Axocef^® (Tablets, Powder) Instructions for Use

ATC Code

J01DC02 (Cefuroxime)

Active Substance

Cefuroxime (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Second generation cephalosporin

Pharmacotherapeutic Group

Antibiotic-cephalosporin

Pharmacological Action

A second-generation cephalosporin antibiotic for parenteral administration. It acts bactericidally (disrupts the synthesis of the bacterial cell wall as a result of binding to the main target proteins). It is active against a wide range of pathogens, including beta-lactamase-producing strains.

It is highly active against gram-positive microorganisms, including strains resistant to penicillins (except for methicillin-resistant strains): Staphylococcus aureus, Streptococcus pyogenes (and other beta-hemolytic streptococci), Streptococcus pneumoniae, Group B Streptococcus (Streptococcus agalactiae), Streptococcus mitis (viridans group), most Clostridium spp.; gram-negative microorganisms:Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Proteus rettgeri, Haemophilus influenzae, including strains resistant to ampicillin; Haemophilus parainfluenzae, including strains resistant to ampicillin; Moraxella catarrhalis, Neisseria gonorrhoeae, including both penicillinase-producing and non-producing strains, Neisseria meningitidis, Salmonella spp., Borrelia burgdorferi; gram-positive and gram-negative anaerobesPeptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Propionibacterium spp.

The following are not susceptible to cefuroxime: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus, Staphylococcus epidermidis, Legionella spp., Streptococcus (Enterococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.

Pharmacokinetics

C_max of cefuroxime in blood plasma after intramuscular administration is observed within 30 to 45 minutes.

33-50% of the drug binds to plasma proteins (depending on the method used).

Cefuroxime concentrations exceeding the minimum inhibitory concentration for most microorganisms can be achieved in bone tissue, synovial and intraocular fluids. In meningitis, it penetrates the blood-brain barrier (BBB). It crosses the placenta and passes into breast milk.

Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion.

The T_1/2 of cefuroxime from serum after intramuscular or intravenous administration is approximately 70 minutes. In newborns, the T_1/2 of cefuroxime may be 3-5 times longer than in adults.

Concomitant administration of probenecid prolongs the excretion of cefuroxime, leading to an increase in the maximum serum concentration of cefuroxime.

Within 24 hours after parenteral administration, Cefuroxime is almost completely (85-90%) excreted by the kidneys unchanged, with the majority of the drug excreted within the first 6 hours.

Serum concentrations of cefuroxime are reduced by dialysis.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to cefuroxime: lower respiratory tract infections (bronchitis, pneumonia, lung abscess, infected bronchiectasis); ENT organ infections (sinusitis, tonsillitis, pharyngitis, otitis media); urinary tract infections (pyelonephritis, cystitis, asymptomatic bacteriuria); skin and soft tissue infections (erysipelas, pyoderma, impetigo, furunculosis, phlegmon, wound infection); bone and joint infections (osteomyelitis, septic arthritis); obstetric and gynecological infections (endometritis, adnexitis, cervicitis); sepsis; meningitis; peritonitis; gonorrhea; Lyme disease (borreliosis).

Prevention of infectious complications during operations on the chest, abdominal cavity, pelvis, during orthopedic operations, operations on the heart, lungs, esophagus and blood vessels with a high risk of infectious complications.

Bacterial sensitivity to cefuroxime varies by region and over time. Where possible, local susceptibility data should be considered.

ICD codes

Dosage Regimen

Tablets

The dosage regimen and duration of therapy are set individually depending on the indications, clinical situation and age.

For optimal absorption, Cefuroxime should be taken with food.

For adults with most infections, the recommended dose is 250 mg twice daily; for severe infections – 500 mg twice daily (for uncomplicated gonorrhea, 1 g as a single dose).

The standard course of therapy is about 7 days (from 5 to 10 days); for borreliosis, the course duration is from 10 to 21 days.

It is recommended to reduce the dose of cefuroxime in patients with severe renal impairment to compensate for delayed excretion.

When treating children, the dose is calculated based on body weight and age. For most infections, the dose for children aged 3 months to 12 years (in appropriate dosage forms) is 10 mg/kg twice daily, but not more than 250 mg per day.

For otitis media and more severe infections, the recommended dose is 15 mg/kg twice daily, but not more than 500 mg per day.

Powder

Administered intravenously or intramuscularly.

The dosage regimen and duration of therapy are set individually depending on the indications, clinical situation and age.

For adults, the recommended dose for most infections is 750 mg three times daily; for severe infections, the dose is increased to 1500 mg 3-4 times daily. The average daily dose is 3-6 g.

For gonorrhea – 1500 mg as a single intramuscular dose. For bacterial meningitis – 3 g intravenously every 8 hours.

In chronic renal failure, dosage adjustment is necessary. It is recommended to reduce the dose of cefuroxime in patients with severe renal impairment to compensate for delayed excretion.

For newborns and children under 3 months, 30 mg/kg/day in 2-3 divided doses is prescribed; for bacterial meningitis – 100 mg/kg/day.

For children over 3 months, 30-100 mg/kg/day in 3-4 divided doses is prescribed; for most infections, the optimal dose is 60 mg/kg/day. For severe infections, the recommended dose is 150-250 mg/kg/day intravenously, divided into 3-4 administrations.

Adverse Reactions

Infections and infestations: rarely – oral and mucosal candidiasis.

Blood and lymphatic system disorders often – neutropenia, eosinophilia; infrequently – leukopenia, decreased hemoglobin level, positive Coombs test; rarely – thrombocytopenia; very rarely – hemolytic anemia.

Cephalosporins as a class tend to be absorbed onto the red blood cell membrane surface and interact with antibodies to the drug, leading to a positive Coombs test (which may affect cross-matching) and very rarely to hemolytic anemia.

Immune system disorders hypersensitivity reactions, including infrequently – skin rash, urticaria and pruritus; rarely – drug fever; very rarely – interstitial nephritis, anaphylaxis, cutaneous vasculitis.

Gastrointestinal disorders infrequently – gastrointestinal upset; very rarely – pseudomembranous colitis.

Hepatobiliary disorders: often – transient increase in liver enzyme activity; infrequently – transient increase in bilirubin concentration. These adverse reactions occur particularly in patients with a history of liver disease, but no symptoms of liver damage were noted.

Skin and subcutaneous tissue disorders very rarely – erythema multiforme, toxic epidermal necrolysis and Stevens-Johnson syndrome.

Renal and urinary disorders: very rarely – increased serum creatinine concentration, increased blood urea nitrogen and decreased creatinine clearance.

Ear and labyrinth disorders very rarely – mild to moderate hearing loss in children treated for meningitis.

General disorders and administration site conditions often – reactions at the injection site, which may include pain and thrombophlebitis. Pain at the intramuscular injection site is more likely with high doses, but this is usually not a reason to discontinue the drug.

Contraindications

Hypersensitivity (including to other cephalosporins, penicillins and carbapenems).

Use with caution in renal failure, gastrointestinal diseases (including history and nonspecific ulcerative colitis), when concomitant use with loop diuretics and aminoglycosides is necessary, in early pregnancy and during lactation, as well as in newborn infants (especially premature infants).

Use in Pregnancy and Lactation

During pregnancy, Cefuroxime should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.

There is no experimental evidence of embryopathic or teratogenic effects of cefuroxime, but, as with the use of other drugs, caution should be exercised when prescribing it in early pregnancy.

Caution should be exercised when prescribing to nursing mothers, since Cefuroxime is excreted in breast milk.

Use in Renal Impairment

In chronic renal failure, dosage adjustment is necessary.

It is recommended to reduce the dose of cefuroxime in patients with severe renal impairment to compensate for delayed excretion.

Pediatric Use

Use with caution in newborn infants (especially premature infants).

Special Precautions

Patients with a history of allergic reactions to penicillins may have hypersensitivity to cephalosporin antibiotics.

Cephalosporin antibiotics in high doses should be prescribed with caution to patients receiving concomitant therapy with potent diuretics (furosemide) or aminoglycosides, as the risk of renal failure increases. Renal function should be monitored when using such a drug combination, especially in elderly patients and patients with a history of kidney disease. When treating meningitis with cefuroxime, some children experienced mild to moderate hearing loss.

During the use of cefuroxime, growth of Candida fungi may be observed. Prolonged therapy with the drug may lead to overgrowth of other non-susceptible microorganisms (e.g., enterococci and Clostridium difficile), in which case it may be necessary to discontinue the course of treatment with the drug.

Cases of pseudomembranous colitis have been described with antibiotic use, the severity of which can range from mild to life-threatening. Therefore, it is important to consider the possibility of pseudomembranous colitis developing in patients with diarrhea during or after antibiotic use. If diarrhea is prolonged, severe, or the patient experiences abdominal cramps, treatment should be discontinued immediately and the patient should be examined. Medications that inhibit intestinal peristalsis should not be used.

Cefuroxime does not affect the results of urine glucose determination using enzymatic methods.

In patients receiving Cefuroxime, it is recommended to use glucose oxidase or hexokinase tests to determine blood glucose concentration.

Cefuroxime does not affect the quantitative determination of creatinine by the alkaline picrate method.

Effect on ability to drive vehicles and operate machinery

The use of cefuroxime does not affect the ability to drive vehicles and operate machinery.

Drug Interactions

Concomitant use with loop diuretics (furosemide) and aminoglycosides slows tubular secretion, reduces renal clearance, increases plasma concentration and increases the T_1/2 of cefuroxime, which increases the risk of nephrotoxic effects.

Cefuroxime in combination with aminoglycosides has an additive effect, but sometimes synergism of action may be observed. Cefuroxime should not be mixed in the same syringe with aminoglycosides.

Cefuroxime may suppress the intestinal flora, which contributes to reduced estrogen reabsorption and reduced effectiveness of oral hormonal contraceptives.

Pharmaceutically compatible with aqueous solutions containing up to 1% lidocaine hydrochloride, 0.9% sodium chloride solution, 5% and 10% dextrose solution, 0.18% sodium chloride and 4% dextrose solution, 5% dextrose and 0.9% sodium chloride solution, Ringer’s solution, Hartmann’s solution, sodium lactate solution, heparin (10 units/ml and 50 units/ml) in 0.9% sodium chloride solution.

Pharmaceutically incompatible with aminoglycosides, 2.74% sodium bicarbonate solution.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.