Sulfasalazine-EH
Sulfasalazin-EN: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Sulfasalazin-EN
ATX code: A07EC01
Active ingredient: Sulfasalazine (Sulfasalazine)
Manufacturer: KRKA, dd (Slovenia)
Description and photo update: 2018-24-10
Prices in pharmacies: from 309 rubles.
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Sulfasalazine-EH is a drug with antimicrobial and anti-inflammatory effects.
Release form and composition
Dosage form of Sulfasalazine-EH - enteric-coated tablets: biconvex with beveled edges, round, with a specific odor, with a yellow or brownish-yellow coating; the core in a cross section is from brownish-orange to orange (10 pcs in a blister, 5 blisters in a cardboard box).
Composition of 1 tablet:
- active substance: sulfasalazine - 500 mg;
- auxiliary components (core): povidone, pregelatinized starch, magnesium stearate, anhydrous colloidal silicon dioxide;
- shell: titanium dioxide, dye yellow iron oxide 10 (E172), macrogol 6000, talc, sodium carmellose, triethyl citrate, copolymer of ethyl acrylate and methacrylic acid (1: 1).
Pharmacological properties
Pharmacodynamics
The active substance, sulfasalazine, tends to selectively accumulate in the connective tissue of the intestine, the thickness of the intestinal wall and serous fluid. Due to the intestinal microflora, the substance decomposes into sulfapyridine and mesalazine (5-aminosalicylic acid).
Sulfapyridine, suppressing the transformation of lymphocytes and neoplasm of T-killer cells, has an antimicrobial effect against streptococci, diplococci, Escherichia coli, gonococci.
Mesalazine has a significant anti-inflammatory effect in the treatment of the large intestine. The mechanism of action of 5-aminosalicylic acid is the binding of free oxygen radicals, local inhibition of lipoxygenase and cyclooxygenase in the intestinal wall, which prevents the formation of leukotrienes, prostaglandins and other inflammatory mediators.
Pharmacokinetics
- absorption: about 30% of the taken dose of sulfasalazine is absorbed in the wall of the small intestine, the remaining 70% in the large intestine under the influence of intestinal microflora decompose to form 60-75% sulfapyridine and 25% - mesalazine. The maximum concentration of the active substance in the blood plasma is reached 3–12 hours after taking the drug;
- distribution: binding of sulfasalazine to blood plasma proteins is 99%, sulfapyridine - 50%, mesalazine - 43%;
- metabolism: sulfapyridine in the liver is metabolized by hydroxylation to form inactive metabolites, mesalazine - by acetylation;
- elimination: the half-life (T 1/2) of sulfasalazine - from 5 to 10 hours, sulfapyridine - from 6 to 14 hours, mesalazine - from 0.6 to 1.4 hours. Through the intestine, 5% of sulfapyridine and 67% of mesalazine are excreted. Through the kidneys, 75–91% of sulfasalazine is excreted within three days.
Indications for use
- Crohn's disease (moderate and mild in the acute phase);
- ulcerative colitis (treatment in the acute phase and supportive therapy in remission);
- rheumatoid arthritis, including juvenile.
Contraindications
Absolute:
- aplastic anemia, granulocytopenia;
- porphyrin disease;
- severe renal failure;
- severe liver dysfunction;
- congenital deficiency of the enzyme glucose-6-phosphate dehydrogenase;
- lactation period;
- children under 5 years old; in the treatment of juvenile rheumatoid arthritis - up to 6 years;
- increased individual sensitivity to sulfasalazine or any auxiliary component of the drug, as well as to sulfonamides and salicylic acid derivatives.
Relative (diseases / conditions, the presence of which requires caution when prescribing Sulfasalazine-EH):
- a history of allergic reactions (possible cross-allergic reactions to furosemide, sulfonylurea derivatives, thiazide diuretics, carbonic anhydrase inhibitors);
- impaired renal and / or liver function;
- bronchial asthma;
- systemic forms of juvenile rheumatoid arthritis (the likelihood of developing serum sickness);
- pregnancy.
Instructions for use of Sulfasalazine-EN: method and dosage
Sulfasalazine-EH tablets 500 mg are taken orally, after meals.
Crohn's disease and ulcerative colitis
Recommended dosage regimen:
- adults and children over 16 years old: the first day - 1 tablet (500 mg) 4 times a day; the second day - 2 tablets (1000 mg) 4 times a day; the third and subsequent days - 3-4 tablets (1500-2000 mg) 4 times a day. After the acute clinical manifestations of ulcerative colitis have subsided, a maintenance dose is recommended - 1 tablet (500 mg) 3-4 times a day for several months;
- children from 10 to 16 years old and / or weighing from 35 to 50 kg: 1 tablet (500 mg) 4 times a day;
- children from 7 to 10 years old: 1 tablet (500 mg) 3-4 times a day;
- children from 5 to 7 years: ½ – 1 tablet (250–500 mg) 3-4 times a day.
Supportive therapy is not recommended for children and adolescents under 16 years of age and / or weighing up to 65 kg.
The maximum daily dose of Sulfasalazine-EH is: for adults - 8000 mg (16 tablets), for children under 16 years old - 2000 mg (4 tablets).
Rheumatoid arthritis and juvenile rheumatoid arthritis
Recommended dosage regimen:
- adults: the first week - 1 tablet (500 mg) once a day, the second week - 1 tablet (500 mg) 2 times a day, the third week - 1 tablet (500 mg) 3 times a day, and so on. Possible therapeutic dose is from 1500 mg (3 tablets) to 3000 mg (6 tablets) per day. The course of therapy is six or more months. The clinical effect appears after 6-10 weeks from the start of treatment;
- children over 16 years old and / or weighing more than 50 kg: 2 tablets (1000 mg) 2 times a day;
- children from 12 to 16 years old and / or weighing from 40 to 50 kg: 1 tablet (500 mg) 3 times a day or 2 tablets (1000 mg) 2 times a day;
- children from 8 to 12 years old and / or weighing from 30 to 39 kg: 1 tablet (500 mg) 2-3 times a day;
- children from 6 to 8 years old and / or weighing from 20 to 29 kg: 1 tablet (500 mg) 2 times a day.
For children, the maximum daily dose is 2000 mg (4 tablets of Sulfasalazine-EH 500 mg) or 40-50 mg / kg of body weight.
Side effects
The development of adverse reactions depends on the level of concentration of sulfapyridine in the blood plasma, especially in patients with slow acetylation. More often, undesirable effects are observed in patients with rheumatoid arthritis.
Possible side reactions when using Sulfasalazine-EH from systems and organs:
- central and peripheral nervous system: dizziness, headache, convulsions, vertigo, hallucinations, tinnitus, sleep disturbances, peripheral neuropathy, depression, aseptic meningitis, ataxia;
- digestive system: diarrhea, nausea, decreased appetite, vomiting, abdominal pain, pancreatitis, drug hepatitis, anorexia;
- urinary system: hematuria, proteinuria, crystalluria, interstitial nephritis, renal dysfunction;
- hematopoietic system: neutropenia, leukopenia, macrocytosis, hemolytic anemia, megaloblastic anemia caused by the carriage of unstable hemoglobins (due to the presence of Heinz-Ehrlich bodies) hemolytic anemia, agranulocytosis, methemoglobinemia, thrombocytopenia, hypoplasmic anemia, aplastothrombinemia;
- respiratory system: cough, shortness of breath, interstitial pneumonitis, infiltrates in the lung tissue, fibrosing alveolitis;
- reproductive system: transient oligospermia, infertility;
- allergic reactions: pruritus, erythema, urticaria, generalized skin rash, Lyell's syndrome (toxic epidermal necrolysis), Stevens-Johnson syndrome (malignant exudative erythema), exfoliative dermatitis, fever, serum sickness, photosensitization, lymphadenteritis, erythematosus nodosum swelling, anaphylactic shock;
- laboratory tests: increased activity of alkaline phosphatase, hyperbilirubinemia, increased levels of hepatic transaminases;
- others: mumps, hyperthermia, possible yellow staining of the skin, urine or soft contact lenses.
Overdose
In case of an overdose of Sulfasalazine-EH, the following symptoms may appear: dizziness, abdominal pain, nausea, vomiting. In case of taking very high doses of the drug, symptoms of nervous system intoxication (convulsions), hematuria, anuria, crystalluria may occur.
The recommended overdose treatment is symptomatic. Induce vomiting, flush the stomach and intestines, alkalinize urine, forced diuresis. In patients with anuria and / or renal insufficiency, fluid and electrolyte intake should be limited.
special instructions
During therapy with Sulfasalazine-EH, it is recommended to periodically monitor the level of liver enzymes in the blood plasma. It is also necessary to do a general blood test (at the initial stage of treatment - 1-2 times a month, then every 3-6 months) and urinalysis (in case of impaired renal function).
During the period of taking the drug, it is recommended to consume an increased amount of liquid.
Application during pregnancy and lactation
According to the instructions, Sulfasalazine-EH can be prescribed to pregnant women only according to the strict indications of the attending physician and in the minimum effective dose. In the third trimester of pregnancy, if the course of the disease allows, the drug must be canceled.
During lactation, if it is necessary to use Sulfasalazine-EH, breastfeeding should be discontinued.
Pediatric use
The use of Sulfasalazine-EH in children under 5 years of age is prohibited.
With impaired renal function
Patients with renal insufficiency should be prescribed Sulfasalazine-EH with caution.
The use of the drug for severe renal dysfunction is contraindicated.
For violations of liver function
With caution, it is necessary to prescribe Sulfasalazine-EH in liver failure.
In patients with severely impaired liver function, the use of the drug is prohibited.
Drug interactions
- folic acid, digoxin: decrease in their absorption;
- anticoagulants, antiepileptic and oral hypoglycemic agents: enhancing their action;
- cytostatics, immunosuppressants, hepato- and nephrotoxic agents: increasing their side effects;
- drugs that have a depressing effect on bone marrow hematopoiesis: increased risk of myelosuppression;
- antibiotics: a decrease in the effectiveness of sulfasalazine in ulcerative colitis (due to the inhibitory effect of antibiotics on the intestinal microflora).
Analogs
Sulfasalazine-EH analogs are Sulfasalazine and Sulfasalazine-native.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C, out of the reach of children.
Shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Sulfasalazine-EN
There are few reviews about Sulfasalazine-EN, and they are quite contradictory. For some patients, the drug helps with arthritis, while not causing undesirable effects, while others, after a fairly long intake, do not feel significant improvements. Of the side reactions, insomnia, bitterness in the mouth, nausea, lack of appetite, and sometimes nervous irritability are noted.
Price for Sulfasalazine-EN in pharmacies
The price for Sulfasalazine-EN 500 mg (50 tablets per pack) is approximately 330–455 rubles.
Sulfasalazine-EN: prices in online pharmacies
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Drug name Price Pharmacy |
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Sulfasalazine-EH tablets p.o. intestinal. 500mg 50 pcs. 309 RUB Buy |
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Sulfasalazine-EH 500 mg enteric-coated tablets 50 pcs. 309 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
