Kefotex - 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 (except for Staphylococcus epidermidis and Staphylococcus aureus, methicillin-resistant), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, 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., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubacterium spp., Propionibacterium spp., Clostridium spp . (incl.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., Borrelia burgdorferi. Most strains of Clostridium difficile are stable.

Resistant to most beta-lactamases of gram-positive and gram-negative microorganisms.

Pharmacokinetics:

After a single intravenous (iv) dose of 0.5 g, 1 g and 2 g, the time to reach the maximum concentration (TCmax) is 5 minutes, the maximum concentration (Cmax) is 39, 101.7 and 214 μg / ml, respectively. After intramuscular (IM) administration in doses of 0.5 and 1 g of TCmax - 30 min, Cmax is 11 and 21 μg / ml, respectively. Connection with blood plasma proteins - 30 - 50%. Bioavailability is 90 to 95%.

Creates therapeutic concentrations in most tissues (myocardium, bone, gallbladder, skin, soft tissue) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. The volume of distribution is 0.25-0.39 l / kg.

The half-life (T1 / 2) -1h for iv injection and 1-1.5 h for v / m administration. 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 two inactive metabolites - M2 and M3).

In chronic renal failure (CRF) and in elderly people, T1 / 2 increases by 2 times. T1 / 2 in newborns - 0.75 - 1.5 hours, 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 For repeated iv in the dose of 1 g every 6 hours for 14 days of cumulation is not observed. Penetrates into breast milk, passes through the placental barrier.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to cefotaxime: central nervous system (meningitis), respiratory tract and LOP

- organs, urinary tract, bones and joints, skin and soft tissues (including infected wounds and burns), pelvic organs; peritonitis, sepsis, endocarditis, gonorrhea, abdominal infections, Lyme disease, infections against the background of immunodeficiency. Prevention of infections after surgical operations (including urological, obstetric-gynecological, on the organs of the gastrointestinal tract).

Contraindications:

- increased sensitivity to cefotaxime (including penicillins, other cephalosporins, carbapenems);

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

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

Pregnancy and lactation:The use of the drug during pregnancy is contraindicated. Cefotaxime is excreted in breast milk, therefore, if it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Intravenous (IV), intramuscularly (IM)

Adults and children with a body weight of 50 kg or more: for uncomplicated infections - in / m or / in, 1 g every 12 h; at infections of average gravity - in / m or in / in, on 1 -2 g every 8 ch; in acute uncomplicated gonorrhea - in / m, 0.5-1 g once; 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.

For the purpose of preventing the development of infections before the surgical operation, enter 1 g during the initial general anesthesia. If necessary, the administration is repeated 6 to 12 hours later.

At caesarean section (at the time of application of the clamps on the umbilical vein) - in / in 1 g, then 6 and 12 hours after the first dose - an additional 1 g.

With the clearance of creatinine (CC) 20 ml / min / 1.73 m² and a lesser daily dose is reduced by a factor of 2.

Premature and newborns up to 1 week - IV 50 mg / kg every 12 hours; aged 1-4 ned - 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 of injection solutions: for intravenous injection as a solvent used water for injection (0.5 -1 g diluted in 4 ml of the solvent), the drug is administered slowly, for 3-5 minutes; for intravenous infusion as a solvent used 0.9% solution of sodium chloride (NaCl) or 5% dextrose solution (1-2 g diluted in 50-100 ml of solvent). The duration of the infusion is 50-60 min. For the / m administration, water for injection or 1% lidocaine solution (for a dose of 250 mg-1 ml, 500 mg - 2 ml, for a dose of 1 g - 4 ml).

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.

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, hepatitis, jaundice, stomatitis, glossitis, pseudomembranous colitis.

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

From the side of 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 "hepatic" transaminases and alkaline phosphatase (APF), hypercreatininemia, hyperbilirubinemia, false-positive Coombs test. Local reactions: phlebitis, soreness along the vein, soreness and infiltration at the site of the / m introduction.

Other: Superinfection (in particular, candidal vaginitis).

Overdose:Symptoms: convulsions, encephalopathy (in case of administration of large doses, especially in patients with renal insufficiency), tremor, increased neuromuscular excitability.Treatment: symptomatic, there is no specific antidote.

Interaction:

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.

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

With the simultaneous use of cefotaxime with potentially nephrotoxic drugs (aminoglycoside antibiotics, furosemide) it is necessary to monitor the function of the kidneys (the risk of nephrotoxic action of the latter).

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 monitor the pattern of peripheral blood.

During treatment with cefotaxime, it is possible to obtain a false-positive Kum-bsa test and a false-positive urine reaction to glucose.

With the simultaneous use of cephalosporin antibiotics and ethanol, it is possible to develop disulfiram-like reactions (facial hyperemia, abdominal cramping, and in the epigastric region, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).

The effect on the ability to drive vehicles or other mechanisms during the treatment with the drug has not been studied. However, given the likelihood of side effects from the central nervous system, caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection of 250 mg, 500 mg, 1000 mg of active ingredient.

Packaging:Powder for the preparation of a solution for intravenous and intramuscular injection of 250 mg, 500 mg,1000 mg of active ingredient in a glass bottle (type I) sealed with a plug of chlorobutyl rubber, crimped with an aluminum cap, with additional packaging in the form of a plastic cap. By 1,3, 5, 6, 10, 30, 50, 60 or 100 together with instructions for use in cardboard pack.

Storage conditions:Store at a temperature not higher than 25 ° C out of the reach of children.

Shelf life:2.5 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N016209 / 01

Date of registration:25.02.2010

The owner of the registration certificate:Jepak InternationalJepak International India

Manufacturer: & nbsp

GEPACH INTERNATIONAL India

Representation: & nbspJEPAK INTERNATIONALJEPAK INTERNATIONALRussia

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Kefotex (Kefotex)