Tsilaspen consists of two components: imipenem, the representative of the class of beta-lactam antibiotics – carbapenems; cilastatin primobolan depot – specific inhibitor of renal dehydropeptidase, significantly increases the concentration of unchanged imipenem in the blood. Tsilastin has its own antibacterial activity, does not inhibit the beta-lactamase bacteria.
Imipenem is a highly effective inhibitor of bacterial cell wall synthesis and is bactericidal against a wide spectrum of pathogenic gram-positive and gram-negative microorganisms, both aerobic and anaerobic.
The stability of imipenem to cleavage by bacterial beta lactamases, including produced by Gram-positive and Gram-negative and penicillinase cephalosporinase ensures its effectiveness.
it is active against Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus faecalis and Bacteroides fragilis. Resistant to bacterial destruction of beta-lactamase, which makes it effective against many microorganisms, such as Pseudomonas aeruginosa, Serratia spp. and Enterobacter spp, which are resistant to most of the beta-lactam antibiotics..
Antibacterial spectrum includes primobolan depot virtually all clinically important pathogens.
Imipenem has a bactericidal effect in vivo primobolan depot on the following microorganisms: Gram-positive aerobes: Enterococcus faecalis, Staphylococcus aureus, including penitsillinazoprodutsiruyuschie strains, Staphylococcus epidermidis, including penitsillinazoprodutsiruyuschie strains, Streptococcus agalactiae (Streptococcus spp group in.), Streptococcus pneumoniae, Streptococcus pyogenes . Gram-negative aerobes: Acinetobacter spp, Citrobacter spp, Enterobacter spp, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp…. , Morganella morganii, Proteus vulgaris, Providencia rettgeri, Pseudomonas aeruginosa, Serratia spp, including S. marcescens.. Gram-positive anaerobes: Bifidobacterium spp, Clostridium spp, Eubacterium spp, Peptococcus spp, Peptostreptococcus spp, Propionibacterium spp……
Gram negative anaerobes : .. Bacteroides spp, including B. fragilis, Fusobacterium spp Imipenem has a bactericidal effect in vitro on the following microorganisms: Gram-positive aerobes: Bacillus spp, Listeria monocytogenes, Nocardia spp, “Staphylococcus saprophyticus, Streptococcus spp… . Groups C, G and viridans Gram-negative aerobes: the Aeromonas hydrophila, of Alcaligenes spp, Capnocytophaga spp, of Haemophilus ducreyi, of Neisseria gonorrhoeae, including strains penitsillinazoprodutsiruyuschie, Pasteurella spp .., Providencia stuartii. ..Gram-negative anaerobes: Prevotella bivia, Prevotella disiens, Prevotella melaninogenica ., Veillonella spp Unaffected: .. Enterococcus faecium, methicillin-resistant spp Staphylococcus, Xanthomonas maltophilia, Pseudomonas cepacia in vitro acts synergistically with aminoglycosides against some strains of Pseudomonas aeruginosa.
Imipenem quickly and well distributed in most tissues and body fluids. The highest concentrations are achieved in pleural fluid, peritoneal, and interstitial fluids and the reproductive organs (testes, prostate gland, vagina, uterus, ovaries). At low concentrations found in the cerebrospinal fluid. The volume of distribution in adults – 0.23-0.31 L / kg in children 2-12 years of age – 0.7 l / kg in the newborn – 0.4-0.5l / kg. Blocking kanaptsevoy imipenem cilastatin secretion leads to inhibition of its renal metabolism and accumulation in the urine in unchanged form. Cilastatin is metabolized to N-acetyl compounds. The on / in the introduction of the primobolan depot of imipenem and cilastatin in adults – 1 hour, children 2-12 years – 1-1.2 hours, in newborns the T ½ imipenem – 1.7-2.4 hours, cilastatin – 3.8-8.4 hours; with impaired renal function the T ½ . imipenem – 2.9-4 hours, cilastatin – 13.3-17.1 hours Report mostly kidneys (70-76% within 10 hours) through glomerular filtration rate (⅔) and active tubular secretion (⅓); 1-2% is excreted in the intestine and 20-25% – by extrarenal (mechanism unknown). Quickly and efficiently (73-90%) is derived by hemodialysis (as a result of a 3-hour session intermittent hemofiltration removes 75% of the administered dose).