Cefantral

Cefantral is a systemic antimicrobial drug from the category of 3rd generation cephalosporins. It also belongs to the group of other β-lactam antibiotics.

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Indications Cefantral

It is used to eliminate infectious lesions caused by the action of microbes sensitive to the drug:

• ENT system (otitis, as well as tonsillitis);
• lesions affecting the respiratory system (pneumonia, bronchitis, abscess, and pleurisy);
• infections in the urogenital system;
• blood poisoning, as well as bacteremia;
• infections localized in the intra-abdominal region (this also includes peritonitis);
• lesions of soft tissues with skin;
• disorders affecting joints with bones;
• meningitis (except for the listeriosis form), as well as other infections in the central nervous system.

To prevent the occurrence of infections after surgical procedures in the digestive system, as well as after obstetric-gynecological or urological operations.

Release form

The product is released in the form of a lyophilisate used in the manufacture of medicinal solutions. The box contains 1 bottle of powder.

Pharmacodynamics

The element cefotaxime is a semi-synthetic antibiotic from the 3rd generation of cephalosporins. It is used parenterally. It has a bactericidal effect and a wide range of medicinal activity.

The following are sensitive to the drug:

• streptococci (except category D), including pneumococcus;
• Staphylococcus aureus, as well as strains that produce and do not produce penicillinase;
• hay bacillus and mushroom bacillus;
• gonococci (strains that produce and do not produce penicillinase), meningococci and other types of Neisseria;
• E. coli;
• Klebsiella (this also includes Friedlander's bacillus);
• Enterobacter (certain strains are resistant) and Serratia;
• Proteus (indole-positive and also indole-negative types);
• salmonella, citrobacter, shigella, providencia, yersinia;
• influenza bacillus and Haemophilus parainfluenzae (strains that produce/do not produce penicillinase, and are also resistant to ampicillin), as well as the Bordet-Gengou bacterium;
• Moraxella, hydrophilic Aeromonas, Veillonella, Clostridium perfringens;
• eubacteria, propionic acid bacteria, fusobacteria, bacteroides, and also Morganella.

The following have variable sensitivity to the drug: Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, Bacteroides fragilis and Clostridium difficile.

Resistance to Cefantral is demonstrated by methicillin-resistant staphylococci, as well as category D streptococci and Listeria.

Pharmacokinetics

Absorption.

After 5 minutes from a single injection of 1 g of the drug, the serum level of the substance reaches 100 mcg/ml. Peak values of the drug in the blood are observed after half an hour and are equal to 24 mcg/ml. Bactericidal indicators in the blood are maintained for another 12 hours.

Distribution values.

Protein synthesis inside the blood plasma is approximately 25-40% (average). Cefotaxime quickly penetrates into tissues with biological fluids. Effective medicinal concentrations are observed inside the synovium, peritoneal and pleural fluid. The drug passes through the BBB. During metabolism, an active decay product is formed.

Excretion.

About 60-70% of the administered dose is excreted as unchanged substance in the urine, and the remainder is excreted as metabolic products. Part of the drug is excreted in the bile.

The half-life is 1 hour after intravenous injection, and 1-1.5 hours after intramuscular injection.

In elderly people, and also in cases of renal failure, the half-life of the drug is extended approximately twofold.

In newborns, the half-life of the drug reaches 0.75-1.5 hours, and in premature babies - approximately 1.4-6.4 hours.

Dosing and administration

The medicine is used for intramuscular and intravenous (drip or jet) injections.

Before using the medication, a skin test should be performed to determine sensitivity to the antibiotic with lidocaine. If lidocaine is used for intramuscular injections as a solvent, it is necessary to take into account the data on the safety of this substance.

For jet injections, 1 g of lyophilisate should be diluted in injection water (8 ml). The rate of administration should be low – the procedure lasts 3-5 minutes.

For intravenous infusion, 50 ml of sodium chloride (0.9%) or glucose (5%) solution is required to dilute 1 g of lyophilisate. This infusion lasts for 50-60 minutes.

If intramuscular administration is performed, 1 g of the drug is diluted in sterile injection water (4 ml) or in a lidocaine solution (1%). The injection is made deep into the buttock muscle.

The duration of the therapeutic course is selected individually by the attending physician.

Children weighing more than 50 kg, as well as adults, need to use the drug in a dosage of 1 g, with intervals of 12 hours. In severe diseases, Cefantral in a portion of 1 g is administered 3-4 times a day.

Patients are allowed to administer no more than 12 g of solution per day.

Frequency of drug administration and portion sizes:

• treatment of uncomplicated infections, as well as lesions in the urinary system - intravenous or intramuscular administration of 1 g of the drug at intervals of 12 hours;
• treatment of the acute stage of uncomplicated gonorrhea - use in a dosage of 1 g, administered once a day intravenously or intramuscularly;
• elimination of moderate infections – use of a solution in a dosage of 1-2 g, at intervals of 12 hours;
• therapy for severe forms of infectious disorders (such as meningitis) – administration of the drug in 2 g doses at intervals of 6-8 hours.

For a child weighing less than 50 kg, the drug should be prescribed in a dose of 50-100 mg / kg / day. This dose should be divided into 3-4 intravenous or intramuscular administration procedures. If the patient has a severe form of the disorder (for example, meningitis), it is allowed to increase the daily dose to 100-200 mg / kg, with intravenous or intramuscular administration 4-6 times.

Premature infants and infants under the age of 7 days should be given 50 mg/kg of the drug per day. This portion is divided into 2 equal parts and administered intravenously.

Infants from 8 days to 1 month of age should be given 50-100 mg/kg of the drug per day. The dosage is divided into 3 equal portions and administered as an intravenous injection.

To prevent the occurrence of infections as a result of surgical operation, it is necessary to give the patient a single injection of 1 g of the drug before administering anesthesia. If necessary, this procedure should be repeated after 6-12 hours.

If a person has problems with kidney function, the dosage of Cefantral should be reduced. With CC values up to 10 ml/minute, the daily dose of the drug should be halved.

Use Cefantral during pregnancy

The use of Cefantral during pregnancy is prohibited.

During therapy, breastfeeding should be discontinued.

Contraindications

Among the contraindications:

• hypersensitivity to cephalosporin antibiotics and other β-lactam antibiotics, as well as intolerance to lidocaine (with intramuscular administration);
• presence of bleeding;
• a history of enterocolitis (especially ulcerative colitis, which is non-specific);
• AV blocks until the heart rate indicator has been determined;
• severe heart failure.

It is prohibited to administer the medicine intramuscularly to children under 2.5 years of age.

Side effects Cefantral

The use of the solution may cause the following side effects:

• digestive disorders: the appearance of bloating, vomiting, abdominal pain, nausea and diarrhea, as well as the development of dysbiosis. Glossitis or stomatitis are occasionally observed, as well as pseudomembranous colitis;
• allergy symptoms: itching, rashes, bronchial spasms, hyperemia, urticaria, erythema multiforme, TEN and Stevens-Johnson syndrome. In addition, the development of Quincke's edema, fever and anaphylactic manifestations. Anaphylaxis is occasionally noted;
• damage to the hepatobiliary system: development of functional liver disorders, hepatitis, jaundice, acute stage of liver failure, and in addition cholestasis;
• biochemical data: increased liver transaminase, alkaline phosphatase, LDH and bilirubin levels, as well as creatinine and urea nitrogen levels. At the same time, a positive Coombs test may be observed;
• peripheral blood flow lesions: development of neutro-, thrombocyto-, and granulocytopenia, as well as transient leukopenia, anisocytosis with agranulocytosis, hypocoagulation, hemolytic anemia, and eosinophilia with hypoprothrombinemia;
• disorders of the nervous system function: dizziness, a feeling of weakness or severe fatigue, as well as cramps and headaches. Treatable encephalopathy may also develop;
• manifestations in the injection area: the appearance of an infiltrate and pain at the injection site, pain spreading along the vein, as well as phlebitis and tissue inflammation;
• symptoms caused by biological influences: superinfection may occur (including vaginitis with candidiasis);
• Others: the appearance of hemorrhages or bleeding, the development of a hemolytic form of anemia of an autoimmune nature or tubulointerstitial nephritis, as well as arrhythmia (if a rapid jet injection is performed).

During therapy for infections caused by spirochetes, complications (such as the Jarisch-Herxheimer reaction) may occur. This may result in chills, fever, joint pain, and headaches.

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Overdose

Signs of poisoning include: leukopenia or thrombocytopenia, fever, acute hemolytic anemia, symptoms of the skin, gastrointestinal tract, and liver, stomatitis, dyspnea, anorexia, and in addition, renal failure, temporary hearing loss, encephalopathy (especially in people with renal failure), and loss of spatial orientation.

The drug has no specific antidote. Plasma values of cefotaxime can be reduced by peritoneal dialysis or hemodialysis. If necessary, symptomatic procedures should be performed.

If the victim develops anaphylaxis, immediate measures must be taken. After the first symptoms of intolerance reaction (such as urticaria, rash, nausea, loss of consciousness and headache) appear, it is necessary to stop the administration of the drug. In case of severe signs of hypersensitivity or anaphylactic manifestations, it is necessary to take appropriate measures (administer GCS or epinephrine to the patient). If other clinical conditions develop, it may be necessary to use additional methods, such as the use of receptor antagonists and artificial respiration. In case of vascular insufficiency, resuscitation procedures are required.

Interactions with other drugs

Combination with nephrotoxic agents (eg, aminoglycosides), as well as potent diuretics (such as furosemide or ethacrynic acid), polymyxin and colistin increases the risk of renal failure.

During therapy with cefotaxime, the effectiveness of oral contraception may be reduced, which is why additional contraceptive measures must be used during treatment.

The drug is prohibited to be combined with bacteriostatic antibiotics (for example, erythromycin, tetracyclines, and also chloramphenicol), because this can cause an antagonistic effect.

It is prohibited to mix cefotaxime and aminoglycoside solutions in the same syringe – they must be administered separately.

Combined use with nifedipine increases the bioavailability of cefotaxime by 70%.

Probenecid blocks the tubular excretion of cefotaxime and prolongs its half-life.

It is prohibited to combine Cefantral with lidocaine:

• for intravenous injections;
• in infants under 2.5 years of age;
• persons with a history of intolerance to lidocaine;
• people with heart block.

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Storage conditions

Cefantral should be kept in a place out of reach of small children. Temperature indicators should not exceed 25°C.

After preparation of the medicinal solution for intramuscular injection, the drug can be stored for another 12 hours at temperatures not exceeding 25°C, and also for a maximum of 7 days in the original package – at temperatures within 2-8°C (refrigerator).

The prepared solution for intravenous injections can be stored for a maximum of 24 hours at a temperature of no more than 25°C, and for a maximum of 5 days at a temperature of 2-8°C.

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Shelf life

Cefantral can be used for 3 years from the date of manufacture of the drug.