Clinical pharmacology of cefuroxime and cefuroxime axetil in infants and children

Abstract

Cefuroxime is a second-generation cephalosporin β-lactamase resistant active against gram-negative and gram-positive organisms and the prodrug cefuroxime axetil is the drug of choice for treatment of Lyme disease. Cefuroxime inhibits bacterial cell wall synthesis, is bactericidal, and is one of the few cephalosporins available for oral, intravenous, and intramuscular administration. Cefuroxime is rapidly absorbed when given by mouth, and its blood concentrations remarkably vary among subjects, but the drug has not adverse-effects even when is given at high doses. The gastrointestinal absorption-rate of cefuroxime axetil is 70%, and after hydrolysis it relays cefuroxime. Parenteral dosing-regimens consist of 25 mg/kg in infants and dosing intervals decrease with increasing postnatal age. Cefuroxime oral dosingregimens are: 10, 20 mg/kg and 250 mg twice-daily in children aged up to one year, 2 to 11 and 12 to 17 years, respectively. Elimination half-live are: 6 hours in the first week of life and 1.8 hours in children aged up to 6 years. Cefuroxime is efficacy and safe for prophylaxis and treatment of respiratory-tract and acute urinary-tract infections, pneumoniae, acute otitis media, and sinusitis in children. Prophylaxis for surgical procedures requires 50 mg/kg before procedure and then 30 mg/kg for up 3 days after intervention. Cefuroxime concentration in cerebrospinal fluid is about 10% of that in plasma and the drug successfully treated meningitis caused by β-haemolytic streptococci, Streptococcus pneumoniae, and Neisseria meningitides, but when Salmonella species are the infective pathogens additional 5 mg dose is given intraventricularly. Some bacteria may become resistant to cefuroxime and antibiotic consumption is associated with increased bacterial-resistance. The aim of this study is to review the published data on cefuroxime and cefuroxime axetil dosing, efficacy, safety, and cefuroxime effects, prophylaxis, treatment, optimization, meningitis, pharmacokinetics and bacterial-resistance.