Cefuroxime

Pharmacological properties

cefuroxime axetil is an oral form of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most β-lactamases and is active against a wide range of gram-positive and gram-negative microorganisms.

The bactericidal effect of cefuroxime is due to inhibition of the synthesis of the cell membrane of microorganisms.

Acquired antibiotic resistance differs in different regions and may vary over time, and for individual strains can vary significantly. If available, it is advisable to refer to local antibiotic sensitivity data, especially in the treatment of severe infections.

Cefuroxime is highly active against the following microorganisms:

Gram-negative aerobes: Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae (including strains producing and non-producing penicillinase), Escherichia colipplesppepp., colippella colipp. rettgeri;

gram-positive aerobes: Staphylococcus aureus (methicillin-sensitive strains) and coagulase-negative staphylococci (methicillin-sensitive strains), Streptococcus pyogenes (and other β-hemolytic streptococci), Streptococcus pneumoniae, Streptocococcus group B (Streptocococcus agal (Streptocococcus) (Streptocococcus agal (Streptocococcus)

anaerobes: gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp.), gram-positive bacteria (including species of Clostridium) and gram-negative bacteria (including species of Bacteroides and Fusobacterium spp.), Propionibacterium spp .;

other microorganisms: Borrelia burgdorferi;

cefuroxime-resistant microorganisms: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Leg

microorganisms, some strains of which are resistant to cefuroxime: Enterococcus (Streptococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.

Pharmacokinetics After oral administration of cefuroxime, axetil is absorbed in the intestine, hydrolyzed in its mucous membrane, and in the form of cefuroxime enters the systemic circulation.

The optimal level of absorption is observed when taking tablets immediately after eating. WITH_max cefuroxime in plasma is observed approximately 2-3 hours after taking the drug. T_½ is about 1–1.5 hours. The degree of binding to blood plasma proteins is 33–55%, depending on the determination procedure. Cefuroxime is excreted by the kidneys unchanged by tubular secretion and glomerular filtration.

The simultaneous use of probenecid increases AUC by 50%. Plasma cefuroxime decreases during dialysis.

Indications

Treatment of infections caused by cefuroxime-sensitive microorganisms:

infections of ENT organs: otitis media, sinusitis, tonsillitis, pharyngitis;

respiratory tract infections: pneumonia, acute bronchitis and exacerbation of chronic bronchitis;

urinary tract infections: pyelonephritis, cystitis and urethritis;

infections of the skin and soft tissues: furunculosis, pyoderma and impetigo;

gonorrhea, acute uncomplicated gonococcal urethritis and cervicitis;

treatment of early manifestations of Lyme disease and subsequent prevention of late manifestations of Lyme disease in adults and children over the age of 12 years.

Application

Typically, the duration of treatment with Axef is 7 days (5-10 days).

For better absorption, the drug is recommended to be taken after meals.

Adults Most infections - 250 mg 2 times a day;

urinary tract infections - 125 mg 2 times a day;

moderate respiratory tract infections (bronchitis) - 250 mg 2 times a day;

more severe respiratory tract infections (suspected pneumonia) - 500 mg 2 times a day;

pyelonephritis - 250 mg 2 times a day;

uncomplicated gonorrhea - once 1 g of the drug;

Lyme disease in adults and children over the age of 12 years - 500 mg 2 times a day for 20 days.

Sequential therapy

Pneumonia: 1.5 g of Axef 2-3 times a day (IM or IV) for 48–72 hours, then Axef in the form of tablets of 500 mg 2 times a day for 7-10 days.

Exacerbation of chronic bronchitis: Acef 750 mg 2-3 times a day (IM or IV) for 48–72 hours, then orally in 500 mg tablets 2 times a day for 5–7 days. The duration of both parenteral and oral administration of the drug is determined by the severity of the infection and the condition of the patient.

Children.The usual dose is 125 mg or 10 mg / kg of body weight 2 times a day (the maximum daily dose is 250 mg). To treat otitis media in children under 2 years of age, prescribe the drug at a dose of 125 mg or 10 mg / kg of body weight 2 times a day (maximum daily dose - 250 mg), for children over the age of 2 years - 250 mg or 15 mg / kg body weight 2 times a day (maximum daily dose - 500 mg). There is no experience of using the drug in children under the age of 3 months.

Elderly patients. There are no special recommendations for this group of patients. Use the usual dose, maximum 1 g / day.

Patients with renal failure. Cefuroxime is excreted by the kidneys. In patients with severe renal impairment, it is recommended to reduce the dose of cefuroxime to compensate for its slow elimination (table).

Contraindications

Hypersensitivity to the group of cephalosporin antibiotics.

Side effects

When using cefuroxime, axetil are moderate and are mostly reversible.

Adverse reactions, information about which is given below, are classified by organs and systems and by the frequency of occurrence. The frequency of occurrence is divided into the following categories: very often (≥1 / 10), often (≥1 / 100 and 1/10), infrequently (≥1 / 1000 and 1/100), rarely (≥1 / 10,000 and 1 / 1000), very rarely (1/10 000).

Infections and infestations: often - excessive growth of Candida.

On the part of the blood system and lymphatic system: often - eosinophilia; infrequently - a positive Coombs test, thrombocytopenia, leukopenia (sometimes severe); very rarely - hemolytic anemia.

Cephalosporins as a class tend to be absorbed on the surface of the erythrocyte membrane and interact with antibodies, which can lead to a positive Coombs test (effect on determining blood compatibility) and (very rarely) hemolytic anemia.

From the side of the immune system: hypersensitivity reactions, including infrequently - skin rash; rarely - urticaria, itching; very rarely - drug fever, serum sickness, anaphylaxis.

From the nervous system: often - headache, dizziness.

From the alimentary canal: often - gastroenterological disorders, including diarrhea, nausea, abdominal pain; rarely - pseudomembranous colitis (see SPECIAL INSTRUCTIONS).

From the hepatobiliary system: often - a transient increase in the level of liver enzymes (AlAT,