Sulfadimethoxin, tablets 200 mg, 10 pcs.

Antimicrobial bacteriostatic agent, long-acting sulfonamide. The mechanism of action is associated with competitive antagonism with PABA, inhibition of dihydropteroat synthetase, disruption of synthesis of tetrahydrofolic acid required for synthesis of purines and pyrimidines.

Active against Gram-positive and Gram-negative microorganisms: Staphylococcus spp, Streptococcus spp. including Streptococcus pneumoniae, Friedlander’s bacillus, Escherichia coli, Shigella dysenteria spp, Shigella flexneri spp, Shigella boydii spp, Shigella sonnei spp, Chlamydia trachomatis.
Pharmacokinetics After oral administration it is detected in blood in 30 minutes, period of maximum concentration – 8 – 12 hours. Unlike other long-acting sulfonamides, it poorly penetrates through the blood-brain barrier and its concentration in the cerebrospinal fluid is low. However in case of meningeal membranes inflammation its blood-brain barrier permeability increases dramatically.

Therapeutic concentration in adults is observed when taking 1 – 2 g during the 1st day and 0.5 – 1 g during the next days. It is well distributed in organs and systems. It penetrates well into pleural fluid (60 – 90% of blood concentration) and biliary system, where its concentrations are 1.5 – 4 times higher than in blood. Unlike other sulphonamides predominant metabolism is conducted via microsomal glucuronidation, – NADPH-dependent and associated with cytochrome P450.

It is eliminated slowly, primarily due to retention in blood by plasma proteins and due to high degree of reabsorption in renal tubules (93 – 97.5 %). Blood contains 5 – 15% of acetylated metabolites, urine contains 10 – 25% of acetyl derivatives and 75 – 90% of sulfadimethoxin glucuronide; the latter is well soluble and does not provoke the development of crystalluria. The acetyl derivative is not reabsorbed and is completely excreted by the kidneys. In 24 hours 20 – 44 % of the taken dose is excreted, in 48 hours – up to 56 %, in 96 hours – up to 83.3 %.

Indications

Active ingredient

Composition

How to take, the dosage

Sulfadimethoxin is taken orally. It is taken every 24 hours: 1-2 g on day 1, 0.5-1 g/day on subsequent days; in children 25 mg/kg/day on the first day and 12.5 mg/kg/day on subsequent days.

Interaction

Sulfadimethoxin reduces the effectiveness of bactericidal antibiotics acting only on fissile microorganisms (including penicillins, cephalosporins).

Special Instructions

During treatment it is recommended to drink plenty of alkaline fluids, monitor blood and urine parameters.

It is used externally as part of the combination therapy.

Contraindications

Side effects

CNS disorders: headache possible.

Digestive system disorders: dyspeptic symptoms, nausea, vomiting, cholestatic hepatitis.

Allergic reactions: skin rashes, drug fever.

Hematopoietic system: rarely – leukopenia, agranulocytosis.