Tsefosin

General characteristics. Structure:

Active ingredient: a tsefotaksima sodium salt sterile (in terms of tsefotaksy) 0,5 g, 1,0 g and 2,0 g.

Pharmacological properties:

Tsefalosporinovy antibiotic of the III generation of a broad spectrum of activity. Works bakteritsidno, breaking synthesis of a cell wall of bacteria.

Tsefosin is active concerning gram-positive bacteria: Staphylococcus spp. (including Staphylococcus aureus / including the strains forming a penicillinase/, Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae), Enterococcus spp., Corynebacterium diphtheriae, Erysipelothrix insidiosa, Bacillus subtilis; gram-negative bacteria: Enterobacter spp., Escherichia coli, Haemophilus influenzae (including the strains forming a penicillinase), Haemophilus parainfluenzae, Citrobacter spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris, Proteus indole), Providencia spp. (including Providencia rettgeri), Klebsiella spp. (including Klebsiella pneumoniae), Serratia spp., Pseudomonas aeruginosa, Morganella morganii, Neisseria gonorrhoeae (including the strains producing a penicillinase), Neisseria meningitidis, Acinetobacter spp.; anaerobic bacteria: Clostridium spp. (including Clostridium perfringens), Eubacterium spp., Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp, Propionibacterium spp.

Tsefotaksim is steady against action β-лактамаз gram-positive and gram-negative bacteria, including against a penicillinase of stafilokokk and Clostridium difficile.

 

Pharmacokinetics. Absorption

After single in/in Tsefosin's introductions in a dose of 500 mg, 1 g and 2 g of Cmax it is reached in 5 min. and makes 39 mkg/ml, 100 mkg/ml and 214 mkg/ml respectively.

After introduction of Tsefosin in oil in a dose of 500 mg and 1 g of Cmax it is reached in 5 min. and makes 11 mkg/ml and 21 mkg/ml respectively.

Distribution

Linkng with proteins of plasma makes 25-40%.

It is found in therapeutic concentration in the majority of fabrics (a myocardium, bones, a gall bladder, skin, soft tissues) and liquids (pleural, peritoneal, synovial, urine, bile, cerebrospinal fluid, a phlegm).

Vd - 0.25-0.39 l/kg.

At repeated in introductions in a dose of 1 g each 6 h during 14 days of cumulation it is not observed.

Tsefotaksim is allocated with breast milk.

Removal

T1/2 of a tsefotaksim at in/in and introduction in oil makes 1 h.

Tsefotaksim is brought with urine (60-70% - in not changed look, other part - in the form of metabolites / and dezatsetilirovanny derivative has bactericidal activity, and other metabolites - do not possess/).

Pharmacokinetics in special clinical cases

At a chronic renal failure and at elderly patients of T1/2 increases twice.

At newborn T1/2 makes of 0.75 h to 1.5 h, at premature newborns increases up to 4.6 h.

Indications to use:

The bacterial infections caused by sensitive microorganisms:

— respiratory infections;

— infections of urinary tract;

— infections of ENT organs;

— infections of bones and joints;

— infections of skin and soft tissues;

— peritonitis;

— abdominal infections;

— infections of bodies of a small pelvis;

— sepsis;

— endocarditis;

— TsNS infections (including meningitis);

— clamidiosis;

— gonorrhea;

— Lyme's disease;

— salmonelloses;

— contaminated wounds and burns;

— infections at patients with an immunodeficiency.

Prevention of infections after surgical interventions (including urological, obstetric and gynecologic, on a GIT).

Route of administration and doses:

Intramusculary and intravenously. For an intramuscular injection dissolve 0,5 g of drug in 2 ml (respectively 1 g in 4 ml) sterile water for injections. Enter deeply into a gluteus. As solvent at intramuscular introduction 1% lidocaine solution is also used (on 0,5 g - 2 ml, on 1 g - 4 ml). For intravenous administration of 0,5 - 1 of a tsefotaksim dissolve in 10 ml of sterile water for injections. Enter slowly within 3-5 minutes. For drop introduction (within 50-60 minutes) dissolve 2 g of drug in 100 ml of isotonic solution of sodium of chloride or 5% of solution of glucose. The usual dose of a tsefotaksim for adults and children is more senior than 12 years - 1 g every 12 hours. In hard cases the dose is increased to 3 or 4 g a day, administer time drug 3 or 4 on 1 g. Depending on disease severity the daily dose can be increased to maximum which makes 12 g. The usual dose for newborns and children is younger than 12 years - 50-100 mg/kg of body weight a day with intervals of introduction from 6 to 12 hours. For premature children the daily dose should not exceed 50 mg/kg. In case of renal failures the dose is reduced. At clearance of creatinine of 10 ml/min. and less daily dose of drug is reduced twice.

Features of use:

Before purpose of drug it is necessary to collect the allergological anamnesis, especially concerning a beta laktamnykh of antibiotics. It is necessary to consider that development of a cross allergy between penicillin and cephalosporins is possible. Drug is appointed with care to the patients having allergic reactions to penicillin in the anamnesis (it is necessary to consider a possibility of development of heavy anaphylactic reactions, up to a lethal outcome).

The pseudomembranous colitis which is shown heavy diarrhea can develop in the first weeks of treatment. At development of this situation treatment by Tsefosin it is necessary to stop and appoint the corresponding therapy, including metronidazole and Vancomycinum inside.

When determining glucose in urine by not euzymatic method (for example, Benedict's method) false positive results are possible.

Lasting therapy more than 10 days it is necessary to control a pattern of peripheral blood.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, a lock, a meteorism, an abdominal pain, dysbacteriosis, abnormal liver functions (increase in activity of ALT, nuclear heating plant, ShchF in a blood plasma, a giperkreatininemiya, a hyperbilirubinemia); seldom - stomatitis, a glossitis, pseudomembranous colitis.

From system of a hemopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolitic anemia, hypocoagulation.

From an urinary system: an azotemia, an oliguria, an anury, increase in content of urea in blood, intersticial nephrite.

From TsNS: headache, dizziness.

From cardiovascular system: at bystry bolyusny introduction to the central vein development of potentially dangerous arrhythmias is possible.

Local reactions: phlebitis, morbidity on the vein course at at in introduction, morbidity and infiltrate - at introduction in oil.

Allergic reactions: small tortoiseshell, fever, fever, rash, itch; seldom - a bronchospasm, an eosinophilia, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, a Quincke's disease, an acute anaphylaxis.

Others: superinfection (including mycotic vulvovaginitis), false positive test of Koombs.

Interaction with other medicines:

At simultaneous use of Tsefosin and nephrotoxic drugs (aminoglikozidny antibiotics, "loopback" diuretics, polymyxin B) strengthening of nephrotoxic action is possible. Therefore it is necessary to control function of kidneys at simultaneous use of these drugs.

At co-administration of Tsefosin with antiagregant, NPVS increases risk of development of bleedings.

At combined use with Tsefosin of drugs, blokirushchy canalicular secretion, plasma concentration of a tsefotaksim increase and its removal is slowed down.

Simultaneous use of Tsefosin with ethanol does not lead to development of disulfiramopodobny reactions.

Pharmaceutical interaction

Tsefosin's solution is incompatible with solutions of other antibiotics in one syringe or a dropper.

Contraindications:

— hypersensitivity to cephalosporins, penicillin, karbapenema.

Drug is not appointed to children in oil aged up to 2.5 years.

With care should appoint drug newborns, patients with a chronic renal failure, nonspecific ulcer colitis (including in the anamnesis), in the period of a lactation.

 

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

Tsefosin's use at pregnancy is possible only when the estimated advantage for mother exceeds potential risk for a fruit.

Tsefotaksim is allocated with breast milk. In need of appointment in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

 

Use at renal failures

At renal failures the dose is reduced. At KK10 ml/min. reduce a daily dose of drug twice.

Overdose:

Symptoms: spasms, encephalopathy (at administration of drug in high doses, especially, at a renal failure), a tremor, a hyperexcitability.

Treatment: symptomatic therapy.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Bottles (1) - packs cardboard.
Bottles (50) - packs cardboard.