Tsefurus

General characteristics. Structure:

Active agent: tsefuroksy sodium (in terms of tsefuroksy) - 0,75 g or 1,5 g.

Pharmacological properties:

Tsefuroksim treats tsefalosporinovy antibiotics of the II generation for parenteral administration. Tsefuroksim is active concerning a wide range of activators, including the strains producing β-lactamelements. Bactericidal action of a tsefuroksim is connected with suppression of synthesis of a cell wall of bacteria.

Tsefuroksim is active in vitro concerning aerobic gram-positive microorganisms: Staphylococcus aureus, Staphylococcus epidermidis (including the strains steady against penicillin and except for strains, resistant to Methicillinum), Streptococcus pneumoniae, Streptococcus pyogenes (and other β-hemolitic streptococci), Streptococcus of group In (Streptococcus agalactiae), Streptococcus mitis (viridans group); aerobic gram-negative microorganisms: Haemophilus influenzae (including ampicillin - resistant strains), Haemophilus parainfluenzae (including ampicillin - resistant strains), Moraxella catarrhalis, Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp. (including Providencia rettgeri), Neisseria gonorrhoeae (including the strains producing a penicillinase and not producing a penicillinase), Neisseria meningitidis, Salmonella spp., Bordetella pertussis; anaerobic microorganisms: gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp.), Clostridium spp., Bacteroides spp. (except Bacteroides fragilis), Fusobacterium spp., Propionibacterium spp.; other microorganisms: Borrelia burgdorferi.

The following microorganisms are steady against a tsefuroksim: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, Methicillinum - resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Enterococcus faecalis; Legionella spp., Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.

 

Pharmacokinetics. Absorption

After administration of drug in oil in a dose of 750 mg of Cmax it is reached in 15-60 min. and makes 27 mkg/ml. At in administration of drug in doses of 750 mg and 1.5 g of Cmax it is reached in 15 min. and makes 50 mkg/ml and 100 mkg/ml respectively. Therapeutic concentration in blood remains 5.3 and 8 h respectively.

Distribution and metabolism

It is not metabolized in a liver.

Linkng with proteins of plasma - 33-50%. Therapeutic concentration are reached 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 widespread microorganisms can be reached in a bone tissue, synovial fluid and intraocular liquid. At meningitis gets through GEB. Passes through a placental barrier and it is allocated with breast milk.

Removal

T1/2 at in/in and introduction in oil - 1.3-1.5 h, at newborn children is 2-2.5 h.

85-90% are removed by glomerular filtering and canalicular secretion 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 bacterial infections caused by sensitive microorganisms:

— respiratory infections (bronchitis, pneumonia, abscess of lungs, pleura empyema);

— infections of ENT organs (sinusitis, tonsillitis, pharyngitis);

— infections of urinary tract (pyelonephritis, cystitis, symptomatic bacteriuria);

— gonorrhea;

— infections of skin and soft tissues (ugly face, pyoderma, impetigo, furunculosis, cellulitis, wound fever, эризипелоид);

— infections of bones and joints (osteomyelitis, septic arthritis);

— infections of bodies of a small pelvis (endometritis, adnexitis, cervicitis);

— sepsis;

— meningitis;

— disease Laima (borreliosis).

Prevention of infectious complications at operations on bodies of a thorax (including at lung, heart, gullet operations), an abdominal cavity, a basin, joints, in vascular surgery at a high risk of infectious complications, at orthopedic operations.

Route of administration and doses:

Intramusculary, intravenously. Intravenously and intramusculary the adult appoint 0.75 g 3 times a day; at infections of a heavy current - the dose is increased up to 1.5 g 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 is more senior than 3 months appoint on 30-100 mg/kg/days in 3-4 introductions. 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 introductions. At gonorrhea - intramusculary, adult 1.5 g once (in the form of 2 injections on 0.75 g with introduction to different areas, for example in both gluteuses). At bacterial meningitis – intravenously, the adult - on 3 g each 8 h; to children of younger and advanced age - 150-250 mg/kg/days in 3-4 introductions, newborn - 100 mg/kg/days in 2-3 introductions. For prevention of postoperative complications: - at heart, lungs, gullet operations and vessels – intravenously, 1.5 g for 0,5 - 1 h before operation and on 0.75 g intravenously or intramusculary each 8 h at long operations during the subsequent 24 – 48 h (at open heart operations the general dose to 6 g); - at an abdominal cavity operations, bodies of a basin and at orthopedic operations - intravenously, 1.5 g at anesthesia induction, then in addition - intramusculary, 0.75 g, in 8 and 16 h after operation; - at full replacement of a joint – 1.5 g of powder mix polymer of methylmethacrylate cement, in a dry form with each package, before addition of liquid monomer. At pneumonia - intramusculary or intravenously, on 1.5 g 2-3 times a day during 48-72 h, then pass to intake (use dosage forms for intake) 0,5 g 2 times a day within 7-10 days. At an exacerbation of chronic bronchitis appoint intramusculary or intravenously, 0.75 g 2-3 times a day during 48-72 h, then pass to intake (use dosage forms for intake) 0,5 g 2 times a day within 5-10 days. At a chronic renal failure correction of the mode of dosing at adults is necessary: at the clearance of creatinine (CC) of 10-20 ml/min. appoint intravenously or intramusculary 0.75 g 2 times a day, at KK less than 10 ml/min. - on 0.75 g of 1 times a day. At a chronic renal failure at children the mode of dosing has to be changed according to recommendations for adults. 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 0.75 g 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 suspension for intramuscular introduction: 0.75 (a bottle of 10 ml) to dissolve in 3 ml of water for injections. To dissolve 1,5 g (a bottle of 20 ml) in 6 ml of water for injections. To stir up carefully before formation of suspension. Preparation of solution for intravenous administration: 0.75 (a bottle of 10 ml) to dissolve in 9 ml of water for injections. To dissolve 1,5 g (a bottle of 20 ml) in 14 ml of water for injections. Solution for intravenous infusions. In case of carrying out short-term intravenous injections (for example, up to 30 min.) 1.5 g dissolve in 50 ml of water for injections. These solutions can be entered directly into a vein or a dropper if to the patient parenterally enter liquids.

Features of use:

The patients having allergic reactions to penicillin in the anamnesis can show hypersensitivity to tsefalosporinovy antibiotics.

In the course of treatment control of function of kidneys, especially at the patients receiving drug in high doses at patients of advanced age, with a disease of kidneys in the anamnesis is necessary, at simultaneous use with aminoglycosides and "loopback" diuretics.

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 tsefuroksy when determining concentration of glucose in blood recommend to use tests with glucose oxydas or a hexokinase.

Pseudomembranous colitis is observed when using a wide range of antibiotics, the possibility of its emergence needs to be meant at patients with the heavy diarrhea which arose in time or after a course of treatment antibiotics.

During treatment it is impossible to use ethanol.

Against the background of treatment of meningitis at children decrease in hearing is possible.

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 there is no clinical effect in 72 h of an initiation of treatment, the parenteral course of therapy has to be continued.

Influence on ability to driving of motor transport and to control of mechanisms

During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Allergic reactions: fever, rash, itch, urticaria; seldom - a mnogoformny erythema, a bronchospasm, Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Lyell's disease), a bronchospasm, medicinal fever, a serum disease, an acute anaphylaxis, a skin vasculitis.

From the alimentary system: diarrhea, nausea, vomiting or lock, meteorism, spasms and abdominal pain, ulcerations of a mucous membrane of an oral cavity, oral cavity candidiasis, glossitis, pseudomembranous coloenteritis, abnormal liver function (increase in activity of nuclear heating plant, ALT, ShchF, LDG), hyperbilirubinemia, cholestasia.

From a reproductive system: an itch in crotches, a vaginitis.

From an urinary system: a renal failure (decrease in clearance of creatinine, increase in content of creatinine and/or an urea nitrogen in blood), a dysuria, intersticial nephrite.

From bodies of a hemopoiesis: eosinophilia, leukopenia, neutropenia, thrombocytopenia, agranulocytosis, hemolitic anemia, decrease in hemoglobin and hematocrit.

From a nervous system: spasms.

From sense bodys: decrease in hearing.

Local reactions: at introduction in oil - pain, irritation and infiltrate in an injection site; at in introduction – phlebitis, thrombophlebitis.

Laboratory indicators: false positive test of Koombs, prothrombinopenia, lengthening of a prothrombin time.

Interaction with other medicines:

Simultaneous peroral purpose 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 interaction

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 (glucose), 0.18% solution of sodium of chloride and 4% solution of a dextrose (glucose), 5% solution of a dextrose (glucose) and 0.9% chloride sodium solution, Ringer's solution, sodium lactate solution, Hartman's solution, heparin (10 PIECES/ml and 50 PIECES/ml) in 0.9% chloride sodium solution.

Pharmaceutical it is incompatible with aminoglycosides, solution of sodium of bicarbonate of 2.74%.

Contraindications:

— hypersensitivity (including to other cephalosporins, penicillin and karbapenema).

With care it is necessary to appoint drug newborn (including premature), at a chronic renal failure, bleedings and gastrointestinal diseases (including in the anamnesis, nonspecific ulcer colitis), to the weakened and exhausted patients, at pregnancy, in the period of a lactation, at simultaneous use with aminoglycosides, "loopback" diuretics.

 

Use of the drug TSEFURUS® at pregnancy and feeding by a breast

Use of drug at pregnancy and during breastfeeding is possible if the expected advantage for mother exceeds potential risk for a fruit and the child.

 

Use at renal failures

At a chronic renal failure correction of the mode of dosing is necessary. At KK of 10-20 ml/min. appoint in/in or in oil on 750 mg 2, at KK less than 10 ml/min. - on 750 mg of 1 times /

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; for the patients who are on haemo filtering of low speed appoint the doses recommended at a renal failure.

 

Use for children

With care it is necessary to appoint drug newborn (including premature).

To children 3 months are more senior appoint drug in/in and in oil on 30-100 mg/kg / in 3-4 introductions. For the majority of infections the optimum dose makes 60 mg/kg /

To newborns and children up to 3 months appoint 30 mg/kg / in 2-3 introductions.

At bacterial meningitis - in children of younger and advanced age - 150-250 mg/kg / in 3-4 introductions, newborn - 100 mg/kg/.

Overdose:

Symptoms: excitement of TsNS, spasm.

Treatment: symptomatic therapy, hemodialysis and peritoneal dialysis.

Storage conditions:

Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 2 years.

After cultivation it is possible to store 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.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 750 mg; bottle of 10 ml, pack cardboard 1.
Powder for preparation of solution for intravenous and intramuscular administration of 1.5 g; bottle of 10 ml, pack cardboard 1.