Cefuroxime aksetil: a modern view of the clinical application

Cefuroxime aksetil - bactericidal beta-lactam antibiotic belonging to the group of second-generation cephalosporins. It pronounced activity against microorganisms of the family Enterobacteriaceae, Haemophilus influenzae and Moraxella catarrhalis (with comparable activity against Gram-positive cocci). This is due to the fact that cefuroxime is highly resistant to beta-lactamase produced by gram-negative pathogens.

A distinctive feature of cefuroxime compared with first-generation cephalosporins (cefazolin, cephalexin, etc.) is

Thus, cefuroxime is active against most aerobic Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, including strains producing betalaktamazu, Streptococcus pneumonae, Streptococcus pyogenes) and Gram-negative (Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria meningitidis, Neisseria gonorrhoeae, Proteus spp., Salmonella spp., Shigella spp., Provdencia spp.) micro-organisms and anaerobes (Peptococ-cus spp., Peptostreptococcus spp., Bacteroides spp., Fusobacterium spp.). For cefuroxime resistant Chlamydia, Mycoplasma, Rickettsia, Legionella.

In recent years there has been increasing resistance of pathogens of nosocomial infections to most antibiotics, including cefuroxime. In particular, according to a multicenter study, training and sensitization of Russia (1999), high resistance to cefuroxime was seen in Proteus spp., K. Pneumoniaei Enterobacter spp. (More than 50% of cases).

Naturally, in accordance with the spectrum of antimicrobial action of the main indications for use of cefuroxime aksetila are infections of the upper and lower respiratory tract infection (bronchitis, community-acquired pneumonia), ear, nose and throat (otitis media, pharyngitis, tonsillitis, sinusitis), urinary tract (urethritis, pyelonephritis , asymptomatic bacteriuria), gonorrhea.

Pharmacodynamics of antimicrobial drug concentration is determined by the relationship with its clinical efficacy. As a surrogate indicator of the interaction using the minimum inhibitory concentration (MIC) of antibiotic. With this release of two antibiotics: a concentration-dependent activity of the source of infection (aminoglycosides, fluoroquinolones) and the activity of which depends on the exposure to the source of infection. Cephalosporins belong to the 2nd group: they are important not so much concentration as the duration of interactions with microorganisms. This means that the concentration of cefuroxime in excess of 2-4 times the IPC should be retained about 50% of the time between the introduction and improvement of the IPC, for example, up to 20 times is not accompanied by an increase in the severity of clinical effect. It follows from this very important conclusion: the dose is not critical to the clinical effects of cefuroxime, is more important duration of the interaction of antibiotic with the microorganism.

Cefuroxime sodium is exclusively for parenteral administration (intramuscular or intravenous), as the sodium salt of cefuroxime is practically not absorbed when taken orally. In the half-life of around 80 minutes therapeutic concentrations of cefuroxime Skye lasts for 5-8 h, depending on the dose. It defines the administration of cefuroxime sodium trehchetyrehkratnoe.

Cefuroxime aksetil in tablet form, in contrast, after oral administration is well absorbed and rapidly hydrolyzed in the intestinal mucosa and blood to cefuroxime (cefuroxime bioavailability aksetila rises to 50% at the reception during the meal!). The maximum concentration of the drug created by 2.5-3 h after dosing. As a result, the melt-tion increasing concentrations of cefuroxime in the application of cefuroxime aksetila increases the exposure to the antibiotic bacterium that can use double the dosage of the drug (250-500 mg).

Side effects when using cefuroxime aksetila are typical for all cephalosporins. It's nausea, vomiting, diarrhea, transient increase in liver enzymes, described cases of psevdomem-branoznogo colitis with prolonged use (due to the strong growth of Clostridium difisile), leuko-and thrombocyte-topeniya, hemolytic anemia, allergic reactions (1-3% cases cross with penicillins), headache, drowsiness, etc.

Diuretics increase the nephrotoxicity of aminoglycosides and cefuroxime. In the cefuroxime sodium sodium concentration is 2.36 mmol / g, which is in violation of renal function may lead to hypernatremia. At the same time, the simultaneous application of cefuroxime aksetilom antacids, proton pump inhibitors and H2-receptor blockers may reduce the bioavailability of the drug.

Thus, cefuroxime aksetil is effective and safe antimicrobial drug for treating the majority of moderately ifektsy flow. Perralnaya form indicates the presence of the drug pharmaco-cost capacity. Cefuroxime can aksetil ═ regarded as one of the antibiotic-ing for deskalatsionnoy therapy of infectious diseases (the term means the translation of the patient after administration of antibiotic parentralnogo to receive oral form). This method of antibiotic therapy is always farmakoekono-nomic advantage over standard parenteral antibiotic therapy.

In Belarus, cefuroxime aksetil registered company Farmakar (Palestine) under the trade to the name of Zineks (Zinex), the release form - tablets of 500 mg № 10 and 250 mg Tablets number 10.