Antibiotic Cefotaxime: indications and instructions for use, reviews. Cefotaxime - a versatile antibiotic: characteristics and uses Cefotaxime solution

3rd generation cephalosporin

Active substance

Cefotaxime (as sodium salt) (cefotaxime)

Release form, composition and packaging

Powder for solution for intravenous and intramuscular administration almost white or yellowish.

Glass bottles (1) - packs of cardboard.

pharmachologic effect

Third generation cephalosporin antibiotic for parenteral administration. Acts bactericidal. The mechanism of action is associated with a violation of the synthesis of the mucopeptide of the cell wall of microorganisms. Has a wide spectrum of action.

A drug active against gram-positive and gram-negative microorganisms, resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus, including strains that form penicillinase, with the exception of methicillin-resistant strains), Staphylococcus epidermidis (with the exception of methicillin-resistant strains), Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococci), Streptococcus agalactiae (group B streptococci), Enterococcus spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains that form penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubacter spp., Propionibacterium spp., Clostridium spp. . (including Clostridium perfringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Serratia spp., some strains Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.

Inconstantly affects on some strains of Pseudomonas aeruginosa, Acinetobacter spp., Helicobacter pylori, Bacteroides fragilis, Clostridium difficile.

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

Pharmacokinetics

Suction

After a single intravenous administration at doses of 500 mg, 1 g and 2 g, T max is 5 minutes, C max is 39, 101.7 and 214 μg / ml, respectively.

After i / m administration at doses of 500 mg and 1 g T max - 0.5 h, C max is 11 and 21 mcg / ml, respectively.

Distribution

Protein binding - 30-50%. Bioavailability - 90-95%. Therapeutic concentrations are achieved in most tissues (myocardium, bones, gallbladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body.

V d - 0.25-0.39 l / kg.

With repeated intravenous administration at a dose of 1 g every 6 hours for 14 days, cumulation is not observed.

Cefotaxime penetrates the placental barrier, is excreted in small concentrations with breast milk.

breeding

T 1/2 with / in the introduction -1h, with the / m administration - 1-1.5 hours. Excreted by the kidneys: 20-36% - unchanged, the rest - in the form of metabolites (15-25% - in the form of pharmacologically active deacetylcefotaxime and 20-25% - in the form of 2 inactive metabolites).

Pharmacokinetics in special clinical situations

In chronic renal failure and in the elderly T 1/2 increases by 2 times. T 1/2 in newborns - 0.75-1.5 hours, in premature newborns (body weight less than 1500 g) increases to 4.6 hours; in children weighing more than 1500 g - 3.4 hours.

Indications

Infectious and inflammatory diseases caused by susceptible microorganisms, including:

- CNS infections (meningitis);

– infections respiratory tract and ENT organs;

– infections urinary tract;

- infections of bones and joints;

- infections of the skin and soft tissues;

- infections of the pelvic organs;

- abdominal infections;

- peritonitis;

- sepsis;

- endocarditis;

- gonorrhea;

— infected wounds and burns;

- salmonellosis;

- Lyme disease;

- infections against the background of immunodeficiency.

Prevention of infections after surgical operations(including urological, obstetric and gynecological, on the digestive tract).

Contraindications

- pregnancy;

— childhood up to 2.5 years (for i / m administration);

- hypersensitivity (including to penicillins, other cephalosporins, carbapenems).

FROM caution the drug should be used in newborns, during lactation (in small concentrations excreted in breast milk), with chronic renal failure, with NUC (including history).

Dosage

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

The drug is prescribed adults and children over 12 years of age (weighing ≥50 kg)

At uncomplicated infections, as well as with urinary tract infections- in / m or / in 1 g every 8-12 hours.

At uncomplicated acute gonorrhea- in / m at a dose of 1 g once.

At moderate infections- in / m or / in 1-2 g every 12 hours.

At severe infections, such as meningitis- in / in 2 g every 4-8 hours, the maximum daily dose is 12 g. The duration of treatment is set individually.

With the aim of prevention of infections before surgery, it is administered during induction of anesthesia once at a dose of 1 g. If necessary, the administration is repeated after 6-12 hours.

At caesarean section - at the time of clamping the umbilical vein - in / in a dose of 1 g, then 6 and 12 hours after the first dose - an additional 1 g.

With QC ≤20 ml / min / 1.73 m 2 the daily dose is reduced by 2 times.

Premature and newborns under 1 week of age– IV at a dose of 50 mg/kg every 12 hours; aged 1-4 weeks- IV at a dose of 50 mg / kg every 8 hours. Children weighing ≤50 kg- in / in or / m (children over 2.5 years old) 50-180 mg/kg in 4-6 injections.

At severe infections (including meningitis) daily dose at the time of administration children increase to 100-200 mg / kg, i.m. or i.v. for 4-6 injections, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions

For IV injection: 1 g of the drug is diluted in 4 ml of sterile water for injection; the drug is administered slowly over 3-5 minutes.

For I/O infusions: 1-2 g of the drug is diluted in 50-100 ml of solvent. A 0.9% solution or a 5% dextrose (glucose) solution is used as a solvent. Duration of infusion - 50 - 60 minutes.

For i / m administration: 1 g is dissolved in 4 ml of solvent. As a solvent, either 1% lidocaine solution is used.

Side effects

From the side of the central nervous system:headache, dizziness.

From the side of the urine excretory system: renal dysfunction, oliguria, interstitial nephritis.

From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbacteriosis, abnormal liver function; rarely - stomatitis, glossitis, pseudomembranous enterocolitis, increased activity of hepatic transaminases and alkaline phosphatase, hyperbilirubinemia.

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

From the side of the cardiovascular system: potentially life-threatening arrhythmias following a rapid central venous bolus.

Laboratory indicators: azotemia, increased blood urea concentration, hypercreatininemia, positive reaction Coombs.

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

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

Others: superinfection (vaginal and oral candidiasis).

Overdose

Symptoms: convulsions, encephalopathy (if administered in high doses, especially in patients with kidney failure), tremor, neuromuscular excitability.

Treatment: symptomatic, there is no specific antidote.

drug interaction

Cefotaxime increases the risk of bleeding when combined with antiplatelet agents, NSAIDs.

The risk of kidney damage increases with simultaneous reception aminoglycosides, and "loop" diuretics.

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

Pharmaceutical interaction

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. At the same time stop taking the drug and prescribe adequate therapy including or metronidazole.

Patients with a history of allergic reactions to penicillins may have hypersensitivity to cephalosporin antibiotics.

When treating with the drug for more than 10 days, it is necessary to control the picture of peripheral blood.

During treatment with cefotaxime, it is possible to obtain a false positive Coombs test and a false positive urine test for glucose.

During treatment, you can not drink alcohol, since there may be effects similar to the action of disulfiram (flushing of the face, spasm in the abdomen and in the stomach, nausea, vomiting, headache, lowering blood pressure, tachycardia, shortness of breath).

Pregnancy and lactation

The drug is contraindicated for use during pregnancy.

If necessary, the appointment of the drug during lactation should stop breastfeeding.

For impaired renal function

Be wary appoint in chronic renal failure.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. The drug should be stored out of the reach of children, dry, dark place at a temperature not exceeding 25°C. Shelf life - 2 years.

Indications for use:
Cefotaxime is prescribed for infections caused by microorganisms sensitive to it: infections of the lower respiratory (bronchitis, pneumonia, pleurisy, abscesses) and urinary tract; kidneys; infections of the ear, nose, throat (tonsillitis, otitis, with the exception of enterococcal); with septicemia; endocarditis; infections of bones and soft tissues, abdominal cavity; with gynecological infectious diseases (uncomplicated gonorrhea, chlamydia); bacterial meningitis (with the exception of listeriosis); Lyme disease, also for the prevention of postoperative infections and complications.

Pharmachologic effect:
Cefotaxime is a semi-synthetic antibiotic of the III generation cephalosporin group, with a wide spectrum of action, for parenteral administration. The drug is effective against many gram-positive and has a high activity against gram-negative bacteria. It has a bactericidal effect on strains of bacteria resistant to penicillin, aminoglycosides, sulfonamides. The mechanism of the antimicrobial action of Cefotaxime is associated with inhibition of the activity of the transpeptidase enzyme by the blockade of peptidoglycan, a violation of the formation of the mucopeptide of the cell wall of microorganisms. The drug is resistant to four out of five beta-lactamases of gram-negative bacteria and staphylococcal penicillinase. Active against Staphylococcus aureus, including those producing penicillinase, Staphylococcus epidermidis, some strains of Enterococcus spp., Streptococcus pneumoniae (especially Diplococcus pneumoniae), Streptococcus pyogenes (group A beta-hemolytic streptococci), Streptococcus agalactiae (group B streptococci) , Bacillus subtilis, Bacillus myroides, Corinebacterium diphtheriae, Erysipelo-thrix insidiosa, Eubacterium, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Acinetobacter spp. Neisseria meningitidis, Neisseria gonorrhoeae, including strains that produce penicillinase, Propionibacterium, Proteus mirabilis, Proteus vulgaris, Proteus inconstans, Serratia spp., Viellonella, Yersitia, Bordetella pertussis, Moraxella, Aeromonas hydrophilia, Fusobacterium, Bacteroides spp., Clostrridium s pecies, Peptosteptococcus species, Peptococus spp. Inconsistently affects some strains of Pseudomonas aeruginosa, Acinetobactery, Helicobacter pylori, Bacteroidesfragtlis, Clostridiun diffcile. May act on multi-resistant strains that are resistant to penicillinase, first-generation cephalosporins, aminoglycosides. The drug is less active against gram-negative cocci than cephalosporins of the first and second generations.

Pharmacokinetics
The maximum concentration in the blood (11 and 21 mcg / ml) later intramuscular injection in doses of 0.5 g and 1 g, respectively, observed after 30 minutes. after the injection. After 5 min. after intravenous administration of 0.5 g, 1 or 2 g, the highest concentration in the blood is 24, 39, 100 mcg / ml, respectively. In the blood, the product binds to proteins by 25-40%. The bactericidal concentration in the blood is maintained for more than 12 hours. The drug penetrates well into tissues (creates an effective concentration in the myocardium, bone tissue, gallbladder, skin, soft tissues), body fluids (determined in effective concentrations in the spinal, pericardial, pleural, peritoneal, synovial fluids), passes through the placenta, passes into breast milk. Cefotaxime-BHFZ is excreted in a significant amount in the urine (90%) (in unchanged form within 60-70% and in the form of active metabolites within 20-30%, of which 15-20% are the main metabolite - deacetylcefotaxime, which has antimicrobial activity). activity). The half-life with intravenous administration is 1 hour, with intramuscular injection - 1-1.5 hours. With repeated intravenous injections at a dose of 1 g after 6 hours for 14 days, cumulation is not observed. In newborns, the half-life is 0.75-1.5 hours, in premature babies - up to 6.4 hours, in patients older than 80 years - 2.5 hours, with renal failure, the half-life does not exceed 2.5 hours. The drug is partially excreted in the bile, also in breast milk.

Cefotaxime route of administration and dosage:
Cefotaxime is prescribed intramuscularly and intravenously, by stream and drip. For intramuscular injections dissolve 0.5 g (1 g) of Cefotaxime in 2-3 ml (4-5 ml) of sterile water for injection and inject deeply into the gluteal muscle.
For intravenous administration, first dissolve 0.5 g (1 g) of Cefotaxime in 2 ml (4 ml) of sterile water for injection, dilute to 10 ml with a solvent and inject slowly over 3-5 minutes. For drip injection into a vein (over 50-60 minutes), dissolve 2 g of the product in 100 ml of isotonic sodium chloride solution or 5% glucose solution. single dose Cefotaxime for adults - 1 g, after 12 hours, in severe cases the dose is increased to 2.0 g, after 12 hours, or the number of injections is increased up to 3-4 times a day, bringing the total daily dose to a maximum of 12 g. In case of renal failure, the dose is reduced by 2 times.
In acute gonorrhea, the product is administered once, intramuscularly, at a dose of 0.5-1 g. For prevention infectious complications before or during induction of anesthesia, 0.5-1 g is administered, if necessary, the injection is repeated after 6-12 hours.

Cefotaxime contraindications:
Increased susceptibility to any antibiotic of the cephalosporin series and to penicillin; bleeding; enterocolitis in history; pregnancy. Care must be taken when prescribing the product to patients with impaired renal and hepatic function.

Cefotaxime side effects:
After the introduction of Cefotaxime, allergic reactions may occur (rashes, hyperemia, exudative erythema multiforme, fever, eosinophilia, anaphylactic reactions, in rare cases, anaphylactic shock), from alimentary canal possible nausea, vomiting, diarrhea, abdominal pain, dysbacteriosis, superinfection, rarely - pseudomembranous colitis. Peripheral blood parameters, including biochemical ones, change (neutropenia, transient leukopenia, thrombocytopenia, hemolytic anemia, arrhythmia (with rapid jet injection), headache, reversible encephalopathy, pain at the injection site, tissue inflammation, phlebitis.

Pregnancy:
During pregnancy and lactation, use only according to strict indications.

Overdose:
Overdose can cause allergic reactions, dysbacteriosis, encephalopathy.
Treatment: desensitizing products, symptomatic agents.

Use with other medicinal products:
With the simultaneous use of Cefotaxime and aminoglycosides, "loop" diuretics, an increase in nephrotoxicity is observed. With simultaneous administration with antiplatelet agents, including non-steroidal anti-inflammatory drugs, the risk of bleeding increases. Probenecid slows down excretion, increases plasma concentration and half-life. Cefotaxime should not be administered in the same syringe with other products due to the possibility of interaction.

Release form:
Powder for solution for injection in vials of 0.5, 1.0 or 2.0 g.

Storage conditions:
Store in a dry, dark place and out of the reach of children, at a temperature not exceeding 25 °C. Shelf life - 2 years.
Conditions for dispensing from pharmacies - by prescription.

Cefotaxime composition:
Cefotaxime;
sodium (6R,7R)-3-[(acetyloxy)methyl]-7-[[(Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetyl]amino]-8-oxo- 5-thia-1-azabicyclo oct-2-ene-2-carboxylate;

Powder white or white with a slightly yellowish tint, hygroscopic.

1 bottle contains cefotaxime sodium salt sterile in terms of cefotaxime 0.5, 1.0 or 2.0 g.

Additionally:
Cefotaxime is prescribed with caution to patients with allergies, including medications. When treating during lactation, it is necessary to stop feeding. Simultaneous administration of Cefotaxime with nephrotoxic products requires monitoring of renal function; when using the product for more than 10 days, control of peripheral blood is necessary. The elderly and debilitated patients need to prescribe vitamin K products (prevention of hypocoagulation). When a symptom of pseudomembranous colitis is established, Cefotaxime is canceled. For children under 2.5 years old, the product is administered intravenously. Dose of Cefotaxime for Infants and Toddlers younger age is 50-100 mg / kg of body weight every day, divided into separate doses, at intervals of 12 to 6 hours. For premature babies, the daily dose should not exceed 50 mg / kg of body weight.

Attention!
Before using the medication "Cefotaxime" you need to consult a doctor.
The instructions are provided solely for familiarization with " Cefotaxime».

The page contains instructions for use Cefotaxime. It is available in various dosage forms drug (injections in ampoules for injections of 500 mg and 1 g), and also has a number of analogues. This annotation has been verified by experts. Leave your feedback about the use of Cefotaxime, which will help other visitors to the site. The drug is used for various diseases(pneumonia, endocarditis, sepsis, etc.) infectious diseases). The tool has a number of side effects and features of interaction with other substances. Doses of the drug differ for adults and children. There are restrictions on the use of the drug during pregnancy and during breastfeeding. Treatment with Cefotaxime can only be prescribed by a qualified doctor. The duration of therapy may vary and depends on specific disease. Ways to dilute the antibiotic (in water or novocaine) and the effect of the drug.

Instructions for use and dosage

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

The drug is prescribed for adults and children over the age of 12 years (weighing ≥50 kg)

In uncomplicated infections, as well as urinary tract infections - in / m or / in 1 g every 8-12 hours.

In uncomplicated acute gonorrhea - intramuscularly at a dose of 1 g once.

For infections of moderate severity - in / m or / in 1-2 g every 12 hours.

In severe infections, for example, with meningitis - in / in 2 g every 4-8 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, it is administered during induction anesthesia once at a dose of 1 g. If necessary, the administration is repeated after 6-12 hours.

For caesarean section - at the time of clamping the umbilical vein - in / in a dose of 1 g, then 6 and 12 hours after the first dose - an additional 1 g.

Premature and newborns under the age of 1 week - in / in a dose of 50 mg / kg every 12 hours; at the age of 1-4 weeks - in / in a dose of 50 mg / kg every 8 hours. Children weighing ≤50 kg - in / in or / m (children over the age of 2.5 years) 50-180 mg / kg in 4-6 introductions.

In severe infections (including meningitis), the daily dose when administered to children is increased to 100-200 mg / kg, intramuscularly or intravenously for 4-6 injections, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions (how to dilute Cefotaxime)

For intravenous injection: 1 g of the drug is diluted in 4 ml of sterile water for injection; the drug is administered slowly over 3-5 minutes.

For intravenous infusion: 1-2 g of the drug is diluted in 50-100 ml of the solvent. As a solvent, 0.9% sodium chloride solution or 5% dextrose (glucose) solution is used. Duration of infusion - 50 - 60 minutes.

For i / m administration: 1 g is dissolved in 4 ml of solvent. As a solvent, water for injection or a 1% solution of lidocaine (novocaine) is used.

Release forms

Powder for the preparation of a solution for intravenous and intramuscular administration (injections in ampoules for injection) 250 mg, 500 mg and 1 gram of powder for dilution in water for injection or novocaine.

Cefotaxime- cephalosporin antibiotic of the 3rd generation of a wide spectrum of action. It has a bactericidal effect by inhibiting the synthesis of the bacterial cell wall. The mechanism of action is due to acetylation of membrane-bound transpeptidases and disruption of peptidoglycan cross-linking, which is necessary to ensure the strength and rigidity of the cell wall.

Highly active against gram-negative bacteria (resistant to other antibiotics): Escherichia coli ( coli), Citrobacter spp., Proteus mirabilis, Providencia spp., Klebsiella spp., Serratia spp., some strains of Pseudomonas spp., Haemophilus influenzae.

Less active against Streptococcus spp. (including Streptococcus pneumoniae), Staphylococcus spp., Neisseria meningitidis, Neisseria gonorrhoeae, Bacteroides spp.

Resistant to most beta-lactamases.

Pharmacokinetics

Rapidly absorbed from the injection site. Plasma protein binding is 40%. Widely distributed in tissues and body fluids. Reaches therapeutic concentrations in cerebrospinal fluid especially with meningitis. Crosses the placental barrier, excreted in breast milk low concentrations. 40-60% of the dose is excreted in the urine unchanged after 24 hours, 20% - in the form of metabolites.

Indications

Infectious and inflammatory diseases caused by susceptible microorganisms, including:

  • CNS infections (meningitis);
  • infections of the respiratory tract and ENT organs;
  • urinary tract infections;
  • bone and joint infections;
  • skin and soft tissue infections;
  • infections of the pelvic organs;
  • abdominal infections;
  • peritonitis;
  • sepsis;
  • endocarditis;
  • gonorrhea;
  • infected wounds and burns;
  • salmonellosis;
  • Lyme disease;
  • infections on the background of immunodeficiency;
  • prevention of infections after surgical operations (including urological, obstetric and gynecological, on the gastrointestinal tract).

Contraindications

  • pregnancy;
  • children's age up to 2.5 years (for intramuscular injection);
  • hypersensitivity (including to penicillins, other cephalosporins, carbapenems).

special instructions

In the first weeks of treatment, pseudomembranous colitis may occur, manifested by severe prolonged diarrhea. At the same time, the drug is stopped and adequate therapy is prescribed, including vancomycin or metronidazole.

Patients with a history of allergic reactions to penicillins may be hypersensitive to cephalosporin antibiotics.

When treating with the drug for more than 10 days, it is necessary to control the picture of peripheral blood.

During treatment with cefotaxime, it is possible to obtain a false positive Coombs test and a false positive urine test for glucose.

During treatment, you can not drink alcohol, since effects similar to the action of disulfiram are possible (flushing of the face, spasm in the abdomen and in the stomach, nausea, vomiting, headache, lowering blood pressure, tachycardia, shortness of breath).

Side effect

  • headache;
  • dizziness;
  • impaired renal function;
  • oliguria;
  • nausea, vomiting;
  • diarrhea or constipation;
  • flatulence;
  • abdominal pain;
  • dysbacteriosis;
  • stomatitis;
  • glossitis;
  • pseudomembranous enterocolitis;
  • hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, agranulocytosis;
  • potentially life-threatening arrhythmias following a rapid central venous bolus;
  • increase in the concentration of urea in the blood;
  • positive Coombs reaction;
  • phlebitis;
  • soreness along the vein;
  • soreness and infiltration at the site of intramuscular injection;
  • hives;
  • chills or fever;
  • rash;
  • skin itching;
  • bronchospasm;
  • eosinophilia;
  • anaphylactic shock;
  • superinfection (vaginal and oral candidiasis).

drug interaction

Cefotaxime increases the risk of bleeding when combined with antiplatelet agents, non-steroidal anti-inflammatory drugs.

The risk of kidney damage increases with the simultaneous use of aminoglycosides, polymyxin B and "loop" diuretics.

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

Pharmaceutical interaction

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

Analogues medicinal product Cefotaxime

Structural analogues for the active substance:

  • Intrataxim;
  • Kefotex;
  • Clafobrin;
  • Claforan;
  • Clafotaxime;
  • Liforan;
  • Oritax;
  • Oritaxim;
  • Rezibelakta;
  • Spirosine;
  • Bid tax;
  • Talcef;
  • Tarcefoxime;
  • Tirotax;
  • Cetax;
  • Cephabol;
  • Cefantral;
  • Cefosin;
  • Cefotaxime Lek;
  • Cefotaxime sodium;
  • Cefotaxime Sandoz;
  • Cefotaxime Vial;
  • Cefotaxime sodium salt.

Use in children

Contraindicated in children under the age of 2.5 years (for intramuscular injection).

Use during pregnancy and lactation

Cefotaxime is contraindicated for use during pregnancy.

If necessary, the appointment of the drug during lactation should stop breastfeeding.

According to medical classification, Cefotaxime is antibacterial drug from the group of third-generation cephalosporins, the active ingredient of which is cefotaxime. The drug belongs to semi-synthetic, produced by domestic or foreign companies. Check out its instructions for use.

Composition and form of release

Cefotaxime (Cefotaxime) is available only in the form of a powder for the preparation of a solution, there are no tablets under this name. The composition of the drug and packaging:

The mechanism of action of the drug

Semi-synthetic antibiotic is administered parenterally, active against microorganisms resistant to sulfonamides, penicillins, aminoglycosides. The mechanism of operation of the agent is to suppress the activity of the transpeptidase enzyme and block peptidoglycan. Injections are given intramuscularly maximum concentration in the blood is registered in half an hour.

Up to 40% of the active ingredient binds to plasma proteins. The bactericidal effect lasts 12 hours, the highest concentration of the substance is created in the soft tissues, the myocardium. The active component penetrates the placenta, is found in pleural, peritoneal, pericardial, synovial fluids. 90% of the dose is excreted in the urine. The half-life is 1-1.5 hours. The drug does not accumulate, slightly excreted in the bile.

Indications for use

The main indications for the use of the drug are infectious diseases. The instruction highlights the following:

  • pleurisy, bronchitis, pneumonia, lung abscess;
  • endocarditis, septicemia;
  • bacterial meningitis;
  • postoperative complications and infections;
  • diseases of the throat, ear, kidneys, nose, urinary tract;
  • Lyme disease.

Method of application and dosage

Instructions for the use of Cefotaxime suggest its parenteral (intramuscular or intravenous) administration to adults every 6-12 hours for 1-2 g. To prevent infection before surgery during anesthesia, the drug is used once at a dose of 1 g. suture on the umbilical vein, the patient is administered 1 g intravenously, after 6 and 12 hours - another 1 g each.

How to breed Cefotaxime

For intravenous injections 1 g of powder is diluted in 4 ml of sterile water, injected slowly for 3-5 minutes. For additional pain relief, you can mix the powder with Novocaine (1 g of the drug per 4 ml of liquid, injected slowly). In addition to Novocaine, the powder can be combined with Lidocaine, sterile water. The injections of the drug are painful.

Cefotaxime for angina

In case of angina, its uncomplicated course, the administration of 1 g of the drug intravenously or intramuscularly every 12 hours is indicated. If the disease occurs with moderate severity of symptoms, the drug is administered intravenously or intramuscularly at a dose of 1-2 g every 12 hours. The duration of treatment is determined by the doctor depending on the time of getting rid of the symptoms of sore throat.

With pneumonia

Cefotaxime for pneumonia in children, severe currents infections or meningitis is administered intravenously or intramuscularly at 100-200 mg / kg of body weight in 3-4 injections. Maximum per day, you can enter no more than 12 grams of funds. The duration of antibiotic therapy continues until the complete disappearance of pathogenic microbial cells in the body (determined by tests).

Cefotaxime for bronchitis

In uncomplicated or complicated bronchitis, administration of 1 g every 8 hours is indicated. Injections are made into the muscle, a maximum of 12 g can be administered per day. Therapy of bronchitis in adults and children lasts until the main symptoms of the disease disappear. The doctor monitors the patient during the entire treatment with the drug, determines the need for dose adjustment, stopping therapy.

special instructions

Cefotaxime belongs to nephrotoxic drugs, therefore, during treatment, they must definitely monitor the performance of the kidneys and excretory system. If therapy lasts more than 10 days, then they also monitor blood functions. Elderly people and debilitated patients are prescribed vitamin K to prevent hypocoagulation (increased blood clotting). If pseudomembranous colitis develops during treatment, therapy is stopped.

Cefotaxime during pregnancy

It is impossible to use the drug during pregnancy during the first trimester. At breastfeeding, in the second and third trimesters of bearing a child, an antibiotic can only be used if the benefit to the mother outweighs the harm to the child. Use during lactation may change the oropharyngeal flora of the child.

Cefotaxime for children

According to the instructions, Cefotaxime for children is used with caution. Daily dosage calculated as 50-180 mg / kg body weight per day in 2-4 injections. Newborns and newborns ahead of schedule children up to one week are administered intravenously 50 mg / kg of body weight, at the age of 1-4 weeks - intravenously every 8 hours at the same dose. Intravenous injections are made with a mass of less than 50 kg, intramuscularly - over 2.5 years.

drug interaction

Loop diuretics (Furosemide, Lasix), aminoglycosides can enhance the nephrotoxicity of the antibiotic. Non-steroidal anti-inflammatory drugs and antiplatelet agents in combination with cefotaxime may increase the risk of bleeding. It is forbidden to mix the drug with other solutions in the same syringe, except for Lidocaine and Novocaine. According to the instructions, the combination of the drug with Probenecid increases the concentration of the active ingredient and slows down its excretion.

Cefotaxime and alcohol

During antibiotic treatment, it is undesirable to take alcohol and drinks based on it. According to the instructions, the combination of the drug with ethanol can cause a fall. blood pressure, flushing of the skin of the face, tachycardia, migraine and headache. Due to the action of ethyl alcohol, spasms, vomiting, shortness of breath will appear. If disulfiram-like symptoms appear, you should consult a doctor.

Side effects

During therapy with Cefotaxime, side effects may develop. The instruction highlights the following:

  • soreness of injections;
  • phlebitis with intravenous infusion of the solution;
  • nausea, colitis, jaundice, hepatitis, diarrhea, vomiting, epigastric pain;
  • hypoprothrombinemia, hemolytic anemia, neutropenia, thrombocytopenia;
  • allergic reactions, eosinophilia, pruritus, angioedema;
  • candidiasis;
  • interstitial nephritis.

Overdose

If large doses are given short terms drug overdose may develop. Its signs are dysbacteriosis, allergic reactions, encephalopathy. To eliminate the symptoms of an overdose, it is indicated to carry out symptomatic treatment, the use of desensitizing medications. Hemodialysis is ineffective to eliminate the consequences.

Contraindications

The drug is prescribed with caution when liver failure, violation of the work of these organs in history. Contraindications, according to the instructions, are:

  • bleeding from internal organs;
  • individual intolerance to the components of the composition;
  • pregnancy, especially the first trimester;
  • enterocolitis in history;
  • combination with antiplatelet agents, other antibiotics.

Terms of sale and storage

The drug belongs to the prescription, stored at temperatures up to 25 degrees for two years.

Analogues

You can replace the medication with drugs based on cefotaxime from the group of cephalosporin antibiotics. Analogues of the drug include:

  • Klaforan - bactericidal powder for the preparation of an injection solution with a similar active substance;
  • Cefosin is an antibacterial solution powder containing sodium salt cefotaxime;
  • Cefabol is a bactericidal powder based on the same component.

Cefotaxime has a high affinity for penicillin-binding proteins of the bacterial cell wall, has a blocking effect on peptidoglycan polymerase, and disrupts the formation of the mucopeptide of the cell wall of microorganisms.

With a single intramuscular injection of 0.5 or 1 g to healthy volunteers, the maximum concentration was reached within 0.5 hours and amounted to 11.7 and 20.5 μg / ml, respectively. After 5 minutes, when administered intravenously, 0.5; 1 or 2 g of the drug, the maximum concentration is 38.9, respectively; 101.7 and 214.4 µg/ml. Cefotaxime binds to plasma proteins by 25–40% (mainly to albumins). The drug creates therapeutic concentrations in many fluids (pericardial, synovial, peritoneal, pleural effusion, spinal, sputum, bile, urine) and tissues (bones, myocardium, gallbladder, soft tissues, skin) of the body; Cefotaxime crosses the placenta and is excreted in breast milk. The plasma half-life is about 1 hour and does not depend on the route of administration. Cefotaxime is excreted by the kidneys - approximately 60% of the dose is excreted within 6 hours after the start of the infusion. 20-36% of the drug is excreted unchanged, 15-25% as the main metabolite of deacetylcefotaxime, which has antibacterial activity, 20-25% - in the form of two other metabolites - M2 and M3, which are inactive. With repeated intravenous injections of 1 g of the drug every 6 hours for 2 weeks, no accumulation of cefotaxime in the body is observed. With a single administration of 50 mg / kg of the drug for 10-15 minutes to a newborn (weighing ≥1500 g), the half-life of cefotaxime was 3.4 hours and was longer (4.6 hours) with a body weight of less than 1500 g (regardless of from age). In patients older than 80 years, the half-life of cefotaxime is 2.5 hours; in renal failure, the half-life does not exceed 2.5 hours.

Cefotaxime has a wide spectrum antimicrobial action, resistant to staphylococcal penicillinase and 4 (out of 5) beta-lactamases of gram-negative microorganisms. Cefotaxime is active against Staphylococcus epidermidis, Staphylococcus aureus (including those producing penicillinase), some strains of Enterococcus spp., Streptococcus pyogenes (group A beta-hemolytic streptococci), Streptococcus pneumoniae (especially Diplococcus pneumoniae), Streptococcus agalactiae (group B streptococci), Bacillus mycoides, Bacillus subtilis, Corynebacterium diphtheriae, Eubacterium, Erysipelothrix insidiosa, Enterobacter aerogenes, Escherichia coli, Enterobacter cloacae, Acinetobacter spp. Proteus mirabilis, Neisseria gonorrhoeae (including strains that produce penicillinase), Propionibacterium, Neisseria meningitidis, Proteus vulgaris, Serratia marcescens, Proteus inconstans, many strains of Pseudomonas aeruginosa, Salmonella spp., Citrobacter spp., Providencia rettgeri, Serratia sp. p., Shigella spp., Veillonella, Bordetella pertussis, Yersinia, Moraxella, Fusobacterium, Aeromonas hydrophilia, Bacteroides spp., Peptostreptococcus species, Clostridium species, Peptococcus spp. Cefotaxime can act on multi-resistant strains that are resistant to first-generation cephalosporins, penicillins and aminoglycosides. Against gram-positive cocci, cefotaxime is less active than cephalosporins of the 1st and 2nd generations. Resistant to cefotaxime: Bacteroides fragilis, Acinetobacter baumannii, Clostridium difficile, Gram negative anaerobes, Enterococcus spp., Listeria monocytogenes, Pseudomonas aeruginosa, cepacia, Methi-R staphylococcus, Stenothrophomonas maltophilia.

There are no long-term animal studies evaluating the carcinogenic effect of cefotaxime. The mutagenic effect of cefotaxime was not detected (in the micronucleus test on mice and the Ames test). No effect on fertility was found in mice when administered intravenously up to 2000 mg/kg/day (0.7 MRH, in mg/m2) and in rats when administered subcutaneously up to 250 mg/kg/day (0.2 MRH, in mg/m2). m2).

Indications

Heavy bacterial infections that are caused by susceptible microorganisms: ENT organs and respiratory tract (except enterococcal), soft tissues and skin (including infected burns and wounds), joints and bones, pelvic organs, urinary tract, obstetric and gynecological (including chlamydia , gonorrhea, including those caused by microorganisms that secrete penicillinase), septicemia, bacteremia, peritonitis, bacterial meningitis (except for listeriosis), intra-abdominal infections, endocarditis, typhoid fever, Lyme disease, infections with immunodeficiency; prevention of infections during surgical operations, including those on the gastrointestinal tract.

Dosing and Administration of Cefotaxime

Cefotaxime is administered intravenously (drip or jet) and intramuscularly. The duration of therapy and the dosage regimen are determined individually, depending on the severity of the infection, indications, sensitivity of the microorganism. Adults usually take 1–2 g every 8–12 hours, the maximum daily dose is 12 g (in 3–4 injections); for children, doses are calculated depending on body weight and age. Dose adjustment is necessary in renal failure.

When using cephalosporins, it is necessary to collect an allergic history (hypersensitivity reactions to beta-lactam antibiotics, allergic diathesis). If the patient has a hypersensitivity reaction, then therapy should be discontinued. The use of cefotaxime is strictly contraindicated in patients with a history of hypersensitivity reactions to cephalosporins. immediate type. If there is any doubt during the first administration of the drug, the presence of a doctor is mandatory due to the possibility of developing an anaphylactic reaction. Exists cross allergy between penicillins and cephalosporins, occurring in 5-10% of cases. In patients with a history of penicillin allergy, cefotaxime should be used with extreme caution. In the first weeks of therapy, pseudomembranous colitis may develop, which is manifested by prolonged and severe diarrhea. The diagnosis is confirmed by histological examination and/or colonoscopy. This complication is regarded as very serious: cefotaxime is immediately canceled and prescribed adequate treatment, which includes oral metronidazole or vancomycin. The combination of cefotaxime with nephrotoxic agents requires monitoring functional state kidneys, use more than 10 days - monitoring cellular composition blood. Weakened and elderly patients should be prescribed vitamin K (to prevent hypocoagulation). During therapy with cefotaxime, a false-positive urine test for glucose and a false-positive Coombs test are possible.

Contraindications for use

Hypersensitivity (including to penicillins, carbapenems, other cephalosporins), breast-feeding, pregnancy, age up to 2.5 years (for intramuscular injection).

Application restrictions

Chronic renal failure, a history of enterocolitis (especially nonspecific ulcerative colitis), neonatal period.

Use during pregnancy and lactation

During pregnancy, the use of cefotaxime is possible if the predicted effects of treatment for the mother are higher than the possible risk to the fetus (strictly controlled and adequate safety studies of the use of the drug in pregnant women are not available). In reproduction studies, when administered intravenously to pregnant female rats up to 1200 mg/kg/day (0.8 MRDC, in mg/m2) or when administered intravenously to pregnant female mice up to 1200 mg/kg/day (0.4 MRDC, in mg/m2), m2) no evidence of teratogenic and embryotoxic effects was found. In studies of postnatal and perinatal development in rats, it was found that at a dose of 1200 mg / kg / day at birth, the body weight of the pups was significantly lower and remained less during 3 weeks of feeding than in the control group. During therapy with cefotaxime, breastfeeding should be discontinued.

Side effects of cefotaxime

Nervous system: dizziness, headache; digestive system: nausea, abdominal pain, vomiting, constipation / diarrhea, flatulence, transient increase in plasma transaminase activity, liver, LDH, bilirubin, alkaline phosphatase, dysbacteriosis, rarely - stomatitis, pseudomembranous colitis, glossitis; blood and circulatory system: cardiac arrhythmias (with jet rapid administration), transient leukopenia, neutropenia, granulocytopenia, thrombocytopenia, eosinophilia, agranulocytosis, autoimmune hemolytic anemia, hypoprothrombinemia;
urinary system: interstitial nephritis, an increase in the content of nitrogen in the blood plasma of creatinine and urea, oliguria, a violation of the functional state of the kidneys;
allergic reactions: flushing, rash, urticaria, erythema multiforme exudative, eosinophilia, Stevens-Johnson syndrome, fever/chills, toxic epidermal necrolysis, anaphylactic shock, angioedema; others: oral and vaginal candidiasis, superinfection;
reactions at the injection site: when administered intravenously: phlebitis, when administered intramuscularly: induration, pain and inflammation of the tissues at the injection site.

Interaction of cefotaxime with other substances

When cefotaxime is co-administered with loop diuretics, polymyxin B, aminoglycosides increase nephrotoxicity. The likelihood of bleeding increases when combined with cefotaxime antiplatelet agents (including non-steroidal anti-inflammatory drugs). Probenecid inhibits excretion, increases plasma levels and half-life of cefotaxime (increases the risk of developing side effects). Pharmaceutically, cefotaxime is incompatible in one infusion solution or syringe with solutions of other antibiotics.

Overdose

With an overdose of cefotaxime, tremors, convulsions, increased neuromuscular excitability, encephalopathy appear (especially in patients with renal insufficiency). Supportive and symptomatic treatment is necessary; there is no specific antidote.

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