Cefabol

Cefabol is an antibiotic that is part of the cephalosporin group.

Indications of the cefabol

It is used in the elimination of infectious processes of severe and moderate degree with different localization, provoked by microbes that are sensitive to cefotaxime - in adults, as well as children, even newborns:

• infectious processes in the central nervous system (among them meningitis);
• infection in the area of ENT organs and the respiratory system (this includes inflammation of the lungs);
• infection in the urinary system (among them pyelonephritis);
• bone and joint infections;
• infectious processes in the area of soft tissues with skin (for example, complications in the area of wounds left after operations);
• infection in the pelvic region (for example, endometritis with pelvioperitonitis, as well as acute adnexitis (or exacerbation of its chronic form));
• tick-borne borreliosis, gonorrhea, as well as sepsis, endocarditis and salmonellosis;
• infection, developed due to immunodeficiency;
• prevention of the development of infections in the postoperative period (this includes the gastrointestinal tract, as well as obstetric-gynecological and urological procedures).

Release form

It is available in the form of a powder for the preparation of injection solutions in 2 doses. Has such packing:

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

Pharmacodynamics

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

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

• staphylococcus (this includes staphylococcus aureus and epidermal, in addition to methicillin-resistant strains) and most streptococci (this includes pneumococcus, streptococcus pyogenes, streptococcus agalactia, Streptococcus bovis, streptococci from the viridans category, etc.);
• enterococci, diphtheria corynebacterium, Erysipelothrix rhusiopathiae, acitetobacter, pertussis, cytrobacterium, enterobacteria and E. Coli;
• Influenza rod (here also includes strains resistant to ampicillin), H. Parainfluenzae, Klebsiella (among them Klebsiella pneumonia), morgana bacterium and gonococcus (among them strains producing β-lactamases);
• meningococcus, proteus mirabilis, vulgar proteus, Providencia spp., Providence of Rettgera, Stewart's providential, Marcesian, Shigella, Salmonella (S. Typhi included) and Yersinia (also Yersinia enterocolitis);
• Borrelia Burgdorfer, bacteroids, (this includes separate strains of bacteroidia fragilis), clostridia (except clostridium difffile), Fusobacterium spp. (among them Plaut's wand), peptococci, peptostreptococci and propionibacteria.

Has a resistance against most β-lactamases of gram-negative and gram-positive bacteria, and in addition penicillinase of staphylococci.

Pharmacokinetics

The peak value of the substance inside the serum after a one-time intravenous injection of the 1st g medication is observed 5 minutes after the administration and is equal to 101.7 mg / l. After half an hour after 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, drug concentrations of the substance are observed inside most tissues (in the myocardium with the lungs, kidneys, bones, skin, peritoneal organs, subcutaneous layer and in the nasal mucosa), and in liquids (cerebrospinal, pleural, pericardial and ascitic , and also in synovia, the fluid of the middle ear, etc.). Low concentrations of drugs penetrate into the 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 ingredient from the serum (for intramuscular or intravenous injections) is approximately 1 hour (in newborns this figure reaches 0.75-1.5 hours). Cefotaxime partially passes the hepatic metabolism, as a result of which the active product of decomposition (M1) - deacetylcefotaxime substance is formed, and in addition 2 inactive components - M2, as well as M3.

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

In elderly people with chronic kidney failure, an increase in half-life is observed in half. This period is also increasing in preterm infants - up to 4.6 hours.

Dosing and administration

Injections are performed in / m and / in the method (jet or drip) - the choice of the method of administration depends on the chosen dosage, regimen and degree of severity of the pathology.

For adolescents from 12 years (or with a weight of 50+ kg) and adults.

In the case of uncomplicated infectious processes, injections are required at a rate of 1 g at intervals of 12 hours intramuscularly or intravenously.

To eliminate uncomplicated gonorrhea in the acute form requires a single injection of 0.5-1 g intramuscularly. With the development of moderate infections, it is necessary to inject in / in or in / m way in the amount of 1-2 grams at intervals of 8 hours. When the need to administer large doses of antibiotic (for example, with sepsis), injections in the amount of 2 g intravenously with intervals of 6-8 hours are prescribed. If the infectious process acquires a life-threatening form, it is allowed to shorten the intervals between the procedures up to 4 hours (no more than 12 g can be administered per day).

With antimicrobial prophylaxis, in order to prevent the appearance of complications of purulent-septic nature after surgery, injections in the amount of 1 g (once a day, half an hour before the procedure) are used. If necessary, you can repeat the injection 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, it is allowed to inject additional injections in the amount of 1 g after 6 and 12 hours after the first dose.

Persons suffering from disorders of renal function in severe form (CC level is 20 ml / minute / 1.73 m ² ), it is required to reduce the daily dose of drugs by half.

Children at the 1st month of life (without taking into account gestational age) are required to administer such doses of the medicine:

• at week 1, an intravenous injection of 50 mg / kg is necessary at intervals of 12 hours;
• period 1-4 weeks - intravenous injection of 50 mg / kg at intervals of 8 hours.

Children, starting with the 1st month and up 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 (eg, meningitis) is observed, the daily dose for the child should be increased to 200 mg / kg (for 4-6 injections).

[1]

Use of the cefabol during pregnancy

Use Cefabol during pregnancy is allowed only in situations where the likely benefits for a woman is higher than the risk of fetal negative consequences.

Cefotaxime is able to pass into the mother's milk, because of what it is required to cancel breastfeeding while using drugs.

Contraindications

The main contraindication: hypersensitivity to cefotaxime and other cephalosporins.

If used in the form of a solvent in the manufacture of a lidocaine solution:

• cardiogenic shock;
• blockade in the heart against the background of an unstated rhythm;
• injection in / in the way;
• children younger than 2.5 years;
• intolerance to lidocaine or other amide anesthetic for topical application.

Caution is required if used for ulcerative colitis of a non-specific type (also if there is an anamnesis) and chronic kidney failure, and also if there is a history of allergy to penicillins.

Side effects of the cefabol

Often the treatment is well tolerated, side effects develop rarely and quickly disappear in the event of drug withdrawal. The following reactions stand out:

• manifestations of allergy: the development of anaphylaxis, eosinophilia, Quincke edema, urticaria, fever and Lyell syndrome or Stevens-Johnson, the appearance of rashes, chills, itching and spasm of the bronchi;
• reactions of the digestive system: constipation or diarrhea, nausea, swelling, abdominal pain and vomiting, and in addition the appearance of glossitis, stomatitis and dysbiosis, as well as pseudomembranous form of colitis and antibiotic-induced diarrhea;
• manifestations of the hematopoietic system: neutron, leuko-, thrombocyto- and granulocytopenia, as well as hemolytic form of anemia;
• organs of the urinary system: development of tubulointerstitial nephritis or oliguria;
• reactions of NS: dizziness with headaches;
• results of laboratory studies: an increase in the urea index and the activity of AP and liver transaminases, as well as the development of azotemia, hypercreatininaemia or hyperbilirubinemia;
• manifestations on the part of the CAS: with fast bolus injection into the central vein area, arrhythmias potentially life-threatening can develop;
• local manifestations: pain along the vein, infiltration and pain in the intramuscular injection site, as well as the development of phlebitis;
• others: the emergence of superinfection (among these are thrush).

Overdose

Overdose can cause the following disorders: tremor, 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 remove abnormalities, it is necessary to provide a supportive state of patient therapy and perform symptomatic treatment.

Interactions with other drugs

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

The drug solution has a pharmaceutical incompatibility with vancomycin, as well as aminoglycosides. In the case of the need for a combination of these drugs, it is prohibited to mix them inside a single syringe or in one infusion. When intramuscular injection is required to inject drugs into different areas of the body. Intravenous injection should be performed separately, in accordance with the required sequence (the maximum long time intervals between the procedures), or use different catheters for intravenous administration. Do not use a solution of sodium bicarbonate to dissolve the powder.

Combination with NSAIDs, as well as antiaggregants, increases the likelihood of bleeding.

Drugs-blockers of tubular secretion increase the level of cefotaxime inside the plasma, and also slow down the rate of its excretion.

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

In the case of a combination with ethyl alcohol, there is no development of disulfiram-like manifestations.

[2], [3]

Storage conditions

Cefabol should be kept in a place that is closed from light and not accessible to young children. The temperature level is a maximum of 25 ° C.

[4]

Shelf life

Cefabol is allowed to be used in the period of 2 years from the date of manufacture of the medicinal solution.