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General characteristics. Structure:

Active ingredient: 1 g of a tsefotaksim (in the form of sodium salt).

Pharmacological properties:

Pharmacodynamics. Tsefotaksim is a tsefalosporinovy antibiotic of the III generation for parenteyoralny introduction. Works bakteritsidno by blocking of a polymerase of a peptidoglikan, breaking biosynthesis of a mukopeptid of a cell wall of a microorganism. It is steady against beta lactamelements of gram-positive and gram-negative bacteria.

Tsefotaksim possesses a broad spectrum of activity; in vitro is active concerning sleyoduyushchy microorganisms:

- gram-positive, such as Staphylococcus aureus (including the strains developing beta lactamazu), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta and hemolitic streptococci of group A), other Streptococcus spp., Borrelia burgdorferi, some Enterococcus spp. (Note: staphylococcus, resistant to Methicillinum/Oxacillinum, are steady against a tsefotaksim; concerning gram-positive cocci tsefotaksy is less active, than cephalosporins I and II of generations);

- gram-negative, such as Acinetobacter spp. (strains of Acinetobacter baumanii of a rezistentna), Citrobacter spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including ampitsillinorezistentny strains), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including the strains developing a penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Serratia spp., some strains of Pseudomonas aeruginosa;

- anaerobic such as Bacteroides spp., (majority of strains of Bacteroides fragilis of a rezistentna), Clostridium spp. (majority of strains of Clostridium difficile of a rezistentna), Fusobacterium spp. (including Fusobacterium hucleatum), Peptococcus spp., Peptostreptococcus spp.

Pharmacokinetics. After single intramuscular introduction of 500 mg and 1,0 g of a tsefotaksim the maximum concentration (Cmax) is reached within 30 min. and makes 11,7 mkg/ml and 20,5 mkg/ml respectively; after intravenous administration of 500 mg, 1,0 g and 2,0 g of Cmax it is reached in 5 min. and makes 38,9 mkg/ml, 101,7 mkg/ml and 214,4 mkg/ml respectively.

30-50% of a tsefotaksim contact blood proteins, are preferential with albumine. Therapeutic concentration is created in the majority of fabrics and liquids of an organism: in a myocardium, bones, a gall bladder, skin and soft tissues, in synovial, pericardiac, peritoneal, spinal and pleural liquids, and also in a phlegm, bile and urine.

Drug gets through a placental barrier, is emitted with breast milk. 20-36% of intravenously entered dose are excreted by kidneys in not changed look; 15-25% - in the form of the main metabolite of the dezatsetiltsefotaksim having antibacterial activity; 20-25% - in the form of two other inactive metabolites. Partially tsefotaksy it is removed with bile.

After intravenous administration of 1,0 g of drug each 6 hours within 14 days of cumulation it is not revealed.

The elimination half-life (T1/2) at adults makes 1-1,5 h, slightly changing depending on a way of introduction. At patients 80 years of T1/2 are more senior increases to 2,5 h. At patients with a renal failure of T1/2 does not exceed 2,5 h. At children about one year with body weight at the birth more than 1500 at single infusion of 50 mg/kg of T1/2 about 3,4 h, and with body weight equals at the birth less than 1500 - about 4,6 h.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to a tsefotaksim:
- respiratory infections, including pneumonia;
- infections of urinary tract and kidneys, including pyelonephritis;
- infections of an abdominal cavity, including peritonitis;
- sepsis;
- meningitis;
- endocarditis;
- infections of bodies of a small pelvis;
- infections of bones and joints;
- infections of skin and soft tissues, including wound and burn infections;
- gonorrhea;
- disease Laima (borreliosis). Prevention of development of an infection after surgeries.

Route of administration and doses:

Tsefotaksim enter intravenously (struyno, kapelno) or intramusculary.

Adults and children are more senior than 12 years (at the body weight of 50 kg and more). In table 1 the recommended doses, frequency and ways of introduction depending on infection type are specified.

Table 1. 

Infection type	Daily dose	Single dose, frequency and way of introduction
Moderately severe uncomplicated infections	2,0-6,0 g	1,0-2,0 g each 8-12 h intramusculary or intravenously
Infections of a heavy current	6,0-8,0 g	2,0 g each 6-8 h intravenously
Infections, life-threatening	To 12,0 g	2,0 g each 4-8 h intravenously
At uncomplicated gonorrhea	0,5-1,0 g	0,5 - 1,0 g once intramusculary

The maximum daily dose should not exceed 12,0 g.

Patients with a renal failure. At clearance of creatinine less than 20 ml/min. / 1,73 sq.m a daily dose are recommended to be reduced twice.

The patients who are on a hemodialysis. 1,0-2,0 g a day depending on weight of an infection. In day of dialysis the drug is administered a donkey of the procedure.

Children up to 12 years. Newborn, including premature children aged up to 1 week - 50 mg/kg of body weight each 12 h intravenously. At the age of 1 - 4 week - 50 mg/kg of body weight each 8 h intravenously. Children from 1 month to 12 years (with body weight less than 50 kg) 50-180 mg/kg/days of 4 or 6 times a day equal doses intramusculary (only for children 2,5 years are more senior) or intravenously; at the heavy course of an infection, including at meningitis, the daily dose is increased to 100-200 mg/kg/days.

At the body weight of 50,0 kg the dosage for adults is also more recommended (see Table 1).

Therapy duration. Is established individually depending on type of a microorganism, its chuvstviyotelnost to a tsefotaksim and the nature of a disease. After normalization of temperature or bacteriological confirmation of an eradikation of an infestant it is necessary to continue introduction of a tsefotaksim 2-3 more days; at the infections caused by a beta hemolitic streptococcus of group A, the drug is administered within not less than 10 days; for treatment of persistent infection several weeks can be required.

Prevention of an infection at surgical interventions. Before surgery of 1,0 g of drug enter intramusculary or intravenously to or during an introduction anesthesia; at Cesarean section of 1,0 g enter intravenously slowly (!) right after imposing of clips on an umbilical cord.
Further according to indications perhaps repeated introduction of 1,0 g of drug intramusculary or intravenously in 6-12 hours.

Intravenous administration. Struyno. Drug is dissolved in 10 ml of water for injections as it is specified in table 2; enter slowly for 3-5 min. Struyno the drug cannot be administered within less than 3 min.!

Kapelno. Drug dissolve 0,9% of solution of sodium chloride or 5% of solution of glucose (dextrose) in 50 - 100 ml as it is specified in table 2. Infusion duration - 50-60 min.

As solvent it is impossible to use hydrosodium carbonate solution for injections!

Intramuscular introduction. Solution is prepared as it is specified in table 2, using water for injections or 1% hydrochloride lidocaine solution; enter into rather large muscle, for example, an upper outside quadrant of a buttock.

At an intramuscular injection it is necessary to carry out aspiration to exclude hit of a needle in a vessel and not to allow administration of solution, especially lidocaine, in blood!

Preparation of solutions. Solvent volumes depending on a necessary dosage and a way of introduction, and also the received approximate concentration of drug are presented in table 2.

Table 2.

 

Dosage of drug and way of introduction	Volume of solvent (ml)	Final volume (ml)	Approximate concentration (mg/ml)
Intravenous administration (struyno)
500 mg	10	10,2	50
1,0 g	10	10,4	95
2,0 g	10	11,0	180
Intravenous introduction (kapelno)
1,0 g	50-100	50-100	20-10
2,0 g	50-100	50-100	40-20
Intramuscular introduction
500 mg	2	2,2	230
1,0 g	3	3,4	300
2,0 g	5	6,0	330

The received solution should not contain any foreign mechanical inclusions!

Features of use:

Pregnancy and lactation. Use in II and III trimesters of pregnancy is possible only if the estimated advantage for mother exceeds potential risk for a fruit. In the period of a lactation in case of administration of drug breastfeeding should be stopped as to tsefotaksy it is allocated with breast milk.

Before purpose of drug it is necessary to collect the allergological anamnesis, especially concerning a beta laktamnykh of antibiotics. At emergence of any allergic reaction administration of drug should be stopped.

At emergence of symptoms of pseudomembranous colitis drug is cancelled; at a medium-weight and heavy current of this complication appoint Vancomycinum or metronidazole.

At treatment by drug over 10 days regular control of a picture of peripheral blood is necessary.

Control of function of kidneys can be required by elderly patients. During treatment tsefotaksimy false positive test of urine on glucose (is possible when using not euzymatic ways of definition of glucose in urine).

Side effects:

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

From the central nervous system: headache, dizziness.

From an urinary system: renal failure, oliguria, intersticial nephrite.

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

From digestive tract: nausea, vomiting, diarrhea or locks, meteorism, abdominal pain, dysbacteriosis, abnormal liver function; seldom - stomatitis, a glossitis, pseudomembranous colitis.

From cardiovascular system: seldom - potentially life-threatening arrhythmias at bystry jet introduction through the central venous catheter.

Laboratory indicators: an azotemia, increase in concentration of urea in blood, increase in activity of "hepatic" transaminases and an alkaline phosphatase, a giperkreatininemiya, a hyperbilirubinemia, false positive test of Koombs.

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

Others: vaginal and oral candidiasis.

Interaction with other medicines:

Pharmaceutical it is incompatible with aminoglycosides in one syringe or a dropper. At simultaneous use of a tsefotaksim with aminoglycosides, polymyxin B or "loopback" diuretics the probability of damage of kidneys increases.

At a combination of a tsefotaksim to antiagregant (including with non-steroidal anti-inflammatory drugs) the risk of development of bleeding increases.

Probenetsid slows down removal of a tsefotaksim and increases its plasma concentration.

Contraindications:

Hypersensitivity to cephalosporins, penicillin, karbapenema; I trimester of pregnancy, lactation period; children's age up to 2,5 years (for intramuscular introduction).

With care. At a renal failure and a liver; at nonspecific ulcer colitis, including in the anamnesis; at heavy heart failure, disturbance of a cordial rhythm; at newborns (for intravenous administration).

Overdose:

Development of reversible encephalopathy in case of introduction of high doses, especially at patients with a renal failure is possible. Symptoms: spasms, tremor, neuromuscular excitement.

Treatment: symptomatic. There is no specific antidote.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 3 years (Taks-au-Bid), 3 years and 3 months (Solvent - water for injections). Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 1 g complete with solvent (water for injections) or without solvent/. On 1 g of a tsefotaksim in the bottle from colourless glass corked by a stopper from rubber, which is rolled up by an aluminum cap with a plastic lid; on 10 ml of water for injections in an ampoule from plastic (polyethylene) with the line of a break. On 1 bottle together with the application instruction in a cardboard pack. On 1 bottle and 1 ampoule together with the application instruction in a cardboard pack. On 50 bottles with the equal number of application instructions in a cardboard pack (for hospitals).