Tsefuroksim Kabi

General characteristics. Structure:

Active ingredient: 750 mg or 1500 mg of a tsefuroksim in the form of a tsefuroksim of sodium.

Pharmacological properties:

Pharmacodynamics. The Tsefalosporinovy antibiotic of the II generation for oral and parenteral administration. Works bakteritsidno (breaks synthesis of a cell wall of bacteria). Possesses a wide range of antimicrobic action.

It is highly active concerning gram-positive microorganisms, including the strains steady against penicillin (except for strains, resistant to Methicillinum): Staphylococcus aureus, Streptococcus pyogenes (and others beta and hemolitic streptococci), Streptococcus pneumoniae, Streptococcus of group In (Streptococcus agalactiae), Streptococcus mitis (viridans group), most Clostridium spp.; gram-negative microorganisms: Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Proteus rettgeri, Haemophilus 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., Borrelia burgdorferi; gram-positive and gram-negative anaerobe bacterias: Peptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Propionibacterium spp.
 
To a tsefuroksim are insensitive: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, strains of Staphylococcus aureus, Staphylococcus epidermidis, Legionella spp, steady against Methicillinum., Streptococcus (Enterococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.

Pharmacokinetics. After introduction in oil 750 mg of Cmax are reached in 15-60 min. and makes about 27 mkg/ml. At in introduction of 750 mg and 1.5 g of Cmax it is reached in 15 min., averages 50 and 100 mkg/ml respectively. Therapeutic concentration remains 5.3 and 8 h respectively. Linkng with proteins of plasma - 33-50%.
 
Therapeutic concentration are created in pleural liquid, bile, a phlegm, a myocardium, skin and soft tissues. The concentration of a tsefuroksim exceeding the minimum overwhelming concentration (MOC) for the majority of microorganisms can be reached in a bone tissue, synovial and intraocular liquids. At meningitis gets through a blood-brain barrier (GEB). Passes through a placenta and gets into breast milk.
 
T1/2 at in oil and in introduction - 1.3-1.5 h, at newborn children is 2-2.5 h. It is not metabolized in a liver.
 
It is removed by kidneys by glomerular filtering and canalicular secretion of 85-90% in not changed look during 8 h (the most part of drug is removed during the first 6 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).

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to a tsefuroksim:

— respiratory tracts (bronchitis, pneumonia, lung abscess, pleura empyema);

— ENT organs (sinusitis, tonsillitis, pharyngitis, otitis);

— urinary tract (pyelonephritis, cystitis, asymptomatic bacteriuria);
 
— skin and soft tissues (ugly face, pyoderma, impetigo, furunculosis, phlegmon, wound fever, эризипелоид);
 
— bones and joints (osteomyelitis, septic arthritis);
 
— bodies of a small pelvis (endometritis, adnexitis, cervicitis);
 
— sepsis;
 
— meningitis;
 
— gonorrhea;
 
— 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 or in oil. The adult appoint 750 mg of 3 times/days; at infections of a heavy current - the dose is increased to 1500 mg of 3-4 times/days. An average daily dose - 3-6 g.

At gonorrhea - intramusculary 1500 mg once (only in the form of 2 injections on 750 mg with introduction to different areas, for example in both gluteuses).

At bacterial meningitis - in/in on 3 g each 8 h.

At an infection of bones and joints - on 1500 mg each 8 h.

At an abdominal cavity operations, bodies of a small pelvis and at orthopedic operations - in/in 1500 mg at anesthesia induction, then in addition - 750 mg in oil, in 8 and 16 h after operation.
 
At heart, lungs, gullet operations and vessels - in/in 1500 mg at anesthesia induction, then - 3 times/days, in oil on 750 mg, during the subsequent 24-48 h.
 
At pneumonia in/in or 2-3 times/days, in oil on 1500 mg, during 48-72 h, then pass to reception of a tsefuroksim in the dosage forms intended for intake in the corresponding dosages.
 
At an exacerbation of chronic bronchitis appoint in/in or 2-3 times/days, in oil on 750 mg, during 48-72 h, then pass to reception of a tsefuroksim in the dosage forms intended for intake in the corresponding dosages.
 
At the chronic renal failure (CRF) correction of the mode of dosing is necessary: at the clearance of creatinine (CC) more than 20 ml/min. are appointed in/in or each 8 h, in oil on 750-1500 mg, at KK of 10-20 ml/min. appoint in/in or each 12 h, in oil on 750 mg, at KK less than 10 ml/min. - on 750 mg each 24 h.
 
To the patients who are on a continuous hemodialysis with use of the arteriovenous shunt or on haemo filtering of high speed in intensive care units appoint 750 mg of 2 times/days; for the patients who are on haemo filtering of low speed appoint the doses recommended at a renal failure.

Use for children. To newborns and children up to 3 months appoint 30 mg/kg/days in 2-3 introductions; at bacterial meningitis - 100 mg/kg/days.
 
To children 3 months are more senior appoint on 30-100 mg/kg/days in 3-4 introductions. At the majority of infections the optimum dose makes 60 mg/kg/days. At heavy and zhiznennougrozhayushchy infections doses of 100 mg/kg/days can be used (but not exceeding a dose at adults). In case of bacterial meningitis the high doses of 200 - 240 mg/kg/days in/in divided into equal doses which are entered each 6-8 h are used.
 
At an infection of bones and joints - 150 mg/kg/days divided into equal doses which are entered each 8 h.
 
At a renal failure frequency rate of introduction has to correspond to frequency rate of use of drug for adults with the accompanying renal failure.
 
Rules of preparation of solution. For introduction in oil 750 mg dissolve in 3 ml of water for injections, carefully stirring up before receiving suspension.
 
For in/in introductions: 750 mg dissolve in 6 ml of water for injections, 1500 mg dissolve in 15 ml of water for injections.

Features of use:

Use at pregnancy and feeding by a breast. At pregnancy drug is used only if the estimated advantage for mother exceeds potential risk for a fruit, at use of drug in the period of a lactation feeding by a breast should be stopped.

Use at renal failures. At the chronic renal failure (CRF) correction of the mode of dosing is necessary: at the clearance of creatinine (CC) more than 20 ml/min. are appointed in/in or each 8 h, in oil on 750-1500 mg, at KK of 10-20 ml/min. appoint in/in or each 12 h, in oil on 750 mg, at KK less than 10 ml/min. - on 750 mg each 24 h.
 
To the patients who are on a continuous hemodialysis with use of the arteriovenous shunt or on haemo filtering of high speed in intensive care units appoint 750 mg of 2 times/days; for the patients who are on haemo filtering of low speed appoint the doses recommended at a renal failure.

Use for children. To newborns and children up to 3 months appoint 30 mg/kg/days in 2-3 introductions; at bacterial meningitis - 100 mg/kg/days.
 
To children 3 months are more senior appoint on 30-100 mg/kg/days in 3-4 introductions. At the majority of infections the optimum dose makes 60 mg/kg/days. At heavy and zhiznennougrozhayushchy infections doses of 100 mg/kg/days can be used (but not exceeding a dose at adults). In case of bacterial meningitis the high doses of 200 - 240 mg/kg/days in/in divided into equal doses which are entered each 6-8 h are used.
 
At an infection of bones and joints - 150 mg/kg/days divided into equal doses which are entered each 8 h.
 
At a renal failure frequency rate of introduction has to correspond to frequency rate of use of drug for adults with the accompanying renal failure.

Special instructions. 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 direct test of Koombs and false positive reaction of urine to glucose is possible.
 
At the patients receiving tsefuroksy when determining concentration of glucose in blood recommend to use tests with glucose oxydas or a hexokinase. П
 
ри transition from parenteral administration to reception of a tsefuroksim in dosage forms for intake it is necessary to consider weight 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 perenteralny introduction.
 
Influence on ability to driving of motor transport and to control of mechanisms. To patients, the accepting tsefuroksy, it is necessary to be careful during the driving of the car and occupations other potentially dangerous types of activity requiring special attention and speed of psychomotor reactions in view of a possibility of side effects from the central nervous system.

Side effects:

Allergic reactions: fever, rash, itch, urticaria, multiformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrolysis, bronchospasm, intersticial nephrite, Quincke's disease, acute anaphylaxis.
 
From a reproductive system: an itch in crotches, a vaginitis.
 
From an urinary system: a renal failure, a dysuria, increase in concentration of creatinine and an urea nitrogen in plasma, decrease in clearance of creatinine.
 
From TsNS: spasms.
 
From the alimentary system: diarrhea, nausea, vomiting, spasms and abdominal pain, ulcerations of a mucous membrane of an oral cavity, oral cavity candidiasis, pseudomembranous colitis.
 
From sense bodys: decrease in hearing.
 
From bodies of a hemopoiesis: decrease in hemoglobin and hematocrit, eosinophilia, tranzitorny neutropenia, leukopenia, hemolitic anemia.

Laboratory indicators: increase in activity of liver enzymes, including ShchF, LDG, hyperbilirubinemia, decrease in triglycerides, false positive test of Koombs.
 
Local reactions: irritation, infiltrate and pain in an injection site, phlebitis.

Interaction with other medicines:

Simultaneous peroral purpose of "loopback" diuretics slows down canalicular secretion, reduces renal clearance, increases concentration in plasma and increases an elimination half-life of a tsefuroksim. At simultaneous use with aminoglycosides and diuretics the risk of emergence of nephrotoxic effects increases.
 
Pharmaceutical we will combine 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.
 
Pharmaceutical it is incompatible with aminoglycosides, solution of Natrii hydrocarbonas of 2.74%.

Contraindications:

Hypersensitivity (including to other cephalosporins, penicillin and karbapenema).
 
With care. The newborn, prematurity, a chronic renal failure, bleedings and diseases of digestive tract (including in the anamnesis, ulcer colitis) weakened and the exhausted patients.

Overdose:

Symptoms: spasms.
 
Treatment: purpose of anticonvulsant drugs, control and maintenance of the vital functions of an organism, hemodialysis and peritoneal dialysis.

Storage conditions:

At a temperature not above 25 °C in the place protected from light to Store in the place, unavailable to children. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

750 mg - bottles glass with a capacity of 15 ml (1) - packs cardboard.
750 mg - bottles glass with a capacity of 15 ml (10) - packs cardboard.
1500 mg - bottles glass with a capacity of 15 ml (1) - packs cardboard.
1500 mg - bottles glass with a capacity of 15 ml (10) - packs cardboard.