Sulfadimethoxine

General characteristics. Structure:

Active ingredient: 500 mg of sulfadimethoxine in 1 tablet.

Excipients: potato starch, silicon dioxide colloid, calcium stearate, gelatin medical.

Antimicrobic bacteriostatic means, streptocide of long action.

Pharmacological properties:

Pharmacodynamics. The mechanism of action is caused by competitive antagonism with paraaminobenzoic acid, oppression of a digidropteroatsintetaza, disturbance of synthesis of the tetrahydrofolic acid necessary for synthesis of purines and pyrimidines.

It is active concerning gram-positive and gram-negative microorganisms: Staphylococcus spp., Streptococcus spp., including Streptococcus pneumoniae, Friedlander's, Escherichia coli, Shigella spp sticks., Chlamydia trachomatis. Sulfadimethoxine does not affect strains of the bacteria steady against streptocides

Pharmacokinetics. After intake in 30 min. it is found in blood, time of achievement of the maximum concentration in blood (TCmax) - 8-12 h Badly get through a blood-brain barrier (GEB). Therapeutic concentration at adults is noted at reception 1 - 2 g in first of all at the expense of high extent of linkng with blood proteins (90-99%).

It is well distributed on bodies and systems. Unlike other representatives of streptocides of long action through GEB also its concentration in liquor low badly gets. However at an inflammation of meningeal covers permeability of GEB sharply increases. Well gets into pleural liquid (60-90% of concentration in blood), in biliary system where its concentration are 1,5-4 times higher, than in blood.

Unlike other streptocides, metabolism is preferential carried out on the way of a microsomal glyukuronirovaniye, NADFN-zavisimogo and connected with P450 cytochrome. It is removed slowly, first of all, due to keeping in blood by proteins of plasma and at the expense of high degree of a reabsorption in tubules of kidneys (93-97,5%). Blood contains 5-15% of acetylized metabolites, in urine - 10-25% of acetyl derivatives and 75-90% - a sulfadimethoxine glucuronide; we will well dissolve the last and does not provoke development of a crystalluria.

Acetyl derivative does not reabsorbirutsya and is completely removed by kidneys. In 24 h 20-44% of the accepted dose, in 48 h - to 56%, in 96 h - to 83,3% are removed

Indications to use:

The infectious and inflammatory diseases caused by sensitive microorganisms: tonsillitis, bronchitis, pneumonia, antritis, otitis, dysentery, inflammatory diseases of bilious and urinary tract, ugly face, wound fever, trachoma.

Route of administration and doses:

Inside, 1 time a day, in the first day - 1-2 g, then - on 0.5-1 g/days. At severe forms apply in a combination with drugs of group of penicillin, erythromycin, etc.

For children over 12 years the initial and supporting doses are equal 1 g and 0,5 g. After normalization of body temperature in maintenance doses apply 2-3 more days.

Contraindications:

Hypersensitivity, oppression of a marrowy hemopoiesis, renal/liver failure, chronic heart failure, inborn deficit glyukozo-6-fosfatdegidrogenazy, porphyria, azotemia, pregnancy, the lactation period, children's age up to 3 months.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. In the place, unavailable to children. Period of validity of 5 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 500 mg. On 10 tablets in a blister strip packaging. 200 planimetric packagings with the equal number of application instructions in a box from a cardboard (for hospitals).