Cephabol - instructions for use

Release form and composition

Cephabol is available in the form of a white or yellowish-white powder that is sensitive to light. The drug is used to prepare a solution for intramuscular or intravenous administration. 1 bottle contains 1000 mg of the active substance - cefotaxime sodium (in terms of cefotaxime). Water for injection in ampoules of 5 ml is used as a solvent.

The drug has the following packaging options:

• 1 bottle in a cardboard box;
• 1 bottle with the drug and 1 ampoule with solvent in a cardboard box;
• 1 bottle with the drug and 1 ampoule with solvent in a blister pack made of polyvinyl chloride film and varnished aluminum foil or without foil. Blistered packaging is supplied in a cardboard box;
• 5 bottles of the drug in a blister pack made of polyvinyl chloride film and lacquered aluminum foil or without foil are supplied in a cardboard box;
• 5 bottles with the drug and 5 ampoules with a solvent in a blister pack made of polyvinyl chloride film and varnished aluminum foil or without foil are supplied in a cardboard box.

Pharmacological properties

Pharmacodynamics

Cephabol is an antibacterial drug for parenteral use. It has a bactericidal and broad spectrum antimicrobial effect. The antibacterial activity of Cephabol is due to the properties of cefotaxime, which is a third generation cephalosporin.

The following gram-positive and gram-negative microorganisms that are resistant to other antibiotics exhibit sensitivity to cefotaxime: Staphylococcus speciales (spp.), Staphylococcus aureus (including penicillinase-forming strains), Streptococcus pneumoniae, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pyogenes, Enterobacter spp., Enterococcus species , Escherichia coli, Haemophilus parainfluenzae, Haemophilus influenzae (including penicillinase-forming strains), Morganella morganii, Klebsiella spp., Klebsiella pneumoniae, Acinetobacter species, Neisseria gonorrhoeae (including penicillinase-forming strains), Corynebacterium diphtheriae, Eubacterium spp., Erysipelothrix insidiosa, Neisseria meningitidis, Propionibacterium spp., Clostridium spp. (including Clostridium perfringens), Bacillus subtilis, Proteus indole, Proteus mirabilis, Proteus vulgaris, Citrobacter spp., Serratia spp., Providencia spp. (including Providencia rettgeri), Pseudomonas aeruginosa, Bacteroides spp. (including some strains of Bacteroides fragilis), Peptococcus spp., Fusobacterium spp. (including Fusobacterium nucleatum), Peptostreptococcus spp.

Cephabol is resistant to most beta-lactamases of gram-positive and gram-negative microorganisms, Clostridium difficile strains, and staphylococcal penicillinase.

Pharmacokinetics

The maximum concentration (Cmax) after a single administration of Cephabol in a dose of 1000 mg with intravenous administration is achieved after 1/12 hour and is 0.1017 mg/ml, with intramuscular administration - after 1/2 hour and is 0.021 mg/ml.

Plasma protein binding ranges from 25% to 40% of the administered dose.

Therapeutic concentrations are created in most body tissues. The drug penetrates into bones, skin, soft tissues, myocardium, gall bladder and fluids (sputum, bile, urine, synovial, pleural, pericardial, cerebrospinal fluid), including breast milk.

Volume of distribution – 0.25–0.39 l/kg.

T1/2 (half-life) with IV and IM administration is 1 hour. 60–70% of cefotaxime is excreted unchanged through the kidneys, the rest is excreted in the form of three metabolites, one of which has bactericidal activity.

T1/2 in chronic renal failure and in elderly patients increases by 2 times. In newborns, T1/2 is 0.75–1.5 hours, and in premature newborns it increases to 4.6 hours. When administered intravenously at a dose of 1000 mg 4 times a day for 14 days, no accumulation is observed.

Indications for use

The drug is prescribed for severe cases of the following bacterial infections caused by microorganisms sensitive to Cephabol:

• meningitis and other infections of the central nervous system;
• pneumonia and other infections of the ENT organs or respiratory tract;
• pyelonephritis in acute and chronic phases and other urinary tract infections;
• joint and bone infections;
• infections of soft tissues and skin (including postoperative wound complications);
• acute and aggravated chronic adnexitis, endometritis, pelvioperitonitis and other infections of the pelvic organs;
• uncomplicated or complicated infections of the abdominal cavity (postoperative abscesses, cholangitis, cholecystitis, peritonitis);
• chlamydia, gonorrhea and other infections of the genitourinary system;
• infections due to immunodeficiency;
• sepsis;
• endocarditis;
• prevention of infections after surgical operations (obstetric-gynecological, urological, gastrointestinal, etc.).

Contraindications

The drug is not prescribed for hypersensitivity to cephalosporin antibiotics (in particular, to the active substance - cefotaxime).

When using lidocaine solution as a solvent, the following contraindications are identified:

• hypersensitivity to lidocaine or other amide-type local anesthetics;
• intracardiac blockade without an established pacemaker;
• cardiogenic shock;
• intravenous administration;
• children's age (less than 2.5 years).

Cephabol

Active substance:

Cefotaxime*

Pharmgroup:

Cephalosporins

Directions for use and dosage

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

Rules for the preparation and use of a solution for intramuscular administration:

• 1 g of sterile dry powder is dissolved in 3-4 ml of 1% lidocaine solution or sterile water for injection;
• the resulting solution is injected deep into the lateral surface of the thigh or the upper outer quadrant of the buttock or other areas of the body that have a pronounced muscle layer;
• To prevent unwanted injection of the drug into a blood vessel, an aspiration test is recommended.

Rules for the preparation and use of a solution for intravenous jet administration:

• 1 g of sterile dry powder is dissolved in 10 ml of sterile water for injection;
• the resulting solution is administered slowly (over 3-5 minutes);
• If the patient receives fluids parenterally, administration through a special port or injection site of an intravenous infusion system is allowed.

Rules for the preparation and use of a solution for intravenous drip administration:

• 1 g of sterile dry powder is dissolved in 4-5 ml of sterile water for injection;
• the resulting solution is introduced into a bottle with 100 or 50 ml of 0.9% sodium chloride solution or 5% dextrose solution.

When treating adults or children over 12 years of age (patients weighing more than 50 kg):

• for uncomplicated infections, 1 g is administered intravenously or intramuscularly every 12 hours;
• for uncomplicated acute gonorrhea - once 0.5-1 g intramuscularly;
• for moderate infections - every 8 hours, 1-2 g intravenously or intramuscularly;
• if it is necessary to administer large doses of an antibiotic (for example, in the treatment of sepsis), 2 g are administered intravenously every 6-8 hours. For infections that pose a risk to life, the frequency of administration of the drug can be reduced to 4 hours (maximum daily dose - 12 g);
• for antimicrobial prevention of postoperative purulent-septic complications, 1 g of the drug is prescribed once 0.5 hours before surgery. If necessary, the procedure is repeated after 6 and 12 hours;
• when performing a caesarean section after clamping the umbilical cord, 1 g of the drug is administered intravenously. If necessary, Cephabol is additionally administered at a dose of 1 g after 6 and 12 hours.

The daily dosage in the treatment of patients with severe renal impairment (with a creatinine clearance of 20 ml/min/1.73 m2) is reduced by 2 times.

Dosages for newborns in the first month of life:

• For children in the first week of life, the drug is prescribed intravenously every 12 hours at 50 mg/kg;
• children aged 1–4 weeks – 50 mg/kg intravenously every 8 hours.

Dosage for the treatment of children from 1 month to 12 years or patients weighing up to 50 kg:

• the daily dose of the drug is 50–180 mg/kg and is administered in 3-4 doses intramuscularly or intravenously;
• the daily dose for severe or life-threatening infections (for example, bacterial meningitis) is increased to 100-200 mg/kg and administered in 4-6 doses intramuscularly or intravenously.

Instructions:

Clinical and pharmacological group

06.010 (III generation cephalosporin)

Release form, composition and packaging

Glass bottles (1) - cardboard packs.

Powder for the preparation of a solution for intravenous and intramuscular administration, white or white with a yellowish tint; sensitive to light.

Solvent: water (5 ml).

Glass bottles with a capacity of 10 ml (1) - cardboard packs. Glass bottles with a capacity of 10 ml (1) complete with solvent (amp. 1 pc.) - packs of cardboard. Glass bottles with a capacity of 10 ml (1) complete with solvent (amp. 1 pc.) 1 pc.) - contour cell packaging (1) - cardboard packs. Glass bottles with a capacity of 10 ml (5) - contour cell packaging (1) - cardboard packs. Glass bottles with a capacity of 10 ml (5) complete with solvent (amp. 5 pcs.) - contour cell packaging (2) - cardboard packs.

pharmachologic effect

Cefotaxime is a third generation cephalosporin antibiotic for parenteral use. Acts bactericidal. Has a wide spectrum of antimicrobial action.

Active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus, including penicillinase-forming strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus species, Enterobacter spp., Escherichia coli, Haemophilus influenzae (including penicillinase-forming strains) , Haemophilus parainfluenzae, Klebssiella spp. (including Kl.pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Acinetobacter species, Corynebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium spp., Propionibacterium spp., Bacillus subtilis, Clostridium spp. . (including Clostridium perfringens, most strains of Clostridium difficile are resistant to the drug), Escherichia coli, Citrobacter spp., Proteus mirabilis, Proteus indole, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Serratia spp., Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.

Resistant to most beta-lactamases of gram-positive and game-negative microorganisms, staphylococcal penicillinase.

Pharmacokinetics

After a single intravenous (IV) administration of 1000 mg of the drug, the maximum concentration (Cmax) is reached after 5 minutes and is 101.7 μg/ml. After intramuscular (IM) administration, Cmax is reached after 0.5 hours and is .21 μg/ml. Bonding with plasma proteins is 25-40%.

Creates therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. Volume of distribution - 0.25-0.39 l/kg.

The half-life (T1/2) for intravenous and intramuscular administration is 1 hour. It is excreted by the kidneys - 60% - 70% unchanged, the rest in the form of metabolites (the deacetylated derivative has bactericidal activity, but the other two metabolites do not).

In chronic renal failure (CRF) and in the elderly, T1/2 increases by 2 times. T1/2 in newborns is 0.75-1.5 hours, in premature newborns it increases to 4.6 hours. With repeated intravenous administrations at a dose of 1000 mg every 6 hours for 14 days, no accumulation is observed. Passes into breast milk.

Dosage

IM and IV (stream, drip).

For intramuscular injection, dissolve 1 g of the drug in 4 ml of sterile water for injection. Injected deep into the gluteal muscle. A 1% solution of lidocaine (per 1 g - 4 ml) is also used as a solvent for intramuscular administration.

For intravenous administration, 1 g of cefotaxime is dissolved in 10 ml of sterile water for injection. Inject slowly over 3-5 minutes. For drip administration (over 50-60 minutes), dissolve 2 g of the drug in 100 ml of isotonic sodium chloride solution or 5% glucose solution.

Adults and children weighing 50 kg or more: for uncomplicated infections, as well as for urinary tract infections, IM or IV, 1 g every 8-12 hours; for uncomplicated acute gonorrhea - 1 g intramuscularly once; for moderate infections - IM or IV 1-2 g every 12 hours; for severe infections, for example, meningitis - 2 g IV every 4-8 hours, maximum daily dose - 12 g. The duration of treatment is determined individually.

Premature and newborns up to 1 week - iv 50 mg/kg every 12 hours; at the age of 1-4 weeks - iv 50 mg/kg every 8 hours; children weighing up to 50 kg - IV or IM 50-180 mg/kg in 4-6 injections. In case of severe infections, incl. meningitis, the daily dose for children is increased to 100-200 mg/kg IM or IV in 4-6 injections.

In order to prevent the development of infections before surgery, 1 g is administered once during induction of general anesthesia. If necessary, the administration is repeated after 6-12 hours.

For caesarean section - at the moment of applying clamps to the umbilical vein - 1 mg intravenously, then 6 and 12 hours after the first dose - an additional 1 g.

In case of renal dysfunction, the dose is reduced. When CC is 10 ml/min or less, the daily dose of the drug is halved.

Overdose

Symptoms: convulsions, encephalopathy (in case of large doses, especially in patients with renal failure), tremor, increased neuromuscular excitability.

Treatment: symptomatic therapy.

Drug interactions

Increases the risk of bleeding when combined with antiplatelet agents and NSAIDs.

Does not lead to the development of disulfiram-like reactions when used together with ethanol.

The likelihood of kidney damage increases when taken simultaneously with aminoglycosides, polymyxin B and loop diuretics. Drugs that block tubular secretion increase plasma concentrations of cefotaxime and slow down its elimination. Pharmaceutically incompatible with solutions of other antibiotics in the same syringe or dropper.

Use during pregnancy and lactation

The use of the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

Cefotaxime is excreted in breast milk, so if it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Side effects

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

From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbacteriosis, liver dysfunction, stomatitis, glossitis, pseudomembranous enterocolitis.

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

From the urinary system: impaired renal function (azotemia, increased urea levels in the blood, oliguria, anuria, interstitial nephritis).

From the nervous system: headache, dizziness.

Laboratory indicators: azotemia, increased urea concentration in the blood, increased activity of liver transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, false-positive Coombs test.

From the cardiovascular system: potentially life-threatening arrhythmias after rapid bolus administration into the central vein.

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

Other: superinfection (in particular, candidal vaginitis).

Storage conditions and periods

List B. In a dry place, protected from light, at a temperature of no more than 25°C. Keep out of the reach of children.

Shelf life: 2 years. Do not use after expiration date.

Indications

Severe bacterial infections caused by sensitive microorganisms:

- infections of the central nervous system (including meningitis);

— infections of the respiratory tract and ENT organs, incl. pneumonia;

- urinary tract infections, incl. acute and exacerbation of chronic pyelonephritis;

— infections of the skin and soft tissues, including postoperative wound complications;

- infections of bones and joints;

— infections of the pelvic organs, incl. acute and exacerbation of chronic adnexitis, pelvioperitonitis, endometritis;

- uncomplicated and complicated infections of the abdominal cavity (peritonitis, postoperative abdominal abscesses, cholecystitis, cholangitis);

— infections of the genitourinary system, including chlamydia, gonorrhea;

- endocarditis;

- Lyme disease (borreliosis);

— salmonellosis;

- sepsis;

- infections due to immunodeficiency;

— prevention of infections after surgical operations (including urological, obstetric-gynecological, gastrointestinal).

Contraindications

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

In children under 2.5 years of age, intramuscular administration of the drug should not be used.

With caution: neonatal period, lactation period; chronic renal failure, nonspecific ulcerative colitis (including history).

special instructions

In the first weeks of treatment, pseudomembranous colitis may occur, manifested by severe, prolonged diarrhea. In this case, stop taking the drug and prescribe adequate therapy, including vancomycin or metronidazole.

Before prescribing the drug, it is necessary to collect an allergic history, especially in relation to beta-lactam antibiotics. Cross-allergy between penicillins and cephalosporins is known. In persons with a history of allergic reactions to penicillin, the drug is used with extreme caution (the possibility of severe anaphylactic reactions, even death, should be taken into account).

When treatment with the drug lasts more than 10 days, it is necessary to monitor the peripheral blood picture.

When determining glucose in urine using a non-enzymatic method (for example, the Benedict method), false positive results are possible.

Use for renal impairment

In case of renal dysfunction, the dose is reduced. When creatinine clearance is 10 ml/min or less, the daily dose of the drug is halved.

Conditions for dispensing from pharmacies

By doctor's prescription.

Side effects

• allergic reactions (chills, fever, urticaria, itching, rash, eosinophilia, bronchospasm, Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic shock, angioedema);
• digestive dysfunction (vomiting, nausea, constipation or diarrhea, abdominal pain, flatulence, liver dysfunction, stomatitis, pseudomembranous enterocolitis, dysbacteriosis, glossitis);
• hematopoietic dysfunction (thrombocytopenia, granulocytopenia, neutropenia, leukopenia, hypocoagulation, hemolytic anemia);
• dysfunction of the urinary system (azotemia, oliguria, increased concentration of urea in the blood, interstitial nephritis, anuria);
• dysfunction of the nervous system (dizziness, headache);
• laboratory abnormalities (increased urea concentration in the blood, azotemia, increased activity of alkaline phosphatase and liver transaminases, hyperbilirubinemia, hypercreatininemia, false-positive Coombs test);
• local reactions (pain along the vein, phlebitis, infiltration and soreness at the site of intramuscular injection);
• dysfunction of the cardiovascular system (rapid bolus injection into the central vein can lead to potentially life-threatening arrhythmias);
• superinfection (for example, candidal vaginitis).

special instructions

Before prescribing Cephabol, it is necessary to collect an allergy history, especially regarding beta-lactam antibiotics. Cross-allergy between cephalosporins and penicillins is possible.

In persons with allergic reactions to penicillin, Cephabol is used with extreme caution, given the possibility of developing a severe anaphylactic reaction (including death).

In the first weeks of taking the drug, there is a possibility of developing pseudomembranous colitis, accompanied by prolonged severe diarrhea. In this case, Cephabol is stopped and adequate therapy is carried out, including metronidazole or vancomycin.

If a non-enzymatic method (for example, the Benedict method) is used to determine glucose in urine, false-positive results are possible.

When treatment lasts more than 10 days, it is necessary to monitor the peripheral blood picture.

pharmachologic effect

Cefotaxime is a third generation cephalosporin antibiotic for parenteral use. Acts bactericidal. Has a wide spectrum of antimicrobial action.

Active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus, including penicillinase-forming strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus species, Enterobacter spp., Escherichia coli, Haemophilus influenzae (including penicillinase-forming strains) , Haemophilus parainfluenzae, Klebssiella spp. (including Kl.pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Acinetobacter species, Corynebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium spp., Propionibacterium spp., Bacillus subtilis, Clostridium spp. . (including Clostridium perfringens, most strains of Clostridium difficile are resistant to the drug), Escherichia coli, Citrobacter spp., Proteus mirabilis, Proteus indole, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Serratia spp., Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.

Resistant to most beta-lactamases of gram-positive and game-negative microorganisms, staphylococcal penicillinase.

Drug interactions

• when combined with anti-inflammatory non-steroidal drugs, antiplatelet agents, the risk of bleeding increases;
• when used together with ethanol, it does not cause the development of disulfiram-like reactions;
• when taken simultaneously with loop diuretics, polymyxin B, aminoglycosides, the likelihood of kidney damage increases;
• the elimination of cefotaxime slows down with an increase in its plasma concentrations while taking medications that block tubular secretion;

Cephabol is pharmaceutically incompatible with solutions of other antibiotics in one dropper or one syringe.