Нацеф®

General characteristics. Structure:

Deystvuyushche substance: 05, or 1,0 g of cefazolin of sodium (in terms of cefazolin).

Tsefalosporinovy antibiotic of the I generation for parenteral use.

Pharmacological properties:

Pharmacodynamics. The Tsefalosporinovy antibiotic of the I generation for parenteral use. Works bakteritsidno, breaking synthesis of a cell wall of microorganisms. Has a broad spectrum of activity, it is active concerning gram-positive (Staphylococcus spp., Staphylococcus aureus (which are not producing and producing a penicillinase; including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis) and gram-negative (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) microorganisms. It is active concerning Haemophilus influenzae, some strains of Enterobacter and Enterococcus.

It is not effective concerning Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., anaerobic microorganisms, metitsillinrezistentny strains of Staphylococcus spp.

Pharmacokinetics. Time of achievement of the maximum concentration (_TCmax at intramuscular introduction (in oil) in a dose of 500 and 1000 mg, respectively-2 and 1 h. The maximum concentration _(Cmax) - 38 and 64 mkg/ml; after _TCmax, intravenous (in/in) introductions, - at the end of infusion, later in/in introductions of 1000 mg _{of Cmax} - 180 mkg/ml.

Gets into joints, fabrics of cardiovascular system, into an abdominal cavity, kidneys and urinary tract, a placenta, a middle ear, airways, skin and soft tissues. In small amounts it is allocated with breast milk. Concentration in tissue of a gall bladder and bile is much higher, than in blood serum. At obstruction of a gall bladder concentration in bile is less, than in plasma. Distribution volume - 0,12 l/kg. Communication with proteins of plasma of 85%. An elimination half-life (Т½) at introduction in oil - 1,8 h, at in introduction of 2 h. At a renal failure of ƽ-20-40 h.

It is removed preferential by kidneys in not changed look: during the first 6 h - 60-90%, in 24 h - 70-95%. _Cmax in urine of 1000 mkg/ml and 4000 mkg/ml after introduction in oil and doses of 500 mg and 1000 mg respectively.

Indications to use:

Bacterial infections of upper and lower respiratory tracts, urinary and biliary tract, bodies of a small pelvis, skin and soft tissues, bones and joints; endocarditis, sepsis, peritonitis, average otitis, osteomyelitis, mastitis; wound, burn and postoperative fevers; other diseases caused by microorganisms, sensitive to cefazolin. Prevention of surgical infections in before - and the postoperative period.

Route of administration and doses:

Intramusculary, intravenously (struyno and kapelno). An average daily dose for adults - 1 g; frequency rate of introduction - 2 times a day. The maximum daily dose - 6 g (in rare instances - 12 g); frequency rate of introduction can be increased to 3-4 times a day.

The average duration of treatment makes 7-10 days. For prevention of a postoperative infection of 1 g - in 30 min. prior to operation, 0,5-1 g - during operation and on 0,5-1 g each 6-8 h within a day after operation.

Patients with renal failures need change of the mode of dosing according to values of the clearance of creatinine (CC). At KK of 55 ml/min. and more or at the content of creatinine in plasma of 1,5 mg of % and less, it is possible to enter a full dose. At KK of 54-35 ml/min. or at the content of creatinine in plasma of 3-1,6 mg of % - it is possible a full dose, but to increase intervals between injections to 8 h. At KK of 34-11 ml/min. or the content of creatinine in plasma of 4,5-3,1 mg of % - 1/2 bucketed doses of 12 h. The patient with KK of 10 ml/min. and less, or at the content of creatinine in plasma of 4,6 mg of % and more - 1/2 average doses each 18-24 h. All recommended doses enter after an initial shock dose.

Average daily dose for children - 20-50 mg/kg; at the heavy course of an infection the dose can be increased to 100 mg/kg/days. Frequency rate of introduction-3-4 times a day. At children with renal failures correction of the mode of dosing is made depending on KK values. At KK of 70-40 ml/min. - 60% of an average daily dose also enter in 12 h. At KK of 40-20 ml/min. - 25% of an average daily dose with an interval of 12 h. To children with KK of 5-20 ml/min. - 10% of an average daily dose each 24 h. All recommended doses enter after an initial shock dose.

Preparation of solutions:
For intramuscular introduction drug is dissolved in 4-5 ml of water for injections, isotonic solution of sodium chloride or 0,25-0,5% novocaine solution.

For intravenous drop administration drug is dissolved in 100-250 ml of isotonic solution of sodium of chloride or 5% glucose solution; the injection is carried out within 20-30 minutes (rate of administering of 60-80 drops in a minute).

For intravenous jet administration the single dose of drug is parted in 10 ml of isotonic solution of sodium of chloride and entered slowly within 3-5 min.

During cultivation bottles vigorously stir up before full dissolution.

Features of use:

The patients who had allergic reactions to penicillin in the anamnesis of a karbapenema can have hypersensitivity to tsefalosporinovy antibiotics.

During treatment by cefazolin receiving positive direct and indirect tests of Koombs, and also false positive reaction of urine to sugar is possible.
At purpose of drug the exacerbation of gastrointestinal diseases, especially colitis is possible.

Safety of use for premature children and children of the first year of life is not established.

Side effects:

Allergic reactions: hyperthermia, skin rash, small tortoiseshell, skin itch, bronchospasm, eosinophilia, Quincke's edema, arthralgia, acute anaphylaxis, multiformny erythema, malignant exudative erythema (Stephens-Johnson's syndrome).

From a nervous system: spasms.

From an urinary system: at patients with diseases of kidneys at treatment by high doses (6 g) - a renal failure (in these cases the dose is reduced and treatment is carried out under control of dynamics of maintenance of an urea nitrogen and creatinine to blood).

From the alimentary system: nausea, vomiting, diarrhea, an abdominal pain, a pseudomembranous coloenteritis, it is rare - cholestatic jaundice, hepatitis.

From bodies of a hemopoiesis: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolitic anemia.
At prolonged treatment - dysbacteriosis, the superinfection caused by antibiotic-resistant strains, a candidiasis (including candidosis stomatitis).

Laboratory indicators: positive reaction of Koombs, increase in activity of "hepatic" transaminases, giperkreatininemiya, increase in a prothrombin time.

Local reactions: at introduction in oil - morbidity (in an injection site), at in introduction - phlebitis.

Interaction with other medicines:

The concomitant use with anticoagulants and diuretics is not recommended. At simultaneous use of cefazolin and "loopback diuretics" there is a blockade of its canalicular secretion.

Aminoglycosides increase risk of development of damage of kidneys. In solution pharmaceutical it is incompatible with aminoglycosides (a mutual inactivation).

The drugs blocking canalicular secretion increase concentration in blood, slow down removal and increase risk of development of toxic reactions.

Contraindications:

Hypersensitivity to drugs of group of cephalosporins and another beta лактамным to antibiotics.

Do not appoint the newborn (up to 1 month).

To pregnant women appoint only according to strict indications, carry out treatment under observation of the doctor. In need of use of drug for the feeding women breastfeeding is stopped.

With care appoint at a renal/liver failure.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C.
To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

0,5 g and 1,0 g of active agent in bottles glass with a capacity of 10 ml.
Solvent – "Water for injections" in glass ampoules of 5 ml.

1 bottle with drug and the application instruction is placed in a pack from a cardboard.

1 bottle with drug and 1 ampoule with solvent is packed into a blister strip packaging. One blister strip packaging and the application instruction are put in a pack cardboard.

5 bottles with drug pack into blister strip packagings. One blister strip packaging and the application instruction are put in a pack cardboard.

5 bottles with drug complete with 5 ampoules of solvent pack into blister strip packagings. One blister strip packaging with drug, one blister strip packaging with solvent and the application instruction is put in a pack cardboard.