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

Cefotaxime is a third generation cephalosporin antibiotic for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. It has a wide spectrum of antimicrobial action.

Pharmacodynamics

Highly 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, resistant to methicillin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus spp., Enterobacter spp., Escherichia coli, Haemophilus influenza (incl.strains forming penicillinase), Haemophilus parainfluenzae, Moraxella cattarhalis, Klebsiella spp., (including Klebsiella pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Acinetobacter spp., Corynebacterium diphtheria, Erysipelothrix rhusiopathie, 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 meningitides, 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 maximum concentration in the blood plasma (Cmax) occurs in 5 minutes and is 39 μg / ml, 101.7 μg / ml and 214 μg / ml, respectively. After intramuscular injection of the drug in doses of 0.5 g and 1 g of Cmax is determined after 0.5 hours and is 11 μg / ml and 21 μg / ml, respectively. Connection with blood plasma proteins - 30-50%. Bioavailability is 90-95%. The bactericidal concentration in the blood persists for more than 12 hours. The drug penetrates well into tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. The volume of distribution is 0.25-0.39 l / kg. In contrast to earlier cephalosporins, it penetrates the hemato-encephalic barrier.

The half-life (T1 / 2) is 1 hour for intravenous administration and 1-1.5 hours for intramuscular injection. It is excreted in significant amounts by kidneys in an unchanged form (20-36%) and in the form of active metabolites (15-25% in pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites - M2 and M3, devoid of antimicrobial action) . Partially excreted with bile through the gastrointestinal tract.

In chronic renal failure and in elderly people, the elimination half-life increases 2-fold. T1 / 2 in newborn - 0.75-1.5 hours in premature neonates (body weight less than 1500 g) was increased to 4.6 hours; in children with a body weight of more than 1500 g is 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, passes through the placental barrier.

Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation: respiratory and ENT organs infections, endocarditis, meningitis; urinary tract infections, kidneys, bones, joints, skin and soft tissues; infection of the pelvic organs,gonorrhea; infected wounds and burns, peritonitis, sepsis, abdominal infections, Lyme disease (borreliosis), salmonellosis, infection against immunodeficiency, prevention of infections after surgery (including urological, obstetric-gynecological, gastrointestinal tract).

Contraindications:Increased sensitivity to cephalosporin antibiotics (including other cephalosporins, penicillins, carbapenems); pregnancy, lactation; children's age to 2.5 years (for intramuscular injection).

Carefully:The period of neonatal (for intravenous administration), chronic renal failure, 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 you need to take the drug during lactation, you should stop breastfeeding.

Dosing and Administration:

Apply cefotaxime intramuscularly and intravenously (drip or drip). Adults and children with a body weight of 50 kg or more: for uncomplicated infections are administered intramuscularly or intravenously, 1 g every 12 hours; with uncomplicated acutegonorrhea - 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 h; for life-threatening infections, for example, with meningitis-intravenously 2 g every 4 hours, the maximum daily dose is 12 g. The duration of treatment is set individually.

In order to prevent the development of infections before surgery, one is administered once during the initial general anesthesia. If necessary, the administration is repeated after 6-12 hours.

At caesarean section - at the moment of imposing the clamps on the umbilical vein - 1 g intravenously is injected, then, 6 and 12 hours after the first dose - 1 g additionally.

When creatinine clearance (CC) is 20 ml / min / 1.73 m2 or less, the daily dose is reduced 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 weighing up to 50 kg - intravenously or intramuscularly 50-180 mg / kg in 4-6 injections. In severe infections, including meningitis, intravenously or intramuscularly in 4-6 procedures, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions: 0.25 g or 0.50 g of the drug in 2 ml (respectively 1 g in 4 ml) of sterile water for injection are dissolved for intramuscular injection, injected deep into the gluteus muscle.As a solvent, intramuscular injection also uses a 1% solution of lidocaine.

For intravenous administration 0.5 g - 1 g of cefotaxime is dissolved in 4 ml (2 g in 10 ml) of sterile water for injection, injected slowly for 3-5 minutes.

For intravenous infusion (within 50-60 minutes), dissolve 1-2 g of the drug in 50-100 ml of 0.9% isotonic sodium chloride solution or 5% solution of dextrose.

Side effects:

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

From the central nervous system: headache, dizziness.

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

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

On the part of the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, rarely - stomatitis, glossitis, pseudomembranous enterocolitis.

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

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

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

Other: Superinfection (in particular, candidal vaginitis).

Overdose:Symptoms: seizures, encephalopathy (in the case of high doses, especially in patients with renal insufficiency), tremor, neuromuscular excitability. Treatment: symptomatic, there is no specific antidote.

Interaction:

With the simultaneous use of cefotaxime with potentially nephrotoxic drugs (aminoglycosides, polymyxin AT, furosemide) it is necessary to monitor the function of the kidneys (the risk of nephrotoxic action of the latter). Increases the risk of bleeding when combined with antiaggregants, non-steroidal anti-inflammatory drugs.

Drugs that block tubular secretion, increase the plasma concentrations of cefotaxime and slow down its excretion.

Solutions cefotaxima pharmaceutically incompatible with solutions of other antibiotics in a single syringe or dropper.

Special instructions:

Before prescribing the drug, you need to collect an allergic medical history, especially with regard to beta-lactam antibiotics. There is a cross-allergy between penicillins and cephalosporins. Patients who had a history of allergic reactions to penicillin may have increased sensitivity to the antibiotics of the cephalosporin group.

When there are reactions of hypersensitivity (which are severe and even lead to death), the drug is canceled.

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.

With a duration of treatment with the drug for more than 10 days, it is necessary to monitor the picture of peripheral blood.

Possible detection of false positive Coombs test.

When determining glucose in the urine by a non-enzymatic method (for example, by the method of Benedict), false positive results are possible.

With the simultaneous use of cefotaxime and ethanol, it is possible to develop disulfiram-like reactions (flushing of the face and skin, stomach and stomach spasms, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).

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

Packaging:Powder for the preparation of a solution for intravenous and intramuscular injection of 250 mg, 500 mg and 1000 mg per bottle of clear, colorless glass, sealed with a rubber stopper and crimped with an aluminum cap and plastic lid; 1 bottle together with the instruction for use is placed in a cardboard box; 5, 20 or 50 bottles together with the instruction for use are placed in a cardboard box with the inscription "For hospitals".

Storage conditions:

At a temperature of no higher than 25 ° C, in a dry, dark place. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N012571 / 01

Date of registration:05.10.2009

The owner of the registration certificate:Aurobindo Pharma Co., Ltd.Aurobindo Pharma Co., Ltd. India

Manufacturer: & nbsp

AUROBINDO PHARMA, Ltd. India

Representation: & nbspAurobindo Pharma, ZAOAurobindo Pharma, ZAO

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Cetax (Cetax)