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Side effects
Adverse reactions to cefuroxime axetil have been generally mild and
transient in nature.
As with other cephalosporins, there have been rare reports of erythema
multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematic
necrolysis) and hypersensitivity reactions including skin rashes, urticaria,
pruritus, drug fever, serum sickness, and very rarely anaphylaxis.
A small proportion of patients
receiving Zinnat have experienced gastrointestinal disturbances including
diarrhoea, nausea and vomiting. As with other broad-spectrum antibiotics,
there have been reports of pseudomembranous colitis. Headache has also been
reported.
Eosinophilia and transient
increases of hepatic enzyme levels [ALT (SGPT), AST (SGOT) and LDH] have
been noted during Zinnat therapy. There have been rare reports of
thrombocytopenia and leucopenia (sometimes profound). As with other
cephalosporins, jaundice has been reported very rarely.
Cephalosporins as a class tend to
be absorbed onto the surface of red cells membranes and react with
antibodies directed against the drug to produce a positive Coomb's test
(which can interfere with crossmatching of blood) and very rarely haemolitic
anaemia.
Overdosage
Overdosage of cephalosporins can cause cerebral irritancy leading to
convulsions. Serum levels of cefuroxime can be reduced by haemodialysis and
peritoneal dialysis.
Pharmaceutical precautions
Storage conditions
Store below 30°C.
Shelf life
3 years
Packaging quantities
Zinnat Tablets 125mg and 250mg are supplied in double foil blister packs of
10's and 50's.
Further information
Bacteriology
Cefuroxime axetil owes its in vivo bactericidal activity to the parent
compound cefuroxime.
Cefuroxime is a well-characterized and effective antibacterial agent which
has bactericidal activity against a wide range of common pathogens,
including -lactamase-producing strains.
Cefuroxime has good stability to bacterial-lactamase, and consequently is
active against many ampicillin-resistant or amoxycillin-resistant strains.
The bacterial action of cefuroxime results from inhibition of cell wall
synthesis by binding to essential target proteins.
Cefuroxime is usually active against the following organisms in vitro:
Aerobes Gram-negative:-
Haemophilus influenzae (including ampicillin-resistant strains)
Haemophilus parainfluenzae Moraxella (Branhamella) catarrhalis
Neisseria gonorrhoeae (including penicillinase and non-penicillinase-producing
strains)
Escherichia coli Klebsiella species Proteus mirabilis Providencia spp
Proteus rettgeri
Aerobes Gram-positive:-
Staphylococcus aureus and Staphylococcus epidermis (including penicillinase-producing
strains but excluding methicillin resistant strains)
Streptococcus pyogenes (and other -haemolytic streptococci)
Streptococcus pneumoniae
Streptococcus Group B (Streptococcus agalactiae)
Anaerobes:-
Gram-positive and Gram-negative cocci (including Peptococcus and
Peptostreptocossus species)
Gram-positive bacilli (including
Clostridium species) and Gram-negative bacilli (including Bacteroides and
Fusobacterium species)
Propionibacterium spp.
Other organisms:-
Borrelia burgdorferi
The following organisms are not susceptible to Cefuroxime:-
Clostridium difficile
Pseudomonas spp.
Campylobacter spp.
Acinetobacter calcoaceticus
Listeria monocytogenes
Methicillin resistant strains of Staphylococcus aureus and Staphylococcus
epidermidis
Legionella spp.
Some strains of the following genera are not susceptible to Cefuroxime:-
Enterococcus (Streptococcus)
faecalis
Morganella morganii
Proteus vulgaris
Enterobacter spp.
Citrobacter spp.
Serratia spp.
Bacteroides fragilis
Pharmacokinetics
After oral administration cefuroxime axetil is slowly absorbed from the
gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and
blood to release cefuroxime into the circulation. Optimum absorption occurs
when it is administered after a meal.
Peak serum levels (2-3 mg/l for a 125mg dose, 4-6 mg/l for a 250mg dose,
5-8mg/l for a 500mg dose and 9-14mg/l for a 1g dose) occur approximately two
to three hours after dosing when taken after food, unlike IV dosing which
peaks immediately.
The absorption of cefuroxime from
the suspension is more prolonged compared with tablets, leading to later,
lower peak serum levels and slightly reduced systemic bioavailability (
4-17% less ). Post peak levels, the serum half-life is between 1 and 1.5
hours. Protein binding has been variously stated as 33-50% depending on the
methodology used. Cefuroxime is not metabolised and is excreted by
glomerular filtration and tubular secretion.
Concurrent administration of
probenecid increases the area under the mean serum concentrations time curve
by 50%.
Serum levels of cefuroxime are
reduced by dialysis.
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