Sulfasalazine is a pharmacological drug from the group. Instructions for use of sulfasalazine, its analogues and cost. Kidney dysfunction

Gross formula

Pharmacological group of the substance Sulfasalazine

Nosological classification (ICD-10)

CAS code

Pharmacology

In the connective tissue of the intestinal wall, it dissociates into 5-aminosalicylic acid, which determines the anti-inflammatory properties of sulfasalazine, and sulfapyridine, a competitive antagonist of para-aminobenzoic acid, which stops the synthesis of folates in microbial cells and determines antibacterial activity. Effective against diplococci, streptococci, gonococci, E. coli.

Poorly absorbed from the gastrointestinal tract (no more than 10%). It is subject to breakdown by intestinal microflora with the formation of 60-80% sulfapyridine and 25% 5-aminosalicylic acid (5-ASA). Plasma protein binding of sulfasalazine is 99%, sulfapyridine is 50%, 5-ASA is 43%. Sulfapyridine undergoes biotransformation in the liver by hydroxylation with the formation of inactive metabolites, 5-ASA is acetylated. T1/2: sulfasalazine - 5-10 hours, sulfapyridine - 6-14 hours, 5-ASA - 0.6-1.4 hours. 5% of sulfapyridine and 67% of 5-ASA are excreted with feces, by the kidneys - 75-91 % sulfasalazine (for 3 days).

Use of the substance Sulfasalazine

Nonspecific ulcerative colitis, Crohn's disease, rheumatoid arthritis.

Contraindications

Hypersensitivity to sulfonamides and salicylic acid derivatives, severe liver and/or kidney dysfunction, anemia, porphyria, glucose-6-phosphate dehydrogenase deficiency, breastfeeding, children under 5 years of age (there is no information on the safety of use in patients of this age group).

Use during pregnancy and breastfeeding

During pregnancy, it is possible only under strict indications and in the minimum effective dose.

Breastfeeding should be stopped during treatment.

Side effects of the substance Sulfasalazine

From the nervous system and sensory organs: headache, dizziness, weakness, fatigue, sleep disturbance, hallucinations, peripheral neuropathy, ataxia, convulsions, tinnitus.

From the cardiovascular system and blood (hematopoiesis, hemostasis): agranulocytosis, leukopenia, thrombocytopenia, hemolytic anemia.

From the gastrointestinal tract: dyspeptic symptoms: nausea, vomiting, diarrhea, abdominal pain, flatulence, anorexia, blood in feces, drug-induced hepatitis, pancreatitis.

From the genitourinary system: renal dysfunction, interstitial nephritis, transient oligospermia and infertility.

Allergic reactions: skin rash, Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic shock.

Others: photosensitivity, fever, interstitial pneumonitis.

Interaction

Strengthens the effect of anticoagulants, anticonvulsants and oral hypoglycemic drugs, as well as the risk of side effects when prescribing cytostatics, immunosuppressants, hepato- and nephrotoxic drugs. Reduces the absorption of folic acid and digoxin.

Overdose

Symptoms: nausea, vomiting, abdominal pain, dizziness.

Treatment: gastric lavage, forced diuresis, symptomatic therapy.

Routes of administration

Inside.

Precautions for the substance Sulfasalazine

Prescribe with caution to patients with impaired renal or liver function, bronchial asthma, allergic reactions. During the treatment period, it is necessary to systematically monitor the blood picture and the level of liver enzymes.

active substance: 1 tablet contains sulfasalazine 500 mg

Excipients: povidone, corn starch, magnesium stearate, colloidal silicon dioxide, hypromellose, propylene glycol.

Dosage form

Film-coated tablets.

Pharmacological group

Anti-inflammatory drugs that are used for intestinal diseases. Sulfasalazine.

ATC code A07E C01.

Indications

• Induction and maintenance of remission in ulcerative colitis; treatment of Crohn's disease in the active stage.
• Treatment of rheumatoid arthritis in adults in case of insufficient effectiveness of non-steroidal anti-inflammatory drugs (NSAIDs).
• Treatment of juvenile polyarticular or oligoarticular rheumatoid arthritis.

Contraindications

Sulfasalazine is contraindicated:

• patients with hypersensitivity to sulfasalazine, its metabolites or to any other component of the drug, sulfonamides and salicylates;
• patients with porphyria;
• children under 6 years of age.

Directions for use and doses

The dose should be selected according to the severity of the disease and possible side effects. The tablets are taken with meals with a glass of water. The missed dose should be taken as soon as possible before there is little time left to take the next dose. In this case, the patient should take only the next scheduled dose.

The tablets should be swallowed whole, not broken or crushed.

Elderly patients There are no special warnings.

ulcerative colitis

adults

Severe course: 2-4 tablets of Sulfasalazine 4 times daily, may be used in combination with steroids as part of an intensive therapy regimen. If the tablets are taken quickly, the effectiveness of the drug may decrease.

The night interval between doses should not exceed 8:00.

Moderate course: 2-4 tablets 4 times a day, can be used in combination with steroids.

Mild course: 2 tablets 4 times daily with or without steroids.

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

children

Reduce the dose in proportion to body weight.

In case of an acute attack or relapse: 40-60 mg/kg per day.

Maintenance treatment: 20-30 mg/kg per day.

Crohn's disease

For Crohn's disease, sulfasalazine should be taken according to the same regimen as for ulcerative colitis (see above).

rheumatoid arthritis

adults

Patients with rheumatoid arthritis and patients who have used NSAIDs for a long time may have a sensitive stomach, so in the case of this disease, sulfasalazine should be used according to the following recommendations. Treatment should begin 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 drug. The action appears slowly and a pronounced effect may not be observed for 6 weeks. Improvement in joint mobility should be accompanied by a decrease in ESR and C-reactive protein levels. The simultaneous use of NSAIDs and Sulfasalazine is possible.

Juvenile polyarticular or oligoarticular rheumatoid arthritis.

Children aged 6 years and older.

30-50 mg/kg/day in 4 equal doses. Typically the maximum daily dose is 2000 mg/day. To reduce possible gastrointestinal intolerance, start with ¼ of the planned maintenance dose and then increase by ¼ each week until the maintenance dose is reached.

Adverse reactions

In general, approximately 75% 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-related and symptoms can often be relieved by reducing the dose of the drug.

Are common.

Sulfasalazine is broken down by intestinal bacteria into sulfapyridine and 5-aminosalicylate, so adverse reactions to the sulfonamide or salicylate are possible. Patients with slow acetylating status are more likely to experience adverse reactions to sulfapyridine.

From the cardiovascular system.

Allergic myocarditis, cyanosis, pericarditis, periarteritis nodosa, vasculitis.

From the gastrointestinal tract.

Abdominal pain, nausea, vomiting, diarrhea, loss of appetite, hepatitis, fulminant hepatitis, pancreatitis, stomatitis, mumps, exacerbation of ulcerative colitis, liver failure, pseudomembranous colitis.

Hematological disorders.

Macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, methemoglobinemia, anemia, agranulocytosis, thrombocytopenia, aplastic anemia, hypoprothrombinemia, anemia with Heinz bodies, pancytopenia.

Patients with porphyria may experience an acute attack.

From the nervous system.

Headache, peripheral neuropathy, dizziness, tinnitus, ataxia, insomnia, hallucinations, convulsions and aseptic meningitis, encephalopathy.

From the mental point of view.

Depression.

From the senses.

Impaired sense of taste, sense of smell, ringing in the ears, vertigo, injection of the conjunctiva and sclera.

From the genitourinary system.

Interstitial nephritis, proteinuria, hematuria, crystalluria, nephrotic syndrome, oligospermia and male infertility, which are reversible.

allergic reactions

Skin rash, urticaria, erythema, itching, exfoliative dermatitis, photosensitive reactions, exanthema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, Sjögren's syndrome, systemic lupus erythematosus, serum sickness, lymphadenopathy, periorbital edema, conjunctival or scleral periarteritis nodosa, anaphylaxis, alopecia, drug rash with eosinophilia and systemic symptoms (DRESS), toxic pustuloderma, lichen planus.

From the respiratory system.

Dyspnea, cough, eosinophilic infiltration, fibrous alveolitis, interstitial lung disease.

From the musculoskeletal system.

Arthralgia.

Laboratory tests.

During treatment with sulfasalazine, the levels of serum amylase, bilirubin, alkaline phosphatase and liver transaminases may increase, and the induction of autoantibodies may occur.

General condition and disorders, this " related to the method of administration of the drug .

Fever, swelling of the face, yellow color of the skin and body fluids.

Overdose

Excessive doses of sulfasalazine cause nausea, vomiting, and abdominal pain. When very high doses are used, anuria, crystalluria, hematuria and symptoms of central nervous system toxicity (convulsions) may occur. Toxicity is proportional to the concentration of sulfapyridine in the blood.

The patient's condition should be carefully monitored, since in some cases methemoglobinemia or sulfhemoglobinemia may occur, which requires appropriate treatment.

If symptoms of overdose appear, it is necessary to induce vomiting, rinse the stomach, cleanse the intestines, alkalize urine, and force diuresis. In case of anuria and/or renal failure, fluid and electrolyte intake should be limited.

The effectiveness of the measures taken can be assessed by the level of sulfapyridine concentration in the blood serum.

Use during pregnancy or breastfeeding.

According to published data on the use of sulfasalazine in pregnant women, there is no evidence of teratogenic risks. The likelihood of a negative effect on the fetus when using sulfasalazine during pregnancy is low. When administered orally, sulfasalazine inhibits the absorption and metabolism of folic acid and may lead to folic acid deficiency. Since harmful effects cannot be completely ruled out, sulfasalazine can be prescribed to pregnant women only under strict indications and in minimally effective doses.

During treatment you should stop breastfeeding.

Children

The drug is contraindicated in children under 6 years of age. The use of the drug in the treatment of children with a systemic form of juvenile rheumatoid arthritis often causes reactions similar to serum sickness; therefore, sulfasalazine is not recommended in these patients.

Features of application

All patients are recommended to undergo blood tests (complete blood count (including leukocyte count) at the beginning of treatment 1-2 times a month, then every 3-6 months), as well as a urine test before starting treatment and during treatment.

During treatment, patients must be kept adequately hydrated.

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

Supervision during treatment with sulfasalazine is necessary for patients with renal or hepatic insufficiency, bronchial asthma and allergies (possible cross-sensitivity to furosemide, thiazide diuretics, sulfonylurea derivatives, carbonic anhydrase inhibitors). If allergic reactions or other serious side effects occur, treatment with sulfasalazine should be discontinued immediately. For mild forms of allergy to sulfasalazine, desensitization may be performed.

The drug is not recommended for systemic forms of juvenile rheumatoid arthritis, as it often causes unwanted effects, such as serum sickness. Typical symptoms are fever, nausea, vomiting, headache, rash, liver dysfunction. This condition is often severe.

Patients should be warned to seek immediate medical attention if clinical signs such as sore throat, fever, malaise, pallor, purpura, jaundice or sudden onset of nonspecific illness occur during treatment with sulfasalazine, which may indicate myelosuppression, hemolysis or hepatotoxicity.

If these signs are present, treatment with sulfasalazine should be discontinued pending blood test results. 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 administered orally, slows down the absorption and metabolism of folic acid, which can lead to its deficiency and lead to serious blood disorders (macrocytosis and pancytopenia). The patient's condition can be normalized with the use of folic or folinic acid (leucovorin).

Since sulfasalazine causes crystalluria and the formation of kidney stones, sufficient fluids should be consumed during treatment.

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

Life-threatening skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported with the use of sulfasalazine. Patients should be warned of the signs and symptoms and closely monitored for skin reactions, especially during the first weeks of treatment. If symptoms or signs of Stevens-Johnson syndrome and toxic epidermal necrolysis (eg, progressive skin rash, often with blisters or mucosal lesions) are present, treatment with sulfasalazine should be discontinued. The best treatment results are achieved with early diagnosis of diseases. If a patient has experienced symptoms or signs of these diseases, the use of sulfasalazine is not recommended to be restarted in that patient at all.

The ability to influence the reaction rate when driving a vehicle or working with other mechanisms.

During treatment, you should refrain from driving vehicles or operating machinery.

Interaction with other drugs and other types of interactions

Sulfasalazine reduces the absorption of folic acid and digoxin. When administered simultaneously with anticoagulants and hypoglycemic agents - sulfonylurea derivatives, the drug enhances their effect. Due to the inhibition of the enzyme thiopurine methyltransferase by sulfasalazine, suppression of bone marrow function and leukopenia may occur with simultaneous use of sulfasalazine and thiopurine-6-mercaptopurine or azathioprine.

The use of sulfasalazine and methotrexate in patients with rheumatoid arthritis does not change the pharmacokinetic characteristics of the drug.

However, an increased incidence of gastrointestinal side effects, particularly nausea, has been reported. Antibiotics may reduce the effectiveness of Sulfasalazine.

Pharmacological properties

Pharmacodynamics.

Sulfasalazine is an anti-inflammatory drug. It has an immunosuppressive effect, especially in connective tissue, the intestinal wall and serous fluid, where its concentration is high. Thanks to the intestinal flora, sulfasalazine breaks down to sulfapyridine and 5-aminosalicylic acid. Sulfapyridine inhibits the proliferation of killer cells and the transformation of lymphocytes. The anti-inflammatory effect of 5-aminosalicylic acid (mesalazine) is most significant for the treatment of inflammatory diseases of the large intestine. Mainly locally, it inhibits cyclooxygenase and lipoxygenase in the intestinal wall, thereby preventing the formation of prostaglandins, leukotrienes and other inflammatory mediators. It also probably binds free oxygen radicals.

Pharmacokinetics.

About 30% of the administered dose of sulfasalazine is absorbed in the small intestine; the remaining 70% is metabolized by intestinal flora in the large intestine into sulfapyridine and 5-aminosalicylic acid. The maximum concentrations of sulfasalazine and its metabolites in plasma vary quite significantly between patients - at low levels of acetylation they are much higher and are associated with increased incidence of adverse events. It binds well to plasma proteins and connective tissue. The largest part of the absorbed amount of sulfasalazine enters the intestine with bile; a small amount is excreted unchanged in the urine. The half-life of sulfasalazine is 5 to 10:00.

The largest part of the declared sulfapyridine is absorbed and reaches its maximum concentration in the blood serum 12-24 hours after taking the drug. Metabolized in the liver (by acetylation, hydroxylation and conjugation with glucuronic acid) and excreted by the kidneys. The half-life ranges from 6 to 14 hours depending on the rate of acetylation. Only about 30% of 5-aminosalicylic acid is absorbed and acetylated in the liver and excreted by the kidneys in the urine. The rest is excreted unchanged in the feces.

Basic physical and chemical properties

round, brownish-yellow, slightly biconvex with beveled edges, covered with a transparent, colorless shell.

Best before date

Storage conditions

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Package

10 tablets in a blister, 5 blisters in a cardboard box.

Vacation category

On prescription.

Manufacturer

KRKA, d.d., Novo Mesto, Slovenia /

KRKA, dd, Novo mesto, Slovenia.

Location

Šmarješka cesta 6, 8501 Novo mesto, Slovenia /

Name:

Sulfasalazine (Sulfasalazinum)

Pharmacological
action:

Sulfasalazine – drug with antimicrobial and anti-inflammatory properties.
The chemical structure is a combination of sulfapyridine and 5-aminosalicylic acid. A smaller portion of sulfazalazine is absorbed from the lumen of the colon, after which it is evenly distributed within the connective tissue.
Sulfasalazine is affected by normal intestinal microflora, and as a result, the active substance molecule breaks down into its constituent components: sulfapyridine and 5-aminosalicylic acid.
It is these substances that have antibacterial and anti-inflammatory activity. Anti-inflammatory effect Due to its low absorption capacity, 5-aminosalicylic acid is determined mainly in the walls of the large intestine.
Sulfapyridine has mainly a general anti-inflammatory effect due to better absorption (up to 30% of the dose taken).

A significant part of Sulfasalazine is subject to enterohepatic recirculation, as a result of which part of the substance again enters the intestine with bile.
Sulfasalazine accumulates predominantly in peritoneal and connective tissue, synovial and pleural fluids.
Approximately one third of 5-aminosalicylic acid is metabolized by acetylation, and elimination occurs through the kidneys.
The remaining two-thirds of the substance is eliminated in the feces.
Metabolism sulfapyridine occurs in the liver, and the rate of metabolic transformations largely depends on the rate of acetylation.

Indications for
application:

Nonspecific 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.

Mode of application:

Sulfasalazine taken before meals without chewing and drinking water (approximately 250 ml). During the period of use of the drug, it is recommended to drink increased amounts of fluid.

For Crohn's disease and nonspecific ulcerative proctitis or colitis
4 times a day, 1-2 g in case of exacerbation (for adults).
Against the background of remission of the disease, it is necessary to gradually reduce the dosage and switch to a dosage regimen to prevent exacerbation (4 times a day, 500 mg).
The prophylactic dosage can be taken for quite a long time.
For children, use a daily dose of 40–60 mg/kg during exacerbation.
Preventive daily dosage for children is 20–30 mg/kg. Prescribed only to children over 2 years of age.

For rheumatoid arthritis
The average dose of Sulfasalazine used is 2–3 g/day.
It is recommended to begin therapy with a daily dosage of 500 mg. This dose can be gradually increased over 1 month to 1 g 2-3 r/day.
Typically, the therapeutic effect of taking the drug is noticeable after 6-10 weeks from the start of treatment. The recommended duration of 1 course of treatment is at least 6 weeks.
In pediatrics, Sulfasalazine is not used for the treatment of children with juvenile rheumatoid arthritis.

Side effects:

From the central nervous system and peripheral nervous system: headache, dizziness, tinnitus, ataxia, convulsions, sleep disturbances, hallucinations, peripheral neuropathy.
From the urinary system: renal dysfunction, interstitial nephritis.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia, hepatitis, pancreatitis.
From the respiratory system: interstitial pneumonitis and other lesions of lung tissue.
From the hematopoietic system: anemia, leukopenia, thrombocytopenia, agranulocytosis.
From the reproductive system: transient oligospermia, infertility.
Allergic reactions: skin rash, fever, anaphylactic shock.
Others: possible yellow coloration of skin, urine, soft contact lenses.

Contraindications:

Blood diseases;
- porphyria;
- severe liver dysfunction;
- severe renal dysfunction;
- deficiency of the enzyme glucose-6-phosphate dehydrogenase;
- children under 5 years of age;
- hypersensitivity to sulfonamides and salicylic acid derivatives.

Carefully The drug should be prescribed to patients with impaired liver and/or kidney function, patients with bronchial asthma, allergic reactions.
It is recommended to conduct an examination, including urine and blood tests, before prescribing Sulfasalazine. The same amount of research should be carried out regularly while taking pills.
With a deficiency of glucose-6-phosphate dehydrogenase, the risk of developing hemolytic anemia increases. With porphyria, an exacerbation of the disease may occur.

Interaction
other medicinal
by other means:

With simultaneous use, Sulfasalazine reduces the absorption of folic acid and digoxin;
- with simultaneous use, Sulfasalazine enhances the effect of anticoagulants and sulfonylurea derivatives;
- with the simultaneous use of Sulfasalazine and antibiotics, the effectiveness of Sulfasalazine may decrease, since antibiotics have an inhibitory effect on the intestinal flora.

Pregnancy:

The use of Sulfasalazine during pregnancy is possible only according to strict indications in the minimum effective dose. If the course of the disease allows, it is recommended to discontinue the drug in the third trimester of pregnancy.
If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided. Do not use the drug after the expiration date indicated on the package.

1 tablet Sulfasalazine contains:
- excipients: anhydrous colloidal silicon, gelatinized starch, magnesium stearate.

1 tablet Sulfasalazine EH contains:
- active ingredient: sulfasalazine - 500 mg;
- excipients: magnesium stearate, pregelatinized starch, povidone, colloidal anhydrous silicon dioxide.

Marina Maksimova

Sulfasalazine is a prescription drug that is included in the list of the most important drugs in the healthcare system.

Release form and composition

1. The product is a round tablet, convex on both sides, with beveled edges.
2. The product has a dark yellow color, sometimes there are inclusions. Each tablet is covered with a film-like coating.
3. The medicine is packaged in blisters of 10 pieces, packaged in cardboard boxes. Each package contains 5 blisters.

Compound:

Active substance – sulfasalazine – 535 mg, coated with povidone K-30.

Excipients:

• Magnesium stearate
• corn starch
• anhydrous colloidal silica

Film casing components:

• propylene glycol
• hypromellose
• pigment – ​​iron oxide yellow E 172

pharmachologic effect

A product with anti-inflammatory and antimicrobial effect.

Pharmacodynamics

Sulfasalazine does not relieve pain or fight fever.

Pharmacokinetics

1. 10-30% active substance absorbed by the walls of the small intestine and distributed throughout the connective tissue. 70-90% is broken down in the large intestine due to microbial exposure to sulfapyridine and 5-ASA.
2. Sulfasalazine reaches its maximum concentration after 3-12 hours. The maximum of metabolic products in the blood is concentrated after 10 hours.
3. Sulfasalizin is 99% bound to plasma proteins: acetylsulfapyridine 90%, sulfapyridine 70%, 5-ASA 43%. The substances are distributed in a volume of about 7 liters.
4. Sulfasalazine mostly accumulates in the joint cavity, connective and peritoneal tissues, pleural cavity.
5. In patients with slow metabolism, the serum concentration of the drug is higher, which is why such patients are more likely to experience undesirable consequences from taking the drug.
6. Sulfapyridine is transformed in the liver mainly through acetylation, partly through the formation of inactive metabolic products. 5-aminosalicylic acid is completely acetylated.
7. The half-life of sulfazalin occurs after 5-10 hours. Sulfapyridine is excreted after 10 hours with fast metabolism and after 15 with slow metabolism. The release time for 5-ASA is from half an hour to one and a half hours. 5% of sulfapyridine and 67% of 5-ASA are excreted in the feces, 75-90% of Sulfasalazine are excreted in the urine within 3 days. The half-life is increased in older people. The reasons for this are not clear. In younger people, the elimination of Sulfasalazine is the same in time, regardless of gender and age.

Indications for use

Sulfasalazine is used as drug therapy for the following pathologies:

• exacerbation of Crohn's disease in mild to moderate form
• exacerbation and remission of mild and moderate ulcerative colitis
• nonspecific ulcerative proctitis in mild and moderate form
• rheumatoid arthritis resistant to non-steroidal anti-inflammatory drugs
• juvenile idiopathic chronic polyarthritis

In severe forms of ulcerative proctitis, the drug is used as an addition to the main therapy.

Use during pregnancy and lactation

Studies in pregnant and lactating women were conducted in small groups.

The effects on pregnant and lactating women, the fetus and breast-fed children have not been sufficiently studied.

If the indications are serious and it is impossible for pregnant women to refuse to take the medication, it is permissible to prescribe Sulfasalazine in a minimal dosage.

Use during breastfeeding is unacceptable. This causes particular harm to premature babies and children with developmental pathologies. If it is impossible to refuse the medication, you should stop breastfeeding.

Use for liver dysfunction

Sulfasalazine should be used cautiously in patients with liver dysfunction.

Use for renal dysfunction

In case of kidney failure, the drug should be used with caution. A systematic examination of blood, urine and plasma for the content of liver enzymes is mandatory.

While using the medication, patients are advised to consume more fluid.

Use in children

The drug is prohibited for use in children under 5 years of age (children under 6 years of age with juvenile idiopathic chronic polyarthritis).

Directions for use and dosage regimen

Sulfasalazine must be taken orally after meals. The drug must not be chewed. The dose depends on age, as well as on the type and severity of the pathology.

Adult dosage:

1. For minor exacerbation, 2 tablets. four r/day/
2. For severe and moderate cases – 2-4 tablets. four r/day.
3. The break between use is no more than 8 hours.

Children's dosage:

1. During exacerbation or remission, 40-60 mg per kg of weight per day is prescribed.

Ulcerative colitis and ulcerative proctitis

Adult dosage:

1. For minor exacerbation, 2 tablets. Sulfasalazine four times a day.
2. In severe and moderate cases - 2-4 tablets. four r/day. The break between use is no more than 8 hours.
3. During remission, 4 tablets/day for life to avoid relapse.

Children's dosage:

1. 40-60 mg/day per kilogram of weight. During remission - 20-30 mg/day for each kg of weight.

Rheumatoid arthritis

Adult dosage:

1. At the beginning of therapy, 1 tablet/day is indicated, the dose is increased weekly by 1 tablet until the dosage is 1 tablet. four times a day or 2 tablets. three r/day. The effect of taking Sulfasalazine occurs at 7-11 weeks of treatment.

Juvenile idiopathic chronic polyarthritis

Children's dosage:

1. 30-50 mg of the product per kilogram of weight is evenly divided into 2-4 doses per day.
2. You can take no more than 4 tablets per day.
3. Therapy begins with taking a quarter of the prescribed volume, then the dose is increased by a quarter weekly.
4. This measure is necessary to prevent disruptions in the functioning of the gastrointestinal tract.

Side effects

During treatment with Sulfasalazine, there is a possibility of undesirable consequences from certain body systems:

• Reproductive system: transient oligospermia, treatable infertility in men.
• Digestive system: abdominal pain, nausea, vomiting.
• Urinary system: kidney pathologies, bleeding in the urine.
• Respiratory system: cough, damage to lung tissue, accumulation of fluid in the lungs.
• Nervous system: seizures, headache, sleep disturbances, anorexia.
• Lymphatic system and blood: decreased leukocyte levels, anemia, decreased platelet levels.
• The immune system: Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic shock.

Contraindications

Sulfasalazine should not be taken under the following conditions:

special instructions

1. Allergies and bronchial asthma require careful use of Sulfasalazine. If allergic reactions occur, the medication should be discontinued.
2. At the beginning of taking the drug, there is a risk of severe skin lesions - Stevens-Johnson syndrome and toxic epidermal necrolysis.
3. If a profuse rash with blisters appears on the skin and mucous membranes, immediately stop and do not resume use of the medication. The earlier the medication is discontinued, the more favorable the prognosis for curing undesirable consequences.

Sulfasalazine does not significantly affect driving or using machinery.

Overdose

Drug interactions

1. When treating UC, antibacterial agents should not be used. They worsen the effect of Sulfasalazine.
2. The effect of antiepileptic and hypoglycemic drugs, anticoagulants is enhanced when used together.
3. Side effects from cytostatics and immunosuppressants occur more often with simultaneous use of Sulfasalazine.
4. The medicine impairs the absorption of digoxin and vitamin B9.
5. Sulfasalazine has been used successfully in combination with metronidazole and corticosteroids.

Alcohol compatibility

Studies have not revealed any incompatibility between alcohol and Sulfasalazine.

However, the drug is partially excreted by the liver, and drinking alcohol increases the load on this organ. As a result, there is a risk of liver failure.

Average cost of sulfasalazine

The price of Sulfasalazine varies between 200-300 rub. .

Storage conditions and periods

1. The medicine is valid for 5 years from the date of manufacture.
2. Use after the expiration date indicated on the packaging is prohibited.
3. Store at a temperature not exceeding 250C, keep away from children.

Analogs

• Salofalk. The medicine eliminates the infection and fights germs. It is used in the treatment of Crohn's disease and UC. Helps prolong remission. Average price - 2800 rub..
• Mesalazine. Fights relapses of ulcerative colitis and Crohn's disease. Used as a prophylactic. Acts as an antioxidant. Well tolerated. Cost from 350 to 700 rub..
• Asakol. Intestinal remedy. Fights germs and infection. Prescribed as prevention and therapy for exacerbations of Crohn's disease and ulcerative colitis. Reduces the likelihood of developing colorectal cancer. The cost of the medicine is from 2000 rub.
• Prednisolone. Glucocorticosteroid medicine. Prescribed for the treatment of many pathologies, including rheumatoid arthritis and UC. Used for artificial immunosuppression, combating allergies and infections. The medicine is sold at a price from 30 to 100 rub..
• Mesacol. Fights infection in the intestines caused by ulcerative colitis and Crohn's disease. The medication will cost an average of 770 RUR.

Drugs with an effect similar to Sulfasalazine are also available in other dosage forms:

• Pentasa(granules, suppositories, suspension) from 3500 rub. .
• Salofalk(granules from 2000 rub., candles from 1500 rub.., suspension from 3800 rub.., rectal foam from 6340 rub. .)
• Prednisolone(solution for injection) approx. 35 rub..

film-coated tablets

Owner/Registrar

ATOLL, LLC

International Classification of Diseases (ICD-10)

Pharmacological group

Anti-inflammatory drug used to treat Crohn's disease and ulcerative colitis

pharmachologic effect

The drug for the treatment of ulcerative colitis is an azo compound of sulfapyridine with salicylic acid. Sulfasalazine selectively accumulates in the connective tissue of the intestine with the release of 5-aminosalicylic acid, which has anti-inflammatory activity, and sulfapyridine, which has an antimicrobial effect against Streptococcus spp., including Streptococcus pneumoniae, Neisseria gonorrhoeae, Escherichia coli.

Pharmacokinetics

Sulfasalazine is poorly absorbed in the intestine (no more than 10%). It is subject to breakdown by intestinal microflora with the formation of 60-80% sulfapyridine and 25% 5-aminosalicylic acid (5-ASA). Plasma protein binding is 99% for sulfasalazine, 50% for sulfapyridine, and 43% for 5-ASA. In the liver, sulfapyridine is biotransformed mainly by hydroxylation with the formation of inactive metabolites, 5-ASA by acetylation. T1/2 of sulfasalazine is 5-10 hours, sulfapyridine - 6-14 hours, 5-ASA - 0.6-1.4 hours. 5% of sulfapyridine and 67% of 5-ASA are excreted in feces; 75-91% of absorbed sulfasalazine is excreted by the kidneys within 3 days.

Nonspecific 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.

Porphyria, anemia, severe liver dysfunction, severe kidney dysfunction, deficiency of the enzyme glucose-6-phosphate dehydrogenase, children under 5 years of age, lactation; hypersensitivity to sulfonamides and salicylic acid derivatives.

From the nervous system: headache, dizziness, tinnitus, ataxia, convulsions, sleep disturbances, hallucinations, peripheral neuropathy.

From the urinary system: renal dysfunction, interstitial nephritis.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia, hepatitis, pancreatitis.

From the respiratory system: interstitial pneumonitis and other lesions of lung tissue.

From the hematopoietic system: anemia, leukopenia, thrombocytopenia, agranulocytosis.

From the reproductive system: transient oligospermia, infertility.

Allergic reactions: skin rash, toxic epidermal necrolysis, malignant exudative erythema, fever, anaphylactic shock.

Others: Possible yellow staining of skin, urine, and soft contact lenses.

special instructions

Use with caution in patients with impaired liver and/or kidney function, patients with bronchial asthma, allergic reactions.

During treatment, the level of liver enzymes, general blood and urine tests should be monitored.

For renal failure

Use with caution in patients with impaired renal function.

In case of liver dysfunction

Use with caution in patients with impaired liver function.

Use during pregnancy and breastfeeding

The use of sulfasalazine during pregnancy is possible only according to strict indications in the minimum effective dose. If the course of the disease allows, it is recommended to discontinue sulfasalazine in the third trimester of pregnancy.

If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

Drug interactions

Enhances the effect of anticoagulants, antiepileptic and oral hypoglycemic drugs, as well as the side effects of cytostatics, immunosuppressants, hepato- and nephrotoxic drugs.

When used simultaneously with sulfasalazine, the toxicity of azathioprine and mercaptopurine increases.

When used simultaneously with ampicillin or rifampicin, the release of 5-aminosalicylic acid from the sulfasalazine molecule in the colon is reduced (due to the suppression, under the influence of ampicillin and rifampicin, of the activity of anaerobic bacteria, with the participation of which this process occurs). In this regard, the effectiveness of sulfasalazine may be reduced. It is believed that the interaction of sulfasalazine with neomycin manifests itself in the same way.

When used simultaneously with digoxin, its absorption may be reduced; with talinolol - absorption of talinolol decreases; with folic acid - the absorption of folic acid may be reduced.

Nonspecific ulcerative colitis and Crohn's disease: when taken orally in adults, use after meals: 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 acute clinical symptoms subside, a maintenance dose of 500 mg 3-4 times a day is used for several months. Children aged 5-7 years - 250-500 mg 3-6 times / day, over 7 years - 500 mg 3-6 times / day.

Rheumatoid arthritis: adults during the first week - 500 mg 1 time / day; for 2 weeks - 500 mg 2 times a day; for 3 weeks - 500 mg 3 times a day. The therapeutic dose is 1.5-3 g/day. The course of treatment is 6 months or more. Children over 6 years of age - 30-50 mg/kg/day in 2-4 doses; for children over 16 years of age, the maximum daily dose is 2 g.