Tsefuroksim

General characteristics. Structure:

Active ingredient: 1 tablet contains a tsefuroksim of an aksetil in the number corresponding of 125 mg, either 250 mg, or 500 mg of a tsefuroksim;

excipients: sodium lauryl sulfate, коповидон, sodium of a kroskarmelloz, magnesium stearate, silicon dioxide colloid, Mannitolum granulated cellulose microcrystallic, кросповидон, talc a cover: Mannitolum, starch soluble, talc, titanium dioxide, aspartame.

Pharmacological properties:

Pharmacodynamics. Tsefuroksim — a tsefalosporinovy antibiotic which bactericidal action is caused by inhibition of synthesis of a cell wall of bacteria. Possesses a wide range of antimicrobic action of gram-positive and gram-negative bacteria, including the strains producing β-lactamelements. Tsefuroksim is steady against action β-лактамаз and therefore shows activity concerning many ampicillin - or amoksitsillinrezistentny strains. 

Tsefuroksim is effective in vitro against the following microorganisms:

gram-negative aerobes: Escherichia coli, Klebsiella spp., Proteus mirabilis, Proteus rettgeri, Providencia spp., Haemophilus influenzae (including ampitsillinrezistentny strains), Haemophilus parainfluenzae (including ampitsillinrezistentny strains), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae (including the strains producing a penicillinase);

gram-positive aerobes: Staphylococcus aureus, Staphylococcus epidermidis (including the strains producing a penicillinase, but excepting metitsillinrezistentny strains), Streptococcus pyogenes (and also other β-hemolitic streptococci), Streptococcus pneumoniae, Streptococcus of group In (Streptococcus agalactiae);

anaerobe bacterias: gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus species);

gram-positive bacteria (including most Clostridium spp.) and gram-negative bacteria (including Bacteroides spp. and Fusobacterium spp.), Propionibacterium spp.;

other microorganisms: Borrelia burgdorferi; 

microorganisms, insensitive to a tsefuroksim: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, metitsillinrezistentny strains of Staphylococcus aureus, metitsillinrezistentny strains of Staphylococcus epidermidis, Legionella spp.; 

some strains of microorganisms, insensitive to a tsefuroksim: Enterococcus (Streptococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis. 

Pharmacokinetics. After oral administration of a tsefuroksim aksetit it is soaked up in a GIT and quickly is exposed to hydrolysis in a mucous membrane of a small intestine and blood with release of active agent — a tsefuroksima. Optimum absorption is noted at reception of a tsefuroksim of an aksetil through short time after meal (50–60%). At this Cmax in a blood plasma it is reached in 2–3 h.

It is widely distributed in fabrics and liquids of an organism, including pleural liquid, a phlegm, a bone tissue, synovial and intraocular fluid. Therapeutic concentration in SMZh are reached only at meningitis. Linkng with proteins of a blood plasma makes 33–55%. Gets through a placenta, it is excreted in breast milk.

Tsefuroksim is not metabolized. The most part is removed with urine in not changed look. Nearly 50% are excreted by glomerular filtering, other part — by renal tubular secretion for 24 h, and the most part of the entered dose is removed for the first 6 h; drug is present at urine in high concentration. In insignificant quantity it is removed with bile.

T½ — 60–90 min.; at patients with renal failures and at newborn T½ it is extended.

Indications to use:

The infections caused by microorganisms, sensitive to a tsefuroksim:

ENT organs — acute average otitis, sinusitis, tonsillitis, pharyngitis;

respiratory organs — acute and chronic bronchitis in an aggravation stage, pneumonia;

infections of urinary tract — cystitis, pyelonephritis, an urethritis;

skin and soft tissues — a furunculosis, a pyoderma, impetigo;

treatment of early displays of a disease of Lyme and prevention of late complications at adults and children is aged more senior than 12 years.

Route of administration and doses:

Usually duration of treatment makes 7 days. For the best assimilation drug is recommended to be accepted after food.

The recommended dosing mode for tablets Tsefuroksim Sandoz:

 

Adults                             dosing Mode

The majority of infections                of 250 mg 2 times a day

Infections of urinary tract            of 125 mg 2 times a day

Upper respiratory tract infections

moderate severity                of 250 mg 2 times a day

Respiratory infections of average

severity (bronchitis)                of 250 mg 2 times a day

Respiratory infections heavy

degrees or suspicion of pneumonia        of 500 mg 2 times a day

Pyelonephritis                         of 250 mg 2 times a day

Uncomplicated gonorrhea                of 1000 mg once

Lyme's diseases at adults and children of 12 years     of 500 mg 2 times a day within 20 days

 

Tsefuroksim release also in the form of sodium salt for parenteral use. It gives the chance to carry out consecutive therapy by one antibiotic upon transition from parenteral administration to oral administration at clinical indications.

Tsefuroksim for oral administration is effective at consecutive treatment of pneumonia and exacerbations of chronic bronchitis after the previous parenteral use of a tsefuroksim of sodium.

Consecutive therapy 

Pneumonia: 1,5 g of a tsefuroksim 2–3 times a day (in/in or in oil) during 48–72 h with the subsequent use of a tsefuroksim on 500 mg 2 times a day for 7 days.

Exacerbation of chronic bronchitis: 750 mg of a tsefuroksim 2–3 times a day (in/in or in oil) during 48–72 h with the subsequent use of a tsefuroksim on 500 mg 2 times a day for 5–7 days.

Duration of both parenteral, and peroral treatment is determined taking into account weight of an infection and a condition of the patient.

Children. The usual dose makes 125 mg or 10 mg/kg of body weight 2 times a day (the maximum daily dose — 250 mg). For treatment of average otitis to children 2 years — 250 mg or 15 mg/kg of body weight 2 times a day are aged more senior (the maximum daily dose — 500 mg).

Patients of advanced age and patients with a renal failure. There are no special cautions for this group of patients. Usual doses, the maximum dose — apply up to 1 g/days.

Features of use:

It is necessary to appoint with care drug sick with disturbance of functions of a liver. For patients with a renal failure the dose is established individually.

Use of a tsefuroksim (as well as other antibiotics) can lead to Candida overgrowth. Prolonged use can also lead to the overgrowth of other insensitive microorganisms (for example Enterococci, Clostridium difficile) that can demand the treatment termination.

Use of a tsefuroksim is not recommended to patients with the heavy disturbances from intestines which are followed by the vomiting and diarrhea leading to decrease in level of absorption. With extra care it is necessary to apply tsefuroksy at patients with a fenilketonuriya as the cover of a tablet contains aspartame.

20-day treatment of a disease of Lyme can increase the frequency of development of diarrhea.

Developing of heavy diarrhea during treatment can be a consequence of development of pseudomembranous colitis. In this case use of drug it is necessary to stop and conduct the corresponding examination.

During use of a tsefuroksim at Lyme's disease noted Yarish's reaction — Gerksgeymera. It arose directly owing to bactericidal action of a tsefuroksim on Borrelia burgdorferi spirochete causing Lyme's disease. The patient has to know that this frequent phenomenon at an antibioticotherapia of a disease of Lyme which is not demanding treatment.

To patients, the accepting tsefuroksy, it is recommended to define concentration of glucose in a blood plasma by methods with glucose oxydas or a hexokinase. Tsefuroksim does not influence definition of creatinine by means of a research with alkaline picrate.

During treatment tsefuroksimy at some children noted decrease in hearing from weak to moderate degree.

Use during pregnancy and feeding by a breast. Tsefuroksim gets through a placental barrier. Because of insufficient experience of use for pregnant women it is possible to appoint drug during this period only after the careful analysis of a ratio risk/advantage (with extra care in the first months of pregnancy). Tsefuroksim in small concentration gets into breast milk therefore feeding by a breast for treatment should be stopped.

Influence on ability to manage vehicles and to work with difficult mechanisms. As drug can cause dizziness, patients should be warned that it is necessary to manage the vehicle or to work with mechanisms with care.

Children. This dosage form is applied at children aged 2 years are more senior.

Side effects:

Criteria for evaluation of frequency of emergence of side effects: often (≥1/100, <1/10); infrequently (≥1/1000, <1/100), it is rare (≥1/10 000, <1/1000), is very rare (<1/10 000).

Infections and invasions: prolonged use of drug can lead to development of the secondary superinfections caused by resistant microorganisms.

From blood and lymphatic system: often — an eosinophilia; seldom — decrease in level of hemoglobin, a leukopenia, a neutropenia and thrombocytopenia, is very rare — hemolitic anemia.

From immune system: Yarish's reaction — Gerksgeymera who can arise at treatment of a disease of Lyme; seldom — a serum disease; very seldom — an anaphylaxis, medicinal fever.

From a nervous system: seldom — a headache, dizziness; very seldom — overexcitement, nervousness, confusion of consciousness.

From a GIT: often — nausea, vomiting, an abdominal pain, diarrhea (frequency of developing of diarrhea increases at prolonged use of drug); seldom — pseudomembranous colitis.

From gepatobiliarny system: seldom — tranzitorny increase in activity of hepatic transaminases (ALAT, ASAT, LDG) and bilirubin in a blood plasma; very seldom — jaundice (mainly cholestatic), hepatitis.

From skin and hypodermic cellulose: infrequently — rash, urticaria, an itch; very seldom — a multiformny erythema, Stephens's syndrome — Johnson, a toxic epidermal necrolysis.

From an urinary system: increase in level of creatinine and urea in a blood plasma, especially at patients with a renal failure; seldom — acute intersticial nephrite.

Laboratory indicators: false positive reaction of Koombs that can influence results of tests of cross compatibility of blood.

Interaction with other medicines:

As well as other antibiotics, tsefuroksy can influence intestines flora that leads to reduction of a reabsorption of estrogen and decrease in efficiency of the combined oral contraceptives. It is recommended to avoid a combination of a tsefuroksim of an aksetil for oral administration with antacids because of increase in pH in a stomach that can influence absorption of a tsefuroksim.

Simultaneous use of a tsefuroksim in high doses with diuretics (Acidum etacrynicum, furosemide), aminoglycosides, Amphotericinum, kolistimetaty sodium and polymyxin increases risk of development of a renal failure.

At simultaneous use with fenilbuzatony or probenetsidy decrease in renal clearance of a tsefuroksim and increase in its concentration in a blood plasma is possible.

At the combined use with erythromycin decrease in efficiency of both antibiotics is possible.

As bacteriostatic drugs can influence bactericidal effect of cephalosporins, use of a tsefuroksim in a combination with tetracyclines, macroleads or chloramphenicol is not recommended.

Tsefuroksim, suppressing an indestinal flora, interferes with vitamin K synthesis. At simultaneous use with the drugs reducing aggregation of thrombocytes (NPVP, salicylates, Sulfinpyrazonum) the risk of development of bleedings increases. For the same reason at simultaneous use with anticoagulants increase in expressiveness of anticoagulating action is noted.

Contraindications:

Hypersensitivity to a tsefuroksim, other cephalosporins or any of drug components; existence in the anamnesis of data on heavy hypersensitivity reactions to penicillin or other β-laktamny antibiotics.

Overdose:

The overdose of tsefalosporinovy antibiotics can lead to development of spasms. Level of a tsefuroksim can be reduced by a hemodialysis or peritoneal dialysis.

Storage conditions:

At a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets п / captivity. cover of 250 mg, No. 14

Tablets п / captivity. cover of 500 mg, No. 14