(cefotaxime
sodium) is a semisynthetic, broad spectrum cephalosporin antibiotic for
parenteral administration.
CLINICAL PHARMACOLOGY :
Following IM administration of a single 500 mg or 1 g to normal volunteers,
mean peak serum concentrations of 11.7 and 20.5 mcg/mL respectively were
attained within 30 minutes. There was a dose-dependent increase in serum
levels after the IV administration of
500 mg, 1 g, and 2 g (38.9, 101.7, and 214.4 mcg/mL) without alteration in
the elimination half-life. There is no evidence of accumulation following
repetitive IV infusion of 1 g doses every 6 hours for 14 days
Approximately 20-36%
of an intravenously administered dose of cefotaxime is excreted by the
kidney as unchanged cefotaxime,
and 15-25% as the desacetyl derivative.
The
desacetyl metabolite has been shown to contribute to the bactericidal
activity.
Microbiology :
The
bactericidal activity of cefotaxime sodium results from inhibition of cell
wall synthesis. Cefotaxime has activity against a wide range of
gram-positive and gram-negative organisms. Cefotaxime sodium has a high
degree of stability in the presence of ß-lactamases both penicillinases and
cephalosporinases
Cefotaxime sodium has been shown
to be active against most strains of the following microorganisms
Aerobes,
Gram-positive:
Enterococcus
spp.
Staphylococcus
aureus*
Staphylococcus
epidermidis
Streptococcus
pneumoniae
Streptococcus
pyogenes
(Group A beta-hemolytic streptococci) Streptococcus
spp.
*Staphylococci which are
resistant to methicillin/oxacillin
must be considered resistant to cefotaxime sodium.
