Composition:
Composition per tablet. Active ingredient: sulfadimethoxine - 500.0 mg. Excipients: microcrystalline cellulose - 42.0 mg, crospovidone (type B) - 26.5 mg, povidone K 25 (polyvinylpyrrolidone medium molecular weight K 25) - 25.5 mg, calcium stearate-6.0 mg.
Pharmacodynamics:
Antimicrobial bacteriostatic agent. The mechanism of action is due to competitive antagonism with para-aminobenzoic acid, inhibition of dihydropteroate synthetase, impaired synthesis of tetrahydrofolate acid, necessary for the synthesis of purines and pyrimidines. Active against gram-positive and gram-negative microorganisms: Staphylococcus spp., Streptococcus spp., Including Streptococcus pneumoniae, Friedlander rods, Escherichia coli, Shigella spp., Chlamydia trachomatis. Sulfadimethoxin does not act on strains of bacteria resistant to sulfonamides.
Pharmacokinetics:
When taken orally, it is absorbed relatively slowly, found in the blood after 30 minutes. With a single dose (at a dose of 1-2 g), the time to reach the maximum concentration in the blood (Tmax) is 8-12 hours. Therapeutic concentration in adults is achieved when taking 1-2 g on 1 day and 0.5-1 g on the following days . Communication with blood proteins - 90-99%. The drug accumulates in the blood, primarily due to the high degree of binding to blood proteins (90-99%). It is well distributed among organs and systems.
But unlike other representatives of long-acting sulfonamides, it penetrates poorly through the blood-brain barrier (BBB) and its concentration in the cerebrospinal fluid is low. However, with inflammation of the meningeal membranes, the permeability of the BBB increases sharply. It penetrates well into the pleural fluid (60-90% of the concentration in the blood), into the biliary system, where its concentration is 1.5-4 times higher than in the blood. Preferential metabolism is carried out along the path of microsomal glucuronidation associated with cytochrome P450 and NADPH-dependent.
A strong connection with plasma proteins and high reabsorption in the tubules of the kidneys (93-97.5%), contributes to the slow removal of the drug from the body. 5-15% of acetylated metabolites are contained in blood, 10-25% of acetyl derivatives in urine and 75-90% of sulfadimethoxin glucuronide; the latter is highly soluble and does not provoke the development of crystalluria. The acetyl derivative is not reabsorbed and is completely excreted by the kidneys. After 24 hours, 20-40% of the dose taken is excreted, after 48 hours - up to 56%, after 96 hours - up to 83.3%.
Side effects:
Allergic reactions; headache, dyspepsia, leukopenia, agranulocytosis, cholestatic hepatitis. Features of the sale of prescription Special conditions During therapy, heavy drinking is recommended, regular monitoring of blood and urine. Impact on the ability to drive vehicles and other mechanisms: During treatment, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Indications:
Diseases caused by sensitive microflora: tonsillitis, otitis media, sinusitis; bronchitis, pneumonia; dysentery; pyoderma; erysipelas; trachoma; wound infections; gonorrhea; diseases of the urinary and biliary tract; malaria (as part of complex therapy).
Contraindications:
Hypersensitivity to sulfadimethoxin or other components of the drug; inhibition of bone marrow hematopoiesis; renal / liver failure, chronic heart failure, congenital deficiency of glucose-6-phosphate dehydrogenase; porphyria; azotemia; pregnancy and the period of breastfeeding, children under 12 years of age (for this dosage form and dosage). Pregnancy and lactation: The use of the drug during pregnancy and during breastfeeding is contraindicated. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding
Drug Interactions:
The effect of sulfadimethoxin is enhanced by combined use with diaminopyrimidine derivatives (trimethoprim, tetroxoprim, pyrimethamine). Reduces the effectiveness of bactericidal antibiotics that act only on fissile microorganisms (including penicillins, cephalosporins). Phenytoin increases the risk of toxic reactions. Methotrexate and other folic acid antagonists increase the risk of folic acid deficiency. Procaine, benzocaine and tetracaine reduce antibacterial activity. PASK and barbiturates enhance the antimicrobial effect. Salicylates increase the activity and toxicity of sulfadimethoxin. Methoxalen promotes the development of photosensitivity. Non-hormonal anti-inflammatory drugs, thioacetazone, chloramphenicol enhance the toxic effect on the blood (leukopenia, agranulocytosis). Enhances the effect of indirect anticoagulants, phenytoin, sulfonamides with hypoglycemic effect; Derivatives of pyrazolone, indomethacin and salicylates increase the free fraction of the drug in the blood. Reduces the effectiveness of oral contraceptives. Enhances the metabolism of cyclosporine.
Dosage:
Inside, once a day. Adults, on the 1st day - 1-2 g, then - 0.5-1 g / day. For children from 12 to 18 years of age: the initial and maintenance doses are 1 g and 0.5 g, respectively.
After normalizing the temperature, the drug is used in maintenance doses for another 2-3 days. The course of treatment, depending on the severity of the disease, is 7-14 days.
