Serum protein binding and extravascular diffusion of methoxyimino cephalosporins. Time courses of free and total concentrations of cefotaxime and ceftriaxone in serum and pleural exudate
Identifieur interne : 000460 ( Istex/Curation ); précédent : 000459; suivant : 000461Serum protein binding and extravascular diffusion of methoxyimino cephalosporins. Time courses of free and total concentrations of cefotaxime and ceftriaxone in serum and pleural exudate
Auteurs : Francesco Scaglione [Italie] ; Mauro Raichi [Italie] ; Franco Fraschini [Italie]Source :
- Journal of Antimicrobial Chemotherapy [ 0305-7453 ] ; 1990.
Abstract
A new approach to the study of the distribution pharmacokinetics of variably bound β-lactams is to plot the concentration time course of their free (dialysable) and total (free and bound) forms. In the present study, the 6-h concentration time course was plotted of the total and free concentrations of cefotaxime and ceftriaxone in scrum and pleural exudate in 12 patients per group, after iv dosing with 1 g of either cefotaxime or ceftriaxone. Samples were taken at 0.5, 1, 1.5, 2, 3, 4 and 6 h after dosing. The results of a study of similar design, but conducted over 24 h in ten patients per group, following iv dosing with either cefotaxime 1 g 12-hourly or ceftriaxone 1 g daily are also reported. Samples were taken at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 14, 16 and 24 h after dosing. Areas under the curve of free cefotaxime in pleural fluid were greater than those of free ceftriaxone, in both the 6 h (+ 54.6%) and 24 h studies (+ 29.8% after 12 h and +71.0% after 24 h). The free cefotaxime/free ceftriaxone Cmax ratio was 1.75 in the 6 h study. Cefotaxime was superior to ceftriaxone in terms of the diffusion of the free (antibacterially active) fraction into a typical inflammatory exudate. Assessment of the effects of protein binding must be taken into account in antibiotic pharmacokinetic profiles.
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DOI: 10.1093/jac/26.suppl_A.1
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<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title>Serum protein binding and extravascular diffusion of methoxyimino cephalosporins. Time courses of free and total concentrations of cefotaxime and ceftriaxone in serum and pleural exudate</title><author><name sortKey="Scaglione, Francesco" sort="Scaglione, Francesco" uniqKey="Scaglione F" first="Francesco" last="Scaglione">Francesco Scaglione</name><affiliation wicri:level="1"><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Institute of Chemotherapy, University of Milan, Milan</wicri:regionArea></affiliation></author><author><name sortKey="Raichi, Mauro" sort="Raichi, Mauro" uniqKey="Raichi M" first="Mauro" last="Raichi">Mauro Raichi</name><affiliation wicri:level="1"><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Institute of Chemotherapy, University of Milan, Milan</wicri:regionArea></affiliation></author><author><name sortKey="Fraschini, Franco" sort="Fraschini, Franco" uniqKey="Fraschini F" first="Franco" last="Fraschini">Franco Fraschini</name><affiliation wicri:level="1"><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Institute of Chemotherapy, University of Milan, Milan</wicri:regionArea></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:D097F41A64098ABD5F8EA8347F7984583801F924</idno><date when="1990" year="1990">1990</date><idno type="doi">10.1093/jac/26.suppl_A.1</idno><idno type="url">https://api.istex.fr/document/D097F41A64098ABD5F8EA8347F7984583801F924/fulltext/pdf</idno><idno type="wicri:Area/Istex/Corpus">000460</idno><idno type="wicri:Area/Istex/Curation">000460</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a">Serum protein binding and extravascular diffusion of methoxyimino cephalosporins. Time courses of free and total concentrations of cefotaxime and ceftriaxone in serum and pleural exudate</title><author><name sortKey="Scaglione, Francesco" sort="Scaglione, Francesco" uniqKey="Scaglione F" first="Francesco" last="Scaglione">Francesco Scaglione</name><affiliation wicri:level="1"><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Institute of Chemotherapy, University of Milan, Milan</wicri:regionArea></affiliation></author><author><name sortKey="Raichi, Mauro" sort="Raichi, Mauro" uniqKey="Raichi M" first="Mauro" last="Raichi">Mauro Raichi</name><affiliation wicri:level="1"><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Institute of Chemotherapy, University of Milan, Milan</wicri:regionArea></affiliation></author><author><name sortKey="Fraschini, Franco" sort="Fraschini, Franco" uniqKey="Fraschini F" first="Franco" last="Fraschini">Franco Fraschini</name><affiliation wicri:level="1"><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Institute of Chemotherapy, University of Milan, Milan</wicri:regionArea></affiliation></author></analytic><monogr></monogr><series><title level="j">Journal of Antimicrobial Chemotherapy</title><idno type="ISSN">0305-7453</idno><idno type="eISSN">1460-2091</idno><imprint><publisher>Oxford University Press</publisher><date type="published" when="1990">1990</date><biblScope unit="volume">26</biblScope><biblScope unit="supplement">suppl_A</biblScope><biblScope unit="page" from="1">1</biblScope><biblScope unit="page" to="10">10</biblScope></imprint><idno type="ISSN">0305-7453</idno></series><idno type="istex">D097F41A64098ABD5F8EA8347F7984583801F924</idno><idno type="DOI">10.1093/jac/26.suppl_A.1</idno></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0305-7453</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract">A new approach to the study of the distribution pharmacokinetics of variably bound β-lactams is to plot the concentration time course of their free (dialysable) and total (free and bound) forms. In the present study, the 6-h concentration time course was plotted of the total and free concentrations of cefotaxime and ceftriaxone in scrum and pleural exudate in 12 patients per group, after iv dosing with 1 g of either cefotaxime or ceftriaxone. Samples were taken at 0.5, 1, 1.5, 2, 3, 4 and 6 h after dosing. The results of a study of similar design, but conducted over 24 h in ten patients per group, following iv dosing with either cefotaxime 1 g 12-hourly or ceftriaxone 1 g daily are also reported. Samples were taken at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 14, 16 and 24 h after dosing. Areas under the curve of free cefotaxime in pleural fluid were greater than those of free ceftriaxone, in both the 6 h (+ 54.6%) and 24 h studies (+ 29.8% after 12 h and +71.0% after 24 h). The free cefotaxime/free ceftriaxone Cmax ratio was 1.75 in the 6 h study. Cefotaxime was superior to ceftriaxone in terms of the diffusion of the free (antibacterially active) fraction into a typical inflammatory exudate. Assessment of the effects of protein binding must be taken into account in antibiotic pharmacokinetic profiles.</div></front></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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