Tsefotaksim-BHFZ

General characteristics. Structure:

International and chemical names: Cefotaxime; sodium (6R,7R)-3-[(atsetiloks) marked]-7-[[(Z)-2 (2-aminothiazol-4-silt)-2-(metoksiimino) acetyl] amine] - 8-oxo-5-thia-1-azabitsiklo [4.2.0.] Oct - 2 - ен - 2 - carboxylat; main physical and chemical properties: powder of white or slightly yellow color. Hydroscopic; structure: 1 bottle contains a tsefotaksim of sodium salt sterile in terms of tsefotaksy 500 mg or 1000 mg.

Pharmacological properties:

Pharmacodynamics. Tsefotaksim-BHFZ - a semi-synthetic antibiotic of group of cephalosporins ІІІ generations, a broad spectrum of activity, for parenteral administration. Drug is effective concerning many gram-positive and shows high activity to gram-negative bacteria. Affects bakteritsidno the strains of bacteria resistant to penicillin, aminoglycosides, streptocides. The mechanism of antimicrobic action Tsefotaksima-BHFZ is connected with oppression of activity of enzyme of transpeptidase, blockade of a peptidoglikan, disturbance of formation of a mukopeptid of a cell wall of microorganisms. Drug resistant in relation to four of five beta лактамаз gram-negative bacteria and a penicillinase of stafilokokk. It is active in relation to Staphylococcus aureus, Staphylococcus epidermidis, some strains of Enterococcus spp., Streptococcus pneumoniae (especially Diplococcus pneumoniae), Streptococcus pyogenes (beta and hemolitic streptococci of group A), Streptococcus agalactiae (group B streptococci), Bacillus subtilis, Bacillus myroides, Corinebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, including ampitsillinorezistentny strains, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Morganella morganii, Neisseria meningitidis, Neisseria gonorrhoeae, including strains developing a penicillinase, Propionibacterium, Proteus mirabilis, Proteus vulgaris, Proteus inconstans, Serratia spp., Veillonella, Yersinia, Bordetella pertussis, Moraxella, Aeromonas hydrophilia, Fusobacterium, Bacteroides spp. Clostridium species, Peptostreptococcus species, Peptococus spp.
Influences some strains of Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, Bacteroides fragilis, Clostridiun difficile. Can affect multiresistant strains which are resistant to penicillin, cephalosporins of the first two generations, aminoglycosides. Drug is less active to gram-positive cocci, than cephalosporins I-II of generations.
To effect of drug of a rack streptococci of group D, Listeria spp. and metitsillinstoyky staphylococcus.

Pharmacokinetics. The maximum concentration in blood after intramuscular administration of drug in doses of 500 mg and 1000 mg is observed in 30 minutes after introduction and makes 11 mkg/ml and 21 mkg/ml respectively. In 5 minutes after intravenous administration of 500 mg, 1000 mg or 2000 mg the maximum concentration in blood makes respectively 39, 100, 214 mkg/ml. In blood drug for 25-40% contacts proteins. Bactericidal concentration in blood remains more than 12 hours. Drug well gets into fabrics (creates effective concentration in a myocardium, a bone tissue, a gall bladder, skin, soft tissues), organism liquids (is defined in effective concentration in spinal, pericardiac, pleural, peritoneal, synovial liquids), passes through a placenta, gets into breast milk. Tsefotaksim-BHFZ is brought in a significant amount with urine (90%) (in not changed look about 60-70% and in the form of active metabolites about 20-30%, from them 15-25% are the main metabolite - dezatsetiltsefotaksimy, having antimicrobic activity). An elimination half-life at intravenous administration - 1 hour, at intramuscular - 1-1,5 hours. At repeated intravenous administrations in a dose of 1000 mg each 6 hours for 14 days of cumulation it is not observed. At babies the elimination half-life makes 0,75-1,5 hours, at premature - from 1,4 to 6,4 hours, at patients 80 years are more senior and at a renal failure the elimination half-life of drug increases approximately twice.

Indications to use:

The infections caused by microorganisms, sensitive to effect of drug:
• infections of an ear, nose, throat (quinsies, otitises);
• respiratory infections (bronchitis, pneumonia, pleurisy, abscesses);
• infections of urinogenital system;
• septicaemia, bacteremia;
• intraabdominal infections (including peritonitis);
• infections of skin and soft tissues;
• infections of bones and joints;
• meningitis (except for listeriozny) and other infections of TsNS;
• prevention of infections after surgeries on a GIT, urological and obstetric and gynecologic operations.

Route of administration and doses:

Tsefotaksim-BHFZ appoint intramusculary and intravenously, struyno and kapelno.
For intramuscular introduction dissolve 500 mg Tsefotaksima-BHFZ in 2 ml, and 1000 mg - in 4 ml of sterile water for injections or 1% of solution of lidocaine and enter deeply into a gluteus.
For intravenous administration dissolve 500-1000 mg Tsefotaksima-BHFZ in 4 ml, and 2000 mg – in 10 ml of sterile water for an injection and enter slowly, for 3 – 5 minutes.
For intravenous infusion dissolve 1000-2000 mg of drug in 50-100 ml of isotonic solution of sodium of chloride or 5% of solution of glucose and enter for 50-60 min.
Single dose Tsefotaksima-BHFZ for adults – 1000 mg every 12 hours, in hard cases increase a dose to 2000 mg every 12 hours or increase the number of introductions to 3-4 times a day, bringing the general daily dose to maximum – 12 g.
At acute gonorrhea the drug is administered disposable, intramusculary, in a dose of 500-1000 mg.
For prevention of infectious complications before or during an introduction anesthesia enter 500-1000 mg, if necessary repeat an injection in 6-12 hours.
At a renal failure (at clearance of creatinine of 10 ml/min. and less) the dose is reduced twice.
At premature and children aged up to 1 week the daily dose of drug makes 50-100 mg/kg, is divided into two introductions in equal doses in days, entered intravenously. At children at the age of 1-4 weeks the daily dose of drug makes 75-150 mg/kg, is divided into three equal doses and entered intravenously.
At children with body weight to 50 kg a daily dose Tsefotaksima-BHFZ makes 50-100 mg/kg and is divided into 3-4 intramuscular or intravenous administrations. At heavy infections, including meningitis, the daily dose is doubled.
To children with the body weight of 50 kg and more drug is appointed in doses for adults.

Features of use:

With care appoint Tsefotaksim-BHFZ the patient with burdened allergoanamnezy.
In case of drug use by the women nursing feeding should be stopped.
Simultaneous use Tsefotaksima-BHFZ with nefrotoksichny drugs demands control of function of kidneys; at drug use more than 10 days control of peripheral blood is necessary. Elderly people and the weakened patients for prevention of hypocoagulation should appoint vitamin K drugs. At establishment of a symptom of pseudomembranous colitis Tsefotaksim-BHFZ cancel.
Tsefotaksim-BHFZ does not influence ability to work with mechanisms and to manage vehicles.

Side effects:

From a GIT: nausea, vomiting, diarrhea, an abdominal pain, дисбиоз, it is rare – pseudomembranous colitis;
Allergic reactions: rash, a multiformny exudative erythema, Stephens-Johnson's syndrome, fever, an eosinophilia, anaphylactic reactions, it is rare – an acute anaphylaxis;
From biochemical indicators: increase in hepatic transaminases, lactate dehydrogenases, alkaline phosphatase and bilirubin, concentration of an urea nitrogen and creatinine;
From peripheral blood: neutropenia, tranzitorny leukopenia, thrombocytopenia, agranulocytosis, prothrombinopenia;
From TsNS: headache, reversible encephalopathy;
Local reactions: pain, inflammation of fabrics, phlebitis;
The effects caused by biological effect: development of superinfection is possible;
Others: bleedings and hemorrhages, autoimmune hemolitic anemia, intersticial nephrite, an acute liver failure, arrhythmia (at bystry jet introduction).

Interaction with other medicines:

At simultaneous use Tsefotaksima-BHFZ with aminoglycosides, "loopback" diuretics is observed increase in nephrotoxicity. At simultaneous introduction with antiagregant, with non-steroidal anti-inflammatory drugs the risk of bleeding increases. Probenetsid slows down excretion, increases concentration in plasma and an elimination half-life. Tsefotaksim-BHFZ it is impossible to enter in one volume with other drugs because of possible interaction.

Contraindications:

Hypersensitivity to antibiotics of a tsefalosporinovy row and another beta лактамным to antibiotics, hypersensitivity to lidocaine (intramuscular introduction); bleeding, a coloenteritis in the anamnesis (especially nonspecific ulcer colitis); pregnancy, feeding period breast.
Intramuscular introduction is contraindicated to children up to 2,5 years.

Overdose:

The overdose of drug can cause encephalopathy.
Treatment - symptomatic therapy.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not over 25 to the °sena to use drug after the termination of the period of validity specified on packaging!

Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Bottles on 500 mg or 1000 mg of powder for injections; on 5 bottles in the cartridge and a case.