Sulfadimethoxin, tablets 500 mg, 10 pcs.

Pharmacotherapeutic group: Antimicrobial agent, sulfonamide

ATX code: J01ED01

Pharmacological properties

.Pharmacodynamics

An antimicrobial bacteriostatic agent. Mechanism of action is due to competitive antagonism with para-aminobenzoic acid, inhibition of dihydropteroate synthetase, disruption of tetrahydrofolic acid synthesis, required for purine and pyrimidine synthesis. Active against Gram-positive and Gram-negative microorganisms: Staphylococcus spp., Streptococcus spp. including Streptococcus pneumoniae, Friedlander’s bacillus, Escherichia coli, Shigella spp, Chlamydia trachomatis.

Pharmacokinetics

In oral administration it is absorbed relatively slowly, detected in blood after 30 minutes. When single administration (in a dose of 1 – 2 g), time to reach maximum concentration in blood (T_Cmax) – 8 – 12 h.

Therapeutic concentration in adults is noted when taking 1-2 g on the first day and 0.5-1 g on the following days. Blood protein binding is 90-99%.

The drug is accumulated in blood, primarily due to a high degree of binding to blood proteins (90-99%). It is well distributed through the organs and systems. But unlike other representatives of long-acting sulfonamides, it poorly penetrates through the blood-brain barrier (BBB) and its concentration in the cerebrospinal fluid is low. However, in inflammation of meningeal membranes the permeability of the GEB increases sharply.

It penetrates well into the pleural fluid (60-90% of its concentration in blood), in the biliary system, where its concentrations are 1.5-4 times higher than in blood. Primarily metabolism is realized by microsomal glucuronidation pathway, which is connected with cytochrome P450 and NADPH-dependent.

The strong connection with blood plasma proteins and high reabsorption in renal tubules (93-97,5%) promotes slow excretion of preparation from the body.

The blood contains 5-15% of acetylated metabolites, the urine contains 10-25% of acetyl derivatives and 75-90% of sulfadimethoxin glucuronide; the latter is well soluble and does not provoke crystalluria. The acetyl derivative is not reabsorbed and is completely excreted by the kidneys. After 24 hours 20-44% of the taken dose is excreted, after 48 hours – up to 56%, after 96 hours – up to 83.3%.

Indications

Diseases caused by sensitive microflora: tonsillitis, otitis, sinusitis, bronchitis, pneumonia, dysentery, pyoderma, erysipelas, trachoma; wound infections; gonorrhea; diseases of the urinary and biliary tract; malaria (as part of complex therapy).

Pharmacological effect

Pharmacotherapeutic group: antimicrobial agent, sulfonamide

ATC code: J01ED01

Pharmacological properties

Pharmacodynamics

Antimicrobial bacteriostatic agent. The mechanism of action is due to competitive antagonism with para-aminobenzoic acid, inhibition of dihydropteroate synthetase, disruption of the synthesis of tetrahydrofolic 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’s bacilli, Escherichia coli, Shigella spp., Chlamydia trachomatis.

Pharmacokinetics

When taken orally, it is absorbed relatively slowly and is detected in the blood after 30 minutes. With a single dose (at a dose of 1 – 2 g), the time to reach maximum concentration in the blood (TCmax) is 8 – 12 hours.

Therapeutic concentration in adults is observed when taking 1-2 g on 1 day and 0.5-1 g on subsequent days. Communication with blood proteins – 90-99%.

The drug accumulates in the blood, primarily due to a high degree of binding to blood proteins (90-99%). Well distributed throughout organs and systems. But unlike other representatives of long-acting sulfonamides, it poorly penetrates 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.

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 occurs via the microsomal glucuronidation pathway associated with cytochrome P450 and NADPH-dependent.

Strong binding with blood plasma proteins and high reabsorption in the kidney tubules (93-97.5%) contribute to the slow elimination of the drug from the body.

The blood contains 5-15% acetylated metabolites, the urine contains 10-25% acetyl derivatives and 75-90% sulfadimethoxine 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, 20-44% of the dose taken is excreted, after 48 hours – up to 56%, after 96 hours – up to 83.3%.

Special instructions

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

It is used externally as part of combination preparations.

Active ingredient

Sulfadimethoxine

Composition

Active ingredient: sulfadimethoxine – 500.0 mg.

Excipients: microcrystalline cellulose – 42.0 mg, crospovidone (type B) – 26.5 mg, povidone K 25 (medium molecular weight polyvinylpyrrolidone K 25) – 25.5 mg, calcium stearate – 6.0 mg.

Contraindications

Hypersensitivity to sulfadimethoxine 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 breastfeeding, children under 12 years of age (for this dosage form and dosage).

Side Effects

From the side of the central nervous system: possible headache.

From the digestive system: dyspeptic symptoms, nausea, vomiting, cholestatic hepatitis.

Allergic reactions: skin rashes, drug fever.

From the hematopoietic system: rarely – leukopenia, agranulocytosis.

Interaction

Sulfadimethoxine reduces the effectiveness of bactericidal antibiotics that act only on dividing microorganisms (including penicillins, cephalosporins).

Storage conditions

Store at a temperature not exceeding 25 °C.
Keep out of the reach of children.

Shelf life

5 years

Manufacturer

Pharmstandard-Leksredstva, Russia