SP) and mesalazine (IU). These connections are also active; Uncleaved sulfasalazine (UASP) is also active for a variety of symptoms. Most of the SP is absorbed and undergoes hydroxylation or glucuronidation; a mixture of unchanged and metabolized SP is determined in the urine. A certain amount of IU undergoes acetylation in the wall of the colon, therefore, AC-ME is mainly excreted in the urine. SASP is excreted unchanged in bile and urine.

In studies of the use of EN-tablets, no statistically significant difference was found between the values ​​of the main parameters of this dosage form and the equivalent dose of SASP in the form of a powder; therefore, the data below are for conventional tablets. There is no evidence that when using Salazopyrin for the treatment of bowel disease, systemic concentrations have any effect that differs from adverse reactions. Thus, at SP concentrations above 50 μg / ml, the risk of adverse reactions increases significantly, especially in patients with a slow acetylation process.

With oral administration of SASP in a single dose of 3 g, Cmax of SASP in blood serum is achieved after 3-5 hours; T1 / 2 was 5.7 ± 0.7 h, the delay period was 1.5 h. min, and for AC-ME - 100 ± 20 ml / min. Free SP first appears in blood plasma 4.3 hours after taking a single dose; the half-absorption period is 2.7 hours. T½ is calculated to be 18 hours.

ME: only AC-ME (non-free ME) was detected in the urine; it is likely that acetylation occurs to a large extent in the mucous membrane of the colon. After taking 3 g of SASP, the delay period was 6.1 ± 2.3 h, the levels of total IU in blood plasma were below 2 μg / ml. T1 / 2 with urine was 6.0 ± 3.1 h, and the half-absorption period, based on these data, is 3.0 ± 1.5 h. The renal clearance constant was 125 ml / min, respectively, to the glomerular filtration rate.

There is no evidence that the kinetics of the preparation in patients with rheumatoid arthritis will differ from the above.

Indications

Induction and maintenance of remission in ulcerative colitis; treatment of active Crohn's disease.

Treatment of rheumatoid arthritis in adults in case of insufficient effectiveness of NSAIDs.

Treatment of juvenile polyarticular or oligosarticular rheumatoid arthritis.

Application

The dose is selected individually, depending on the severity of the disease and the tolerability of the preparation. the tablets should be swallowed whole, not broken or crumbled.

Elderly patients: there are no special warnings.

Ulcerative colitis

Adults

Severe seizure: 2-4 tablets of Salazopyrin 4 times a day, possibly in combination with steroids as part of an intensive care regimen. With the rapid passage of tablets, the effectiveness of the preparation may decrease.

The night interval between doses should not exceed 8 hours.

Moderate seizures: 2-4 tablets 4 times a day, possibly in combination with steroids.

Light severity: 2 tablets 4 times a day with or without steroids.

Maintenance therapy: after induction of remission, the dose is gradually reduced to 4 tablets per day. At this dose, the preparation must be taken continuously, since if treatment is discontinued, even several years after an acute attack, the risk of recurrence increases 4 times.

Children. The dose is reduced in proportion to body weight. In case of an acute attack or relapse: 40-60 mg / kg / day.

Maintenance therapy: 20-30 mg / kg / day.

Crohn's disease

In Crohn's disease in the acute stage, Salazopyrin-EN-tabs should be taken in the same way as in the attacks of ulcerative colitis (see above).

Rheumatoid arthritis

Adults

In patients with rheumatoid arthritis and patients who have received NSAIDs for a long time, stomach reactions are possible, therefore, in the case of this disease, Salazopyrin-EN-tabs is used according to the following recommendations. Treatment should be started with 1 tablet per day, gradually increasing the dose by 1 tablet per day every week until the dose is 1 tablet 4 times a day or 2 tablets 3 times a day, depending on the tolerability and effectiveness of the preparation. The action of the preparation appears slowly and a pronounced effect may not be observed for 6 weeks. An improvement in joint mobility should be accompanied by a decrease in ESR and CRP levels. The simultaneous use of NSAIDs and Salazopyrin-EN-tabs is possible.

Juvenile polyarticular or oligosarticular rheumatoid arthritis.

Children aged 2 years and older.

30-50 mg / kg / day, divided into 4 equal doses. Usually the maximum dose is 2000 mg / day. To reduce possible gastrointestinal adverse reactions, start with ¼ of the planned maintenance dose and then increase it by ¼ every week until the maintenance dose is reached.

Contraindications

Hypersensitivity to sulfasalazine, its metabolites or to other components of the preparation, as well as sulfonamides or salicylates; porphyria; age up to 2 years.

Side effects

In general, approximately 75% of cases of adverse reactions occur during the first 3 months of treatment, and more than 90% - during the first 6 months. some adverse events are dose-dependent and often the manifestation of symptoms can be alleviated by reducing the dose of the preparation.

Are common

Sulfasalazine is cleaved by intestinal bacteria to sulfapyridine and 5-aminosalicylate, so unwanted reactions to sulfonamide or salicylate are possible. Patients with a slow acetylation status are more likely to experience adverse reactions to sulfapyridine. The most common adverse reactions are nausea, headache, rash, lack of appetite, and fever.

Specific

Adverse reactions observed in clinical trials of sulfasalazine are listed below by class and frequency (very common (≥1 / 10); often (≥1 / 100 - 1/10); infrequently (≥1 / 1000 1/100)). In cases where an adverse reaction has been noted with different frequencies in clinical studies, the highest reported frequency is indicated. Additional reactions reported in the post-marketing period are also included in the following list with a frequency of "unknown" (frequency cannot be determined from the available data).

Infections and invasions: unknown - pseudomembranous colitis.

On the part of the blood and lymphatic system: often - leukopenia; rarely - thrombocytopenia (for more details see SPECIAL INSTRUCTIONS); unknown - agranulocytosis, aplastic anemia, hemolytic anemia, anemia with Heinz bodies, hypoprothrombinemia, lymphadenopathy, macrocytosis, megaloblastic anemia, methemoglobinemia, neutropenia, pancytopenia.

Immune system disorders: unknown - anaphylaxis, polyarteritis nodosa, serum sickness.

From the side of metabolism and nutrition: unknown - loss of appetite.

Mental disorders: often - insomnia; infrequently - depression; unknown - hallucinations.

From the side of the nervous system: often - dizziness, headache, change in taste; rarely - convulsions; unknown - aseptic meningitis, ataxia, encephalopathy, peripheral neuropathy, impaired sense of smell.

From the organ of hearing and labyrinth: often - ringing in the ears; infrequently - vertigo.

From the side of the organ of vision: often - injection of the conjunctiva and sclera.

From the side of the heart: unknown - allergic myocarditis, cyanosis, pericarditis.

From the vascular system: infrequently - vasculitis.

From the respiratory system, chest and mediastinal organs: often - cough; infrequently - dyspnea, unknown - fibrous alveolitis, eosinophilic infiltration, interstitial lung disease.

From the gastrointestinal tract: very often - indigestion, nausea; often - abdominal pain, diarrhea, vomiting, stomatitis; unknown - exacerbation of ulcerative colitis, pancreatitis, mumps.

From the liver: unknown - liver failure, fulminant hepatitis, hepatitis (for more details see SPECIAL INSTRUCTIONS).

On the part of the skin and subcutaneous tissue: often - itching; infrequently - alopecia, urticaria; unknown - epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, preparation rash with eosinophilia and systemic symptoms (DRESS), acute generalized exanthematous pustulosis, erythema, exanthema, exfoliative dermatitis, periorbital edema, lichen planus, photosensitivity.

From the side of the musculoskeletal system and connective tissue: often - arthralgia; unknown - systemic lupus erythematosus.

From the urinary system: often - proteinuria; unknown - nephrotic syndrome, interstitial nephritis, crystalluria (for more details see SPECIAL INSTRUCTIONS), hematuria.

On the part of the reproductive system and mammary glands: reversible oligospermia (for more details see SPECIAL INSTRUCTIONS).

General condition and disorders associated with the method of administration of the preparation: often - fever; rarely - swelling of the face; unknown - yellow staining of skin and body fluids.

Research: infrequently - increased activity of liver enzymes; unknown - induction of autoantibodies.

special instructions

Before the start of therapy and during the first 3 months of treatment, all patients should be monitored for the indicators of a detailed blood test (including leukocyte count), determination of indicators of liver and kidney function (including urinalysis). in the future, these indicators are monitored according to clinical indications. patients should be warned about the need to immediately consult a doctor if clinical signs such as sore throat, fever, malaise, pallor, purpura, jaundice or sudden nonspecific illness occur during treatment with sulfasalazine, this may indicate myelosuppression, hemolysis or hepatotoxicity. if these signs are present, treatment with sulfasalazine should be discontinued pending blood test results.

Sulfasalazine should not be prescribed to patients with impaired liver or kidney function, or with pathological changes in the blood, unless the potential benefit outweighs the risk.

Sulfasalazine should be used with caution in patients with severe allergies or asthma.

The use of the preparation in the treatment of children with systemic juvenile rheumatoid arthritis often causes reactions similar to serum sickness; therefore, sulfasalazine is not recommended for these patients.

Since sulfasalazine can cause the development of hemolytic anemia, it should be used with caution in patients with glucose-6-phosphate dehydrogenase deficiency.

Sulfasalazine, when taken orally, slows down the absorption and metabolism of folic acid, which can lead to its deficiency and lead to serious blood disorders (for example, macrocytosis and pancytopenia), the patient's condition can be normalized with the use of folic or folinic acid (leucovorin).

Because sulfasalazine causes crystalluria and kidney calculi, a sufficient amount of fluids should be consumed during treatment.

Oligospermia and infertility are possible in men treated with sulfasalazine. After discontinuation of sulfasalazine therapy, these effects disappear within 2-3 months.

During pregnancy and breastfeeding.

Pregnancy

According to published data on the use of sulfasalazine in pregnant women, there is no evidence of the risks of teratogenic effects. The likelihood of a negative effect on the fetus when using sulfasalazine during pregnancy is low. When taken orally, sulfasalazine inhibits the absorption and metabolism of folic acid and can lead to folate deficiency. Since a negative effect cannot be completely ruled out, sulfasalazine is prescribed during pregnancy only if absolutely necessary.

Lactation

Small amounts of sulfasalazine and sulfapyridine are determined in breast milk, so the preparation should be used with caution during breastfeeding, especially in the case of premature infants and glucose-6-phosphate dehydrogenase deficiency. The decision to stop breastfeeding or discontinue the preparation is made by the attending physician based on a careful assessment of the benefit to the mother / risk to the child ratio.

Children. The preparation is contraindicated in children under 2 years of age. The use of the preparation in the treatment of children with systemic juvenile rheumatoid arthritis often causes reactions similar to serum sickness; therefore, sulfasalazine is not recommended for these patients.

Influence on the ability to drive vehicles or work with other mechanisms. The effect of sulfasalazine on the reaction rate when driving or operating other mechanisms has not been systematically evaluated.

Interactions

A decrease in digoxin absorption has been reported, leading to subtherapeutic serum concentrations of the latter, when used concomitantly with the oral form of sulfasalazine.

In terms of chemical properties, sulfonamides have a certain similarity with some oral hypoglycemic preparations. In patients taking sulfonamides, hypoglycemia was observed. It is necessary to carefully monitor the condition of patients taking sulfasalazine and hypoglycemic agents.

Since sulfasalazine inhibits thiopurine methyltransferase, simultaneous use of oral salazopyrine and thiopurine-6-mercaptopurine or its prodrugs (azathioprine) may inhibit bone marrow function and develop leukopenia.

The simultaneous use of sulfasalazine and methotrexate in patients with rheumatoid arthritis does not change the pharmacokinetic characteristics of the preparations. However, an increase in the frequency of gastrointestinal adverse reactions, in particular nausea, has been reported.

Overdose

In the absence of hypersensitivity, the acute toxicity of the preparation when administered orally is low. there is no specific antidote, supportive treatment should be carried out.

Storage conditions

At a temperature not higher than 25 ° C.