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/Corpus ); 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 ; Mauro Raichi ; Franco FraschiniSource :
- 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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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><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation></affiliation></author><author><name sortKey="Raichi, Mauro" sort="Raichi, Mauro" uniqKey="Raichi M" first="Mauro" last="Raichi">Mauro Raichi</name><affiliation><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation></affiliation></author><author><name sortKey="Fraschini, Franco" sort="Fraschini, Franco" uniqKey="Fraschini F" first="Franco" last="Fraschini">Franco Fraschini</name><affiliation><mods:affiliation>Institute of Chemotherapy, University of Milan, Milan, Italy</mods:affiliation></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><istex><corpusName>oup</corpusName><author><json:item><name>Francesco Scaglione</name><affiliations><json:string>Institute of Chemotherapy, University of Milan, Milan, Italy</json:string></affiliations></json:item><json:item><name>Mauro Raichi</name><affiliations><json:string>Institute of Chemotherapy, University of Milan, Milan, Italy</json:string></affiliations></json:item><json:item><name>Franco Fraschini</name><affiliations><json:string>Institute of Chemotherapy, University of Milan, Milan, Italy</json:string></affiliations></json:item></author><subject><json:item><lang><json:string>eng</json:string></lang><value>Articles</value></json:item></subject><language><json:string>eng</json:string></language><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. 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Cefotaxime was superior to ceftriaxone in terms of the diffusion of the free (antibacterially active) fraction into a typical inflammatory exudate. 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Time courses of free and total concentrations of cefotaxime and ceftriaxone in serum and pleural exudate</article-title></title-group><contrib-group><contrib contrib-type="author"><name><surname>Scaglione</surname><given-names>Francesco</given-names></name></contrib><contrib contrib-type="author"><name><surname>Raichi</surname><given-names>Mauro</given-names></name></contrib><contrib contrib-type="author"><name><surname>Fraschini</surname><given-names>Franco</given-names></name><xref ref-type="corresp" rid="cor1"></xref></contrib><aff><institution>Institute of Chemotherapy, University of Milan</institution> <addr-line>Milan, Italy</addr-line></aff></contrib-group><author-notes><corresp id="cor1">Corresponding author: Professor Franco Fraschini, Dipartimento di Farmicologia, Via VaNvitelli 32, 20129 Milano, Italy</corresp></author-notes><pub-date pub-type="ppub"><year>1990</year></pub-date><volume>26</volume><issue>suppl_A</issue><fpage>1</fpage><lpage>10</lpage><copyright-statement>© 1990 The British Society for Antimicrobial Chemotherapy</copyright-statement><copyright-year>1990</copyright-year><abstract><p>A new approach to the study of the distribution pharmacokinetics of variably bound <italic>β</italic>-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 <italic>C</italic><sub>max</sub> 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.</p></abstract></article-meta></front></article></istex:document></istex:metadataXml><mods version="3.6"><titleInfo><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></titleInfo><titleInfo type="alternative" contentType="CDATA"><title>Serum protein binding and extravascular diffusion of methoxyimino cephalosporins. 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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. 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