Cefuroxime is the first commercially-available second-generation cephalosporine to be widely used in
therapy; it is a semi-synthetic
cephalosporin obtained from the 7-cephalosporanic
acid nucleus of
cephalosporin C.
Cefuroxime axetil is the acetoxyethyl
ester of
cefuroxime. The majority of micro-organisms associated with
respiratory infections are highly sensitive to
cefuroxime. These include Haemophilus influenzae, Streptococcus pneumoniae, Streptococcus pyogenes and the other streptococci (excluding group D streptococci), and Moraxella catarrhalis. Bacteria sensitive to
cefuroxime include the enterobacteria (Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella and Shigella and Straphylococcus aureus (
methicillin-sensitive strains). The pharmacokinetic studies show that the maximum plasma concentration of
cefuroxime after
oral administration of 250 mg and 500 mg of
cefuroxime axetil after a meal are respectively 4.6 and 7.9 mg/l. The absolute bioavailability of
tablets is 68% (extremes 63-73%) after
oral administration of 500 mg
cefuroxime axetil. The protein binding
is 33+/-5.7%. Tissue diffusion was studied in the interstitial fluid, the bronchial mucosa, the tonsils, and the bronchial secretions.
Cefuroxime axetil is available as
capsule-shaped
tablets containing 125, 250 or 500 mg. An oral
suspension dosage form for paediatric purposes is also available as granules in multidose bottles and sachets. Constitution gives a
suspension containing 125 mg or 250 mg
cefuroxime (as
cefuroxime axetil).
Cefuroxime axetil is indicated for the treatment of
infections caused by susceptible bacteria. Indications include: lower
respiratory tract infections (e.g., acute and
chronic bronchitis and
pneumonia);
upper respiratory tract infections (e.g., ear, nose and throat
infections such as
otitis media,
sinusitis tonsillitis and
pharyngitis); genito-
urinary tract infections (e.g.,
pyelonephritis,
cystitis and
urethritis, gonorrhoea, acute uncomplicated gonococcal
urethritis and
cervicitis); and skin and
soft tissue infections (e.g.,
furunculosis,
pyoderma and
impetigo). For most
infections, a dose of 250 mg twice daily is appropriate. In some
urinary tract infections, 125 mg twice daily has been shown to be effective. If
pneumonia is suspected or in more severe lower
respiratory tract infection, doses of 500 mg bd should be used. Uncomplicated gonorrhoea has been shown to respond to a single 1-g dose of
cefuroxime axetil. Adverse reactions to
cefuroxime have generally been mild and transient in nature (gastrointestinal disturbances, including diarrhoea,
nausea and
vomiting).