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An. R. Acad. Nac. Farm., 2009, 75 (2): 217-231

ARTÍCULO

(Cu)II in vivo interaction with cefotaxime

Antonio L. Doadrio 1 *, Pilar Madrigal 2, Juan de Dios Casas 2

1 Department of Inorganic Chemistry and Bioinorganic.
School of Pharmacy. University Complutense. Madrid. Spain.
2 Dirección Department of Toxicology and Legal Medicine.
School of Medicine. University Complutense. Madrid. Spain.
Recibido el 9 de diciembre de 2008.

ABSTRACT

The presence of Cu(II) in penicillin and cephalosporin solutions,
has been proved, to promote in vitro the antibiotic degradation to
the corresponding acid derivates. HPLC studies provided an
additional evidence for the reaction mechanism. The mechanisms of
Cu(II) catalysis involve a ternary complex. This work was undertaken
to study the consequences of this degradation in vivo upper the
pharmacokinetic, pharmacodynamic and activity of the antibiotic
cefotaxime. It is one of the most used «third-generation»
cephalosporin in the world, this is because of that the interaction
cefotaxime-metal deserved our attention. Our results remarked a
lower concentration of free cefotaxime in blood, liver, spleen, kidney,
lung and heart in organs from animals suffering Cu-intoxication.
The differences more significant between intoxicated and control
rats were observed in liver, lung and kidney. In addition cefotaxime
linked to copper lose most of the microbicidal activity against
bacterial strains of Bacillus subtilis CECT 356, Escherichia coli CECT
434, Escherichia coli CECT 616, Staphilococus aureus spp aureus
CECT 435, Staphilococus aureus spp aureus CECT 239, in plate tests.
It means that cefotaxime would become ineffective as antibiotic in
metal poisoned patients.

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