Cefuroxime Axetil

Abstract

Cefuroxime axetil, a prodrug of the cephalosporin cefuroxime, has proven in vitro antibacterial activity against several Gram-positive and Gram-negative organisms, including those most frequently associated with various common community-acquired infections. Cefuroxime axetil, a cephalosporin antibacterial agent, prevents bacterial growth primarily by inhibiting penicillin-binding protein 3, resulting in bacterial elongation and leakage and, eventually, cell death. The drug shows good activity against a broad range of Gram-positive and Gram-negative bacteria in vitro, including those most commonly associated with respiratory tract infections [e.g. Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, S. pyogenes and methicillin-sensitive Staphylococcus aureus (MSSA)]. The lipophilic acetoxyethyl-ester prodrug cefuroxime axetil is well absorbed from the gastrointestinal tract and is rapidly hydrolysed by nonspecific esterases in the intestinal mucosa and blood to cefuroxime and the ester group. Upper respiratory tract infections: In adult and adolescent patients with acute sinusitis, randomised controlled trials have shown that cefuroxime axetil (250mg twice daily for 8 to 10 days) provided comparable clinical and bacteriological efficacy to that of 7 to 10 days’ treatment with a quinolone agent, including moxifloxacin, gemifloxacin, sparfloxacin and ciprofloxacin. In clinically evaluable patients, satisfactory clinical responses occurred in 83 to 90% of cefuroxime axetil recipients versus 83 to 97% of patients receiving a quinolone comparator agent. Overall presumed or documented bacteriological eradication paralleled satisfactory clinical response rates, with eradication occurring in 89 to 95% of microbiologically evaluable cefuroxime axetil recipients versus 94 to 97% of those receiving a quinolone. Cefuroxime axetil also provided comparable clinical efficacy to that of clarithromycin or amoxicillin/clavulanic acid as assessed by clinical and bacteriological criteria. Furthermore, clinical (85 vs 87% of patients) and bacteriological response rates (89 vs 91%) indicated that 5 days’ treatment with cefuroxime axetil (250mg twice daily) was as effective as 10 days’ treatment in a double-blind trial. Pharmacoeconomic analyses of cefuroxime axetil have generally considered costs associated with treatment only from an institutional perspective. Indirect and societal costs have not been assessed to date. Oral cefuroxime axetil 250mg or 500mg twice daily for 5 to 10 days was generally well tolerated in children and adults with various bacterial infections. The majority of adverse events were mild to moderate in intensity and reversible upon discontinuation of treatment, with very few serious adverse events reported. Less than 1 to 6% of patients withdrew because of adverse events attributable to cefuroxime axetil treatment. For adults and children aged ≥13 years with mild to moderate upper and lower respiratory tract infections caused by susceptible bacteria, the usual effective dose of cefuroxime axetil is 250mg twice daily for 7 to 10 days. To optimise absorption, cefuroxime axetil should be administered with food. The treatment of severe lower respiratory tract infections, including CAP, requires a higher dosage of cefuroxime axetil (usually 500mg twice daily). Currently, in the US prescribing information there are no dosage recommendations available for the use of intravenous cefuroxime/oral cefuroxime axetil sequential therapy. In the UK, in patients with AECB the recommended dosages for sequential therapy are intravenous or intramuscular cefuroxime 750mg twice daily for 2 to 3 days followed by oral cefuroxime axetil 500mg twice daily for 7 days; in patients with CAP, the recommended dosage of parenteral cefuroxime is 1.5g twice daily for 2 to 3 days, followed by cefuroxime axetil 500mg for 7 days.