Cefotaxime-Norton

Cefotaxime-norton is a semi-artificial antibiotic with a wide range of therapeutic effects. It is administered parenterally.

The bactericidal properties of the drug develop when the processes of binding of the bacterial cell membrane are slowed down. The drug has a high stability index under the influence of β-lactamases. At the same time, it demonstrates the activity of a relatively large number of pathogens resistant to the activity of ampicillin, other cephalosporins, gentamicin and other antimicrobial drugs.

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Indications Cefotaxime-Norton

It is used for severe infections caused by bacteria that are sensitive to the action of cephalosporins:

• respiratory tract lesions (pneumonia of bacterial origin, bronchitis in the active or chronic phase, pulmonary abscess, bronchiectatic pathology of infectious origin and complications caused by infection after operations in the sternum area);
• bacteremia or septicemia;
• meningitis (except listeria) and other infections affecting the central nervous system;
• infections of joints with bones (osteomyelitis or septic arthritis);
• lesions of the subcutaneous tissue with the epidermis;
• obstetric and gynecological infections (inflammations affecting the pelvic area);
• infections in the peritoneum (including peritonitis);
• lesions of the urinary tract (cystitis, pyelonephritis in the active or chronic phase and bacteriuria occurring without the development of symptoms);
• gonorrhea.

Prevention of infections in people after gynecological or urological surgeries, as well as procedures in the gastrointestinal tract.

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Release form

The drug is released in the form of an injection lyophilisate; 1 or 10 vials with powder inside the pack.

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Pharmacodynamics

Cefotaxime generally demonstrates activity against some bacteria in clinical settings and in vitro tests.

Gram-positive aerobes: Staphylococcus aureus (including strains that produce and do not produce penicillinase), enterococci, epidermal staphylococci, pneumococci, pyogenic streptococci (β-hemolytic from subgroup A), and agalactiae streptococci.

Gram-negative aerobes: enterobacter, meningococci, Citrobacter species, Haemophilus influenzae (including those resistant to ampicillin), Klebsiella (including Klebsiella pneumoniae), Escherichia coli, Haemophilus parainfluenzae, Proteus vulgaris, gonococci (with strains that produce and do not produce penicillinase), Morgan bacteria, Proteus mirabilis, Acinetobacter, Providencia Roettgerii and Serratia species.

Many strains of the bacteria described above, resistant to other antibiotics (for example, cephalosporins, penicillins and aminoglycosides), are sensitive to cefotaxime Na.

Cefotaxime demonstrates activity against certain strains of Pseudomonas aeruginosa.

Anaerobes: bacteroides (including individual strains of Bacteroides fragilis), peptococci, clostridia (most strains of Clostridium difficile are resistant), Fusobacterium species (including Plaut's bacillus), and peptostreptococci.

Cefotaxime has activity against Providence, Salmonella species (including S. typhi) and Shigella in vitro, but the clinical significance of this has not yet been determined.

Cefotaxime together with aminoglycosides exerts a synergistic effect in vitro against individual strains of Pseudomonas aeruginosa.

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Pharmacokinetics

The cefotaxime component easily penetrates tissues with fluids, achieving values that significantly exceed the MIC of a large number of pathogenic microbes. With a single use of 1 g of cefotaxime, the average plasma values of Cmax are 23.5 mg/l after half an hour.

The half-life of the substance is 1.2 hours. After 12 hours from the moment of drug administration, the antibiotic indicators are still quite high and allow to reveal the bactericidal effect on sensitive bacteria.

The drug is excreted through the kidneys (approximately 20-36% in an unchanged state). 15-25% is excreted in the form of the main metabolic element desacetylcefotaxime (has bactericidal activity). Another 20-25% of the drug is excreted in the form of 2 inactive metabolic components. Some of the drug is also excreted with bile.

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Dosing and administration

The method of application, dosage sizes and intervals between applications are determined by the degree of sensitivity of the bacteria that caused the pathology and the severity of the lesion.

The drug can be used intravenously (via infusion or bolus), as well as intramuscularly after performing a skin test for antibiotic tolerance.

Bolus (jet) application.

It is necessary to dilute 0.25, 0.5 or 1 g of lyophilisate in sterile injection liquid (4 ml). If 2 g of powder is taken, 10 ml of liquid is required. The medicine is administered by jet method, at low speed (3-5 minutes).

Administration of intravenous infusions.

It is necessary to dilute 1-2 g of the medication in 0.9% NaCl or 5% glucose solution (Ringer's lactate solution or other infusion fluid, excluding Na carbonate) - 40-100 ml of liquid is required.

A short infusion (2 g of powder per 40 ml of liquid) lasts 20 minutes. A longer infusion (2 g of lyophilisate per 0.1 l of liquid) is administered within 50-60 minutes.

Intramuscular injections.

1 g of the drug should be diluted in a sterile liquid or 1% lidocaine solution (4 ml; or 2 ml per 0.25-0.5 g of the substance). The drug is injected into the gluteal muscle, deeply.

Dosage portion sizes for different diseases.

For adults:

• gonorrhea in the active phase without complications – 1-time intramuscular injection of 1 g of the drug;
• infections affecting the urinary tract and uncomplicated lesions - jet intravenous injection or intramuscular injection of 1 g of the substance at 12-hour intervals;
• lesions of moderate severity: 1-2 g of the drug is administered intramuscularly or intravenously with 12-hour breaks;
• very severe forms of infection (for example, meningitis): intravenous administration of 2 g of the drug at 6-8 hour intervals;
• to prevent infectious complications after operations: together with the introduction of anesthesia, 1 g of the drug is used intravenously once. If necessary, a repeat injection can be performed after 6-12 hours.

It is allowed to use no more than 12 g of Cefotaxime-Norton per day.

Children over 1 month and up to 12 years of age (weight less than 50 kg): 0.1-0.15 g/kg of the substance is administered intramuscularly or intravenously per day (only for children over 2.5 years of age). This portion is divided into 3-4 injections (with a 6-8 hour interval), taking into account the intensity of the infection. In case of severe stages of infection, daily portions of 0.2 g/kg can be used.

Children weighing over 50 kg are prescribed standard adult dosages with a maximum daily dose of 12 g.

Infants aged 1-4 weeks and premature babies: intravenous administration of 50 mg/kg per day is allowed (in 3-4 injections, with 6-8 hour intervals). In case of severe disorders, 0.15-0.2 g/kg of the drug is allowed per day.

Infants up to 7 days of age and premature babies: intravenous injection of 50 mg/kg per day, divided into 2 injections in equal portions (12-hour intervals).

The duration of the treatment cycle is selected individually.

In case of problems with kidney function, the portion size is selected taking into account the severity of the renal disorder. At the initial phase of anuria (the level of CC is less than 10 ml per minute), the standard portion of the drug is halved, without changing the interval between doses.

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Use Cefotaxime-Norton during pregnancy

Cefotaxime-Norton is prohibited to prescribe to pregnant women, especially in the first trimester. The only exceptions are situations with use according to strict indications. This is due to the fact that there is no confirmed data regarding the safety of the drug for pregnant women.

A small amount of the drug is excreted in breast milk, therefore, if it is necessary to administer the component during breastfeeding, it is necessary to first stop breastfeeding for the duration of therapy.

Contraindications

Contraindications include: severe intolerance to the effects of cephalosporin antibiotics.

In cases where the injected fluid contains lidocaine:

• personal intolerance to lidocaine;
• intracardiac blocks in individuals who do not have a pacemaker;
• having severe heart failure;
• intravenous injections.

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Side effects Cefotaxime-Norton

Main side effects:

• signs of allergy: rash, bronchospasm, urticaria, itching and Quincke's edema. Occasionally, SJS, MEE, anaphylaxis, eosinophilia, TEN and fever are observed;
• liver and digestive system damage: vomiting, diarrhea, loss of appetite, abdominal pain and nausea are occasionally observed, as well as an increase in transaminase or bilirubin, alkaline phosphatase and LDH. When using Cefotaxime Norton or after the end of therapy, pseudomembranous colitis caused by the action of Clostridium difficile may occur;
• disorders of hematopoietic processes: thrombocyto-, neutro- or leukopenia, hemolytic anemia, agranulocytosis and eosinophilia;
• urinary dysfunction: tubulointerstitial nephritis;
• problems with the central nervous system: headaches or treatable encephalopathy (when using large doses, especially in people with renal insufficiency);
• Adverse effects caused by biological influences: long-term therapy may lead to candidiasis, dysbacteriosis or superinfection caused by drug-resistant strains;
• Others: candidiasis affecting the mucous membranes and an increase in temperature. Excessively high fluid intake rate can cause arrhythmia;
• local symptoms: pain in the injection area, as well as phlebitis that occurs in the case of intravenous injection.

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Overdose

Possible signs of poisoning include: thrombocytopenia or leukopenia, fever, dyspnea, active hemolytic anemia, anorexia, gastrointestinal or epidermal manifestations, and liver manifestations, as well as stomatitis, loss of spatial orientation, renal failure, transient hearing loss, and encephalopathy (especially in the case of renal failure).

The drug has no antidote. The required symptomatic measures are taken to support vital functions of the body.

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Interactions with other drugs

Combined use of the drug with aminoglycosides caused an increase in the nephrotoxic effect. Similar effects are also exerted by diuretics - derivatives of ethacrynic acid with pyrethadine and other diuretic drugs (for example, furosemide).

Combination with nifedipine increases the bioavailability of cefotaxime by 70%.

When using probenecid, the excretion of cefotaxime through the tubules is blocked and its half-life is prolonged.

Administration together with NSAIDs (such as diclofenac, aspirin or indomethacin) increases the likelihood of bleeding (including within the digestive system).

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Storage conditions

Cefotaxime-Norton should be stored in a dark place, out of the reach of small children. Temperature indicators - no more than 25 ° C. The prepared solution remains stable for 24 hours at temperatures of 2-8 ° C.

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Shelf life

Cefotaxime-Norton can be used for a period of 24 months from the date of sale of the drug.

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Application for children

The drug can be administered to infants aged 1-12 months only if there are strict indications. The drug should also not be administered intramuscularly to children under 2.5 years of age.

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Analogues

The analogs of the drug are Loraxim, Cefotaxime with Taxtam, and in addition Sefotak, Cefantral and Fagocef with Tax-O-Bid.

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