Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients
Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chrom...
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Veröffentlicht in: | European journal of clinical pharmacology 1996, Vol.49 (5), p.401-405 |
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description | Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r > 0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 micrograms.ml-1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r = 0.79). The urinary concentrations ranged from 1.2 micrograms.ml-1 to 82.4 micrograms.ml-1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium. |
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L ; ROYER-MORROT, M. J ; LOZNIEWSKI, A ; TRACKOEN, G ; DELAVAULT, P ; ROYER, R. J</creator><creatorcontrib>MOREAU, J. L ; ROYER-MORROT, M. J ; LOZNIEWSKI, A ; TRACKOEN, G ; DELAVAULT, P ; ROYER, R. J</creatorcontrib><description>Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r > 0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 micrograms.ml-1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r = 0.79). The urinary concentrations ranged from 1.2 micrograms.ml-1 to 82.4 micrograms.ml-1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium.</description><identifier>ISSN: 0031-6970</identifier><identifier>EISSN: 1432-1041</identifier><identifier>DOI: 10.1007/BF00203786</identifier><identifier>PMID: 8866637</identifier><language>eng</language><publisher>Heidelberg: Springer</publisher><subject>Administration, Oral ; Adult ; Aged ; Aged, 80 and over ; Anti-Infective Agents - administration & dosage ; Anti-Infective Agents - pharmacokinetics ; Anti-Infective Agents - urine ; Anti-Infective Agents, Urinary - administration & dosage ; Anti-Infective Agents, Urinary - pharmacokinetics ; Anti-Infective Agents, Urinary - urine ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Biological and medical sciences ; Chromatography, Liquid ; Epithelium - metabolism ; Female ; Humans ; Male ; Medical sciences ; Microbial Sensitivity Tests ; Middle Aged ; Norfloxacin - blood ; Norfloxacin - pharmacokinetics ; Norfloxacin - urine ; Pefloxacin - administration & dosage ; Pefloxacin - blood ; Pefloxacin - pharmacokinetics ; Pefloxacin - urine ; Pharmacology. Drug treatments ; Regression Analysis ; Urinary Bladder - metabolism</subject><ispartof>European journal of clinical pharmacology, 1996, Vol.49 (5), p.401-405</ispartof><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4021,27921,27922,27923</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2980391$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8866637$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>MOREAU, J. L</creatorcontrib><creatorcontrib>ROYER-MORROT, M. J</creatorcontrib><creatorcontrib>LOZNIEWSKI, A</creatorcontrib><creatorcontrib>TRACKOEN, G</creatorcontrib><creatorcontrib>DELAVAULT, P</creatorcontrib><creatorcontrib>ROYER, R. J</creatorcontrib><title>Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients</title><title>European journal of clinical pharmacology</title><addtitle>Eur J Clin Pharmacol</addtitle><description>Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r > 0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 micrograms.ml-1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r = 0.79). The urinary concentrations ranged from 1.2 micrograms.ml-1 to 82.4 micrograms.ml-1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium.</description><subject>Administration, Oral</subject><subject>Adult</subject><subject>Aged</subject><subject>Aged, 80 and over</subject><subject>Anti-Infective Agents - administration & dosage</subject><subject>Anti-Infective Agents - pharmacokinetics</subject><subject>Anti-Infective Agents - urine</subject><subject>Anti-Infective Agents, Urinary - administration & dosage</subject><subject>Anti-Infective Agents, Urinary - pharmacokinetics</subject><subject>Anti-Infective Agents, Urinary - urine</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Chromatography, Liquid</subject><subject>Epithelium - metabolism</subject><subject>Female</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Middle Aged</subject><subject>Norfloxacin - blood</subject><subject>Norfloxacin - pharmacokinetics</subject><subject>Norfloxacin - urine</subject><subject>Pefloxacin - administration & dosage</subject><subject>Pefloxacin - blood</subject><subject>Pefloxacin - pharmacokinetics</subject><subject>Pefloxacin - urine</subject><subject>Pharmacology. Drug treatments</subject><subject>Regression Analysis</subject><subject>Urinary Bladder - metabolism</subject><issn>0031-6970</issn><issn>1432-1041</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkEFrFTEUhYMo9bW6cS9kIS6E0ZtJJpMsbbFVqOhC10NecuOLZJIxyYBd-dedRx_t6tzL-e65cAh5xeA9Axg_XF4D9MBHJZ-QHRO87xgI9pTsADjrpB7hOTmv9TcAGzTwM3KmlJSSjzvy7zsmbMW0kBPNni7oY_5rbEjUJEdDq9RhnbEd7iLdxOxzDA1pSC3TdkC6loxL2KYY1pka37BQQxVA9_WG1pB-RaS5mEhdrsczelhnk-iyfcTU6gvyzJtY8eVJL8jP608_rj53t99uvlx9vO1sP0LrtBGIei-15d5a51AwtxcGYNu1ZKi0F1b1iF46NQyMWeOlHNwoeq6t0PyCvL3PXUr-s2Jt0xyqxRhNwrzWaVRCwNAfwXf3oC251oJ-WkqYTbmbGEzHtqfHtjf49Sl13c_oHtBTvZv_5uSbak30xSQb6gPWawVcM_4fAo6INA</recordid><startdate>1996</startdate><enddate>1996</enddate><creator>MOREAU, J. L</creator><creator>ROYER-MORROT, M. 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J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c270t-9a4ee9b69c3fccdde41db4a00c3f961e89f4c82eef6d85511caf665d74239c493</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Administration, Oral</topic><topic>Adult</topic><topic>Aged</topic><topic>Aged, 80 and over</topic><topic>Anti-Infective Agents - administration & dosage</topic><topic>Anti-Infective Agents - pharmacokinetics</topic><topic>Anti-Infective Agents - urine</topic><topic>Anti-Infective Agents, Urinary - administration & dosage</topic><topic>Anti-Infective Agents, Urinary - pharmacokinetics</topic><topic>Anti-Infective Agents, Urinary - urine</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Chromatography, Liquid</topic><topic>Epithelium - metabolism</topic><topic>Female</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Microbial Sensitivity Tests</topic><topic>Middle Aged</topic><topic>Norfloxacin - blood</topic><topic>Norfloxacin - pharmacokinetics</topic><topic>Norfloxacin - urine</topic><topic>Pefloxacin - administration & dosage</topic><topic>Pefloxacin - blood</topic><topic>Pefloxacin - pharmacokinetics</topic><topic>Pefloxacin - urine</topic><topic>Pharmacology. Drug treatments</topic><topic>Regression Analysis</topic><topic>Urinary Bladder - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>MOREAU, J. L</creatorcontrib><creatorcontrib>ROYER-MORROT, M. J</creatorcontrib><creatorcontrib>LOZNIEWSKI, A</creatorcontrib><creatorcontrib>TRACKOEN, G</creatorcontrib><creatorcontrib>DELAVAULT, P</creatorcontrib><creatorcontrib>ROYER, R. J</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of clinical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>MOREAU, J. L</au><au>ROYER-MORROT, M. J</au><au>LOZNIEWSKI, A</au><au>TRACKOEN, G</au><au>DELAVAULT, P</au><au>ROYER, R. J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients</atitle><jtitle>European journal of clinical pharmacology</jtitle><addtitle>Eur J Clin Pharmacol</addtitle><date>1996</date><risdate>1996</risdate><volume>49</volume><issue>5</issue><spage>401</spage><epage>405</epage><pages>401-405</pages><issn>0031-6970</issn><eissn>1432-1041</eissn><abstract>Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r > 0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 micrograms.ml-1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r = 0.79). The urinary concentrations ranged from 1.2 micrograms.ml-1 to 82.4 micrograms.ml-1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium.</abstract><cop>Heidelberg</cop><cop>Berlin</cop><pub>Springer</pub><pmid>8866637</pmid><doi>10.1007/BF00203786</doi><tpages>5</tpages></addata></record> |
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subjects | Administration, Oral Adult Aged Aged, 80 and over Anti-Infective Agents - administration & dosage Anti-Infective Agents - pharmacokinetics Anti-Infective Agents - urine Anti-Infective Agents, Urinary - administration & dosage Anti-Infective Agents, Urinary - pharmacokinetics Anti-Infective Agents, Urinary - urine Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Chromatography, Liquid Epithelium - metabolism Female Humans Male Medical sciences Microbial Sensitivity Tests Middle Aged Norfloxacin - blood Norfloxacin - pharmacokinetics Norfloxacin - urine Pefloxacin - administration & dosage Pefloxacin - blood Pefloxacin - pharmacokinetics Pefloxacin - urine Pharmacology. Drug treatments Regression Analysis Urinary Bladder - metabolism |
title | Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients |
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