Tsefroksim J.

General characteristics. Structure:

Active ingredient: 750 mg or 1500 mg of a tsefuroksim in 1 bottle.

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 (etc. 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., including Providencia 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, Bordetella pertussis.

Gram-positive (Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp.) and gram-negative anaerobe bacterias (Fusobacterium 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., Enterococcus faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.

Pharmacokinetics. After intramuscular introduction of 750 mg (in oil) the maximum concentration (Cmax) is reached in 15-60 min., at intravenous (in/in) - in 15 min. Therapeutic concentration remains about 5 and 8 h respectively.
Communication with proteins of plasma - 33-50%. 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). T1/2 at in/in and introduction in oil – on average 1.5 h, at newborn children is 2-2,5 h.

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 for the majority of microorganisms are reached in a bone tissue, synovial and intraocular liquids. At meningitis gets through a blood-brain barrier. Passes through a placenta and gets into breast milk.

Indications to use:

The bacterial infections caused by sensitive microorganisms:
- respiratory tracts (bronchitis, pneumonia, abscess of lungs, pleura empyema, etc.),
- ENT organs (including sinusitis, tonsillitis, pharyngitis, otitis),
- urinary tract (including pyelonephritis, cystitis, asymptomatic bacteriuria, gonorrhea),
- skin and soft tissues (ugly face, pyoderma, impetigo, furunculosis, phlegmon, wound fever, эризипелоид, etc.),
- bones and joints (osteomyelitis, septic arthritis, etc.),
- bodies of a small pelvis (endometritis, adnexitis, cervicitis),
- sepsis, meningitis, disease Laima (borreliosis),
- prevention of infectious complications at operations on bodies of a thorax, abdominal cavity, small pelvis, 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 oil, in / century. In/in and in oil the adult each 8 h appoint 750 mg; at infections of a heavy current - the dose is increased to 1500 mg by each 6-8 h. An average daily dose - 3-6 g. An average course of treatment – 5-10 days.

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 - in/in on 3 g each 8 h.

At an infection of bones and joints – 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, in oil on 750 mg, a day during the subsequent 24-48 h.

At pneumonia - in oil or in/in on 1500 mg 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 in oil or in/in on 750 mg 2-3 times a day during 48-72 h, then pass to intake, 500 mg 2 times a day within 5-10 days.

At a chronic renal failure correction of the mode of dosing is necessary: at KK more than 20 ml/min. - are appointed in/in or each 8 h, in oil on 750-1500 mg, 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 2 times a day at the end of a hemodialysis session; for the patients who are on haemo filtering of low speed appoint the doses recommended at a renal failure.

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. At heavy and zhizneugrozhayushchy 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. To newborns and children up to 3 months appoint 30 mg/kg/days in 2-3 receptions; at bacterial meningitis - 100мг/кг/сут.

Features of use:

Pregnancy and lactation. In need of use of drug during pregnancy it is necessary to correlate advantage for mother and risk for a fruit as data at the person on development of embriotoksichesky or teratogenic effects of a tsefuroksim are absent. Tsefuroksim is allocated with breast milk therefore nursing mothers should show care at appointment it, correlating advantage for mother and risk for the baby.

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.

Solution, ready to the use, can be stored at the room temperature during 7 h, in the refrigerator - during 48 h. Use of the solution which turned yellow for storage time is allowed.

At the patients receiving tsefuroksy 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. Tsefroksim contains sodium that should be considered at purpose of drug to the patients who are on a diet with the lowered content of sodium. After cultivation solutions of drug can be stored at the room temperature during 24 h, in the refrigerator during 48 h (at a temperature of 5 ºС). Use of the solution which turned yellow for storage time is allowed.

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 urinogenital system: an itch in crotches, a vaginitis.

From the central nervous system: spasms.

From an urinary system: increase in creatinine and an urea nitrogen in plasma, decrease in clearance of creatinine.

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.

Laboratory indicators: increase in activity of "hepatic" enzymes, including alkaline phosphatase, lactate dehydrogenase, hyperbilirubinemia, false positive test of Koombs.

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

Interaction with other medicines:

Simultaneous oral administration of "loopback" diuretics slows down canalicular secretion, reduces renal clearance, increases concentration in plasma and increases T1/2 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 neonatality period, prematurity, a chronic renal failure, bleedings and diseases of digestive tract (including in the anamnesis, ulcer colitis) weakened and the exhausted patients, pregnancy, the lactation period.

Overdose:

Symptoms: excitement of the central nervous system, spasm.

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

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. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 750 mg, 1500 mg. On 750 mg and 1500 mg of active ingredient in the bottle of transparent glass corked by a stopper from the chlorbutyl rubber which is pressed out by an aluminum ring; on 1 bottle together with the application instruction in a cardboard pack. On 10, 25, 48 or 100 bottles with the equal number of instructions on a medical use in a cardboard box (for hospitals).