Crohn's disease - intestinal pathology, which has a tendency to progression. The inflammatory process applies transmurally and is characterized by various complications of local and system form. The disease amazes the entire thickness of the intestinal wall, narrows its lumen, form infiltrates, abscesses and ulcers. To suspend the process of the disease, the patient is prescribed anti-inflammatory funds.

To such effective drugs to eliminate and include medical means Sulfasalazine-EN and Sulfasalazine. Medicines are also prescribed with rheumatoid arthritis for pain relief and inflammation. Like many drugs, they have their own contraindications and side effects. What is the preparation of Sulfasalazin-EN, the difference from Sulfasalazina in what is it? All information will be able to learn from the article.

Release form and clinical group of Sulfasalazin-EN

The medicine has an anti-inflammatory property and is used to treat Crohn's disease and niac. It is made in tablet form, light brown color. Unlike the Sulfasalazine preparation, Sulfasalazin-EN tablets are covered with a special shell, which dissolves only in the intestine. The basic substance in the composition of the drug is sulfasalazine in a dosage of 500 mg. The remedy is packed in blisters of 10 capsules.

Act

Used drug Treatment To eliminate the symptoms of Crohn's disease and nyak. Sulfasalazine is exempt to what is an anti-inflammatory effect on the place of education of erosion. Sulfapyridine is also formed, which has antimicrobial activity and oppresses the functions of gonococcal, streptococci and intestinal sticks.

If you get inside the tablet almost not absorbed in the intestine. Here, they are split under the influence of intestinal microflora and form sulfapyridine by 75% and aminoalicyl acid by 25%. Over the course of three days, substances are mainly derived by the kidneys and only in a meager percentage ratio - feces. Such an action on the patient's body has a means of Sulfasalazine-EN. Difference from Sulfasalazina, reviews about the preparation - all this information should be examined before starting treatment.

When is a medicine?

The medicine is prescribed under the following pathologies:

• crohn's disease;
• rheumatoid arthritis.

Forbidden medication in such cases:

• kidney and liver disease;
• anemia;
• porphyria;
• pregnancy;
• lactation;
• increased sensitivity to substances included in the drug.

Before the beginning of therapeutic process, it is carefully necessary to study all contraindications for receiving the Sulfasalazin-EN medication. Difference from Sulfasalazina, special instructions - All information is important. The drug can be used after agreeing with a specialist.

What dosage is prescribed treatment?

After inspection, examination and clarification of the diagnosis, the doctor prescribes a means for the treatment of Crohn's disease and the medicine is accepted by a special scheme:

• the first day - 500 mg three or four times;
• the second day - 1 gram every six hours;
• all other days the medicine is accepted by 2 or 1.5 g.

After improving the state, the patient leaves a dose to maintain for another few months. The drug rate is 500 mg several times a day. Correction of treatment can only be performed by a specialist.

Children after 5 and up to 7 years old, the medication is prescribed at 250-500 mg several times a day. After 7 years of age, the dosage will be 500 mg to 6 times a day.

With rheumatoid arthritis, the adult medicine is also dosed on a specific algorithm:

• the first week is 1 tablet at a dose of 500 mg times per day;
• the second week is 500 mg twice a day;
• the third week is 500 mg three times.

The course of treatment is up to six months and more, depending on the severity of the disease and individual characteristics of the body.

The daily rate should not be more than 3 g for the Sulfasalazin-EN medication. The difference from Sulfasalazine instruction describes in sufficient detail. This also applies to the means of receiving the means.

Children with rheumatoid arthritis the medicine is prescribed at the rate of 50 mg per 1 kg of weight per day divided into two or three uniform receptions. For patients after 16 years, the maximum permissible dose is 2 g. The medicine is prescribed orally after meals. It is necessary to drink a large amount of liquid and not chew.

• weakness
• abdominal pain;
• dizziness;

The patient prescribe symptomatic treatment, washing the stomach. It is important to monitor urination.

According to the instructions, Sulfasalazin-EN drug instructions. The difference from Sulfasalazine (properties, form of release) is insignificant. However, it is worthwhile to ask the doctor, in what form it is better to take a medicine.

Preparation "Sulfasalazine"

The medical facility relates to a group of anti-inflammatory drugs, is prescribed for therapy of the disease Crown and a nym. It is produced in the tablet form of yellow-brown. The composition of the medicine includes sulfasalazine (500 mg).

The drug has anti-inflammatory and antimicrobial effects. It also has an immunosipressive and antiperscript. The main substance of tablets, sulfasalazine, has a positive effect on the intestines due to two active components. This is sulfopyridinone and aminoalicyl acid. It has a bacteriostatic effect on diplococci, staphylococcal and intestinal sticks preparation Sulfasalazin-EN. Difference from Sulfasalazina, a description of the operating component - all information is presented in the instructions.

Indications and contraindications

The medicine is prescribed with such pathologies:

• crohn's disease;
• various forms rheumatoid arthritis.

Contraindications:

• severe pathology of the kidneys and liver;
• blood diseases;
• age up to 5 years;
• increased hypersensitivity to components.

It has a non-essential drug "Sulfasalazin - EN" difference from Sulfasalazina. Instructions for use describes similar indications and contraindications. What medication to use in a particular case will tell a specialist.

Dosage

In the first day of treatment for adults, the medicine is prescribed at a dose of 500 mg 4 times, then on the second day - 1 g 4 times, in the future the tool is taken from 1.5 to 2 g per day. The course of treatment depends on the severity of the process and the individual characteristics of the body.

Overdose can lead to the development of the following symptoms:

• migraine;
• convulsions;
• insomnia;
• epigastric pain;
• vomiting;
• diarrhea;
• allergy.

Not such pronounced side effects has the preparation of Sulfasalazin-EN. The difference from Sulfasalazine is that the medication is covered with a shell.

If any of the described drugs acquire in the pharmacy failed, the specialist will select a high-quality substitute.

Preparation "Salofalk"

The medicine has an anti-inflammatory property and is prescribed for Crohn and Nyak's disease. Produced in the form of yellow tablets. The drug includes Mesalazin at a dose of 250 and 500 and 1 g. The remedy has anti-inflammatory, antioxidant effect on the intestinal walls

Indications:

• crohn's disease

Contraindications:

• blood disease;
• children of preschool age;
• hypersensitivity to components.

At the beginning of the medical process, it should be carefully examined by all the features of the drug "Salofalc" and "Sulfasalazin-EN". The difference from Sulfasalazina for use is insignificant. Preparations are accepted by a similar scheme.

Dosage

Patients medicine is assigned 500 mg three times a day. In severe cases, the dose can increase to 3 g per day. The tool is accepted for three months.

Medicine "Sulfasalazin-EN". Difference from Sulfasalazina: patient reviews

Two identical preparations in their composition. The only difference is that Sulfalazine-EN is covered with a shell, soluble only in the intestine, unlike sulfasalazine tablets, which are covered with film. Also, the first medicine causes a greater degree of allergic reactions that appear in the form of rashes and itching on the skin. If you believe the reviews of patients, the preparation "sulfasalazine" is in great demand.

Specialists noted that both drugs can lead to development side phenomena. It happens nausea, vomiting and pain in the stomach. At the same time, it has a slight tool "sulfasalazine-en" the difference from Sulfasalazine. Photos of medicines are also similar.

Experts note that this drug group is equally helped by all. These funds are not sufficiently reliable when the peripheral joints are damaged. To avoid development urolithiasis, Tablets are desirable to drink mineral water in large quantities, drink a lot of fluid during the day. What else does sulfasalazine-en distinguish between Sulfasalazina? Analogue (the drug "Salofalc") although it is prescribed with similar pathologies, but has much more incompatience. This is due to the difference in compositions.

Outcome

If the patient has problems with the stomach, then he is better to take Sulfasalazin-EN, which will not dissolve in the stomach, but only in the intestine. In a small part of patients in the early deadlines for the reception of this group, fever can be observed, skin rashes that pass on their own after several days of therapy.

Doses of drugs are chosen individually, depending on the intestinal damage and the development stage of the disease. During the period of exacerbation, the dosing of the medicine reaches maximum indicators, then, to improve the state, is slightly reduced. If a patient when taking medicines Site effects are largely manifested, then this should be informed of the attending physician. According to the reviews of patients, there is no significant difference between the drugs. The difference from Sulfasalazina, Sulfasalazin-EN drug, is only that the medicine dissolves in the stomach and may cause pain in the epigastric area.

If you regularly take tablets according to the specified scheme, you can suspend the process of breaking bones with rheumatoid arthritis. The medicine can be appointed by adults and children after 5 years. Do not exceed the dosage not to cause side effects that are fraught with serious complications from other organs and systems. Also, the tablets are better to drink immediately after eating and drink them with alkaline solutions, such as mineral water. After one month of treatment, an improvement in the state will be observed. The medicine is prescribed for a long period, but does not cause exciting and cancellation syndrome. The "Sulfasalazine-EN" and Sulfasalazine and Sulfasalazine are released at a prescription pharmacy.

**** Krka Krka D.D. Krka D.D. Novo Place of JSC / Vector-Medica, CJSC Krka D.D., Novo Place / Krka-Rus, OOO Krka, D.D., Novo Place Tedele, OOO

Country of origin

Russia Slovenia Slovenia / Russia

Group of goods

Digestive tract and metabolism

The drug with anti-inflammatory effect used to treat Crohn's disease and Nyak

Forms of release

• 10 - blisters (5) - packs cardboard. 10 - Packaging Cell Contour (5) - Cardboard packs.

Description of the dosage form

• Tablets covered with an intestine-soluble shell from yellow to brownish yellow color, round, double-screw, with a bevelled edge, with a characteristic odor; At the break - from orange to brownish-orange. Tablets covered with a film shell of brownish yellow color, round, double-screw, with a bevelled edge; Enclosures are allowed.

pharmachologic effect

Sulfasalazine selectively accumulates in connective tissue The intestine with the release of 5-aminoalcyl acid (5-ASC), which has anti-inflammatory activity, and sulfapyridine, which has antimicrobial bacteriostatic activity against diplococci, streptococcal, gonococcal, intestinal sticks. Pharmacokinetics. About 30% sulfasalazine in pasta-soluble shell tablets are absorbed from fine intestine, The remaining 70% is subjected to cleavage of the intestinal microflora with the formation of sulphapyridine 60-80% and 25% - 5-ASC. Sulfasalazine reaches a maximum concentration 3-12 hours after taking tablets coated with an intestinal-soluble shell. Communication with Sulfasalazine plasma proteins - 99%, sulfapyridine - 50%, 5-ASC - 43%. Sulfapyridine is subjected to metabolism in the liver by hydroxylation with the formation of inactive metabolites, 5-ASC - by acetylation. The half-life of sulfasalazine - 5-10 hours, sulphapyridine - 6-14 hours, 5-ASK - 0.6-1.4 h. Excluded through the intestine - 5% sulfapyridine and 67% 5-ASK, kidneys - 75-91% of Vostea Sulfasalazine (within 3 days).

Pharmacokinetics

Suction sulfasalazine is poorly absorbed in the intestine (no more than 10%). It is subjected to cleavage of the intestine microflora with the formation of 60-80% sulfapyridine and 25% 5-aminosalcyl acid (5-ASC). The distribution binding to plasma proteins is: for sulfasalazine - 99%, for sulfapyridine - 50%, for 5-ASC - 43%. Metabolism in the liver Sulfapyridine biotransformated mainly by acetylation, 5-ASC - by acetylation. The removal of T1 / 2 sulfasalazine is 5-10 hours, sulfapyridine - 6-14 hours, 5-ASK - 0.6-1.4 hours. 5% sulfapyridine is derived and 67% 5-ASK; 75-91% of sulfasalazine is excreted by the kidneys within 3 days.

Special conditions

During the period of treatment, periodic control of the level of "liver" enzymes in blood plasma is recommended, general analysis blood (at the beginning of therapy: 1-2 times a month, then every 3-6 months of treatment) and urine analysis (when renal failure), use increased quantity liquids. Sulfasalazine is recommended to assign patients with caution with systemic forms of juvenile rheumatoid arthritis, because There is a risk of developing unwanted effects, incl. serum disease (fever, nausea, vomiting, headache, rash and violation of the liver function). Impact on the ability to control the car and other mechanical means: there were no messages about the meaning of sulfasalazine-en on the ability to control the car and other mechanisms.

Structure

• 1 tablet contains: kernel: active substance: sulfasalazine coated (corresponds to 500 mg of sulfasalazine) 535,000 mg auxiliary substances: starch preelectinized, magnesium stearate, silicon colloidal dioxide, anhydrous. Shell: titanium dioxide, iron dye oxide yellow 10 (E172), talc, triethyl citrate, macrogol-6000, sodium carmellosis, methacrylic acid and ethyl acrylate copolymer (1: 1) (dry matter). SulphazAlazine 500 mg Auxiliary substances: Starch gelatinated, magnesium stearate, silicon oxide colloid anhydrous. The composition of the shell: hypimelloosis, propylene glycol. SulfaAlazine500 mg Auxiliary substances: Starch gelatinated, magnesium stearate, silicon oxide colloidal anhydrous. The composition of the shell: hypimon, propylene glycol

Sulfasalazine testimony for use

• - nonspecific ulcerative colitis (treatment of exacerbations and supporting therapy in the phase of remission); - Crohn disease (light and medium-free forms in the aggravation phase); - rheumatoid arthritis; - Juvenile rheumatoid arthritis.

Sulfasalazine contraindications

• - Porphyria; - anemia; - pronounced liver function; - pronounced disorders of the kidney function; - Glucose-6-phosphate dehydrogenase enzyme deficiency; - childhood up to 5 years; - lactation period; - increased sensitivity to sulfanimide and salicylic acid derivatives.

Sulfasalazine Dosage

• 500 mg 500 mg 10pcs.,

Sulfasalazine Side effects

• Side effects are associated with the degree of plasma concentration of sulfapyridine, especially in people with slow acetylation. More often, side effects are observed in patients with rheumatoid arthritis. From the central and peripheral nervous system: Headache, peripheral neurophated, vertigo, dizziness, hallucinations, cramps, ataxia, sleep disorder, depression, aseptic meningitis. From side gastrointestinal tract: nausea, vomiting, diarrhea, decline in appetite, pancreatitis, stomatitis, abdominal pain, medicinal hepatitis. From the Blood Organs: macrocytosis, leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia due to enzyme disorders - with unstable hemoglobin molecules (heinz-erlich), methemoglobinemia, agranulocytosis, thrombocytopenia, egoistic anemia, hypoprothrombinemia. From the urogenital system: proteinuria, hematuria, crystalluria, nephrotic syndrome, transient oligospermia and infertility. From the respiratory system: shortness of breath, cough, interstitial pneumonite, fibrosing alveolit, infiltrates in the pulmonary fabric. From the sovereign organs: noise in the ears. Laboratory data: hyperbilirubinemia, an increase in alkaline phosphatase activity, "liver" transaminase. Allergic reactions: generalized skin rash, urticaria, erythema, skin itch, exfoliative dermatitis, photosensibilization, toxic epidermal necroliza (Lailela syndrome), malignant exetamental erythema (Stevenson syndrome), fever, lymphoaciadenopathy, serum disease, periorubital swelling, eosinophilic, nodular polymeritis, anaphylactic shock. Others: Hyperthermia, steaming, possibly staining urine, leather or soft contact lenses In yellow-orange color.

Medicinal interaction

Sulfasalazine reduces suction folic acid and Digoxin. Enhances the effect of anticoagulants, anti-epileptic and oral hypoglycemic agents, as well as side effects of cytostatics, immunosuppressants, hepato and nephrotoxic agents. Drugs, inhibiting bone marrowing, increase the risk of myelosuppression. Antibiotics due to the depressing effect on the intestinal flora reduce efficiency with ulcerative colitis.

Overdose

Symptoms: nausea, vomiting, abdominal pain, dizziness. When using very high doses, there may be: anuria, crystalluria, hematuria, symptoms of toxic damage to the central nervous system (seizures). Treatment: symptomatic. It is necessary: \u200b\u200bprovoke vomiting, rinse the stomach, intestines; Conduct urine sickness, forced diuresis. With anuria and / or renal failure: fluid consumption and electrolytes should be limited.

Storage conditions

• bear from children

Information provided

Catad_pgroup intestinal anti-inflammatory and antimicrobial

Sulfasalazine EN - Instructions for use

Registration doner:

N015099 / 01-160717

Trade name:

Sulfasalazine-Ene

International non-proprietary name:

sulfasalazine

Dosage form:

intestinal pills covered with film shell

Structure

1 Incore-soluble tablet, film shell, contains:

Core:

Active substance:

Sulfasalazine covered with povedium, 535.00 mg (equivalent to sulfasalazine 500 mg)

Excipients:starch premaritalized, magnesium stearate, silicon colloid dioxide, anhydrous

Shell:

Titanium dioxide (E171), iron dye oxide yellow (E172), talc, triethyl citrate, macrogol-6000, sodium carmellosis, methacrylic acid and ethyl acrylate copolymer (1: 1) *

* Dry substance

Description

Round biconvecake tablets with a beveled edge, covered with a shell from yellow to brownish yellow with a characteristic odor.

At the breakfast rough mass from orange to brownish-orange color.

Pharmacotherapeutic Group:

antimicrobial and anti-inflammatory intestine

Codath: A07ES01.

Pharmacological properties:

Pharmacodynamics

Sulfasalazine selectively accumulates in the intestinal connective tissue with
the release of 5-aminoalcyl acid (5-ASC), which has anti-inflammatory activity, and sulphapyridine, which has antimicrobial bacteriostatic activity against diplococci, streptococcal, gonococcal, intestinal sticks.

Pharmacokinetics

About 30% sulfasalazine in intestinal-soluble tablets are absorbed from the small intestine, the remaining 70% are subjected to cleavage of the intestinal microflora with the formation of sulfapyridine and 5-ASC, 60-80% and 25%, respectively. Sulfasalazine reaches a maximum concentration in the blood plasma 3-12 hours after taking intestinal tablets.

Communication with sulfasalazine blood plasma proteins - 99%, sulfapyridine - 50%, 5-ASC -43%. Sulfapyridine is subjected to metabolism in the liver by hydroxylation with the formation of inactive metabolites, 5-ASC - by acetylation. Sulfasalazine semi-alone period - 5-10 hours, sulfapyridine - 6-14 hours, 5-ASK - 0.6-1.4 hours. Examined through the intestines of 5% sulfapyridine and 67% 5-ASK, the kidneys - 75-91% of the sulfasalazine seeds (for 3 days).

Indications for use

• Ulcerative colitis (exacerbation treatment and maintenance therapy in the remission phase);
• crohn's disease (light and medmetry forms in the exacerbation phase);
• rheumatoid arthritis, juvenile rheumatoid arthritis in the ineffectiveness of non-steroidal anti-inflammatory drugs (NSAID).

Contraindications

• Hypersensitivity to sulfasalazine or other components of the drug, as well as sulfonamides or salicylates;
• porphyria;
• granulocyptopenia;
• aplastic anemia;
• congenital shortage of glucose-6-phosphate dehydrogenase (risk of jaundice development);
• liver and / or renal failure;
• children under 10 years old and / or with a body weight of less than 35 kg with chronic inflammation of the intestine, children under 6 years old with juvenile rheumatoid arthritis (for this given dosage form and dosages) (efficiency and security are not proven);
• obstruction of intestines or urinary tract;
• breastfeeding period.

Carefully

Bronchial asthma, atopic dermatitis, allergic reaction In history (it is possible to cross allergic reaction to furosemide. Tiazide diuretics, sulfonylurea derivatives. Carbonithic inhibitors), system forms of juvenile rheumatoid arthritis (risk of serum disease), pregnancy.

Application during pregnancy and in breastfeeding period

During pregnancy, the use of sulfasalazine drug is possible only by strict indications and in a minimum effective dose. If the course of the disease allows the course of the disease, in the last III trimester of pregnancy, the use of sulfasalazine-EN drug should be stopped (sulfasalazine displaces bilirubin due to blood plasma proteins, thereby increasing the risk of developing nuclear jaundice and hyperbilirubinemia in newborns - toxic lesion of brain nerve centers). In newborns with a glucose-6-phosphate dehydrogenase deficiency, hemolytic anemia is possible.

Sulfasalazine is normally stand out in maternal milk in a very small amount. In premature newborn and children in high-risk groups increase the risk of developing nuclear jaundice. The concentration of sulphapyridine in maternal milk is 40% of the concentration in the plasma of the mother.

If necessary, the use of a sulfasalazine drug during lactation should be resolved by the issue of cessation of breastfeeding.

Method of application and dose

Inside, after meals.

Ulcerative colitis, Crohn's disease

in the 1st day of 500 mg 4 times a day, in the 2nd day of 1 g 4 times a day, in the 3rd and subsequent days 1.5-2 g 4 times a day. After anemia of sharp clinical symptoms Ulcerative colitis

adults and children over 16 years old and / or withbody weight more than 65 kgassign a supporting dose of 500 mg 3-4 times a day for several months.

Children aged 10 to 16 years old and / or with a mass of body from 35 kg to 50 kg:500 mg 4 times a day.

Supporting therapy for children under 16 years and / or body weight less than 65 kgnot recommended.

Maximum daily dose For adults - 8 g, for children up to 16 years old - 2 g.

Rheumatoid arthritis and juvenile rheumatoid arthritis

Adults and children over 16 years old:during the first week, 500 mg is scheduled 1 time per day, during the second week - 500 mg 2 times a day, within the third week - 500 mg 3 times a day, etc. Therapeutic dose can be from 1, 5 g to 3 g per day.

Clinical effect appears after 6-10 weeks of therapy. The course of treatment is 6 months or more.

Children from 6 to 8 years and / or with a mass of body 20-29 kg:1 tablet 2 times a day.

Children from 8 to 12 years and / or with a body weight 30-39 kg:1 tablet 2-3 times a day.

Children from 12 to 16 years and / or with a mass of body 40-50 kg:1 Tablet 3 times a day or 2 tablets 2 times a day.

Children over 16 years old and / or with a mass of body more than 50 kg: 2tablets 2 times a day.

The maximum daily dose for children is 2 g or 40-50 mg / kg body weight.

Side effect

Side effects are associated with the degree of plasma concentration of sulfapyridine, especially in people with slow acetylation. More often, side effects are observed in patients with rheumatoid arthritis.

Blood violations and lymphatic system:macrocytosis. leukopenia, neutropenia, megaloblastic anemia, hemolytic anemia, hemolytic anemia with the formation of the Taurus of Geinz-Erlich, methemoglobinemia, agranulocytosis. Thrombocytopenia, aplastic anemia, hypoprothrombinemia.

Immunuted violations:generalized skin rash, urticaria, erythema, skin itching, exfoliative dermatitis, photosensibilization, fever, lymphoaciadenopathy, serum disease, periorubital swelling, eosinophilia, nodery periarteritis, anaphylactic shock.

Psyche violations:hallucinations, sleep disorder, depression.

Violations from the nervous system:headache, peripheral polyneuropathy, vertigo, dizziness, cramps, ataxia, aseptic meningitis.

Violations by the hearing body and labyrinth violations:noise in ears.

Disorders of the respiratory system, organs chest and mediastinum:dyspnea, cough, interstitial pneumonite, fibrusing alveolitis, infiltrates in pulmonary fabric.

Violations from digestive system: nausea, vomiting, diarrhea, decline in appetite, pancreatitis, stomatitis, abdominal pain, medicinal hepatitis.

Violations from the rut and subcutaneous fabrics:heavy skinless unwanted reactions: very rare cases of development of Stevens-Johnson syndrome (CDS) and toxic epidermal necrolis (TEN) were reported.

Disorders from the kidneys and urinary tract:proteinuria, hematuria. Crystaluria, nephrotic syndrome.

Disorders from the genital organs and breasts:transient oligospermia and infertility.

Laboratory and instrumental data:hyperbilirubinemia. Improving the activity of alkaline phosphatase, "liver" trisaminatez in the blood plasma.

General disorders and disorders at the injection site:hyperthermia, steaming, possibly staining urine, leather or soft contact lenses in yellow-orange color.

Overdose

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

Treatment:symptomatic. It is necessary to provoke vomiting, rinse the stomach and intestines, to hold urine squeezing, forced diuresis. With anuria and / or renal failure, the consumption of fluid and electrolytes should be limited.

Interaction with other medicines

Sulfasalazine reduces suction folic acid and digoxin.

Enhances the action anticoagulants, antiepileptic and hypoglycemicmeans for intakes, as well as side effects cytostaticsimmunosuppressants, hepato and nephrotoxicfunds.

Drugs, depressing bone marrowing,increase the risk of the development of myelosuppression.

Antibioticsdue to the depressing effect on the intestinal flora, the efficiency of sulfasalazine is reduced with ulcerative colitis.

special instructions

During the period of treatment, it is recommended: periodic control of the activity of "liver" enzymes in the blood plasma, a general blood test (at the beginning of therapy - 1-2 times a month. Then every 3-6 months of treatment) and urine analysis (with renal failure), consumption of increased The amount of fluid. Sulfasalazine is recommended with caution to prescribe patients with systemic forms of juvenile rheumatoid arthritis, since there is a risk of developing unwanted effects, including serum disease (fever, nausea, vomiting, headache, skin rash and liver function).

Against the background of the use of the sulfasalazine drug, skin-threatening skin reactions were recorded: SSD and TEN.

Patients should be warned about clinical manifestations and symptoms and should closely monitor the development of skin reactions. The highest risk of developing CDD and TEN during the first weeks of treatment.

When appearance clinical manifestations Or symptoms of SSD and TEN (for example, progressive skin rash is often with blisters or lesions of the mucous membrane) should be discontinued with sulfasalazine-en.

The best results of the treatment of SSD and TEN are achieved with early diagnosis and immediate stopping the use of any suspicious drug. Early cancellation of the drug is associated with the best forecast.

If the patient, when using the sulfasalazine preparation, the SUDD or TEN developed, to resume sulfasalazine therapy in this patient cannot be.

Impact on the ability to manage vehicles, mechanisms

Care must be taken when driving and working with complex technical devices due to the possibility of dizziness.

Form release

Tablets are intestinal soluble, film coated, 500 mg.
10 tablets in PVC blister / aluminum foil.
5 blisters in a pack of cardboard, along with instructions for use.

Storage conditions

At a temperature not higher than 25 ° C, in the original packaging. Keep out of the reach of children.

Shelf life

5 years.
Do not apply the drug after the expiration date.

Conditions of vacation

Released on the recipe.

Name and address of the holder (owner) registration certificate

Production of the finished dosage form

JSC "Krka, D.D., Novo Place", Shmariška Cesta 6, 8501 Novo Place, Slovenia

Primary packaging

JSC "Krka, D.D., Novo Place", Shmariška Cesta 6, 8501 Novo Place, Slovenia

Secondary / consumer packaging

JSC "Krka, D.D., Novo Place", Shmariška Cesta 6, 8501 Novo Place, Slovenia
JSC "Krka, D.D., Novo Place", Rada Street Pashenyaka 10, 9240 Lutomer, Slovenia

CJSC "Vector-Medica", 630559, Russia, Novosibirsk region, Novosibirsk paradise r. p. Koltsovo, Corp. 13, Corp. 15, Corp. 38.

Manufacturer (issuing quality control)

JSC "Krka, D.D., Novo Place", Shmariška Cesta 6, 8501 Novo Place, Slovenia
LLC KRKA-RUS, 143500, Russia, Moscow region, Istra, ul. MOSCOW, D. 50
CJSC "Vector-Medica", 630559, Russia, Novosibirsk region, Novosibirsk district. R. p. Koltsov, Corp. 13, Corp. 15, Corp. 38.

The name and address of the organization accepting consumer claims

Krka-Rus, OOO, 125212, Moscow, Golovinskoye Highway, House 5, Corpus 1

Description

Round, brownish yellow, slightly twofolding tablets, with beveled edges, covered with a transparent colorless film.

The heterogeneity of staining in the form of brighter inclusions and / or spots is allowed.

Structure

One tablet covered with film shell contains 500 mg of sulfasalazine (salazosulfapyridine).

Excipients: Povidone, starch premaritalized, magnesium stearate, silicon dioxide colloidal, hypimon, propylene glycol.

Pharmacotherapeutic group

Anti-diagracial, intestinal anti-inflammatory / anti-infectious drugs. Aminosalcyl acid and its derivatives. ATX code: A07ES01.

Pharmacological properties

Pharmacodynamics

Sulfasalazine (Salazosulfapyridine) has an immunosuppressive, anti-inflammatory and bactericidal action.

Its action is the result of the influence of two metabolites, which local affect the intestinal wall, while at the same time, providing a systematic action.

Sulfapyridine inhibits the effect of natural killer cells (NK cells) and the transformation of lymphocytes.

Anti-inflammatory effect of 5-aminosalcyl acid, possibly the most important property in the treatment of inflammatory bowel diseases, since it inhibits cyclooxygenase and lipoxygenase in the intestinal wall and thereby prevents the formation of prostaglandins, leukotrienes and other inflammation mediators, and also probably binds free oxygen radicals.

Sulfasalazine does not have an anesthetic effect.

Pharmacokinetics

Suction

About 30% of the accepted sulfasalazine is absorbed from the small intestine; The remaining 70% is metabolized by intestinal intestinal bacteria with the formation of sulfapyridine and 5-aminosalcyl acid. Distribution

There are large differences in the maximum serum concentration of sulfasalazine and its metabolites; In slow acetyluorors, they are much higher and are associated with a more frequent occurrence of side effects. Sulfasalazine reaches the maximum serum concentration within 3-12 hours after taking the drug. Communication with plasma and connective tissue proteins is very high. Most of the absorbed sulfasalazine returns with bile in the intestines; A small part is removed unchanged with urine. The half-life of sulfasalazine - 5-10 hours.

Most of the formed sulfapyridine is absorbed and reaches the maximum concentration in serum 12-24 hours after receiving the drug.

Metabolism and elimination

Sulfapyridine is subjected to metabolism in the liver (acetylation, hydroxylation and conjugation with glucuronic acid) and is excreted by the kidneys. The half-life period is 6-14 hours, depending on the speed of acetylation.

Only about 30% of 5-aminosalcyl acid is absorbed and acetylated in the liver, and then excreted by the kidneys. The rest is removed unchanged with the feces.

Indications for application

For treatment acute manifestations and exacerbations of crown disease, ulcerative colitis and proctitis, for supporting therapy in the phase of the remission of ulcerative colitis and proctitis, for the treatment of rheumatoid arthritis and juvenile idiopathic chronic polyarthritis, resistant to non-steroidal anti-inflammatory drugs.

Sulfasalazine can be used in combination with corticosteroids and metronidazole.

Method of application and dosage

The dosage must be established depending on the severity of the disease and possible unwanted effects. Tablets should be taken while eating, drinking liquid.

The missed dose should be taken as soon as possible, if the time of the next reception is not coming. Otherwise, only another dose should be adopted, in accordance with the treatment scheme.

Acute seizures of ulcerative colitis and proctitis, crown disease

Adults and children over 16 should take 2-4 tablets (1-2 g) 4 times a day.

Children over two years old can give 40 - 60 mg of drug per kilogram body weight per day.

When remission reach, the dose should be gradually reduced. Supporting therapy in the phase of the remission of ulcerative colitis and proctitisRecommended supporting dose for adults and children over 16 years old - 1 tablet (500 mg) 4 times a day.

Children over 2 years old can give 20-30 mg of sulfasalazine per kilogram of body weight per day.

The duration of supporting therapy is not limited.

Rheumatoid arthritis and juvenile idiopathic chronic polyarthritis

Recommended dose for adults and children over 16 years old: 2-3 g per day. Start therapy follows from 1 tablet (500 mg) sulfasalazine per day. The dosage should be increased gradually, from weekly intervals, so that after 4 weeks the dose was 2 tablets (1 g) 2-3 times a day. The clinical effect becomes apparent to 6-10 week of therapy. The drug should be taken at least 6 months.

Children over 6 years old can give 30-50 mg of the drug per kilogram of body weight per day in 2-3 receptions. Begin treatment follows from 1/3 or 1/4 recommended dose, for example, from one tablet for the night. Dosage should be increased gradually, from weekly intervals, until the recommended dose is achieved. The maximum daily dose should not exceed 2 g (4 tablets).

Special groups of patients

Elderly people

Dose correction is not required

Patients with renal failure

It should be used in patients with renal failure in patients (creatinine clearance less than 60 ml / min). Such patients do not require a dose correction. Recommended before, and sometimes during treatment to monitor urine analysis. During treatment, patients should use a sufficient amount of fluid.

Patients with hepatic insufficiency

It should be used in patients with hepatic insufficiency in patients. Such patients do not require a dose correction.

Side effect

Sulfasalazine side effects are mainly associated with high concentration Sulfapyridine in the blood, especially among people whose decay occurs slower (slow acetyluoris). Side effects are more common in patients with rheumatoid arthritis.

Side effects that may occur in the process of sulfasalazine treatment are divided into the following groups in the frequency of occurrence:

Very frequent (≥ 1/10), frequent (≥ 1/100 to each group side effects Presented in descending order of their gravity. The frequency of side effects is listed for individual system systems.

Research

Infrequent: Enhance the serum concentration of amylase, bilirubin, alkaline phosphatase and hepatic levels Transaminase

Blood violations and lymphatic system

Frequent: leukopenia, neutropenia, macrocytosis are infrequent: Megaloblastic anemia, hemolytic anemia, agranulocytosis, thrombocytopenia Very rare: Aplastic anemia, methemoglobinemia, anemia with Heints Tales, Hypoprothrofilia, Lymphadenopathy, Eosinophilia Disorders of the nervous system Frequent: Headache Rare: peripheral neuropathy, dizziness, cramps, Ataxia Very rare: Aseptic meningitis

Violation of hearing and equilibrium

Infrequent: ringing in the ears

Respiratory, thoracic disorders and violations by the mediastinal

Rare: pulmonary infiltration, dysnae, cough very rare: fibrous alveolo

Gastrointestinal disorders

Frequent: nausea, vomiting are infrequent: diarrhea, stomatitis, rare paotes: pancreatitis

Disorders from the kidneys and the urogenital system

Rare: nephrotic syndrome, hematuria, proteinuria, crystalluria

Violations of metabolism and nutritional disorders

Frequent: anorexia is infrequent: in patients with porphyria, sulfasalazine can lead to exacerbation of the disease

Disorders of the immune system

Very rare: serum disease, generalized skin rash, multiform examination, exfoliative dermatitis, photosensibilization, drug-induced fever, periorebital swelling, nodule polyarterite conjunctiva or cornea, urticaria, itching, redness.

Disturbing from the skin and subcutaneous fiber

Very rare: Stevens-Johnson syndrome, toxic epidermal necroliz

Hepatobiliary violations

Rare: hepatitis; Staining urine, leather or soft contact lenses in yellow-orange color.

Disorders of the reproductive system and breast disorders

Infrequent: reversible oligospermia, reversible male infertility

Mental violations

Infrequent: Depression, insomnia Rare: Hallucinations

If serious side effects are observed, the treatment must be stopped.

Contraindications

Hypersensitivity K. active substance, sulfonamidam, salicylate or any of the aids.

The drug cannot be taken to patients with acute porphyria and / or granulocytopenia.

The drug is not recommended for children up to 2 years old with chronic inflammatory colon diseases and children under 6 years old with juvenile idiopathic chronic polyarthritis, since the safety and effectiveness of treatment have not been proven. In addition, the drug is not recommended in the system form of juvenile idiopathic chronic polyarthritis, as it can often entail unwanted consequences, including serum-like reactions.

Overdose

Too large doses cause nausea, vomiting and abdominal pain. At very high doses, Anururia, crystalluria, hematuria and symptoms of toxic damage to the central nervous system (seizures) can develop.

Toxicity is proportional to the concentration of sulfapyridine in serum.

Treatment: Preventing the absorption of the drug (vomiting, washing the stomach, intestinal emptying), urine sickness, forced diuresis. In the case of Anururia and / or renal failure, fluid consumption and electrolytes should be limited. The effectiveness of the measures taken may be monitored by determining the concentration of sulfapyridine in the blood plasma.

Precautions

It is recommended before the treatment of sulfasalazine and, if necessary, during treatment with the drug, to do blood tests (clinical blood test: at the beginning of treatment 1-2 times a month, then every 3-6 months) and urine.

During treatment, patients should use a sufficient amount of fluid.

In the treatment of sulfasalazine, special attention should be paid to patients with renal (creatinine clearance less than 60 ml / min) or hepatic insufficiency, bronchial asthma and allergies (it is possible to cross hypersensitivity to furosemide, thiazide diuretics, sulfonylurea derivatives and carbonic henching inhibitors).

With softer allergy forms on sulfasalazine, patients may be desensitized.

When using sulfasalazine, life-threatening skin reactions were recorded: Stevens-Johnson syndrome and toxic epidermal necrolis. The patient must be reported signs of Stevens-Johnson syndrome and toxic epidermal necrolis. The patient must closely monitor the skin reactions. The greatest risk of Stevens-Johnson's syndrome and toxic epidermal necrolize during the first week of treatment. If symptoms or signs of Stevens-Johnson syndrome and toxic epidermal necrolize are observed (for example: the progression of the skin rash is more often in the form of a bullous lesion or lesion of the mucous), the treatment of sulfasalazine should be discontinued.

In the early diagnosis of Stevens-Johnson's syndrome and toxic epidermal necrolis, good results are achieved in the management of this disease. Early termination of the use of the drug is associated with best predictions. Patients, in the history of which were recorded signs of Stevens-Johnson syndrome and toxic epidermal necrolis, when taking sulfasalazine, should not receive this drug.

Pregnancy and lactation

The data collected with the participation of a limited number of pregnant patients does not demonstrate the negative effect of sulfasalazine on pregnancy or on the health of the fetus and a newborn baby. To date, there are no other relevant epidemiological data. Pregnant women prescribe a drug with caution. Pregnant women can take sulfasalazine with the obvious necessity and in minimally effective doses. Sulfasalazine is not recommended in the last trimension of pregnancy, because It can exhibit bilirubin from plasma protein binding centers in newborns and be the cause of nuclear jaundice. In newborns with a deficiency of glucose-6-phosphate-dehydrogenase, this can lead to hemolytic anemia.

A very small amount of sulfasalazine stands out from breast milk; Thus, the probability of the development of nuclear jaundice in a healthy newborn is insignificant, which is also confirmed by experience. Difficulties may arise from premature babies or other newborns with risk. Sulfopyridine situation is different: its concentration in milk reaches 40% of the plasma concentration, but it, however, is moderately associated with plasma proteins. Since the consequences of taking sulfasalazine in children on breastfeedingwere not well understood quite well, then breastfeeding during treatment is not recommended.

Impact on the ability to drive a car or other mechanisms

Sulfasalazine does not either have a slight impact on the ability to control the car or other mechanisms.

Packaging

50 tablets covered with film shell, 500 mg (blister 10 pills, 5 blisters in a cardboard pack).

Information about the manufacturer

Krka, D.D., Novo, Schmariška Cesta, 6, 8501 Novo, Slovenia.

Sulfasalazine is an anti-inflammatory and antibacterial agent used in gastroenterology and rheumatology. Inflammatory bowel diseases (Crohn's disease, nonspecific ulcerative colitis) - are relevant problem in gastroenterological practice. However, despite certain successes in the development of new methods for the diagnosis and treatment of these diseases, there is still a lack of knowledge in the field of etiology of the development of inflammatory processes in the intestine. Thus, one of the decisions of the issues facing scientists is to increase the efficiency of already known drugs. The principle "New is well forgotten old", as it turns out, works in relation to pharmacology. Sulfasalazine is not new to the pharmaceutical front: it is applied for over 50 years. This medicinal product was synthesized by binding nitrogen group Two substances: aminoalicyl acid and sulfapyridine. Pharmacological effect The drug is based on the properties of both its structural components. Salicylic acid With an amino group in 5, it has anti-inflammatory activity, the synthesis of mediators of inflammation of prostaglandins is inhibited and the cyclooxygenase action levels. Sulfapyridine, in turn, has an antibacterial (bacteriostatic) action directed towards streptococci, gonococci, diplococci and intestinal wand. After taking sulfasalazine tablets, about 25% of the dose is already absorbed in the upper gastrointestinal sections, while due to the portal-biliary circulation of bile acids more than half of this amount is subsequently returned to the intestine.

As a result, about 90% of the drug fall into the colon, which should be considered very high indicator. Clinical trials of sulfasalazine showed the effectiveness of treatment with the drug and medium forms of non-specific ulcerative colitis (the improvement was noted in 64-80% of patients at 30% improvement when receiving placebo). The same studies have demonstrated the dose-dependence of the sulfasalazine effect, while the increase in the dose was often associated with an increase in the risk of the occurrence of certain adverse reactions.

Another area of \u200b\u200bapplication of sulfasalazine is the treatment of rheumatoid arthritis. This is one of the most common. chronic diseases joints based on which lies inflammatory process. In recent years, the possibilities of rheumatologists in the fight against this fraught disability increased incl. Due to the emergence of new medicines. From this point of view, sulfasalazine can be viewed as the "new old" drug with a newly proven in the 80s with antiordheretical activity. The positive effect of this drug is associated with its ability to influence the microflora of a large intestine. Clinical researches 63% showed - success in the treatment of patients with the articular form of rheumatoid arthritis after the year of reception of the drug.

Sulfasalazine is only available in tablet form. The drug should be taken after meals. The dose and the multiplicity of reception is established by the attending physician.

Pharmacology

Sulfasalazine is selectively accumulated in the intestinal connective tissue with a release of 5-aminosalcyl acid, which has anti-inflammatory activity, and sulfapyridine that has antimicrobial effect.

Pharmacokinetics

Suction

Sulfasalazine is poorly absorbed in the intestine (no more than 10%). It is subjected to cleavage of the intestine microflora with the formation of 60-80% sulfapyridine and 25% 5-aminosalcyl acid (5-ASC).

Distribution

The binding of plasma proteins is: for sulfasalazine - 99%, for sulfapyridine - 50%, for 5-ASC - 43%.

Metabolism

In the liver, sulfapyridine biotransformed mainly by acetylation, 5-ASC - by acetylation.

Election

T 1/2 of sulfasalazine is 5-10 hours, sulfapyridine - 6-14 hours, 5-ASK - 0.6-1.4 hours. 5% sulfapyridine is derived and 67% 5-ASK; 75-91% of sulfasalazine is excreted by the kidneys within 3 days.

Form release

Tablets covered with a film shell of brownish yellow color, round, double-screw, with a bevelled edge; Enclosures are allowed.

Auxiliary substances: starch premaritalized, magnesium stearate, silicon oxide colloid anhydrous.

The composition of the shell: hypimelloosis, propylene glycol.

10 pieces. - Packaging cell contour (5) - packs cardboard.

Dosage

Adults on the first day of treatment are prescribed at a dose of 500 mg 4 times / day; in the 2nd day - 1 g 4 times / day; In the 3rd and subsequent days - 1.5-2 g 4 times / day. After an element of acute clinical symptoms of ulcerative colitis, a drug is prescribed in a supporting dose of 500 mg 3-4 times / day for several months.

The drug should be taken after meals.

Overdose

Symptoms: nausea, vomiting, abdominal pain, dizziness.

Treatment: stomach wash, forced diuresis; Symptomatic therapy.

Interaction

With the simultaneous use of sulfasalazine reduces the absorption of folic acid and digoxin.

With the simultaneous use of sulfasalazine enhances the effect of anticoagulants and sulfonyl mooring derivatives.

With the simultaneous use of sulfasalazine and antibiotics, a decrease in sulfasalazine efficiency is possible, since antibiotics have an inhibitory effect on the intestinal flora.

Side effects

From the CNS and the peripheral nervous system: headache, dizziness, noise in ears, ataxia, cramps, sleep disorders, hallucinations, peripheral neuropathy.

From the urinary system: disorders of the kidney function, interstitial jade.

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

By the respiratory system: interstitial pneumonite and other lesions of the pulmonary fabric.

From the side of the blood formation system: anemia, leukopenia, thrombocytopenia, agranulocytosis.

From the reproductive system: transient oligospermia, infertility.

Allergic reactions: skin rash, fever, anaphylactic shock.

Others: It is possible to stain in yellow skin, urine, soft contact lenses.

Indications

• nonspecific ulcerative colitis (treatment of exacerbations and supporting therapy in the Remission phase);
• crown disease (light and medium-free forms in the aggravation phase);
• rheumatoid arthritis;
• juvenile rheumatoid arthritis.

Contraindications

• blood diseases;
• porphyria;
• pronounced liver disorders;
• pronounced disorders of the kidney function;
• shortage of enzyme glucose-6-phosphate dehydrogenase;
• children's age up to 5 years;
• increased sensitivity to sulfanimide and salicylic acid derivatives.

Features of application

Application in pregnancy and breastfeeding

The use of sulfasalazine during pregnancy is possible only by strict indications in the minimally effective dose. If the course of the disease is allowed, it is recommended to cancel the drug in the third trimester of pregnancy.

If necessary, the use of the drug during the lactation period should be resolved about the cessation of breastfeeding.

Application with violations of liver function

Contraindicated with expressed liver disorders.

Application with violations of the kidney function

Contraindicated with pronounced renal function.

Application in children

The drug is contraindicated to children under 5 years old.

Children at the age of 5-7 are prescribed 250-500 mg 3-6 times / day, children over 7 years old - 500 mg 3-6 times / day.

special instructions

Caution should be prescribed to the drug with patients with impaired liver function and / or kidney, patients with bronchial asthma, allergic reactions.