Structure

Active ingredient: tsefotaksy;

1 bottle supports a tsefotaksim (in the form of a tsefotaksim of sodium salt sterile) 500 mg or 1000 mg.

Dosage form

Powder for solution for injections.

Main physical and chemical properties: powder of white or slightly yellow color, hydroscopic.

Pharmacotherapeutic group

Antimicrobial means for system use. beta laktamnye antibiotics. cephalosporins of the third generation. code atkh j01d d01.

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 in relation to many gram-positive and shows high activity to gram-negative bacteria. Affects bakteritsidno strains of the 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 the attitude towards four of five beta laktamaz gram-negative bacteria and penicillinase of stafilokokk. It is active in the relation to Staphylococcus aureus, Staphylococcus epidermidis, some strains of Enterococcus spp., Streptococcus pneumoniae (especially Diplococcus pneumoniae), Streptococcus pyogenes (beta and hemolytic 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, podutsiruyushchy 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 influence multi-medicament resistant strains which resistant to penicillin, cephalosporins of the first two generations, aminoglycosides. Drug is less active in relation to gram-positive cocci, than cephalosporins I-II of generations.

To effect of medicament of a rack streptococci of group D, Listeria spp. and metitsillinstoyky staphylococcus.

Pharmacokinetics

Maximum concentration in blood after intramuscular administration of medicament in doses of 500 mg and 1000 mg is observed by

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 medicament for 25–40% contacts blood 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 antimicrobial activity). 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 till 6.4 o'clock, at patients 80 years are more senior and in a renal failure the elimination half-life of medicament increases approximately twice.

Clinical characteristics

Indication

Infection caused by microorganisms, sensitive to effect of drug:

• an infection of ENT organs (tonsillitis, otitises);
• respiratory infection (bronchitis, pneumonia, pleurisy, abscesses);
• an infection of an urinogenital system;
• septicaemia, bacteremia;
• intraabdominal infections (including peritonitis);
• an infection of skin and soft tissues;
• an infection of bones and joints;
• meningitis (except for listeriozny) and other infections of central nervous system;
• prevention of infections after surgeries on a GIT, urological and obstetric and gynecologic operations.

Contraindication

Hypersensitivity to antibiotics of a tsefalosporinovy row and another beta laktamnym to antibiotics, hypersensitivity to lidocaine (intramuscular introduction); bleeding, a coloenteritis in the anamnesis (especially nonspecific ulcer colitis).

AV blockade without the established driver of a warm rhythm, heavy heart failure.

Interaction with other medicines and other types of interactions

With nefrotoksichny medicaments (aminoglycosides) and strong diuretics (Acidum etacrynicum, furosemide), colistin, polymyxin increases risk of developing a renal failure.

With bacteriostatic antibiotics (for example, tetracyclines, erythromycin and chloramphenicol) the antagonistic effect is possible

.

With solutions of aminoglycosides should not be mixed, they need to be entered separately.

With nifedipine the bioavailability of a tsefotaksim increases by 70%.

by

C probenetsidy blocks canalicular secretion of a tsefotaksim and its elimination half-life is extended.

Tsefotaksim not to apply

together with lidocaine:

• at intravenous administration;
• to children up to 30 months;
• to patients with hypersensitivity to lidocaine in the anamnesis;
• to patients with heart block.

during treatment tsefotaksimy the efficiency of oral contraceptives therefore during this period it is necessary to use additional contraception can decrease.

by

Feature of use

With care to appoint medicament in renal failures and a liver; in renal failures the dose of medicament should be reduced taking into account severity of a renal failure and sensitivity of the activator.

At prolonged use of medicament should control function of kidneys, to carry out prevention of dysbacteriosis. Reasonablly regularly to control cellular composition of peripheral blood, function of a liver. At use of medicament the development of false positive test of Koombs is possible.

Anaphylactic reactions. Use of cephalosporins demands specification of the allergological anamnesis (allergic diathesis, reactions of hypersensitivity to a beta laktamnym to antibiotics). At development in the patient of reaction of hypersensitivity the treatment should be stopped. Use of a tsefotaksim is strictly contraindicated to patients with existence in the anamnesis of reaction of immediate hypersensitivity to cephalosporins. In case of any doubts the presence of the doctor at the first administration of medicament is obligatory because of possible development of anaphylactic reaction. Cross allergic reaction between cephalosporins and penicillin which arises in 5–10% of cases is known.

Pseudomembranous colitis. In the first weeks of treatment there can be pseudomembranous colitis which is shown heavy long diarrhea. The diagnosis is confirmed at colonoscopy and/or a histologic research. These complications are regarded as very serious: immediately it is necessary to stop administration of medicament and to appoint the adequate therapy including oral administration of Vancomycinum or metronidazole.

Combination of use of a tsefatoksim to nefrotoksichny medicaments demands control of a fuktion of kidneys, use more than 10 days — control of composition of blood. To the elderly and weakened patients to appoint vitamin K (prevention of hypocoagulation).

Each gram of medicament contains about 0.048 g of sodium that the patients adhering to a diet with the controlled content of sodium need to consider.

As well as at reception of other antibiotics of a broad spectrum of activity, prolonged use can lead to the increased growth of insensitive microorganisms that demands the treatment termination. If during treatment there is superinfection, it is necessary to perform antimicrobic therapy.

by

When determining level of glucose in urine by method of restoration false positive results can be received. For prevention of it it is necessary to use the fermental test.

during treatment cannot apply alcohol as the effects similar to effect of Disulfiramum are possible (hyperaemia of the person, a spasm in a stomach and in a stomach, nausea, vomiting, a headache, a lowering of arterial pressure, tachycardia, breath difficulty).

At use of lidocaine as solvent at intramuscular introduction before an injection should take skin samples on tolerance of lidocaine.

Incompatibility

should not be entered in one container with other medicines, except the solutions specified in the instruction.

Use during pregnancy or feeding by a breast to

Use of medicament during pregnancy is contraindicated to

.

for treatment should stop feeding by a breast.

Ability to influence speed of response at control of motor transport or other mechanisms

Because of possibility of side reactions from nervous system should avoid control of vehicles or work with other mechanisms during treatment.

Route of administration and doses

needs to carry out by

Before use of medicament skin tests on shipping.

Tsefotaksim-BHFZ to appoint

intramusculary and intravenously, struyno and by drop infusion.

For intramuscular introduction to 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 to enter deeply into a gluteus.

For intravenous administration to dissolve 500 mg Tsefotaksima-BHFZ in 4 ml, 1000 mg — in 8 ml, and 2000 mg — in 10 ml of sterile water for an injection and to enter slowly, within 3–5 minutes.

For intravenous infusion to dissolve 1000–2000 mg of medicament in 50–100 ml of 0.9% of isotonic solution of sodium of chloride or 5% of solution of glucose and to enter within 50–60 minutes.

Duration of a course of treatment the doctor establishes

individually.

Single dose Tsefotaksima-BHFZ to adults and children with the body weight of 50 kg and more — to 1000 mg is each 12 hours, in hard cases to increase a dose to 2000 mg each 12 hours or to increase the number of introductions to 3–4 times a day, bringing the general daily dose to maximum — 12 g

For prevention of infectious complications before surgical intervention during introduction to an anesthesia to enter 1000 mg of drug, if necessary to repeat an injection in 6–12 hours.

In uncomplicated infections and also in infections of urinary tract medicament to appoint intramusculary or intravenously in a dose of 1 g each 12 hours;

in uncomplicated acute gonorrhea to administer the medicament intramusculary or intravenously in a dose of 1 g of 1 times a day;

by

in moderately severe infections to appoint medicament in a dose of 1-2 g each 12 hours;

by

in heavy infections (meningitis) to appoint in a dose 2 g of medicament intravenously each 6–8 hours.

At premature children and children up to 1 week the daily dose of medicament makes 50 mg/kg, is divided into two introductions in equal doses, to enter intravenously.

to Children about 1–4 weeks the daily dose of medicament makes 50–100 mg/kg, is divided into 3 equal doses and entered intravenously.

to 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. In heavy infections, including meningitis, it is recommended to increase a daily dose to 100–200 mg/kg of body weight and to enter for 4–6 times intravenously or intramusculary.

a dose to reduce

In a renal failure (at clearance of creatinine of 10 ml/min. and less) twice.

Children

to Children up to 2.5 years intramusculary not to administer the drug.

Overdose

Symptoms: fever, a leukopenia, thrombocytopenia, acute hemolytic anemia, skin, gastrointestinal reactions and reactions from a liver are possible, short wind, a renal failure, stomatitis, anorexia, a temporary hearing loss, loss of orientation in space, spasms, encephalopathy (especially in a renal failure).

Treatment: specific antidote is absent. Level of a tsefotaksim in blood serum can be reduced a hemodialysis or peritoneal dialysis. In case of need to carry out symptomatic therapy.

At emergence of an acute anaphylaxis should take the appropriate measures immediately. At the first signs of hypersensitivity reaction (skin rashes, urticaria, a headache, nausea, a loss of consciousness) the introduction of a tsefotaksim should be stopped. In case of heavy hypersensitivity reaction or anaphylactic reaction it is necessary to begin the corresponding therapy (administration of epinephrine and/or glucocorticoids). At these clinical states additional measures, for example, artificial respiration, use of antagonists of histamine receptors can be required. In case of vascular insufficiency it is necessary to take resuscitation measures.

Side reactions

Digestive tract: nausea, vomiting, diarrhea, meteorism, abdominal pain, disbioz, stomatitis, glossitis, pseudomembranous colitis.

Immune system, skin and hypodermic cellulose: hyperaemia, rash, itching of skin, urticaria, sharp generalized exanthematous pustulez, bronchospasm, multiformny exudative erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis (Lyell's disease), fever, anaphylactic reactions, Quincke's disease, acute anaphylaxis.

Gepatobiliarnaya system: hepatitis, acute liver failure, abnormal liver functions, jaundice, cholestasia.

Biochemical indicators: increase in level of hepatic transaminases, lactate dehydrogenases, alkaline phosphatase and bilirubin, concentration of urea nitrogen and creatinine, positive test of Koombs.

Blood: granulocytopenia, neutropenia, tranzitorny leukopenia, thrombocytopenia, agranulocytosis, anisocytosis, prothrombinopenia, hemolytic anemia, eosinophilia, hypocoagulation.

Nervous system: headache, dizziness, spasms, reversible encephalopathy, increased fatigue, weakness.

Local reactions: pain and infiltrate in the injection site, inflammation of fabrics, phlebitis.

Effects caused by biological effect: development of superinfection is possible (including candidiasis, a vaginitis).

Others: bleedings and hemorrhages, autoimmune hemolytic anemia, interstitial nephrite, arrhythmia (at fast jet introduction).

At treatment of the infections caused by a spirochete the complication similar to Gerksgeymer's reaction can arise. It can lead to fever, a fever, a headache and a joint pain.

Expiration date

2 years.

solution can be stored by

After preparation within 24 hours in the fridge at a temperature of 5±3 °C in the place protected from light and 12 hours at the room temperature (20±5 °C) without protection against light hit.

From the microbiological point of view drug, ready to use, needs to be used immediately. If not to use it immediately, then responsibility for time and storage conditions in the course of use is assigned to the consumer.

Storage conditions.

In original packing at a temperature not above 25 °C.

to Store

out of children's reach!

Packing

Bottle No. 1 (without pack): on 55 bottles in a box; bottle No. 1 (in a pack): on 1 bottle in a pack; bottles No. 5 (in a case): on 5 bottles in the cartridge, 1 cartridge in a case; bottle No. 1 (in a pack): on 1 bottle complete with solvent (water for injections) on 5 ml in an ampoule in the cartridge, 1 cartridge in a pack; bottle No. 1 (in a pack): on 1 bottle complete with solvent (water for injections) on 5 ml in an ampoule in a pack with a cardboard partition.

Category of release

According to the prescription.

Producer

""Borshchagovsky Chemical and Pharmaceutical Plant" research and production center" Public joint stock company.

Location of the producer and its address of the place of implementation of activity

Ukraine, 03134, Kiev, Mira St., 17.