Cefabol

Cephabol is an antibiotic that belongs to the cephalosporin group.

Indications Cefabola

It is used to eliminate severe and moderate infectious processes with different localizations, caused by microbes that are sensitive to cefotaxime - in adults, as well as children, even newborns:

• infectious processes in the central nervous system (including meningitis);
• infections in the ENT organs and respiratory system (this includes pneumonia);
• infections in the urinary system (including pyelonephritis);
• bone and joint infections;
• infectious processes in the area of soft tissues with skin (for example, complications in the area of wounds remaining after operations);
• infections in the pelvic area (for example, endometritis with pelvic peritonitis, as well as acute adnexitis (or exacerbation of its chronic form));
• tick-borne borreliosis, gonorrhea, as well as sepsis, endocarditis and salmonellosis;
• infections that develop as a result of immunodeficiency;
• prevention of infection development in the postoperative period (this includes the gastrointestinal tract, as well as obstetric-gynecological and urological procedures).

Release form

It is produced in the form of powder for the preparation of injection solutions in 2 doses. It has the following packaging:

• 1 bottle (0.5 or 1 g) with powder and 1 ampoule (5 ml) with solvent per pack;
• 50 vials with powder of 0.5 or 1 g per pack;
• 5 vials with powder of 0.5 or 1 g per package.

Pharmacodynamics

Cefotaxime is an antibiotic from the cephalosporin group (3rd generation), used parenterally. It has bactericidal properties: it is synthesized with transpeptidases, and at the same time prevents the final stages of bacterial cell wall binding. The drug has a wide range of antimicrobial action.

It actively affects gram-negative and gram-positive bacteria (this includes microbes resistant to cephalosporins and penicillins of the 1st and 2nd generations):

• staphylococci (including Staphylococcus aureus and Staphylococcus epidermidis; in addition to methicillin-resistant strains) and most streptococci (including pneumococcus, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus bovis, viridans streptococci, etc.);
• enterococci, diphtheria corynebacterium, Erysipelothrix rhusiopathiae, acinetobacter, whooping cough bacillus, citrobacter, enterobacter and Escherichia coli;
• influenza bacillus (including strains resistant to ampicillin), H. parainfluenzae, Klebsiella (including Klebsiella pneumoniae), Morgan bacteria and gonococcus (including strains producing β-lactamases);
• meningococcus, Proteus mirabilis, Proteus vulgaris, Providencia spp., Providencia roettgerii, Providencia stuartii, Serratia marcescens, Shigella, Salmonella (this includes S. typhi) and Yersinia (also Yersinia enterocolitica);
• Borrelia burgdorferi, bacteroides (including individual strains of Bacteroides fragilis), clostridia (except Clostridium difficile), Fusobacterium spp. (including Plaut's bacillus), peptococci, peptostreptococci, and propionibacteria.

It is resistant to most β-lactamases of gram-negative and gram-positive bacteria, as well as to staphylococcal penicillinase.

Pharmacokinetics

The peak value of the substance in the serum after a single intravenous injection of 1 g of the drug is observed 5 minutes after administration and is 101.7 mg/l. Half an hour after an intramuscular injection of a similar dose, the peak value of the drug is 20.5 mg/l.

The level of bioavailability of the substance with intramuscular injection reaches 90-95%. Synthesis with plasma protein is 25-40%.

After intramuscular and intravenous injections, medicinal concentrations of the substance are observed inside most tissues (in the myocardium with lungs, kidneys, bones, skin, peritoneal organs, subcutaneous layer and in the mucous membrane of the nasal sinuses), and also in fluids (cerebrospinal, pleural, pericardial and ascitic, as well as in synovium, middle ear fluid, etc.). Low concentrations of the drug penetrate into mother's milk, as well as through the placental barrier. The distribution volume is 0.25-0.39 l/kg.

The half-life of the active component from serum (with intramuscular or intravenous injections) is approximately 1 hour (in newborns this figure reaches 0.75-1.5 hours). Cefotaxime partially undergoes hepatic metabolism, as a result of which an active decay product (M1) is formed - the substance deacetylcefotaxime, and in addition to this, 2 inactive ones - components M2, as well as M3.

Approximately 80% of cefotaxime is excreted in the urine (44-61% of the substance remains unchanged, and the remainder is excreted in the form of deacetylcefotaxime (13-24%) and inactive degradation products M2 and M3 (7-16%)). After repeated intravenous injections of 1 g at 6-hour intervals for a period of 2 weeks, the substance does not accumulate in the body.

In elderly people with chronic renal failure, the half-life is doubled. This period is also increased in premature infants – up to 4.6 hours.

Dosing and administration

Injections are performed intramuscularly and intravenously (jet or drip) - the choice of administration method depends on the selected dosage, regimen and severity of the pathology.

For teenagers from 12 years old (or weighing 50+ kg) and adults.

In case of development of uncomplicated infectious processes, it is necessary to administer injections in the amount of 1 g at intervals of 12 hours intramuscularly or intravenously.

To eliminate uncomplicated gonorrhea in acute form, a single injection of 0.5-1 g intramuscularly is required. In the case of moderate infections, it is necessary to give intravenous or intramuscular injections in the amount of 1-2 g at intervals of 8 hours. If it is necessary to administer large doses of antibiotic (for example, in sepsis), injections of 2 g intravenously are prescribed at intervals of 6-8 hours. If the infectious process acquires a life-threatening form, it is allowed to reduce the intervals between procedures to 4 hours (no more than 12 g can be administered per day).

For antimicrobial prophylaxis to prevent the development of purulent-septic complications after surgical operations, injections of 1 g are used (once, half an hour before the procedure). If necessary, the injection can be repeated after 6 and 12 hours. Patients undergoing cesarean section are required to administer 1 g of the solution intravenously immediately after the umbilical cord has been clamped. Further, if necessary, additional injections of 1 g are allowed after 6 and 12 hours after the first dose.

Individuals with severe renal impairment (creatinine clearance level is 20 ml/minute/1.73 m2 ⁾ are required to reduce the daily dose of the drug by half.

For children in the first month of life (without taking into account gestational age), the following doses of the drug are required:

• during the 1st week, an intravenous injection of 50 mg/kg is required at 12-hour intervals;
• period 1-4 weeks – intravenous injection of 50 mg/kg at intervals of 8 hours.

For children from 1 month to 12 years (or weighing less than 50 kg), the daily dose of the solution (50-180 mg/kg) should be divided into 4-6 injections (intravenously or intramuscularly). If a severe infection is observed (e.g. meningitis), the daily dose for the child should be increased to 200 mg/kg (into 4-6 injections).

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Use Cefabola during pregnancy

The use of Cefabol during pregnancy is permitted only in situations where the probable benefit to the woman is higher than the risk of negative consequences for the fetus.

Cefotaxime can pass into breast milk, which is why breastfeeding must be stopped while using the drug.

Contraindications

Main contraindication: hypersensitivity to cefotaxime and other cephalosporins.

When used in the form of a solvent in the preparation of lidocaine solution:

• cardiogenic shock;
• heart blockages with an unestablished rhythm;
• intravenous injection;
• children under 2.5 years old;
• intolerance to lidocaine or other amide anesthetic for local application.

Caution is required when used in non-specific ulcerative colitis (also if present in the anamnesis) and chronic renal failure, as well as in the presence of a history of allergy to penicillins.

Side effects Cefabola

Treatment is often well tolerated, side effects are rare and disappear quickly when the drug is discontinued. The following reactions are distinguished:

• manifestations of allergy: development of anaphylaxis, eosinophilia, Quincke's edema, urticaria, fever and Lyell's or Stevens-Johnson syndromes, the appearance of rashes, chills, itching and bronchospasm;
• reactions of the digestive organs: constipation or diarrhea, nausea, bloating, abdominal pain and vomiting, as well as the occurrence of glossitis, stomatitis and dysbacteriosis, as well as pseudomembranous colitis and antibiotic-induced diarrhea;
• manifestations from the hematopoietic system: neutro-, leukopenia-, thrombocyto- and granulocytopenia, as well as hemolytic anemia;
• urinary system organs: development of tubulointerstitial nephritis or oliguria;
• NS reactions: dizziness with headaches;
• laboratory test results: an increase in the urea level and the activity of alkaline phosphatase and liver transaminases, as well as the development of azotemia, hypercreatininemia or hyperbilirubinemia;
• manifestations from the cardiovascular system: with a rapid bolus injection into the central vein, arrhythmias may develop that are potentially life-threatening;
• local manifestations: pain along the vein, infiltrate and pain at the site of intramuscular injection, as well as the development of phlebitis;
• others: the appearance of superinfection (among these is thrush).

Overdose

Overdose may cause the following disorders: tremors, seizures, increased excitability of the neuromuscular system, as well as cyanosis and encephalopathy (when injected in high doses, especially in people with kidney failure).

To eliminate the disorders, it is necessary to provide supportive therapy to the patient and perform symptomatic treatment.

Interactions with other drugs

The combination of the drug with aminoglycosides causes the development of additive and synergistic effects.

The drug solution has pharmaceutical incompatibility with vancomycin and aminoglycosides. If a combination of these drugs is required, it is prohibited to mix them in one syringe or in one infusion. Intramuscular injection requires administering drugs to different areas of the body. Intravenous injection must be performed separately, observing the required sequence (the longest possible time intervals between procedures), or use different catheters for intravenous administration. It is prohibited to use sodium bicarbonate solution to dissolve the powder.

Combination with NSAIDs and antiplatelet agents increases the likelihood of bleeding.

Tubular secretion blocking drugs increase plasma levels of cefotaxime and also inhibit its excretion rate.

The risk of developing functional renal disorder increases in the case of a combination of Cefabol with polymyxin B, as well as loop diuretics and aminoglycosides.

In case of combination with ethyl alcohol, the development of disulfiram-like manifestations is not observed.

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Storage conditions

Cephabol must be kept in a place protected from light and inaccessible to small children. Temperature level – maximum 25°C.

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Shelf life

Cefabol is permitted to be used for a period of 2 years from the date of manufacture of the medicinal solution.