Cefotaxime instructions for use: how many days to inject. Pharmacological group of the substance Cefotaxime. Release form and composition

Often, most diseases have to be treated with antibacterial drugs. One of them is Cefotaxime. The medication is available in the form of a powder that must be diluted.

Action of Cefotaxime

Cefotaxime is a broad-spectrum antibiotic that belongs to the group of 3rd generation cephalosporins. The medication has an antibacterial mechanism of action on pathogenic microorganisms. Effective against many gram-positive and gram-negative bacteria resistant to penicillin, aminoglycosides and sulfonamides.

The mechanism of the antimicrobial action of the drug is associated with inhibition of the activity of the transpeptidase enzyme, blockade of peptidoglycan and destruction of the mucopeptide of the cell wall of microorganisms. The drug is administered only intravenously or intramuscularly.

Cefotaxime during lactation (breastfeeding, breastfeeding): compatibility, dosage, elimination period

Dilution of antibiotics

LIDOCAINE, local anesthetic, instructions, mechanism of action, side effects

The antibacterial agent accumulates well in tissues in which inflammatory processes occur. It is also concentrated in the heart muscle, subcutaneous fatty tissue, gall bladder and skin. Easily penetrates into the cerebrospinal, pleural and synovial fluids. The medication causes almost no damage to the liver. Excreted 90% in urine.

Action of Lidocaine

The drug has local anesthetic and antiarrhythmic effects. It is used for conduction, infiltration and terminal anesthesia. The anesthetic effect occurs due to inhibition of nerve conduction, due to the blockade of sodium channels in nerve fibers and endings.

The antiarrhythmic effect is due to the ability of the drug to increase the permeability of membranes to potassium, block sodium channels and stabilize cell membranes.

Can I take it at the same time?

Since Cefotaxime injections are very painful, it is recommended to mix the drug with lidocaine to dull the pain.

How to dilute Cefotaxime with lidocaine?

The drugs are diluted only for intramuscular injections in the following proportion: 0.5 g of Cefotaxime per 2 ml of 1% lidocaine solution. For a dose of 1 g you will need 4 ml of anesthetic liquid. You can also dilute 1 g of Cefotaxime in powder form with water for injection (2 ml) and 2 ml of lidocaine (1%).

An anesthetic liquid is injected into the antibiotic bottle using a syringe. After this, the bottle of antibiotic is thoroughly shaken so that all the ingredients are mixed until smooth.

Mode of application

Before administering the drug, it is necessary to do a skin test for sensitivity to the antibiotic and lidocaine.

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Dosage regimen:

  1. For adults, a single dose is 1 g every 12 hours. If necessary, the doctor can increase the dosage to 2 g every 12 hours or increase the number of injections to 3-4 times a day. The maximum daily dose is 12 g.
  2. In case of impaired renal function, half the dosage is administered.
  3. In the presence of acute gonorrhea, the medication should be administered once in a dose of 0.5-1 g.
  4. Children weighing up to 50 kg (over 2.5 years) are prescribed a dosage of 50-180 mg/kg in 4-6 administrations. In difficult situations, 100-200 mg of the substance per 1 kg of weight is prescribed. The maximum daily volume is 12 g.

The solution is injected slowly and deeply into the gluteal muscle. After completing the manipulation, it is necessary to massage the injection site with alcohol-preserved cotton wool to prevent the formation of a lump. The solution cannot be prepared for future use. The course of treatment is determined individually.

Prolonged diarrhea may occur after starting treatment. In this case, it is necessary to stop therapy with this drug.

Contraindications to the use of Cefotaxime and Lidocaine

It is prohibited to give injections under the following conditions and pathologies:

  • individual intolerance to Cefotaxime or Lidocaine;
  • the appearance of allergies;
  • 1st and 4th trimesters of pregnancy;
  • lactation period;
  • presence of bleeding;
  • enterocolitis;
  • acute colitis;
  • children's age up to 2.5 years.

Injections should be prescribed with caution to people suffering from impaired liver and kidney function.

Side effects of Cefotaxime and Lidocaine

During treatment, negative manifestations may occur such as:

  • allergic reactions: rash, urticaria, fever, Quincke's edema;
  • vomit;
  • nausea;
  • pain in the abdominal cavity;
  • intestinal disorder;
  • jaundice;
  • colitis;
  • changes in blood composition;
  • migraine;
  • soreness and hardness at the injection site;
  • interstitial nephritis;
  • hemolytic anemia.

If side effects occur, you should consult your doctor.

Cefotaxime is a drug belonging to the group of latest generation antibiotics.

Due to its composition and pharmacological action, it is used to treat a wide variety of infectious diseases.

Presented in the form of a white powder, sold in glass bottles. The powder is used to prepare a solution.

The white powder of the drug is presented in the form of a sodium salt and consists of anhydrous cefotaxime.

The drug is administered intramuscularly or intravenously.

pharmachologic effect

The drug acts as a bactericidal agent, since it is active against gram-positive and gram-negative microorganisms.

In addition, it has a broad spectrum antimicrobial effect. Due to its composition, it is often used in the treatment of infectious diseases of the kidneys and lungs.

Pharmacokinetics of the drug

Cefotaxime is a quickly absorbed drug. Rapid absorption is noted - within 5 minutes after application, the constituent components enter the bloodstream and increase performance.

The biological availability of the drug is 95%. Removal of the presented drug from the body occurs within 1-1.5 hours, depending on the method of administration.

Up to 40% of the constituent components are excreted from the body in the urine. The remaining part of the substances turns into metabolites.

Mechanism of action

After administration of the drug, active destruction of the cell walls of existing microorganisms occurs.

Due to the destruction of the wall, their breathing is significantly impaired, as a result of which microorganisms die and their reproduction stops.

It should also be noted that due to the destruction of cells, fewer toxins and harmful substances enter the human body, which have an adverse effect on the general condition and further development of the disease.

Use of the product for treatment and prevention

Indications for use of Cefotaxime:

Contraindications for use

Despite its beneficial pharmacological actions, Cefotaxime has many contraindications.

These include:

  • individual intolerance and hypersensitivity to the constituent components of the drug - penicillins and cephalosporins;
  • cannot be used for treatment during pregnancy and lactation;
  • should not be used to treat diseases in children under two years of age.

Due to its rather serious contraindications, for example, hypersensitivity to components, the drug is used to treat diseases only as prescribed by a doctor.

Assignment scheme

Before using Cefotaxime, you should carefully study the instructions for use and permissible dosages of the drug.

Use of injection solution

Preparation of the solution requires compliance with the rules and dosage of the drug, which differ significantly depending on the method of administration.

There are three methods of treatment using the presented medicine:

  1. Intravenous injection– per 1 g of active substance there are 4 ml of special sterile water intended for preparing the solution. The prepared injection composition is injected into the vein slowly, over at least 3 minutes.
  2. Intravenous infusion– use 1-2 g of active substance and 50-100 ml of solvent. The composition of the solvent may vary depending on the nature and severity of the disease. A solution of sodium chloride with a percentage of 0.9%, as well as glucose 5%, can be used here. The infusion time is at least 50-60 minutes.
  3. Intramuscular injection– the method of dissolving the active substance is the same as in the case of intravenous injection. A 1% lidocaine solution can also be used as a solvent.

Compliance with the proportions in preparing the solution for injection is very important. The slightest mistakes can lead to an overdose and side effects.

Details on how to dilute antibiotics:

Basic doses

The dosage of Cefotaxime may vary dramatically depending on the degree and nature of the disease.

After conducting the necessary examination, the specialist will draw up an administration regimen and dosage.

  1. Treatment of simple infections without complications carried out by injecting the solution every 8-12 hours. To prepare the solution, 1 g of the active ingredient is used.
  2. Moderate infections require administration of the drug every 12 hours, where 1-2 g of the active substance is used for preparation.
  3. Serious illnesses require administration of the drug every 4-8 hours. The solution is made using 2 g of active substance.
  4. As a preventive measure no more than 1 g of substance is used in preparing the solution. The frequency of injections should not exceed 6 hours.

The severity of the disease will be determined only by the attending physician based on the data obtained from the examination. Independent use and “prescribing” of the drug is strictly prohibited.

Overdose and additional instructions

If the dosage of the drug is not observed, unpleasant side effects may occur, which will only aggravate the patient’s already serious condition.

Side effects include nausea and vomiting, headaches and dizziness, increased or decreased blood pressure, diarrhea or constipation, and skin rashes.

The most dangerous side effects include convulsions and increased body temperature with fever. True, this is only possible in the case of a fairly serious overdose.

When using the medicine as treatment and prevention, you should remember:

  1. Side effects may occur in the first 2-3 days of using the drug. In most cases, in such situations, the medication is discontinued or the dosage and regimen of use are revised.
  2. Drinking alcohol during treatment is strictly contraindicated. since this combination can lead to abdominal pain and other side effects.
  3. Interactions with other medications may result in bleeding and skin lesions. The specialist who determines the treatment regimen takes this factor into account.
  4. Prohibited for use during pregnancy and lactation– the active substance penetrates the placenta and enters breast milk.
  5. Children can only take this product from 2.5 years of age.. In emergency cases, it is prescribed to premature and newborn babies. The dosage of the drug in one injection should not exceed 50 mg/kg.

The drug must be carefully studied and used carefully, since the chemical composition of the drug can cause many side effects and lead to deterioration of health.

This is important - the opinion of doctors and patients

In order to know how effective and safe Cefotaxime is, as well as the nuances of its use, we recommend studying reviews from patients and specialists.

For severe urinary problems, I always prescribe Cefotaxime to my patients. This drug has already proven itself as a fast-acting drug.

In case of non-compliance with the dosage, problems are noted in the form of side effects.

Petr Valentov, urologist, Moscow

I often have exacerbations and... I dropped some medicine. I have not suffered from pain or other troubles for several months now.

Tatyana Somova, 29 years old, St. Petersburg

I work as a loader, so a slight breeze is dangerous for me. With pyelonephritis, he is immediately taken away in an ambulance. They always inject Cefotaxime. After just a couple of days, the first symptoms and pain disappear.

Now they use this remedy as a preventive measure. The doctor prescribed it. Helps.

Oleg Grishin, 41 years old, Vladivostok

From all the available reviews about treatment with this drug, we can conclude that Cefotaxime has a positive effect on the body in the treatment and prevention of inflammatory and infectious diseases.

During use, it is important to follow the dosage prescribed by your doctor.

Purchase and storage

Cefotaxime is produced in glass bottles, the price of one with 1 gram of the active drug is no more than 25 rubles.

The shelf life of the drug is 2 years. Storage temperature should not exceed +25 degrees Celsius.

The sale of the medicine is carried out only with a prescription from a doctor.

If there is no medicine in the pharmacy

Among the most famous analogues of Cefotaxime are:

  1. Ceftriaxone. This analogue has a similar composition and effect. However, as a side effect, bile stagnation is also noted here, which was not detected in Tsifotaxime. Therefore, the answer to the question of whether it is better to use Cefotaxime or Ceftriaxone is obvious.
  2. Claforan. This analogue is no different from Tsifotaxim. But due to the fact that the drug is imported, its price is higher and lies within 120 rubles.

Pharmacological group: antibiotics
Systematic (IUPAC) name: (6R,7R,Z)-3-(acetoxymethyl)-7-(2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido)-8-oxo-5-thia -1-azabicyclooct-2-ene-2-carboxylic acid
Trade names Claforan; Cefatam (LGls)
Legal status: Available by prescription only
Application: intravenous
Metabolism: liver
Half-life: 0.8-1.4 hours
Elimination: 50-85% renal
Formula: C 16 H 17 N 5 O 7 S 2
Mol. mass: 455.47 g/mol

Cefotaxime is a third generation cephalosporin antibiotic. Like other third-generation cephalosporins, it has a broad spectrum of activity against gram-positive and gram-negative bacteria. In most cases, the drug is considered equivalent to Ceftriaxone in terms of safety and effectiveness.

Mechanism of action

Cefotaxime inhibits bacterial cell wall synthesis by binding to one or more of the penicillin binding proteins (PBPs). This inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus preventing cell wall biosynthesis. The bacteria are eventually lysed due to the continued activity of autolytic cell wall enzymes (autolysins and murein hydrolases) while cell wall formation is delayed. Cefotaxime, like other β-lactam antibiotics, not only blocks the division of bacteria, including cyanobacteria, but also blocks the division of cyanella, the photosynthetic organelles of Glaucophytes, and the division of bryophyte chloroplasts. However, the drug does not have any effect on the plastids of highly developed vascular plants. This supports the endosymbiotic theory and points to the evolution of plastid partitioning in land plants.

Bacterial sensitivity spectrum

Cifotaxime is used to treat a wide range of diseases associated with the activity of bacteria that cause infections of the bones, central nervous system, skin and lower respiratory tract. Known species include Streptococcus, Staphylococcus, Enterococcus and Escherichia. The susceptibility data for several microorganisms of medical importance are presented below.

Haemophilus influenzae: ≤ 0.007 µg/ml - 0.5 µg/ml Staphylococcus aureus: 0.781 µg/ml - 172 µg/ml Pneumococcus: ≤ 0.007 µg/ml - 8 µg/ml

Clinical Application

Cefotaxime is used for infections of the respiratory tract, skin, bones, joints, genitourinary system, meninges and blood. It generally has a broad spectrum of activity against most gram-negative bacteria, with the exception of Pseudomonas. It is also effective against most gram-positive cocci, except enterococcus. It has moderate activity against the anaerobic organism Bacteroides fragilis. For meningitis, Cefotaxime crosses the blood-brain barrier better than Cefuroxime.

Cefotaxime: instructions for use

Lower respiratory tract infections, including pneumonia caused by Streptococcus pneumoniae (with reduced sensitivity to penicillin), E. coli, Klebsiella spp., H. influenzae (including ampicillin-resistant strains), P. mirabilis, S. marcescens i Enterobacter spp. Urinary tract infections caused in particular by Citrobacter SPP, Enterobacter SPP, E. coli, Klebsiella SPP, P. mirabilis, Proteus vulgaris, M. morganii, Providencia rettgeri and S. marcescens.. Cases of gonorrhea without complications, including those caused strains of gonococci producing penicillinase. Infections in the pelvic area, including those caused by E.coli, P. Mirabilis, anaerobic cocci - Peptostreptococcus spp. and Peptococcus spp., as well as some strains of Bacteroides spp, including B. fragilis, Clostridium spp. Sepsis and/or bacteremia caused, in particular, by strains of E. coli, Klebsiella spp, S. marcescens. Skin and soft tissue infections caused by E.coli, Enterobacter SPP, Klebsiella SPP, P. Mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Pseudomonas SPP, S. marcescens, Bacteroides spp. and anaerobic cocci - Peptostreptococcus spp. i Peptococcus spp. Intra-abdominal infections, including peritonitis caused by E.coli, Klebsiella spp., Bacteroides spp., Peptostreptococcus spp. and Peptococcus spp. Infections of bones and joints, including those caused by strains of H. influenzae, Streptococcus spp., P. mirabilis. CNS infections, including meningitis caused by N. meningitidis, H. influenzae, S. pneumoniae, K. pneumoniae and E. coli. Prevention of infections in the postoperative period, numerous studies have shown that its effectiveness does not exceed the effectiveness of prevention using first generation cephalosporins.

Contraindications

Hypersensitivity to cephalosporins. Caution should be used in patients allergic to penicillin, due to the possibility of a cross-reaction, gastrointestinal diseases (especially colitis), elderly patients or patients with renal failure. Cefotaxime should be used with caution in patients concurrently taking aminoglycoside antibiotics or potent diuretics. For children under 2 months of age, the drug is administered intravenously only.

Drug interactions

Cefotaxime exhibits a synergistic effect with aminoglycoside antibiotics, vancomycin, and anticoagulants (coumarin derivatives). Probenecid, azlocillin and mezlocillin significantly lengthen the time of its action. For infections involving anaerobes, it must be used in combination with metronidazole or clindamycin. Do not mix with aminoglycoside antibiotics, metronidazole, sodium bicarbonate due to incompatibility. Solutions of cefotaxime should not be mixed (for example, in the same syringe) with solutions of aminoglycosides, and if used simultaneously, injections of these drugs must be administered to different sites. During the use of cefotaxime, false-positive results of reduction tests for the presence of glucose in the urine are possible. In serological tests, the Coombs test result may be false positive.

Cefotaxime: side effects

Local reactions: phlebitis after intravenous injection, pain at the injection site, induration and soreness after intramuscular injection; hypersensitivity: rash, itching, urticaria, bronchospasm, fever; gastrointestinal disorders: diarrhea, sometimes nausea and vomiting, very rarely pseudomembranous colitis; temporary increase in the activity of liver transaminases and alkaline phosphatase; temporary increase in serum creatinine levels; changes in blood composition: granulocytopenia, leukopenia, eosinophilia, neutropenia, hemolytic anemia, thrombocytopenia; headache; superinfection caused by Candida (inflammation of the vaginal mucosa). In case of overdose, especially in patients with renal failure, there is a risk of developing reversible encephalopathy. Symptomatic treatment. Hemodialysis or peritoneal dialysis can be used.

Cefotaxime: dosage

Intramuscular or intravenous Adults and children aged 12 years: 2 g per day in 2 doses, moderate and severe infections 3-6 g per day in 3 doses, for severe infections requiring higher doses, for example, sepsis 6-8 g per day in 3-4 intravenous injections, for life-threatening infections intravenously 12 g per day in 6 injections. For gonorrhea, a single dose of 1 g intramuscularly. The maximum dose is 12 g per day. Children. Premature children and infants under 7 days of age - iv 50-100 mg/kg body weight per day in 2 injections. Infants aged 7 days to 1 month - IV 75-150 mg/kg body weight per day in 3 injections. Infants over 2 months and children under 12 years of age: children weighing less than 50 kg intramuscularly or intravenously 50-180 mg/kg body weight per day in 4-6 injections. Higher doses should be used for severe infections, including meningitis; in children weighing more than 50 kg, the same dose is usually used as in adults. The maximum dose is 12 g per day. Children under 2.5 years of age should not be administered solutions of the drug with lidocaine. As a prophylaxis, 1 g 30-90 minutes before surgery. Depending on the indications, the dose can be re-administered after 6 and 12 hours. In individuals with a creatinine clearance of 5-20 ml/min, it is recommended to reduce the dose by half; at clearance<5 мл / мин вводить 0,5 г через каждые 12 часов.

Availability:

Cefotaxime is used to treat severe bacterial infections caused by sensitive microorganisms: central nervous system infections (meningitis); infections of the respiratory tract and ENT organs; urinary tract; bone and joint infections; skin and soft tissue infections; pelvic organ infections; chlamydia; gonorrhea; infected wounds and burns; peritonitis; sepsis; abdominal infections; endocarditis; Lyme disease (borreliosis); salmonellosis; infections due to immunodeficiency. The drug is also used to prevent infections after surgical operations (including urological, obstetric-gynecological, and gastrointestinal). The drug is available with a prescription.

Notes

It is recommended to monitor renal function in seriously ill patients receiving high doses of antibiotics. In patients taking cefotaxime for more than 10 days, blood morphology should be monitored.

Bacterial infections are often caused by pathogenic microorganisms that are resistant to most antibiotics used. In addition, microbes can acquire resistance to drugs during therapy. In such cases, cephalosporins are prescribed, which are strong antibacterial drugs with an extended spectrum of activity. These include Cefotaxime - injections of this medication can stop the proliferation of gram-positive and gram-negative microorganisms that are resistant to other antimicrobial agents.

Effect of injections of the antibiotic Cefotaxime

The presented drug is a 3rd generation cephalosporin, which combines high efficiency and the highest possible safety.

Cefotaxime leads to rapid and irreversible destruction of the cell walls of bacteria, which causes their instant death.

It is worth noting that, in addition to most known pathogenic microorganisms, this medication is active against some strains of Helicobacter pylori. In addition, the drug also acts on multi-resistant bacteria that are resistant to earlier generations of cephalosporins, penicillins, and aminoglycosides.

Indications for the use of Cefotaxime injections

  • peritonitis;
  • pelvic organ infections;
  • gonorrhea;
  • infections of the central nervous system, including meningitis, except listeria form;
  • sepsis;
  • Lyme disease;
  • kidney and urinary tract infections;
  • endocarditis;
  • infections of soft tissues and skin, including infected burns and purulent wounds;
  • abdominal infections;
  • immunodeficiencies with the addition of bacterial lesions;
  • infections of joints and bone tissue.

Cefotaxime injections are also prescribed for sinusitis and sore throat, other inflammatory diseases of the ENT organs and respiratory tract caused by pathogenic bacteria:

  • bronchitis;
  • abscesses;
  • pneumonia;
  • sinusitis;
  • otitis, excluding the enterococcal form.

Additionally, this cephalosporin can be used for the prevention of nosocomial infections and complications after surgical interventions in urological, obstetric, gynecological and gastroenterological practice.

How many days should Cefotaxime injections be given?

The duration of therapy with the described antibiotic is determined individually, in accordance with the diagnosis and condition of the patient.

As a rule, Cefotaxime is prescribed only during the acute period of the disease, so the duration of the course does not exceed 5 days. In some cases, 1-2 times of administration of the medication is sufficient.

How and how many times a day to give Cefotaxime injections?

The presented medicine can be administered intramuscularly and intravenously (stream and drip). The dosage varies according to the diagnosis.

For infections of the urinary system and mild forms of other bacterial lesions - 1 g of the drug every 8-12 hours. In the case of gonorrhea, a single dose is sufficient.

For moderate infections - up to 2 g every 12 hours.

Severe bacterial lesions require administration of the drug every 4-8 hours, 2 g intravenously. The maximum dose per day is 12 g.

Before performing an injection or infusion, the medication needs to be diluted.

For intramuscular administration - 1 g of Cefotaxime with 4 ml of water for injection or Lidocaine solution (1%). For jet intravenous administration, the dilution is the same, only Lidocaine is not used.

In the case of infusions, 1-2 g of the drug is required for 50-100 ml of glucose, dextrose (5%) or sodium chloride (0.9%) solution. The rate of administration depends on whether the patient responds normally to an injection of Cefotaxime. It is usually recommended to do the injections slowly (1-2 minutes) and infusions (about 1 hour), as the procedures are quite painful.

Dosage form:  

Powder for preparing a solution for intravenous and intramuscular administration.

Compound: Composition for 1 bottle: cefotaxime sodium (in terms of cefotaxime) - 1.0 g. Description: Powder is white or white with a yellowish tint. Pharmacotherapeutic group:Antibiotic cephalosporin. ATX:  

J.01.D.D.01 Cefotaxime

Pharmacodynamics:

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

Active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus,

including penicillinase-producing strains), Staphylococcus epidermidis (for

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 influenzae (including strains that form penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, Neisseria meningitidis, Neisseria gonorrhoeae (including penicillinase-producing strains), Acinetobacter spp., Corynebacterium diphthenae, 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 resistant.

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

Pharmacokinetics:

After a single intravenous administration of the drug in doses of 0.5 g, 1.0 g and 2.0 g, the time required to achieve the maximum concentration (Cmax) is 5 minutes, and the maximum concentration is about 39, 101.7 and 214 mcg/ ml respectively. After intramuscular administration of the drug in doses of 0.5 g and 1.0 g, the maximum concentration is reached after 0.5 hours and is about 11 and 21 μg/ml, respectively. Communication with plasma proteins - 30-50%. Bioavailability - 90-95%.

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

The half-life (T1/2) is about 1 hour when administered intravenously and about 1-1.5 hours when administered intramuscularly. Excreted by the kidneys - 20-36% unchanged, the rest - in the form of metabolites (15-25% - in the form of pharmacologically active desacetylcefotaxime, which retains bactericidal activity; 20-25% - in the form of 2 metabolites - M2 and MZ, not having antimicrobial effects).

In chronic renal failure (CRF) and in the elderly, the half-life increases by 2 times. The half-life (T1/2) in newborns is about 0.75-1.5 hours, in premature newborns (body weight less than 1500 g) it increases to 4.6 hours, in children weighing more than 1500 g - about 3. 4 hours. With repeated intravenous administrations at a dose of 1.0 g every 6 hours for 14 days, no accumulation is observed.

Indications:

Infectious and inflammatory diseases caused by microorganisms sensitive to cefotaxime: infections of the central nervous system (meningitis), respiratory tract and ENT organs, urinary tract, bones, joints, skin and soft tissues, pelvic organs, gonorrhea, infected wounds and burns, peritonitis , sepsis, abdominal infections, endocarditis, Lyme disease, salmonellosis, infections due to immunodeficiency.

Prevention of infections after surgical operations (including urological, obstetric-gynecological, gastrointestinal tract).

Contraindications:

Hypersensitivity (including to penicillins, other cephalosporins, carbapenems);

Pregnancy 1st trimester;

Intracardiac block without an established pacemaker;

Severe heart failure;

Children up to 2.5 years of age (for intramuscular administration).

When using lidocaine as a solvent: hypersensitivity to lidocaine or other amide-type local anesthetic.

Carefully:

Neonatal period (for intravenous administration), chronic renal failure, ulcerative colitis (including history).

Pregnancy and lactation:

Cefotaxime penetrates the placental barrier and is excreted in breast milk. Use in the second and third trimesters of pregnancy is possible when the expected benefit to the mother outweighs the potential risk to the fetus; If it is necessary to prescribe the drug during lactation, breastfeeding should be suspended.

Directions for use and dosage:

The drug is administered intravenously (stream or drip) and intramuscularly.

Adults and children weighing 50 kg or more:

For uncomplicated infections - intramuscularly or intravenously, 1 g every 12 hours;

For uncomplicated acute gonorrhea, 0.5 - 1 g intramuscularly once;

For moderate infections, 1-2 g intravenously or intramuscularly every 8 hours;

For sepsis - 2 g intravenously every 6-8 hours;

For life-threatening infections (meningitis) - 2 g intravenously every 4 hours, maximum daily dose - 12 g.

The duration of treatment is determined individually.

In order to prevent the development of infections before surgery, 1 g is administered once during induction of general anesthesia. If necessary, the administration is repeated after 6-12 hours.

During caesarean section (at the moment of applying clamps to the umbilical vein) -

1 g intravenously, then 6 and 12 hours after the first dose - an additional 1 g.

When creatinine clearance is 20 ml/min/1.73 sq.m or less, the daily dose is reduced by 2 times.

For children:

Premature and newborns up to 1 week - intravenously 50 mg/kg every 12 hours;

At the age of 1-4 weeks - intravenously 50 mg/kg every 8 hours;

Children from 1 month to 12 years with body weight less than 50 kg - intravenously or intramuscularly (children over 2.5 years old) 50-180 mg/kg in 4-6 injections.

In case of severe infections, incl. meningitis, intravenously or intramuscularly in 4-6 doses, the maximum daily dose is 12 g.

Rules for preparing injection solutions:

For intravenous injection, water for injection is used as a solvent. (1 g of the drug is diluted in 10 ml of solvent). Inject slowly over 3-5 minutes.

For intravenous infusion 0.9% sodium chloride solution or 5% dextrose solution is used as a solvent (1 g diluted in 50 ml of solvent). Duration of infusion - 50-60 minutes.

For intramuscular administration use water for injection or 1% lidocaine solution (1 g of the drug is diluted in 4 ml of solvent). Injected deep into the gluteal muscle.

Side effects:

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

From the nervous system: headache, dizziness, encephalopathy, movement disorders, convulsions;

From the urinary system: renal dysfunction, oliguria, interstitial nephritis.

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

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

Co aspects of the cardiovascular system: Potentially life-threatening arrhythmias following rapid central venous bolus administration.

Local reactions: phlebitis, pain along the vein, pain 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, false-positive Coombs test.

Others:superinfection (in particular, candidal vaginitis).

Overdose:

Symptoms: convulsions, encephalopathy (in case of large doses, especially in patients with renal failure), tremor, neuromuscular irritability.

Treatment: symptomatic therapy.

Interaction:

Increases the risk of bleeding when combined with antiplatelet agents and non-steroidal anti-inflammatory drugs.

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

Medicines that block tubular secretion (including diuretics) increase plasma concentrations of cefotaxime and slow down its elimination.

Cefotaxime is pharmaceutically incompatible with solutions of other antibiotics in the same syringe or dropper.

Special instructions:

In the first weeks of treatment, pseudomembranous colitis may occur, manifested by severe, prolonged diarrhea. In this case, stop taking the drug and prescribe adequate therapy, including or.

When treating with cefotaxime for more than 10 days, monitoring the number of blood cells is necessary.