Tsefotaksim
Producer: CJSC Pharmaceutical Firm LEKKO Russia
Code of automatic telephone exchange: J01DD01
Release form: Liquid dosage forms. Powder for preparation of solution for injections.
General characteristics. Structure:
Active ingredient: substance - tsefotaksy (in the form of a tsefotaksim of sodium) - 1,0 g.
Description: Powder, white or white with a yellowish shade.
Pharmacological properties:
Pharmacodynamics. The Tsefalosporinovy antibiotic of the III generation for parenteral administration. Works bakteritsidno, breaking synthesis of a mukopeptid of a cell wall of microorganisms. Possesses a broad spectrum of activity. It is active concerning the gram-positive and gram-negative microorganisms steady against other antibiotics: Staphylococcus spp. (including Staphylococcus aureus, including the strains forming a penicillinase), Staphylococcus epidermidis (except for Staphylococcus epidermidis and Staphylococcus aureus steady against Methicillinum), Streptococcus pneumoniae, Streptococcus pyogenes (beta and hemolitic streptococci of group A), Streptococcus agalactiae (group B streptococci), Enterococcus spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including the strains forming a penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), Morganella morganii, Neisseria gonorrhoeae (including the strains forming a penicillinase), Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubacter spp., Propionibacterium spp. Clostridium spp. (including Clostridium perfringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Serratia spp., some strains of Pseudomonas aeruginosa, Neisseria meningitidis, Neisseria gonorrhoeae, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. Changeably influences some strains of Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, Bacteroides fragilis, Clostridium difficile. It is steady against the majority beta лактамаз gram-positive and gram-negative microorganisms
Pharmacokinetics. After single intravenous administration in doses of 0,5, 1 and 2 g time of achievement of the maximum concentration (Smakh) - 5 minutes, Smakh makes 39, 101,7 and 214 mkg/ml, respectively. After intramuscular introduction in doses of 0,5 and 1 g achievement time Smakh of-0,5 h, also makes 11 and 21 mkg/ml respectively. Communication with proteins of plasma - 30-50%. Bioavailability - 90-95%. Creates therapeutic concentration in the majority of fabrics (a myocardium, bones, a gall bladder, skin, soft tissues) and liquids (synovial, pericardiac, pleural, a phlegm, bile, urine, medullispinal liquid) an organism. Distribution volume - 0,25-0,39 l/kg. An elimination half-life (T1/2) - 1 h at intravenous administration and 1-1,5 h - at intramuscular introduction. 20-36% - in not changed look, other quantity - in the form of metabolites are removed by kidneys (15-25% - in the form of pharmacological active dezatsetiltsefotaksim and 20-25% - in the form of 2 inactive metabolites). At a chronic renal failure and at elderly people of T1/2 increases twice. T1/2 at newborns - 0,75-1,5 h, at premature newborn children (body weight less than 1500) increases up to 4,6 h; children with body weight have more than 1500 - 3,4 h. At repeated intravenous administrations in a dose of 1 g each 6 h within 14 days of cumulation it is not observed. Tsefotaksim passes through a placenta, in insignificant concentration gets into breast milk.
Indications to use:
The infectious and inflammatory diseases caused by sensitive microorganisms: infections of the central nervous system (meningitis), airways and ENT organs, urinary tract, bones, joints, skin and soft tissues, bodies of a small pelvis, peritonitis, sepsis, endocarditis; gonorrhea; contaminated wounds and burns; abdominal infections, salmonellosises, Lyme's disease, infections against the background of an immunodeficiency, prevention of infections after surgeries (including urological, obstetric and gynecologic, on bodies of digestive tract).
Route of administration and doses:
The drug is administered intravenously (struyno or kapelno) and intramusculary.
To adults and children 12 years are more senior (with the body weight of 50 kg and more): at uncomplicated infections, and also at infections of urinary tract - intramusculary or intravenously, on 1 g each 8-12 h; at uncomplicated acute gonorrhea – intramusculary, 1 g once; at moderately severe infections - intramusculary or intravenously, on 1-2 g each 12 h; at the heavy course of infections, for example at meningitis - intravenously, on 2 g each 4-8 h, the maximum daily dose - 12 g. Duration of treatment is established individually.
For the purpose of prevention of development of infections before surgery enter into time of an introduction anesthesia once 1 g. If necessary, introduction is repeated in 6-12 h. At Cesarean section - at the time of imposing of clips on an umbilical vein - intravenously, 1 g, then in 6 and 12 h after the first dose - in addition on 1 g.
At clearance of creatinine of 20 ml/min. / 1,73 sq.m and less, reduce a daily dose by 2 times.
Premature and newborn up to 1 week - intravenously, 50 mg/kg each 12 h; at the age of 1-4 weeks - intravenously, 50 mg/kg each 8 h; to children, with a body weight up to 50 kg - intravenously or intramusculary, 50-180 mg/kg in 4-6 introductions. At the heavy course of infections, including at meningitis, the daily dose to children is increased to 100-200 mg/kg, intramusculary or intravenously, in 4-6 receptions, the maximum daily dose - 12 g.
Rules of preparation of injection solutions:
for an intravenous injection as solvent use water for injections (0,5-1 g part in 4 ml of solvent, 2 g - in 10 ml); the drug is administered slowly within 3-5 min.
for intravenous infusion as solvent NaCl solution or 5% dextrose solution use 0,9% (1-2 g part in 50-100 ml of solvent). Infusion duration - 50-60 minutes;
for intramuscular introduction use water for injections or 1% lidocaine solution (for a dose of drug of 0,5 g - 2 ml, for a dose of 1 g - 4 ml).
Features of use:
- in the first weeks of treatment there can be pseudomembranous colitis which is shown heavy long diarrhea. At the same time stop administration of drug and appoint adequate therapy, including Vancomycinum or metronidazole;
- the patients who had allergic reactions to penicillin in the anamnesis can have hypersensitivity to tsefalosporinovy antibiotics;
- at treatment by drug over 10 days control of a picture of peripheral blood is necessary. During treatment tsefotaksimy receiving false positive test of Koombs and false positive reaction of urine to glucose is possible;
- in need of purpose of drug in the period of a lactation, it is necessary to stop breastfeeding;
- during treatment it is impossible to use ethanol - the effects similar to action of Disulfiramum are possible (a hyperemia of the person, a spasm in a stomach and in a stomach, nausea, vomiting, a headache, a lowering of arterial pressure, tachycardia, short wind).
Side effects:
Allergic reactions: a small tortoiseshell, a fever or fever, rash, a skin itch, it is rare - a bronchospasm, an eosinophilia, a malignant exudative erythema (Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease), a Quincke's disease, an acute anaphylaxis.
From an urinary system: renal failure, oliguria, intersticial nephrite.
From digestive tract: nausea, vomiting, diarrhea or locks, a meteorism, an abdominal pain, dysbacteriosis, an abnormal liver function, it is rare - stomatitis, a glossitis, a pseudomembranous coloenteritis.
From bodies of a hemopoiesis: hemolitic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, agranulocytosis, hypocoagulation.
From cardiovascular system: potentially life-threatening arrhythmias after bystry bolyusny introduction to the central vein.
Laboratory indicators: an azotemia, increase in concentration of urea in blood, increase in activity of "hepatic" transaminases and an alkaline phosphatase, a giperkreatininemiya, a hyperbilirubinemia, positive reaction of Koombs.
Local reactions: phlebitis, morbidity on the vein course, morbidity and infiltrate in the place of intramuscular introduction.
Other: superinfection (in particular, vaginal and oral candidiasis).
Interaction with other medicines:
- increases risk of bleedings at a combination to antiagregant, non-steroidal anti-inflammatory drugs;
- the probability of damage of kidneys increases at a concomitant use of aminoglycosides, polymyxin B and "loopback" of diuretics;
- the medicines blocking canalicular secretion increase plasma concentration of a tsefotaksim and slow down its removal;
- pharmaceutical it is incompatible with solutions of other antibiotics in one
syringe or dropper.
Contraindications:
- hypersensitivity (including to penicillin, other cephalosporins, karbapenema);
- pregnancy;
- children's age up to 2,5 years (for intramuscular introduction).
With care:
- in the period of a neonatality;
- in the period of a lactation (in insignificant concentration it is allocated with milk);
- at a chronic renal failure;
- at nonspecific ulcer colitis (including in the anamnesis).
Overdose:
Symptoms: spasms, encephalopathy (in case of introduction of high doses, especially at patients with a renal failure), a tremor, neuromuscular excitability.
Treatment: symptomatic, there is no specific antidote.
Storage conditions:
List B. In the dry, protected from light place at a temperature not higher than 25 ° C. To store in the place, unavailable to children.
Issue conditions:
According to the recipe
Packaging:
Powder for preparation of solution for intravenous and intramuscular administration of 1,0 g. On 1,0 g in bottles polymeric or glass.
On 1 bottle on 1,0 g with 1 application instruction in a box from a cardboard.
On 5 bottles on 1,0 g with 1 application instruction in a box from a cardboard.
On 30 bottles on 1,0 g with 1 application instruction in a box from a cardboard.
