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|Azulfidine 500 mg|
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Pharmacological action of Azulfidine
A drug for the treatment of NUC 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 gonorrhoe coli, Escherichia.
Sulfasalazine is poorly absorbed in the intestine (no more than 10%). Undergoes splitting by the 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% sulfapyridine and 67% 5-ASA are excreted with feces; 75-91% of the absorbed sulfasalazine is excreted by the kidneys within 3 days.
Indications for the active substances of the drug Sulfasalazine
Ulcerative colitis (treatment of exacerbations and maintenance therapy in the remission phase); Crohn's disease (mild and moderate forms in the acute phase); rheumatoid arthritis; juvenile rheumatoid arthritis.
Dosing regimen of Azulfidine
Ulcerative colitis and Crohn's disease: when taken orally in adults, it is used after meals: on the 1st day, 500 mg 4 times / day; on the 2nd day, 1 g 4 times / day; on the 3rd and subsequent days, 1.5-2 g 4 times / day. After the acute clinical symptoms subside, a maintenance dose of 500 mg is used 3-4 times / day for several months. Children aged 5-7 years - 250-500 mg 3-6 times / day, over 7 years old - 500 mg 3-6 times / day.
Rheumatoid arthritis: adults during the first week - 500 mg 1 time / day; within 2 weeks - 500 mg 2 times / day; within 3 weeks - 500 mg 3 times / day. The therapeutic dose is 1.5-3 g / day. The course of treatment is 6 months or more. Children over the age of 6 years - 30-50 mg / kg / day in 2-4 doses; for children over 16 years of age, the maximum daily dose is 2 g.
Contraindications to the use of
Porphyria, anemia, severe liver dysfunction, severe renal dysfunction, deficiency of the enzyme glucose-6-phosphate dehydrogenase, children under 5 years of age, lactation period; hypersensitivity to sulfonamides and salicylic acid derivatives.
Application during pregnancy and lactation
The use of sulfasalazine during pregnancy is possible only under strict indications in the minimum effective dose. If the course of the disease allows, it is recommended to cancel sulfasalazine in the third trimester of pregnancy.
If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be resolved.
Application for violations of liver function
Use with caution in patients with impaired liver function.
Application for impaired renal function
Use with caution in patients with impaired renal function.
Use in children
Contraindicated in children under 5 years of age.
Use with caution in patients with impaired liver and / or kidney function, patients with bronchial asthma, allergic reactions.
During the period of treatment, it is recommended to consume an increased amount of liquid.
During the period of treatment, the level of liver enzymes, a complete blood count and urine test should be monitored.
Enhances the effect of anticoagulants, antiepileptic and oral hypoglycemic drugs, as well as the side effects of cytostatics, immunosuppressants, hepato- and nephrotoxic drugs.
With simultaneous use with sulfasalazine, the toxicity of azathioprine and mercaptopurine increases.
With simultaneous use with ampicillin or rifampicin, the release of 5-aminosalicylic acid from the sulfasalazine molecule in the colon decreases (due to the suppression of the activity of anaerobic bacteria under the influence of ampicillin and rifampicin, with the participation of which this process occurs). In this regard, a decrease in the effectiveness of sulfasalazine is possible. It is believed that the interaction of sulfasalazine with neomycin is manifested in the same way.
With simultaneous use with digoxin, it is possible to reduce its absorption; with talinolol - the absorption of talinolol decreases; with folic acid - a decrease in the absorption of folic acid is possible.
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 the lung tissue.
From the hematopoietic system: anemia, leukopenia, thrombocytopenia, agranulocytosis.
On the part of the reproductive system: transient oligospermia, infertility.
Allergic reactions: skin rash, toxic epidermal necrolysis, malignant exudative erythema, fever, anaphylactic shock.
Others: it is possible to stain the skin, urine, soft contact lenses yellow.