powder for solution for injections preparation, 0,5 g and 1,0 g
Cefazolinum Natrium 0,5 et 1,0 pro injectionibus
international nonproprietary name
Cefazolin – Cefazolinum
Antibiotic of cephalosporin group.
Composition of the preparation
One vial contains 500 mg or 1000 mg Cefazolin sodium.
Cefazolin sodium is a cephalosporin antibiotic of a wide spectrum of action. It possesses bactericidal effect. It is active in relation to gram-positive bacteria: Staphylococcus spp. (the strains which are producing and not producing of penicillinase), Streptococcus spp. (including Streptococcus pneumoniaе), Corynebacterium diphtheriae, Bacillus anthracis; Gram-negative bacteria: Neissеria meningitidis, Neisseria gonorrhoae, Shigella spp., Salmonella spp., Escherichia coli, Klebsiella spp.. It is active also in relation to Spirochaetаceae, Leptospira spp. It is inactive in relation Pseudomonas aeruginosa, indole-positive strains of Proteus spp., Mycobacterium tuberculosis, anaerobic bacteria.
It reacts with specific penicillin-binding proteins on cytoplasmic membrane surface, inhibits synthesis peptidoglycan layer of cell wall (inhibits transpeptidase, suppresses formation of cross-links ofpeptidoglycan chains), releases autolytic enzymes of cell wall, causing its damage and bacteria death.
Cefazolin sodium is destroyed in gastrointestinal tract.
The high concentration of the preparation is formed in blood after parenteral introduction. The period of half-elimination (Т1/2) is 1,8-2 hours. In patients with kidneys function failure the values of Т1/2are increased. Cefazolin gets into an osteal tissue, in ascitic fluid, pleural and synovial fluids, bile; easily passes through a placental barrier, however, it is not able to get through a hematoencephalic barrier. It is eliminated by kidneys in non-changed form (from 80 up to 100 % of the entered dose is eliminated during 24 h), in insignificant quantities it is eliminated with breast milk.
Cefazolin is administrated at the infection-inflammatory diseases caused by microorganisms sensitive to it.
Indications to the preparation administration are: infections of upper and lower parts of respiratory tract (acute bronchitis and exacerbation of chronic bronchitis, infected bronchiectasias, bacteriemic pneumonias, empyema and lung abscesses); infections of ENT-organs (including otitis media, mastoiditis); infections of urinary tract (including acute and chronic pyelonephritis); infections of bilinary tract; infections of a skin and soft tissues (including cellulitis, erysipelas, anthrax, phlegmon, wound and burn infections); infections of bones and joints (including osteomyelitis, septic arthritis); gynecologic and puerperal infections (including septic abortion, endometritis, postnatal infections); hematosepsis, endocarditis, peritonitis, lues, gonorrhea; prophylaxis of postoperative infectious complications.
At occurrence of serious diarrhea, characteristic for pseudomembranous colitis, Cefazolin sodium should be withdrawn and corresponding treatment should be administrated. During treatment the patients should abstain from the use of alcohol. At long application of the preparation the control of peripheral blood pattern and function of kidneys is necessary; it is necessary to carry out prophylaxis of dysbacteriosis. The preparation should be administrated with care at liver and kidneys function failure, colitis, decrease of blood coagulability. With extra care it is indicated simultaneously with loop diuretics.
Dosage and method of administration
Regimen of dosage is established individually. The daily dose of Cefazolin is from 1 to 4 gfor adults (sometimes more) and depends on severity of infection, species of pathogenic organism and its sensitivity to the antibiotic. If infections are caused by gram-positive microorganisms, the single dose of Cefazolin for adults is usually 0,25-0,5 g, the preparation is introduced every 8 h. At the infections of respiratory tract of moderate severity caused by pneumococcuses, at diseases of urinary tract caused by microorganisms sensitive to the antibiotic, the preparation should be administrated per 0,5-1,0 gevery 12 h. At the diseases caused by gram-negative microorganisms sensitive to the antibiotic, Cefazolin should be administrated per 0,5-1,0 gevery 6-8 h. The daily dose at sepsis, endocarditis and other severe diseases is up to 6 g.
The maximal daily dose of the preparation is 6 g. Duration of treatment is 7-10 days.
For prophylaxis of postoperative infections the preparation should be indicated in a dose of 1 gin 30 min before an operation, 0,5-1,0 g- during operation and 0,5-1,0 g- every 6-8 h within a day after operation.
In patients with kidneys secretory function failure Cefazolin sodium is administrated in reduced doses in order to prevent a cumulation.
Signs:sleepiness, paresthesia, headache, convulsions, especially in patients with renal failure are possible. Changes of laboratory indexes at overdosage: rising of creatinine level in blood serum, change of functional hepatic tests, positive Coombs’ test, thrombocytosis, thrombocytopenia, eosinophilia, leukopenia, prothrombin time elongation a.
Treatment:symptomatic therapy. At occurrence of convulsive seizures anticonvulsant therapy is carried out. In case of a serious overdosage, especially in patients with renal failure, hemodialysis and a hemosorption should be applied.
Nausea, vomiting, diarrhea, pains in epigastric area, pseudomembranous colitis, rising of hepatic enzymes concentration (AST, АLТ, alkaline phosphatase, LDH) in blood, neutropenia, leukopenia, agranulocytosis, thrombocytopenia, lymphocytosis, hemolitic anemia, candidomycosis, allergic manifestations (dermal rash, itch, toxic epidermal necrosis, Stevens-Johnson’s syndrome, multiform erythema, angioedema, anaphylactic shock), reactions in a place of introduction: formation of infiltrates and abscesses, phlebitises and thrombophlebites.
Hypersensitivity, including to another beta-lactam antibiotics, pregnancy, breast feeding (should be stopped for the period of treatment). Safety of the preparation in children in the age of under 1 month and in prematurely born children is not established, therefore the use of Cefazolin sodium in this category of patients is not recommended.
Interactions with other medicinal preparations
Probenecid slows down an elimination of Cefazolin sodium and promotes its cumulation. It is impossible to mix Cefazolin sodium sat in one vial or syringe with other antibiotics (especially with antibiotics of aminoglycoside group). At рНvalue of the solution more than 8,5 Cefazolin sodium is subjected to hydrolysis, at рНbelow 4,5 the sediment (insoluble Cefazolin) is formed.
The form of release
Powder for injection solution preparation for intravenous and intramuscular introduction in vials per 500 and 1000 mg.