Cefotaxime - instructions for use, dose, side effects, contraindications

Cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide range of action.

It is active against Gram-positive and Gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus, including strains forming penicillinase), Staphylococcus epidermidis (with the exception of Staphylococcus epidermidis and Staphylococcus aureus, methicillin resistant), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus spp., Enterobacter spp., Escherichia coli, Borrelia burgdorferi, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, Neisseria meningitidis, Neisseria gonorrhoeae (including strains forming penicillinase), Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubacterium 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, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. Most strains of Clostridium difficile are stable.Resistant to most beta-lactamases of gram-positive and gram-negative microorganisms.

Pharmacokinetics:After a single intravenous dose of 0.5 g, 1 g and 2 g, the time to reach the maximum concentration is 5 minutes, the maximum concentration is 39, 101.7 and 214 μg / ml, respectively. After intramuscular injection at doses of 0.5 and 1 g, the time to reach the maximum concentration is 0.5 hours and the maximum concentration is 11 and 21 μg / ml, respectively. The connection with plasma proteins is 30-50%. Bioavailability is 90-95%. Creates therapeutic concentrations in most tissues (myocardium, bone tissue, gall bladder, skin, soft tissue) and fluids (synovial, peri-cardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. The volume of distribution is 0.25-0.39 l / kg. Half-life - 1 hour with intravenous administration and 1-1.5 hours - with intramuscular injection. It is excreted by the kidneys - 20-36% unchanged, the rest is in the form of metabolites (15-25% in pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites-M2 and M3). In chronic renal failure and in elderly people, the elimination half-life increases 2-fold.Half-life in newborns is 0.75-1.5 hours, in preterm infants (body weight less than 1500 g) it increases to 4.6 hours; in children with a body weight of more than 1500 g - 3.4 hours. With repeated intravenous doses of 1 g every 6 hours for 14 days of cumulation is not observed. Penetrates into breast milk.

Indications:Infectious-inflammatory diseases caused by microorganisms susceptible to cefotaxime: infections of the central nervous system (meningitis), respiratory tract and LOP organs, urinary tract, bones, joints, skin and soft tissues (including infected wounds and burns), pelvic organs, peritonitis , bacteremia, septicemia, intra-abdominal infections, endocarditis, Lyme disease, gonorrhea, infections against the background of immunodeficiency. Prevention of infections after surgical operations (including urological, obstetric-gynecological, on the gastrointestinal tract).

Contraindications:Hypersensitivity to cefotaxime (including penicillins, other cephalosporins, carbapenems), children's age (intramuscular injection - up to 2.5 years when used as a solvent lidocaine).

Carefully:The period of neonatal (for intravenous administration), chronic renal failure, ulcerative colitis (including in the anamnesis).

Pregnancy and lactation:

Application in pregnancy is possible only in cases where the potential benefit to the mother exceeds the risk to the fetus. Adequate and strictly controlled studies in pregnant women were not conducted.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:Adults and children with a body weight of 50 kg or more: for uncomplicated infections - intramuscularly or intravenously, 1 g every 12 hours; with uncomplicated acute gonorrhea-intramuscularly, 0.5-1 g once; for infections of moderate severity - intramuscularly or intravenously, 1-2 g every 8 hours; with sepsis - intravenously, 2 g every 6-8 hours, with life-threatening infections (with meningitis) - intravenously, 2 g every 4 hours, maximum daily dose - 12 g. Duration of treatment is set individually.

For the purpose of preventing the development of infections before the surgical operation is introduced during the introductory general anesthesia once 1 g.If necessary, the administration is repeated after 6-12 hours.

At caesarean section (at the time of application of the clamps on the umbilical vein) - intravenously 1 g, then 6 and 12 hours after the first dose - an additional 1 g. When creatinine clearance is 20 ml / min / 1.73 m2 and less daily dose reduce by 2 times. Premature and newborn before 1 week - intravenously 50 mg / kg every 12 hours; at the age of 1-4 weeks - intravenously 50 mg / kg every 8 hours; children, with a body weight of up to 50 kg - intravenously or intramuscularly 50-180 mg / kg in 4-6 injections. In severe infections, including meningitis, the daily dose is increased to 100-200 mg / kg, intramuscularly or intravenously, in 4-6 receptions, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions: for intravenous injection, water for injections is used as a solvent (1 g is diluted in 4 ml of a solvent); for intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1 g is diluted in 50-100 ml of the solvent). The duration of the infusion is 50-60 minutes. For intramuscular injection water for injection or 1% lidocaine solution (1 g diluted in 4 ml of solvent) is used.

Side effects:

Allergic reactions: urticaria, chills or fever, rash, itching, bronchospasm, eosinophilia, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), angioedema, anaphylactic shock.

From the nervous system: headache, dizziness, encephalopathy, motor disorders, convulsions.

From the urinary system: disturbance of kidney function, oliguria, interstitial nephritis.

From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, stomatitis, glossitis, pseudomembranous colitis, hepatitis, jaundice.

From the hematopoiesis: hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hypocoagulation, agranulocytosis.

From the cardiovascular system: potentially life-threatening arrhythmias after a rapid bolus injection into the central vein.

Laboratory indicators: azotemia, increased urea concentration in the blood, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, hyperbilirubinemia, false positive Coombs test.

Other: Superinfection (in particular, candidal vaginitis).

Local Reactions: phlebitis, pain along the vein, soreness and infiltration at the site of intramuscular injection.

Overdose:Symptoms: convulsions, encephalopathy (in the case of the administration of large doses, especially in patients with renal insufficiency), tremor, increased neuromuscular excitability.

Treatment: symptomatic, maintenance of vital functions. There is no specific antidote.

Interaction:

Pharmaceutically incompatible with solutions of other antibiotics in one syringe or dropper.

Increases the risk of bleeding when combined with antiaggregants, non-steroidal anti-inflammatory drugs.

The probability of kidney damage increases with simultaneous administration with aminoglycosides, polymyxin B and "loop" diuretics.

Drugs that block tubular secretion, increase plasma concentrations of cefotaxime and slow its elimination.

Special instructions:

In the first weeks of treatment, pseudomembranous colitis can occur, which is manifested by severe prolonged diarrhea. At the same time, stop taking the drug and prescribe adequate therapy, including vancomycin or metronidazole.

Patients who had a history of allergic reactions to penicillins, may have increased sensitivity to cephalosporin antibiotics.

When the drug is treated for more than 10 days, it is necessary to control the number of blood cells. During treatment with cefotaxime, it is possible to obtain a false positive sample of Coombs and a false positive urine reaction to glucose.

With simultaneous use of cephalosporin antibiotics and ethanol, development of disulfiram-like reactions is possible, however, in clinical studies of cefotaxime (Claforan) no similar effect was observed when it was simultaneously used with ethanol.

Effect on the ability to drive transp. cf. and fur:During the treatment period, one should refrain from managing motor transport and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 1.0 g.

Packaging:

By 1.0 g of active substance into 10 ml vials, hermetically sealed with stoppers made of rubber compound, crimped with aluminum caps or caps combined.

Vials with a drug of 50 pieces are placed in boxes of cardboard with an equal number of instructions for the use of the drug (for hospitals).

1 bottle with the drug and instructions for use are placed in a pack of cardboard.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 of the year. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002117

Date of registration:06.12.2011

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)