Cefotaxime sodium 0.5 and 1.0 g
Cefotaxim-natrium 0.5 et 1.0
International nonproprietary name
1 vial containû 500 or 1000 mg of Cefotaximesodium.
Pharmacological action -antimicrobial, bactericidal.
Cefotaxime possesses high binding ability to penicillin-binding proteins of microorganisms’ membranes, inhibits peptidoglycan polymerase, breaks a biosynthesis of mucopeptide of microbe cell wall.
Cefotaxime is characterized by a wide spectrum of antimicrobial action. It is resistant to four of five beta-lactamases of gram-negative bacteria and to penicillinase of staphilococcuses. It is active in relation to Staphylococcus aureus, including penicillinase-producing, some strains of Enterococcus spp., Streptococcus pneumoniae (especially Diplococcus pneumoniae), Streptococcus pyogenes (beta-hemolytic streptococcuses of A group), Streptococcus agalactiae (streptococcuses of B group), Bacillus subtilis, Bacillus mycoides, Corynebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium, Enterobacter aerogenes, Enterobacter cloacaàå, Escherichia coli, Acinetobacter spp., Haemophilus influenzae, including ampicillin-resistant strains, Haemophilus parainfluenzae, Klebsiella oxótoca, Klebsiella pneumonia, Morganella morganii, Neisseria meningitidis, Neisseria gonorrhoeae, including the penicillinase-producing strains, Propionibacterium, Proteus mirabilis, Proteus vulgaris, Proteus inconstans, Serratia marcescens, many strains of Ðseudomonas aeruginosa, Citrobacter spp., Salmonella spp., Providencia rettgeri, Shigella spp., Serratia spp., Veillonella, Yersinia spp., Bordetella pertussis, Moraxella (Branhamella) catarrhalis, Aeromonas hydrophilia, Fusobacterium, Bacteroides spp., Clostridium spp., Peptostreptococcus spp., Peptococcus spp. Changeably influences some strains Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, Bacteroides fragilis, Clostridium difficile. It can affect multiresistant strains, resistant to penicillins, cephalosporins of the first generations and aminoglycosides. In relation to gram-positive coccuses is less active than cephalosporins of the first and the second generations.
After single intramuscular introduction of 0,5 or 1,0 g of Cefotaximethe maximal concentration in blood is reached in 30 min and is 12 and 20 mkg/ml. In 5 mines after intravenous introduction of 0,5, 1,0 and 2,0 g of Cefotaxime theconcentration in blood plasma is 38, 102 and 215 mcg/ml.
Cefotaxime binds with proteins in blood in 25-40 %. It reaches therapeutic concentration in the majority of tissues (myocardium, bones, gallbladder, skin, soft tissues) and fluids (sinovial, pericardiac, peritoneal, cerebrospinal, pleural effusion, sputum, bile, urine).
Cefotaxime passes through placenta, gets into breast milk.
Time of half-elimination (Ò1/2) at intravenous introduction is 1 hour, at intramuscular introduction - 1-1,5 hours.
It is excreted mainly by kidneys: 30-60 % in not changed form and 15-25 % in the form of desacetylcefotaxime(the basic metabolite retaining bactericidal activity). Other two metabolites of Cefotaximedo not possess antimicrobial action. Besides, Cefotaxime is eliminated with bile.
At repeated intravenous introductions of the preparation in a dose of 1 geach 6 hours within 14 days, the cumulation is not observed.
In newborns ÒS is 0,75-1,5 h, in prematurely born - up to 6,4 h, in patients elder 80 years - 2,5 h, at renal failure ÒSdoes not exceed 2,5 hours.
Cefotaxime is administrated at severe infections of respiratory tract and an ENT-organs (except for enterococcus), skin and soft tissues (including infested wounds and burns), bones and joints, genitourinary system, organs of pelvis minor, gynecologic (clamidiosis, uncomplicated gonorrhea, including caused by the microorganisms excreting penicillinase), bacteriemia, septicemia, peritonitis, intraperitoneal abscesses and other infections of organs of abdominal cavity, bacterial meningitis (except for listeriosis), etc. diseases of CNS, endocarditis, Lime disease, typhoid fever, infections on a background of immunodeficiency, for prophylaxis of postoperative infectious complications.
Dosage and method of administration
The preparation is introduced intravenously (streamly or dropwise) and intramusculary.
For intramuscular injection 0,5 g of Cefotaxime isdissolved in 2 ml (accordingly 1 gand 2 gin 3 ml and 5 ml) sterile water for injections. It is injected deeply intogluteus. For introduction in vein 0,5 g of the preparation is dissolve in 2 ml (or 1 gin 4 ml and 2 gin 10 ml) of sterile water for injections. It is introduced slowly during 3-5 min. For dropwise introduction (during 50-60 mines) 2 gof the preparation is dissolved in 100 ml of isotonic sodium chloride solution or 5 % glucose solution.
Cefotaxime is administrated to adults and children elder 12 years in a dose of 1 geach 12 hours. In serious cases a dose is increased in 2 geach 12 hours or number of introductions is increased up to 3-4 times a day, bringing the total daily dose up to maximal dose of 12 g.
It is administrated to newborns and younger children in a dose of 50-100 mg/kg a day, divided into separate doses with intervals from 12 to 6 h. For prematurely born children the daily dose should not exceed 50 mg/kg.
A dose is reduced in case of kidneys function failure. At anuria of initial stage (excretion of creatinine -- 5 ml/min) a dose is usually reduced by half.
At acute gonorrhea the preparation is introduced intramusculary in a single dose of 0,5-1,0 g.
For prophylaxis of postoperative complications should be administrated before or during narcosis introduction in a dose of 1 g; if necessary it is introduced repeatedly in 6-12 hours.
At Cefotaxime intake the nausea, vomiting, abdominal pain, diarrhea, pseudomembranous colitis, transitional rising of hepatic transaminases, lactate dehydrogenase, alkaline phosphatase activity and bilirubin in blood plasma, neutropenia, transitional leukopenia, eosinophilia, thrombocytopenia, agranulocytosis, prothrombinopenia, bleedings and hemorrhages, autoimmune hemolitic anemia, rising of concentration of urea nitrogen and creatinine in blood plasma are possible, interstitial nephritis, acute renal failure, cardiac arrhythmias (at rapid stream introduction), headache, reversible encephalopathy is possible in patients with renal failure. Allergic reactions can be observed: eruption, hyperemia, multiform exudative erythema, Stevens-Johnson's syndrome, fever, anaphylactic shock; dysbacteriosis, superinfection, vaginal and oral candidiasis; in a place of introduction the pain, infiltration and inflammation of tissues, phlebitis are possible.
Hypersensitivity (including to penicillins, other cephalosporins, carbapenems), presence in the anamnesis of bleedings, enterocolitis (especially nonspecific ulcerative colitis). Pregnancy. Lactation (the termination of breast feeding is obligatory). Children's age under 2,5 years (for intramuscular introduction).
The preparation is administrated with care to patients with allergy (including to medicinal preparations). The combination with nephrotoxic preparations requires the control of kidneys function. At Cefotaxime application for more than 10 days the control of blood cell pattern is necessary. The elderly patients and patients with broken health vitamin K should be administrated (prophylaxis of hypocoagulation). At occurrence of pseudomembranous colitis signs Cefotaxime should be withdrawn.
Interactions with other medicinal preparations
Increases nephrotoxicity of aminoglycosides and other preparations affected kidneys. Increases risk of bleedings at combination with antiaggregants (including NSAID). Probenecid slows down an excretion, raises concentration in plasma and half-elimination time of Cefotaxime(the probability of the preparation side effects appearance is increased). At combined application with azlocyllin or mezlocyllin the Cefotaxime clearance decreases, and it is necessary to reduce a level of applied doses of the preparation.
It is incompatible in one syringe with aminoglycoside’s solutions.
Treatment:there is no specific antidote. Maintenance of vital functions.
The form of release
0,5 and 1,0 g of active substance in vials of 10 ml capacity.