Цефурабол®

General characteristics. Structure:

Active ingredient: 0,25 g, 0,75 g or 1,5 g of a tsefuroksim of sodium salt (in terms of tsefuroksy).

Tsefalosporinovy antibiotic of the II generation for parenteral use.

Pharmacological properties:

Pharmacodynamics. The Tsefalosporinovy antibiotic of the II generation for parenteral use. Works bakteritsidno (breaks synthesis of a cell wall of a bacterium). Possesses a wide range of antimicrobic action. It is highly active in the relation:
- gram-positive microorganisms, including the strains steady against penicillin (except for strains, resistant to Methicillinum): Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, etc. beta and hemolitic streptococci, Streptococcus pneumoniae, Streptococcus of group In (Streptococcus agalactiae), Streptococcus mitis (viridans group);

- gram-negative microorganisms: Bordetella pertussis, Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Hamophilus influenzae, including strains, resistant to ampicillin, Haemophilus parainfluenzae, including strains, resistant to ampicillin, Moraxella catarrhalis, Neisseria gonorrhoeae, including the strains which are producing and not producing a penicillinase, Neisseria meningitidis, Salmonella spp., Bacteroides spp., Fusobacterium spp., Propionibacterium spp., Borrelia burgdorferi;

- gram-positive and gram-negative anaerobe bacterias, including Clostridium spp., Peptococcus spp., Peptostreptococcus spp.

To a tsefuroksim are insensitive: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, Staphylococcus aureus strains, steady against Methicillinum, strains of Staphylococcus epidermidis, Legionella spp, steady against Methicillinum., Streptococcus (Enterococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.

Pharmaklkinetika. After intramuscular introduction of 750 mg (in oil) the maximum concentration _(Cmax) is reached in 15-60 min. and makes 27 mkg/ml. At intravenous (in) introduction of 750 mg and 1,5 g _{of Cmax} in 15 min. makes 50 and 100 mkg/ml respectively. Therapeutic concentration remains 5,3 and 8 h respectively.
 

Elimination half-life (Т½) at in/in and introduction of 1,3-1,5 h in oil, newborn children have 2-2,5 h. Communication with proteins of plasma - 33-50%.
In an organism it is not metabolized.

It is removed by kidneys by glomerular filtering and canalicular secretion of 85-90% of a dose in not changed look during 8 h (the most part of drug would be removed during the first h, creating at the same time high concentration in urine); in 24 h it is removed completely (50% - by canalicular secretion, 50% - by glomerular filtering).

Therapeutic concentration are registered in pleural liquid, bile, a phlegm, a myocardium, skin and soft tissues. The concentration of a tsefuroksim exceeding MPK for the majority of microorganisms can be reached in a bone tissue, synovial and intraocular liquids. At meningitis gets through GEB. Passes through a placenta, in small concentration gets into breast milk.

Indications to use:

The bacterial infections caused by microorganisms, sensitive to a tsefuroksim: infectious diseases of respiratory tracts (bronchitis, pneumonia, abscess of lungs, a pleura empyema, etc.), ENT organs (sinusitis, tonsillitis, pharyngitis, otitis, etc.), urinary tract (pyelonephritis, cystitis, a symptomatic bacteriuria, gonorrhea, etc.), skin and soft tissues (an ugly face, a pyoderma, impetigo, a furunculosis, cellulitis, a wound fever, эризипелоид, etc.), bones and joints (osteomyelitis, septic arthritis, etc.), bodies of a small pelvis (in obstetrics and gynecology), a septicaemia, meningitis, a disease Laima (borreliosis), prevention of infectious complications at operations on bodies of a thorax, abdominal cavity, a basin, joints, (including at lung, heart, gullet operations, in vascular surgery at a high risk of infectious complications, at orthopedic operations).

Route of administration and doses:

In/in and in oil the adult appoint 750 mg 3 times a day; at infections of a heavy current - the dose is increased up to 1500 mg by 3-4 times a day (if necessary the interval between introductions can be reduced to 6 h). An average daily dose - 3-6 g.

To children appoint on 30-100 mg/kg/days in 3-4 receptions. At the majority of infections the optimum dose makes 60 mg/kg/days. To newborns and children up to 3 months appoint 30 mg/kg/days in 2-3 receptions.

At gonorrhea - 1500 mg in oil once (or in the form of 2 injections on 750 mg with introduction to different areas, for example, in both gluteuses).
At bacterial meningitis - on 3 g in/in each 8 h; to children of younger and advanced age - 150-250 mg/kg/days in 3-4 receptions, the newborn - on 100 mg/kg/days.

At pneumonia - on 1500 mg in oil or by 2-3 times a day during 48-72 h, then pass to intake, 500 mg 2 times a day within 7-10 days.
At an exacerbation of chronic bronchitis appoint 750 mg in oil or by 2-3 times a day during 48-72 h, then pass to intake, 500 mg 2 times a day within 5-10 days.

For a perioperatsionny antibiotikoprofilaktika at an abdominal cavity operations, bodies of a basin and at orthopedic operations - 1500 mg in/in at anesthesia induction, then in addition - on 750 mg in oil in 8 and 16 h after operation.

At heart, lungs, gullet operations and vessels - 1500 mg in/in at anesthesia induction, then - on 750 mg in oil 3 times a day during the subsequent 24-48 h.

At full replacement of a joint - 1500 mg of powder mix polymer, in a dry form with each package, marked - methacrylate cement before addition of liquid monomer.

At HPN correction of the mode of dosing is necessary: at the clearance of creatinine (CC) of 10-20 ml/min. appoint in/in or 2 times, in oil on 750 mg, a day, at KK less than 10 ml/min. - on 750 mg of 1 times a day.

To the patients who are on a continuous hemodialysis with use of the arteriovenous shunt or haemo filtering of high speed in intensive care units appoint 750 mg 2 times a day; for the patients who are on haemo filtering of low speed appoint the doses recommended at a renal failure.

Preparation of solution for injections.
Solution for injections in oil:
To add 1 ml of water for injections to 250 mg of Tsefurabol or 3 ml of water for injections to 750 mg of Tsefurabol. To stir up carefully before formation of suspension.

Solution for in/in introductions:
To dissolve:
- 250 mg of Tsefurabol in 2 or more ml of water for injections,
- 750 mg of Tsefurabol in 6 or more ml of water for injections,
- 1,5 g of Tsefurabol in 15 or more ml of water for injections.

For short-term in/in infusions (up to 30 min.) 1,5 g of drug dissolve in 50 ml of water for injections. These solutions can be entered directly into a vein or into a tube of infusional system.

When mixing solution of Tsefurabol (1,5 g in 15 ml of water for injections) and metronidazole (50 mg / 100 ml) both components keep the activity to 24 h at a temperature of 4 °C or to 6 h at a temperature below 25 °C.

Tsefurabol's solution (5 mg/ml) in 5% or 10% solution of a ksilitol can be stored to 24 h at a temperature below 25 °C.

Tsefurabol is compatible to the aqueous solutions containing up to 1% of lidocaine of a hydrochloride.

Tsefurabol is compatible to the most widely applied liquids for in/in introductions. Drug is stable to 24 h at the room temperature when mixing with the following solutions:
- 0,9% chloride sodium solution;
- 5% dextrose solution;
- Ringer's solution;
- Hartman's solution.

Tsefurabol remains stable in 0,9% solution of sodium chloride and in 5% dextrose solution in the presence of a phosphate sodium hydrocortisone.

Tsefurabol is compatible to the following solutions during 24 h at the room temperature:
- heparin (10 pieces/ml and 50 pieces/ml) in 0,9% sodium chloride solution;
- potassium chloride (10 ¼Ø¬/l and 40 ¼Ø¬/l) in 0,9% sodium chloride solution.
Tsefurabol it is not necessary to mix in one syringe with antibiotics from group of aminoglycosides.

Solution of sodium bicarbonate of 2,74% has an indicator рН, Tsefurabola significantly influencing color of solution therefore it is not recommended to use for cultivation. However if to the patient enter sodium bicarbonate solution, then in need of it it is possible to enter directly into a tube of infusional system.

Features of use:

The patients who had allergic reactions to penicillin in the anamnesis can have hypersensitivity to tsefalosporinovy antibiotics. In the course of treatment control of function of kidneys, especially at the patients receiving drug in high doses is necessary. Treatment is continued during 48-72 h after disappearance of symptoms; in case of the infections caused by Streptococcus pyogenes, a course of treatment - not less than 7-10 days.

During treatment false positive forward reaction of Koombs and false positive reaction of urine to glucose is possible. At the patients receiving Tsefurabol when determining concentration of glucose in blood recommend to use tests with glucose oxydas or a hexokinase.

Upon transition from parenteral administration to intake it is necessary to consider weight of an infection, sensitivity of microorganisms and the general condition of the patient. If in 72 h after reception of a tsefuroksim improvement inside is not noted, it is necessary to continue parenteral administration.

Freshly cooked solution of drug is good for use during 24 h at a temperature not above 25 °C, during 96 h at storage in the refrigerator.

Side effects:

Allergic reactions: a fever, rash, an itch, urticaria, it is rare - a multiformny exudative erythema (including Stephen-Johnson's syndrome), a bronchospasm, a malignant exudative erythema, an acute anaphylaxis.

From the alimentary system: diarrhea or a lock, nausea, vomiting, a meteorism, spasms and an abdominal pain, ulcerations of a mucous membrane of an oral cavity, oral cavity candidiasis, a glossitis, pseudomembranous colitis, an abnormal liver function (increase in activity of "hepatic" enzymes in plasma - aspartate aminotransferases, alaninaminotranspherases, an alkaline phosphatase, a lactate dehydrogenase, concentration of bilirubin), a cholestasia.

From urinogenital system: renal failures (decrease in clearance of creatinine, increase in content of creatinine and residual nitrogen of urea in blood), a dysuria, an itch in crotches and a vaginitis.

From bodies of a hemopoiesis: decrease in a hematocrit and hemoglobin, anemia (aplastic or hemolitic), eosinophilia, neutropenia, leukopenia, agranulocytosis, thrombocytopenia, prothrombinopenia, lengthening of a prothrombin time.

Local reactions: irritation, infiltrate and pain in an injection site, phlebitis.

From TsNS: spasms.

From sense bodys: decrease in hearing.

Interaction with other medicines:

Simultaneous peroral purpose of "loopback" diuretics slows down canalicular secretion, reduces renal clearance, increases concentration in plasma and Tsefurabola increases Т½.

At simultaneous use with aminoglycosides and diuretics the risk of emergence of nephrotoxic effects increases.

Pharmaceutical we will combine with metronidazole, azlotsilliny, xylitol, with the aqueous solutions containing to 1% of lidocaine of a hydrochloride, 0,9% solution of sodium of chloride, 5% and 10% solution of a dextrose, 0,18% solution of sodium of chloride and 4% solution of a dextrose, 5% solution of a dextrose and 0,9% chloride sodium solution, Ringer's solution, Hartman's solution, lactate sodium solution, heparin (10 pieces/ml and 50 pieces/ml) in 0,9% chloride sodium solution.
In solutions pharmaceutical it is incompatible with aminoglycosides, solution of Natrii hydrocarbonas of 2,74%.

Contraindications:

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

With care drug is used at newborn and premature; during pregnancy and in the period of a lactation; at the weakened and exhausted patients; at the chronic renal failure (CRF), diseases of a large intestine (including nonspecific ulcer colitis in the anamnesis).

Overdose:

Symptoms: excitement of TsNS, spasm.

Treatment: purpose of antiepileptic medicines, control and maintenance of the vital functions of an organism, hemodialysis and peritoneal dialysis.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

On 0,25 g, 0,75 g of active agent in bottles with a capacity of 10 ml, and on 1,5 g of active agent in a bottle with a capacity of 20 ml.

On 1 or 5 bottles in a cardboard pack together with the instruction on a medical use.

On 1 or 5 bottles in a blister strip packaging complete with solvent (water for injections). Each planimetric packaging is placed in a cardboard pack together with the instruction on a medical use.

On 1 bottle complete with solvent in a pack cardboard without planimetric packaging. Put one application instruction in a pack.

On 50 bottles place in a box with 1-5 application instructions (for hospitals).