It is bactericidal antimicrobial broad-spectrum, both in terms of gram-positive and gram-negative flora. The advantage of the preparation is most active against anaerobic gram-positive cocci and fluoroquinolones compared with previous generations. With respect to deca durabolin flora is active, close to aminoglycosides.
Microorganisms bactericidal effect only during division and in the rest period, since not only affects gyrase, but also causes lysis of the cell wall.
It prevents transcription of the genetic material of bacteria required for normal metabolism, which leads to a rapid decrease in the ability of bacteria to divide. As a result of its action does not occur parallel generating resistance to other antibiotics, not belonging to the group of gyrase inhibitors, which makes it highly effective against bacteria but which are resistant to aminoglycosides e.g., penicillins, cephalosporins, tetracyclines, and many other antibiotics.
Sparfloxacin characterized by high activity against Mycobacterium tuberculosis, including strains mnozhestvennorezistentnye.
Enterococcus faecium, Ureaplasma urealyticum, Xocardia asteroides, usually sensitive to sparfloxacin.
The following microorganisms have moderate sensitivity: Gardnerella spp, Flavobacterium spp, Alcaligenes spp, deca durabolins agalactiae, Enterococcus faecalis, Streptococcus pyogenes, Streptococcus viridans, Mycoplasma hominis, Mycobacterium fortuitum….
With a few exceptions, anaerobes are moderately sensitive (Peplococcus spp., Peptostreptococcus spp.) Or resistant (Bacteroides spp.). Sparfloxacin are not effective against Treponema pallidum.
Sparfloxacin resistance develops very slowly, because, on the one hand, after its validity remains virtually persistent microorganisms, and on the other hand, in the bacterial cells have enzyme inactivating it.
There was no cross-resistance to other antimicrobial agents.
With respect to Paeruginosa and bacilli ciprofloxacin inferior in activity.
It has postantibioticski effect: microorganisms do not grow for 0.5 – 4 hours after the disappearance of plasma drug.
The absorption after ingestion – about 90%. The extent of absorption is not changed by taking the drug with food or milk. Food intake slows but does not alter the extent of absorption, so that the maximum observed concentration of sparfloxacin approximately 30 minutes later than in deca durabolin the fasting state.
It is well distributed in the body tissues (tissue excluding rich fats, including neural tissue) concentration in the tissues and fluids of the lower respiratory tract than the concentration in plasma. It is found in high concentrations in the alveolar macrophages. Therapeutic concentrations achieved in saliva, bile, intestine, the abdomen and pelvic organs, kidneys and urinary organs, lung tissues, bronchial secretions, bone, muscle, synovial fluid and articular cartilage, peritoneal fluid, skin. The cerebrospinal and intraocular fluid is detected in 10% of the drug concentration in plasma.
The drug has a large volume of distribution – 3,9 ± 0,8 l / kg, exceeding the figure for other fluoroquinolones. Communication with the plasma proteins (mainly albumin) is about 45%.
The time to reach maximum concentration after oral administration of 400 mg – 3.6 hours, concentration in tissue of 2-12 times higher than in plasma. The concentration of drug in the blood serum has a linear dependence on the value received to the square.
Activity decreases slightly at acidic pH.
Metzboliziruetsya in the liver, is excreted in the feces (30-50%) and urine (tubular filtration and tubular secretion) – of them, in an unmodified form, about 10% of the orally adopted vines. The half – 16-30 hours, in patients with renal insufficiency, the deca durabolin is prolonged.
In chronic renal failure percentage of the drug that is output from the kidneys. reduced but creatinine clearance greater than 20 mL / min cumulation it occurs in the body, as it happens in parallel increase in metabolism and excretion in the feces.
The infectious-inflammatory diseases caused by sensitive microflora: