Tsefotaksim

General characteristics. Structure:

Active ingredient: 1 g of a tsefotaksim of sodium salt (in terms of tsefotaksy).

Bactericidal antibiotic of a wide range of antimicrobic action.

Pharmacological properties:

Pharmacodynamics. Tsefotaksim is a tsefalosporinovy antibiotic of the III generation for parenteral use. Works bakteritsidno. Possesses a wide range of antimicrobic action.

It is active concerning the gram-positive and gram-negative microorganisms steady against other antibiotics: Staphylococcus spp. (including Staphylococcus aureus including a penicillinase forming strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus species, Enterobacter spp., Escherichia coli Haemophilus influenzae (including the strains forming a penicillinase), Haemophilus parainfluenzae, Klebssiella spp. (including KLpneumoniae), Morganella morganii, Neisseria gonorrhoeae (including the strains forming a penicillinase), Acinetobacter species, Corynebacterium diphtheriae, Erysipelo:hrix insidiosa, Eubacterium spp. Propionibacterium spp., Bacillus subtilis, Clostridium spp. (including Clostridium perfringens), Escherichia coli, Citrobacter sppj, Proteus mirabilis, Proteus indole, Proteus vulgaris, Providencia spp. (including Providenfia rettgeri), Serratia spp. Pseudomonas aeruginosa, Neisseria meningitidis, Bacterdides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. It is steady against the majority beta лактамаз gram-positive and gram-negative microorganisms, a penicillinase of stafillokok of Clostridium difficile

Pharmacokinetics. After single in/in introductions of 0.5, 1 and 2 g the maximum concentration (Cmax) is reached in 5 min. and makes 39 mkg/ml, 100 mkg/ml and 214 mkg/ml, respectively. After in oil 0.5 and 1 g of Cmax are reached in 0.5 h and makes 11 and 21 mkg/ml, respectively. Communication with proteins of plasma - 25-40%.

Creates therapeutic concentration in the majority of fabrics (a myocardium, bones, a gall bladder, skin, soft tissues) and liquids (synovial, pericardiac, pleural, a phlegm, bile, urine, spino-brain liquid) an organism. Distribution volume - 0.25-0.39 l/kg.

Elimination half-life (T1/2) at in / the item and introduction in oil - 1 h. It is removed by kidneys - 60% - 70% in not changed look, other quantity - derivative has bactericidal activity, and 2 other metabolites do not possess). At the chronic renal failure (CRF) and at age of T1/2 increases twice, tl/2 at newborn premature newborn children increases up to 4,6 h. At repeated in introductions in a dose of 1 g each 6 h during 14 days of cumulation it is not observed. Gets into breast milk

Indications to use:

The bacterial infections of a heavy current caused by sensitive microorganisms: - infections of the central nervous system (meningitis), airways and ENT organs, urinary tract, bones, joints, skin and soft tissues, bodies of a small pelvis, clamidiosis, gonorrhea, contaminated wounds and burns, peritonitis, sepsis, abdominal infections, an endocarditis, a disease Laima (borreliosis), salmonellosises, infections against the background of an immunodeficiency, prevention of infections after surgeries (including urological, obstetric and gynecologic, on digestive tract).

Route of administration and doses:

Intramusculary and intravenously. For an intramuscular injection dissolve 0,5 g of drug in 2 ml (respectively 1 g in 4 ml) sterile water for injections. Enter deeply into a gluteus. As solvent at intramuscular introduction 1% lidocaine solution is also used (on 0,5 g - 2 ml, on 1 g - 4 ml).

For intravenous administration 0,5 - of a tsefotaksim is dissolved in 10 ml of sterile water for injections. Enter slowly within 3-5 minutes For drop introduction (within 50-60 minutes) dissolve 2 g of drug v100 ml of isotonic solution of sodium of chloride or 5% of solution of glucose. The usual dose of a tsefotaksim for adults and children is more senior than 12 years - 1 g every 12 hours.

In hard cases the dose is increased to 3 or 4 g a day, administer time drug 3 or 4 on 1 g. Depending on disease severity the daily dose can be increased to maximum which makes 12 g. The usual dose for newborns and children is younger than 12 years - 50-100 mg/kg of body weight a day with intervals of introduction from |6 to 12 hours.

For premature children the daily dose should not exceed 50 mg/kg. In case of renal failures the dose is reduced. At clearance of creatinine of 10 ml/min. and less daily dose of drug is reduced twice

Features of use:

Use of drug during the periods of pregnancy and a lactation is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit.

Tsefotaksim is allocated with breast milk therefore in need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

In the first weeks of treatment there can be pseudomembranous colitis which is shown heavy long diarrhea. At the same time stop administration of drug and appoint adequate therapy, including Vancomycinum or metronidazole.

Before purpose of drug it is necessary to collect the allergological anamnesis, especially concerning a beta laktamnykh of antibiotics. The cross allergy between penicillin and cephalosporins is known. At persons in whose anamnesis there are instructions on allergic reactions to penicillin drug is used with extreme care (it is necessary to consider a possibility of development of heavy anaphylactic reactions, up to a lethal outcome).

At treatment duration drug over 10 days it is necessary to control a pattern of peripheral blood.

When determining glucose in urine by not euzymatic method (for example, Benedict's method) false positive results are possible.

With care to appoint to the persons managing transport and who are engaged in the types of activity demanding the increased concentration of attention and bystry motor reaction.

Side effects:

Allergic reactions: small tortoiseshell, fever or fever, rash, itch, bronchospasm, eosinophilia, malignant exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), Quincke's disease, acute anaphylaxis.

From the alimentary system: nausea, vomiting, diarrhea or lock, meteorism, abdominal pain, dysbacteriosis, abnormal liver function (increase in activity of "hepatic" transaminases, alkaline phosphatase, giperkreatininemiya, hyperbilirubinemia), stomatitis, glossitis, pseudomembranous coloenteritis.

From bodies of a hemopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolitic anemia, hypocoagulation.

From an urinary system: a renal failure (an azotemia, increase in content of urea in blood, an oliguria, an anury, intersticial nephrite).

From a nervous system: headache, dizziness.

Laboratory indicators: false positive test of Koombs.

From cardiovascular system: potentially life-threatening arrhythmias after bystry bolyusny introduction to the central vein.

Local reactions: phlebitis, morbidity on the vein course, morbidity and infiltrate in the place in oil of introduction.

Others: superinfection (in particular, mycotic vulvovaginitis).

Interaction with other medicines:

Increases risk of development of bleedings at a combination to antiagregant, non-steroidal anti-inflammatory drugs.

Does not lead to development of disulfiramopodobny reactions at combined use with ethanol.

The probability of damage of kidneys increases at a concomitant use with aminoglycosides, polymyxin B and "loopback" diuretics.

The medicines blocking canalicular secretion increase plasma concentration of a tsefotaksim and slow down its removal.

Pharmaceutical it is incompatible with solutions of other antibiotics in one syringe or a dropper.

Contraindications:

Hypersensitivity (including to penicillin, other cephalosporins, karbapenema).

At children up to 2,5 years it is impossible to use intramuscular administration of drug.

With care. The neonatality period, the lactation period (in insignificant concentration it is allocated with milk); chronic renal failure, nonspecific ulcer colitis (including anamnesis).

Overdose:

Symptoms: spasms, encephalopathy (in case of introduction of high doses, especially at patients with a renal failure), a tremor, the increased nervnomyshechny excitability.

Treatment: symptomatic therapy.

Storage conditions:

Period of validity 2 years. Not to use the List B after expiry date. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration on 1 g in bottles. On 1, 5 or 10 bottles in a cardboard pack together with the instruction on a medical use, or with equal amount of solvent of water for injections. On 50 bottles place in a box cardboard with 3 - 5 application instructions (for hospitals)