Klaforan powder for preparation of injection solution 1g, No. 1

Cefotaxime is indicated for the treatment of infections caused by microorganisms that are sensitive to the drug.

• respiratory tract infections;

• urinary tract infections;

• septicemia, bacteremia;

• endocarditis;

• intra-abdominal infections (including peritonitis);

• meningitis (with the exception of listeria) and other infections of the central nervous system;

• infections of the skin and soft tissues;

• infections of bones and joints;

• Prevention of infections after surgical operations on the gastrointestinal tract, urological and obstetric-gynecological operations.

Reception mode is individual

Powder for preparation of a solution for intravenous and intramuscular administration of white or yellowish-white, crystalline.

1 fl.

cefotaxime sodium 1.048 g,?

which corresponds to the content of cefotaxime 1 g

• Hypersensitivity to cephalosporins;

  for forms containing lidocaine:

• hypersensitivity to lidocaine or other local anesthetic of the amide type;

• intra-vascular blockade without an established pacemaker;

• severe heart failure;

• intravenous administration

• children under the age of 2.5 years (intramuscular injection)

Pharmacological properties
Pharmacodynamics
Semisynthetic antibiotic of the third generation cephalosporin group for parenteral use. Cefotaxime has a bactericidal effect. It is also resistant to the action of most ?-lactamases.
Usually sensitive to the drug: Aeromonas hydrophila; Bacillus subtilis; Bordetella pertussis; Borrelia burgdorferi; Moraxella (Branhamella) catarrhalis; Cirtobacter diversus; Clostridium perfringens; Corynebacterium diptheriae; Escherichia coli; Enterobacter spp. (sensitivity depends on epidemiological data and on the level of resistance in each specific country); Erysipelothrix insidiosa; Eubacterium; Haemophilus penicillinase-forming and non-penicillinase-forming strains including ampi-R; Klebsiella pneumoniae; Klebsiella oxytoca; Methi-S-Staphylococcu, including penicillinase-forming and non-penicillinase-forming strains; Morganella morganii; Neisseria gonorrhoeae, including penicillinase-forming and non-penicillinase-forming strains; Neisseria meningitidis; Propionibacterium; Proteus mirabilis, vulgaris; Providencia; Streptococcus pneumoniae,Salmonella; Seratia spp. (sensitivity depends on epidemiological data and on the level of resistance in each specific country); Shigella, Streptococcus spp .; Veillonella; Yersinia (sensitivity depends on epidemiological data and country-specific resistance level).
Resistant to the drug: Acinetobacter baumanii, Bacteroides fragilis; Clostridium difficile; Enterococcus; Gram negative anaerobes; Listeria monocytogenes, Methi-R staphylococcus; Pseudomonas aeruginosa, cepacia; Stenotrophomonas maltophilia.

Pharmacokinetics
In adults, 5 minutes after a single intravenous injection of 1 g of cefotaxime, the plasma concentration is 100 ?g / ml. After i / m administration of cefotaxime in the same dose, the maximum concentration in blood plasma is detected after 0.5 hours and ranges from 20 to 30 ?g / ml.
The half-life of the drug is 1 hour with intravenous administration and 1-1.5 hours with intravenous administration.
Plasma protein binding (mainly albumin) averages 25-40%.
About 90% of the administered dose is excreted in the urine: 50% - unchanged and about 20% in the form of deacetylcefotaxime metabolite.
In the elderly, the half-life of cefotaxime increases to 2.5 hours in patients over 80 years of age.
In adults with impaired renal function, the volume of distribution does not change, and the half-life does not exceed 2.5 hours, even in the last stages of renal failure.
In children, newborns and prematurely born infants, the level of cefotaxime in plasma and the volume of distribution are similar to those in adults receiving the same dose of the drug in mg / kg body weight. The half-life of cefotaxime is from 0.75 to 1.5 hours.
In newborns and premature babies, the plasma level of cefotaxime and the volume of distribution are similar to those in children.
The average elimination half-life of cefotaxime is 1.4 to 6.4 hours.

Application during pregnancy and lactation
Cefotaxime crosses the placental barrier. Studies carried out on animals did not reveal a teratogenic effect of the drug. However, the safety of using cefotaxime during pregnancy in humans has not been determined, so the drug should not be used during pregnancy.
Cefotaxime passes into breast milk, therefore, if it is necessary to prescribe the drug, breastfeeding should be interrupted.

Side effect

Anaphylactic reactions: angioedema, bronchospasm, weakness, rarely - anaphylactic shock.

Skin reactions: rash, redness, urticaria. As with other cephalosporins, complications such as erythema multiforme, Stevens-Johnson syndrome, toxic skin necrosis are very rarely possible.

Gastrointestinal reactions: nausea, vomiting, abdominal pain, diarrhea may occur. As with the appointment of other broad-spectrum antibiotics, diarrhea can be a symptom of enterocolitis, which in some cases is accompanied by the appearance of blood in the stool. A special form of enterocolitis is pseudomembranous colitis (see 'Special instructions').

Liver reactions: increased liver enzymes (ALT, ACT, LDH, gamma-HT, alkaline phosphatase) and / or bilirubin.

Reactions from peripheral blood: neutropenia, rarely -granulocytosis, eosinophilia, thrombocytopenia, isolated cases of hemolytic anemia.

Reactions from the kidneys: deterioration of renal function (increase in creatinine levels), especially when combined with aminoglycosides, cases of interstitial nephritis are very rare.

Reactions from the central nervous system: encephalopathy (in the case of large doses), especially in patients with renal failure.

Reactions from the cardiovascular system: in isolated cases of arrhythmias, following a bolus administration through a central venous catheter (see 'Method and duration of use').

Others: fever, inflammation at the injection site, superinfection.

When treating borreliosis: Jarisch-Herxheimer reaction (during the first days of treatment), skin rash, itching, fever, leukopenia, increased liver enzymes, shortness of breath and discomfort in the joints.
In addition to the above, the rate of administration of the drug should be monitored (see 'Dosage and Administration'), as well as kidney function should be monitored in all cases of combined use of cefotaxime with aminoglycosides.
In patients requiring sodium restriction, the sodium
content of cefotaxime sodium salt (48.2 mg / g) should be taken into account. If the duration of the course of treatment is more than 10 days, the number of leukocytes should be monitored and, in the case of neutropenia, treatment should be discontinued.

Overdose
There is a risk of developing reversible encephalopathy when using high doses of ?-lactam antibiotics, including cefotaxime. There is no specific antidote.

Interaction with other medicinal products
Probenicid delays excretion and increases plasma concentrations of cephalosporins.
As with other cephalosporins, cefotaxime can potentiate the nephrotoxic effect of nephrotoxic drugs.
During therapy with cephalosporins, a positive Coombs test may occur.
The use of glucose oxidase methods for determining blood sugar levels is recommended, due to the development of false-positive results when using nonspecific reagents.
Compatibility notes: cefotaxime should not be mixed with other antibiotics, either in the same syringe or in the same infusion solution. This also applies to aminoglycosides.
For infusion, the following solutions can be used (concentration of cefotaxime 1 g / 250 ml): water for injection, 0.9% sodium chloride solution, 5% dextrose, Ringer's solution, sodium lactate, as well as: Hemaccel, Yonosteril, Macrodex 6%, Reomacrodex 12%, Tutofuzin V.

Special instructions
Anaphylactic reactions:

-the appointment of cephalosporins requires the collection of an allergic history (allergic diathesis, hypersensitivity reactions to ?-lactam antibiotics);

- if the patient develops a hypersensitivity reaction, then the treatment should be discontinued;

- The use of cefotaxime is strictly contraindicated in patients with a history of an immediate hypersensitivity reaction to cephalosporins. In case of any doubt, the presence of a doctor at the first administration of the drug is mandatory, due to a possible anaphylactic reaction.

- Known cross-allergy between cephalosporins and penicillins, which occurs in 5-10% of cases. For persons with a history of allergy to penicillins, the drug is used with extreme caution. Pseudomembranous colitis.
In the first weeks of treatment, pseudomembranous colitis may occur, manifested by severe, prolonged diarrhea. The diagnosis is confirmed by colonoscopy and / or histological examination. This complication is regarded as very serious: the administration of Claforan is stopped immediately and adequate therapy is prescribed, including oral vancomycin or metronidazole. When using lidocaine as a solvent, it is necessary to take into account the information provided in the section. 'Contraindications'.