Alcefur-AG (Powder) Instructions for Use

Marketing Authorization Holder

Altegra, JSC (Russia)

ATC Code

J01DC02 (Cefuroxime)

Active Substance

Cefuroxime (Rec.INN registered by WHO)

Dosage Forms

	Alcefur-AG	Powder for preparation of solution for intravenous administration and suspension for intramuscular administration 250 mg
		Powder for preparation of solution for intravenous administration and suspension for intramuscular administration 750 mg
		Powder for preparation of solution for intravenous administration and suspension for intramuscular administration 1500 mg

Dosage Form, Packaging, and Composition

Powder for preparation of solution for intravenous administration and suspension for intramuscular administration

250 mg – vials – cardboard packs – By prescription

Powder for preparation of solution for intravenous administration and suspension for intramuscular administration

750 mg – vials – cardboard packs – By prescription

Powder for preparation of solution for intravenous administration and suspension for intramuscular administration

1500 mg – vials – cardboard packs – By prescription

Clinical-Pharmacological Group

Second generation cephalosporin

Pharmacotherapeutic Group

Systemic antibacterial agents; other beta-lactam antibacterial agents; second-generation cephalosporins

Pharmacological Action

Cephalosporin antibiotic of the II generation for parenteral use. 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, Streptococcus group B (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 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.

It binds to plasma proteins by 33-50% (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 passes through the placenta and penetrates 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 concentration of cefuroxime in serum.

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 decrease during dialysis.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to cefuroxime: infections of the lower respiratory tract (bronchitis, pneumonia, lung abscess, infected bronchiectasis); ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media); urinary tract (pyelonephritis, cystitis, asymptomatic bacteriuria); skin and soft tissues (erysipelas, pyoderma, impetigo, furunculosis, phlegmon, wound infection); bones and joints (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.

The sensitivity of bacteria to cefuroxime varies by region and over time. Where possible, local susceptibility data should be taken into account.

ICD codes

Dosage Regimen

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 3 times/day; in severe infections, the dose is increased to 1500 mg 3-4 times/day. 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, adjustment of the dosage regimen 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 is prescribed in 2-3 administrations; for bacterial meningitis – 100 mg/kg/day.

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

Adverse Reactions

Infectious and parasitic diseases: rarely – candidiasis of the oral cavity and mucous membranes.

From the hematopoietic system 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 on the surface of the red blood cell membrane and interact with antibodies to the drug, leading to a positive Coombs test (which may affect cross-matching) and very rarely to hemolytic anemia.

From the immune system hypersensitivity reactions, including infrequently – skin rash, urticaria and itching; rarely – drug fever; very rarely – interstitial nephritis, anaphylaxis, cutaneous vasculitis.

From the digestive system infrequently – gastrointestinal disorder; very rarely – pseudomembranous colitis.

From the liver and biliary tract: often – transient increase in liver enzyme activity; infrequently – transient increase in bilirubin concentration. These adverse reactions occur in particular in patients with a history of liver disease, but no symptoms of liver damage were noted.

From the skin and subcutaneous tissues very rarely – erythema multiforme, toxic epidermal necrolysis and Stevens-Johnson syndrome.

From the urinary system: very rarely – increased serum creatinine concentration, increased blood urea nitrogen and decreased creatinine clearance.

From the hearing organ and labyrinthine disorders very rarely – mild to moderate hearing loss in children during treatment of 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).

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

Use in Pregnancy and Lactation

During pregnancy, Cefuroxime is used only if the intended 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, adjustment of the dosage regimen is necessary.

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

Pediatric Use

Should be used with caution in newborn children (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 strong diuretics (furosemide) or aminoglycosides, as the risk of renal failure increases. Renal function should be monitored when using such a combination of drugs, especially in elderly patients and in 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 fungi of the genus Candida 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 developing pseudomembranous colitis in patients with diarrhea during or after antibiotic use. If diarrhea is prolonged, or is severe, or the patient experiences abdominal cramps, treatment should be stopped 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 mechanisms

The use of cefuroxime does not affect the ability to drive vehicles and other mechanisms.

Drug Interactions

Simultaneous administration 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 acts additively, 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 a decrease in estrogen reabsorption and a reduction in the effectiveness of oral hormonal contraceptives.

It is 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 IU/ml and 50 IU/ml) in 0.9% sodium chloride solution.

It is pharmaceutically incompatible with aminoglycosides and a 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.