Cefotaxime-LEXVM - 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, Borrelia burgdorferi, Enterococcus spp., Enterobacter spp ., Escherichia coli, 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., Clostridium spp. (including Clostridium perfringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris, Providencia stuartii, Providencia rettgeri, Serratia marcescens, some strains of Pseudomonas aeruginosa, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.

It has in vitro activity against most strains of the following microorganisms,although the clinical significance of this is unknown: Salmonella spp. (including Salmonella typhi), Shigella spp.

Most strains of Clostridium difficile are stable.

Cefotaxime is resistant to most beta-lactamases of Gram-positive and Gram-negative microorganisms.

Pharmacokinetics:

After a single intravenous, (iv) injection at doses of 0.5, 1 and 2 g, the time to reach the maximum concentration (Tc_m_Oh) - 5 min, the maximum concentration in the blood plasma (C_m_Oh) is 39, 101.7 and 214.4 μg / ml, respectively. After intramuscular (IM) administration in, doses of 0.5 and 1 g of Tc_m_Oh - 0.5 h, C_m_Oh is 11.7 and 20.5 μg / ml, respectively. Connection with proteins plasma-30-50%. Biocontainment-90-95%. Cefotaxime easily penetrates into tissues and body fluids, including through the blood-brain barrier. Creates therapeutic concentrations in most tissues (myocardium, bone tissue, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. Cefotaxime penetrates the placental barrier, penetrates into breast milk. The volume of distribution is 0.25-0.39 l / kg.

Cefotaxime is partially metabolized in the liver, and one of the metabolites, deacetylcefotaxime, is pharmacologically active.

The half-life (T1 / 2) after IM is 1.0-1.5 h, after intravenous administration - 1.0 h. About 90% of cefotaxime is excreted by the kidneys, while 20-36% is unchanged, the rest is metabolites (15-25% in the form of pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites - M2 and M3). About 10% of cefotaxime is excreted with bile.

In chronic renal failure and in the elderly T1 / 2 cefotaxime is increased 2 times. T1 / 2 in newborns, 0.75-1.5, h, in preterm infants (body weight less than 1500 g) increases to 4.6 h; in children with a body weight of more than 1500 g - 3.4 hours. With repeated iv injections in a dose of 1 g every 6 h during 14 days of cumulation is not observed.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to cefotaxime: infections of the central nervous system (meningitis), lower respiratory

pathogens, ENT organs, urinary tract, bones, joints, skin and soft tissues (including infected wounds and burns), pelvic organs, uncomplicated gonorrhea, intra-abdominal infections (including peritonitis), bacteremia, septicemia, endocarditis, Lyme disease (borreliosis) , infection on the background of immunodeficiency. Prevention of infections after surgery (incl.urological, obstetric-gynecological, on the gastrointestinal tract).

Contraindications:

- increased sensitivity to cefotaxime, other cephalosporins, penicillins, carbapenems;

- hypersensitivity to lidocaine or other local anesthetic of the amide type; -heavy heart failure (when using lidocaine as a solvent);

- intracardiac blockades without an established pacemaker;

- the presence of bleeding in the anamnesis;

- children's age (in / m administration - up to 2.5 years when used as a solvent lidocaine).

Carefully:Newborn period (for intravenous administration), chronic renal failure, ulcerative colitis (including anamnesis).

Pregnancy and lactation:The use of the drug during the II and III period of pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

The drug is administered intravenously or intramuscularly.

Adults and children with a body weight of 50 kg or more: for uncomplicated infections - in / m or / in,

1 g every 12 hours; with uncomplicated acute gonorrhea - in / m, 0.5-1 g once; at infections of average gravity - in / m or iv; for 1-2 g every 8 hours; with sepsis - in / in, 2 g every 6-8 h, with life-threatening infections (with meningitis) - iv, 2 g every 4 h, maximum daily, dose -12 g. Duration of treatment is set individually.

In order to prevent the development of infections before surgery, injected IV or IM

during an initial general anesthesia once 1 g. If necessary, the administration is repeated

in 6-12 hours.

At caesarean section (at the moment of imposing of clamps on an umbilical vein) - in / in 1 g, then through

6 and 12 hours after the first dose - in addition to 1 g.

With a creatinine clearance of 20 ml / min / 1.73 square meters or less, the daily dose is reduced by a factor of 2.

Premature and newborn before 1 week - IV 50 mg / kg every 12 hours; at the age of 1-4 weeks-in / in 50 mg / kg every 8 hours; children, with a body weight of up to 50 kg - in / in or / m 50-180 mg / kg in 4-6 injections. In severe infections, incl. meningitis, the daily dose is increased to 100-200 mg / kg, IM or IV, in 4-6 receptions, the maximum daily dose is 12 g.

Rules for the preparation and administration of solutions: for intravenous injection as a solvent used water for injection (0.5-1 g diluted in 4 ml of solvent), injected slowly,within 3-5 minutes; for intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as a solvent (1 g dilute 50-100 ml of solvent). The duration of the infusion is 50-60 minutes. For the / m introduction, use as a solvent water for injection or 1% lidocaine solution (for a dose of 500 mg - 2 ml, for a dose of 1 g - 4 ml).

The solution containing lidocaine, can not be administered intravenously!

Side effects:

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

From the nervous system: headache, dizziness, reversible encephalopathy (especially in patients with renal insufficiency), motor disorders, convulsions.

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

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

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

Laboratory indicators: an increase in the activity of "liver" transaminases, lactate dehydrogenase, alkaline phosphatase, hyperbilirubinemia, an increase in the concentration of urea nitrogen and creatinine in the blood plasma, a false positive Coombs test.

From the urinary system: interstitial nephritis, impaired renal function, oliguria.

Other: superinfection, candidal vaginitis, candidiasis of the oral mucosa.

Local Reakies: with the / m introduction - soreness and infiltration at the injection site; with iv introduction - phlebitis, tenderness along the vein.

Overdose:

Symptoms: increased neuromuscular excitability, convulsions, tremor, encephalopathy (especially in patients with renal insufficiency).

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

Interaction:

With simultaneous administration with aminoglycosides, polymyxin B and "loop" diuretics, nephrotoxicity is enhanced.Increases the risk of bleeding when combined with antiaggregants, non-steroidal anti-inflammatory drugs. Drugs that block tubular secretion, increase plasma concentrations of cefotaxime and slow its elimination.

Pharmaceutically it is not compatible with solutions of other antibiotics in one syringe or dropper.

Special instructions:

The appointment of cephalosporins requires the collection of an allergic anamnesis (allergic diathesis, hypersensitivity reactions to β-lactam antibiotics). Patients who had a history of allergic reactions to penicillins, may have increased sensitivity to cephalosporin antibiotics.

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

When the drug is treated for more than 10 days, it is necessary to control the number of blood cells.

During treatment with the drug, it is possible to obtain a false-positive Coombs test and

a false positive urine reaction to glucose.

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

Effect on the ability to drive transp. cf. and fur:Given the profile of possible effects during the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection 0.5 g and 1 g.

Packaging:

For 0.5 g or 1 g of active substance is placed in bottles of glass, sealed with stoppers, crimped aluminum caps. 1 bottle is put in a pack with instructions for use.

10 bottles are placed in a box of cardboard box with instructions for use. For hospitals: 50 bottles are placed in a box of cardboard box with an equal number of instructions for use.

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 years 4 months. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001545

Date of registration:28.02.2012

The owner of the registration certificate:REDKINSKY EXPERIMENTAL FACTORY, CJSC REDKINSKY EXPERIMENTAL FACTORY, CJSC Russia

Manufacturer: & nbsp

REDKINSKY EXPERIMENTAL FACTORY, CJSC Russia

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Cefotaxime-LEXMM® (Cefotaxime-LEKSVM®)