Cefotaxime

CEFOTAXIM-BHFZ powder for injection 1000 mg

Instruction manual

For medical use of the drug

Structure:

Active ingredient: cefotaxime;

1 bottle contains cefotaxime (in the form of cefotaxime sterile sodium salt) 500 mg or 1000 mg.

Dosage form.

Powder for injection.

Basic physical and chemical properties: white or slightly yellow powder, hygroscopic.

Pharmacotherapeutic group.

Antimicrobial agents for systemic use. beta-lactam antibiotics. third generation cephalosporins. atx code j01d d01.

Pharmacological properties.

Pharmacodynamics

Cefotaxime-BCHPZ is a semi-synthetic antibiotic of the third generation cephalosporins group, a wide spectrum of action, for parenteral administration. The drug is effective against many gram-positive and is highly active against gram-negative bacteria. It acts bactericidal on bacterial strains resistant to penicillin, aminoglycosides, sulfonamides. The antimicrobial mechanism of cefotaxime-BCPP is associated with inhibition of the activity of the transpeptidase enzyme, peptidoglycan blockade, and mucopeptide formation of the cell wall of microorganisms. The drug is resistant to four of the five beta-lactamases of gram-negative bacteria and penicillin staphylococci. It is active against Staphylococcus aureus, Staphylococcus epidermidis, some strains of Enterococcus spp., Streptococcus pneumoniae (especially Diplococcus pneumoniae), Streptococcus pyogenes (beta-hemolytic streptococci group A), Streptococcus bacillus, Streptococcus bacillus Bacterida bacillidae, Streptococcus bacillus, Bacteris bacillidae, diphtheriae, Erysipelothrix insidiosa, Eubacterium, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, including ampicillin-resistant strains, Haemophilus parainfluenzae, Klebsiella morinella, Neissa moriella , Propionibacterium, Proteus mirabilis, Proteus vulgaris, Proteus inconstans, Serratia spp., Veillonella, Yer sinia, Bordetella pertussis, Moraxella, Aeromonas hydrophilia, Fusobacterium, Bacteroides spp., Clostridium species, Peptostreptococcus species, Peptococus spp.

Affects some strains of Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, Bacteroides fragilis, Clostridiun difficile. May affect multi-resistant strains that are resistant to penicillins, first-generation cephalosporins, aminoglycosides. The drug is less active against gram-positive cocci than cephalosporins of I-II generations.

To the action of the drug resistant group D streptococci, Listeria spp. and methicillin-resistant staphylococci.

Pharmacokinetics

The maximum concentration in the blood after intramuscular administration of the drug in doses of 500 mg and 1000 mg is observed 30 minutes after administration and is 11 μg / ml and 21 μg / ml, respectively. 5 minutes after intravenous administration of 500 mg, 1000 mg or 2000 mg, the maximum concentration in the blood is 39, 100, 214 μg / ml, respectively. In blood, the drug is 25-40% bound to blood proteins. The bactericidal concentration in the blood lasts more than 12 hours. The drug penetrates well into tissues (creates an effective concentration in the myocardium, bone tissue, gall bladder, skin, soft tissues), body fluids (determined in effective concentrations in the cerebrospinal, pericardial, pleural, peritoneal, synovial fluids), passes through the placenta, penetrates into breast milk. Cefotaxime-BCHPZ is excreted in a significant amount with urine (90%) (unchanged, about 60–70% and in the form of active metabolites, about 20–30%, of which 15–25% is the main metabolite - deacetylcefotaxime, which has antimicrobial activity). The half-life with intravenous administration is 1 hour, with intramuscular administration - 1-1.5 hours. With repeated intravenous doses of 1000 mg every 6 hours for 14 days, cumulation is not observed. In infants, the half-life is 0.75–1.5 hours, in premature infants — from 1.4 to 6.4 hours, in patients older than 80 years and with renal failure, the half-life of the drug increases by approximately 2 times.

Clinical characteristics.

Indications.

Infections caused by microorganisms sensitive to the action of the drug:

• infections of ENT organs (tonsillitis, otitis media);
• respiratory tract infections (bronchitis, pneumonia, pleurisy, abscesses);
• urinary tract infections;
• septicemia, bacteremia;
• intra-abdominal infections (including peritonitis);
• infections of the skin and soft tissues;
• infections of bones and joints;
• meningitis (except listeriosis) and other central nervous system infections;
• prevention of infections after surgery on the digestive tract, urological and obstetric-gynecological operations.

Contraindications

Hypersensitivity to cephalosporin antibiotics and other beta-lactam antibiotics, hypersensitivity to lidocaine (intramuscular injection); history of bleeding, history of enterocolitis (especially ulcerative colitis).

AV blockade without an established heart rate driver, severe heart failure.

Interaction with other drugs and other types of interactions.

With nephrotoxic drugs (aminoglycosides) and potent diuretics (ethacrylic acid, furosemide), colistin, polymyxin, the risk of developing renal failure increases.

With bacteriostatic antibiotics (e.g. tetracyclines, erythromycin and chloramphenicol), an antagonistic effect is possible.

With aminoglycoside solutions should not be mixed, they must be entered separately.

With nifedipine, the bioavailability of cefotaxime is increased by 70%.

With probenecid, tubular secretion of cefotaxime is blocked and its half-life is prolonged.

Do not use cefotaxime with lidocaine:

• with intravenous administration;
• children under 30 months;
• patients with a history of hypersensitivity to lidocaine;
• heart block patients.

During treatment with cefotaxime, the effectiveness of oral contraceptives may decrease, therefore, additional contraception must be used during this period.

Features of the application.

With caution, prescribe the drug for impaired renal and hepatic function; in case of impaired renal function, the dose should be reduced taking into account the severity of renal failure and the sensitivity of the pathogen.

With prolonged use of the drug, kidney function should be monitored, and dysbiosis should be prevented. It is advisable to regularly monitor the cellular composition of peripheral blood, liver function. When using the drug, the development of a false positive Coombs test is possible.

Anaphylactic reactions. The use of cephalosporins requires clarification of the allergological history (allergic diathesis, hypersensitivity reactions to beta-lactam antibiotics). If a patient develops a hypersensitivity reaction, treatment should be discontinued. The use of cefotaxime is strictly contraindicated in patients with a history of immediate hypersensitivity reactions to cephalosporins. In case of any doubt, the presence of a doctor at the first injection of the drug is necessary due to the possible development of an anaphylactic reaction. A cross-allergic reaction between cephalosporins and penicillins is known, which occurs in 5–10% of cases.

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. These complications are regarded as very serious: immediately stop administering the drug and prescribe adequate therapy, including oral administration of vancomycin or metronidazole.

The combination of cefatoxime with nephrotoxic drugs requires monitoring of renal function, the use of more than 10 days - monitoring of blood composition. For elderly and debilitated patients, prescribe vitamin K (prevention of hypocoagulation).

Each gram of the drug contains approximately 0.048 g of sodium, which should be considered for patients on a diet with a controlled sodium content.

As with other broad-spectrum antibiotics, long-term use can lead to increased growth of insensitive microorganisms, which requires discontinuation of treatment. If superinfection occurs during treatment, antimicrobial therapy should be used.

When determining the level of glucose in the urine by the recovery method, false-positive results can be obtained. An enzyme test should be used to prevent this.

During treatment, alcohol cannot be used, since effects similar to disulfiram are possible (facial flushing, cramping in the abdomen and stomach, nausea, vomiting, headache, lowering blood pressure, tachycardia, difficulty breathing).

When using lidocaine as a solvent for intramuscular injection, a skin test for lidocaine tolerance should be done before injection.

Incompatibility.

It should not be administered in the same container with other drugs, except for the solutions indicated in the instructions.

Use during pregnancy or lactation.

The use of the drug during pregnancy is contraindicated.

For the period of treatment should stop breast-feeding.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Due to the possibility of adverse reactions from the nervous system, you should avoid driving or working with other mechanisms during the treatment period.

Dosage and administration.

Before using the drug, it is necessary to conduct skin tests for tolerance.

Cefotaxime-BHFZ administered intramuscularly and intravenously, in a stream and drip.

For intramuscular administration, dissolve 500 mg of Cefotaxime-BCHPZ in 2 ml, and 1000 mg in 4 ml of sterile water for injection or 1% lidocaine solution and inject deep into the gluteus muscle.

For intravenous administration, dissolve 500 mg of Cefotaxime-BCHPZ in 4 ml, 1000 mg in 8 ml, and 2000 mg in 10 ml of sterile water for injection and inject slowly, for 3-5 minutes.

For intravenous infusion, dissolve 1000–2000 mg of the drug in 50–100 ml of 0.9% isotonic sodium chloride solution or 5% glucose solution and administer for 50-60 minutes.

The doctor sets the duration of the course of treatment individually.

A single dose of Cefotaxime-BCPP for adults and children weighing 50 kg or more - 1000 mg every 12 hours, in severe cases, increase the dose to 2000 mg every 12 hours or increase the number of administrations up to 3-4 times a day, bringing the total daily dose to maximum - 12 g.

To prevent infectious complications, before surgery, during administration of anesthesia, introduce 1000 mg of the drug, and if necessary, repeat the injection after 6-12 hours.

For uncomplicated infections, as well as for urinary tract infections, the drug should be administered intramuscularly or intravenously at a dose of 1 g every 12 hours;

with uncomplicated acute gonorrhea, the drug is administered intramuscularly or intravenously at a dose of 1 g once a day;

for moderate infections, prescribe the drug in a dose of 1-2 g every 12 hours;

in severe infections (meningitis), appoint a dose of 2 g of the drug intravenously every 6-8 hours.

In premature infants and children up to 1 week old, the daily dose of the drug is 50 mg / kg, divided into two doses in equal doses, administered intravenously.

For children from 1-4 weeks, the daily dose of the drug is 50-100 mg / kg, divided into 3 equal doses and administered intravenously.

For children weighing up to 50 kg, the daily dose of Cefotaxime-BCHFZ is 50-100 mg / kg and is divided into 3-4 intramuscular or intravenous doses. In severe infections, including meningitis, it is recommended that the daily dose be increased to 100-200 mg / kg body weight and administered 4-6 times intravenously or intramuscularly.

In renal failure (with creatinine clearance of 10 ml / min or less), reduce the dose by 2 times.

Children.

For children under 2.5 years of age, do not intramuscularly administer the drug.

Overdose.

Symptoms: fever, leukopenia, thrombocytopenia, acute hemolytic anemia, skin, gastrointestinal and liver reactions, shortness of breath, renal failure, stomatitis, anorexia, temporary hearing loss, loss of orientation in space, convulsions, encephalopathy (especially in renal failure).

Treatment: there is no specific antidote. Serum cefotaxime can be reduced by hemodialysis or peritoneal dialysis. If necessary, carry out symptomatic therapy.

If anaphylactic shock occurs, appropriate measures should be taken immediately. At the first signs of a hypersensitivity reaction (skin rashes, urticaria, headache, nausea, loss of consciousness), cefotaxime should be discontinued. In case of a severe hypersensitivity reaction or anaphylactic reaction, appropriate therapy should be started (administration of epinephrine and / or glucocorticoids). In these clinical conditions, additional measures may be required, for example, artificial respiration, the use of histamine receptor antagonists. In case of vascular insufficiency, resuscitation measures should be taken.

Adverse Reactions

Digestive tract: nausea, vomiting, diarrhea, flatulence, abdominal pain, dysbiosis, stomatitis, glossitis, pseudomembranous colitis.

Immune system, skin and subcutaneous tissue: hyperemia, rash, pruritus, urticaria, acute generalized exanthematous pustulosis, bronchospasm, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome), fever, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, anaphylactic, shock.

Hepatobiliary system: hepatitis, acute liver failure, impaired liver function, jaundice, cholestasis.

Biochemical parameters: increased levels of hepatic transaminases, lactate dehydrogenase, alkaline phosphatase and bilirubin, urea nitrogen and creatinine concentrations, positive Coombs test.

Blood: granulocytopenia, neutropenia, transient leukopenia, thrombocytopenia, agranulocytosis, anisocytosis, hypoprothrombinemia, hemolytic anemia, eosinophilia, hypocoagulation.

Nervous system: headache, dizziness, cramps, reversible encephalopathy, increased fatigue, weakness.

Local reactions: pain and infiltration at the injection site, tissue inflammation, phlebitis.

Effects due to biological effects: superinfection is possible (including candidiasis, vaginitis).

Other: bleeding and hemorrhage, autoimmune hemolytic anemia, interstitial nephritis, arrhythmia (with rapid jet administration).

In the treatment of spirochete infections, a complication similar to the Herxheimer reaction may occur. This can lead to fever, chills, headaches, and joint pain.

Shelf life.

2 years.

After preparation, the solution can be stored for 24 hours in a refrigerator at a temperature of 5 ± 3 ° C in a dark place and 12 hours at room temperature (20 ± 5 ° C) without protection from light.

From a microbiological point of view, a ready-to-use preparation should be used immediately. If it is not used immediately, then the responsibility for the time and storage conditions during use rests with the consumer.

Storage conditions.

In the original packaging at a temperature not exceeding 25 ° C.

Keep out of the reach of children!

Packaging.

Bottle No. 1 (without pack): 55 bottles in a box; bottle number 1 (in a pack): 1 bottle in a pack; bottles No. 5 (in a pencil case): 5 bottles in a cartridge, 1 cartridge in a pencil case; bottle number 1 (in a pack): 1 bottle complete with solvent (water for injection), 5 ml in an ampoule in a cassette, 1 cassette in a pack; bottle No. 1 (in a pack): 1 bottle complete with a solvent (water for injection), 5 ml in an ampoule in a pack with a cardboard partition.

Vacation category.

On prescription.

Manufacturer.

Public Joint Stock Company “Scientific and Production Center“ Borshchag Chemical and Pharmaceutical Plant ”.

The location of the manufacturer and his address of the place of business.

Ukraine, 03134, Kiev, st. peace, 17.