Effect of ciprofloxacin on the pharmacokinetics of ropivacaine
To assess the effect of ciprofloxacin on the pharmacokinetics of ropivacaine. METHODS. In a double-blind, randomised, cross-over study, nine healthy volunteers were treated for 2.5 days with 500 mg oral ciprofloxacin or placebo twice daily. On day 3, they received a single dose of 0.6 mg/kg ropivaca...
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| Veröffentlicht in: | European journal of clinical pharmacology 2003-02, Vol.58 (10), p.653-657 |
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| creator | JOKINEN, Mika J OLKKOLA, Klaus T AHONEN, Jouni NEUVONEN, Pertti J |
| description | To assess the effect of ciprofloxacin on the pharmacokinetics of ropivacaine. METHODS. In a double-blind, randomised, cross-over study, nine healthy volunteers were treated for 2.5 days with 500 mg oral ciprofloxacin or placebo twice daily. On day 3, they received a single dose of 0.6 mg/kg ropivacaine intravenously over 30 min. Ropivacaine, 3-hydroxyropivacaine (3-OH-ropivacaine), and (S)-2',6'-pipecoloxylidide (PPX) in venous plasma and urine were measured for up to 12 h and 24 h, respectively.
Ciprofloxacin decreased the mean clearance (CL) of ropivacaine by 31% (P |
| doi_str_mv | 10.1007/s00228-002-0540-8 |
| format | Article |
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Ciprofloxacin decreased the mean clearance (CL) of ropivacaine by 31% (P<0.05), with a considerable inter-individual variation (range from -52% to +39%). It also decreased the area under the plasma concentration-time curve (AUC) of 3-OH-ropivacaine by 38% (P<0.05) and urinary excretion of 3-OH-ropivacaine by 27% (P<0.05). Ciprofloxacin increased the AUC of PPX by 71% (P<0.01) and urinary excretion of PPX by 97% (P<0.01).
Ciprofloxacin modestly decreased the mean ropivacaine CL by inhibiting the CYP1A2-mediated formation of 3-OH-ropivacaine. At the same time, the CYP3A4-mediated formation of PPX was increased. There was a marked inter-individual variation in the extent of the interaction, and, for some individuals, the concomitant use of ciprofloxacin with ropivacaine might produce toxic symptoms.</description><identifier>ISSN: 0031-6970</identifier><identifier>EISSN: 1432-1041</identifier><identifier>DOI: 10.1007/s00228-002-0540-8</identifier><identifier>PMID: 12610740</identifier><language>eng</language><publisher>Heidelberg: Springer</publisher><subject>Adult ; Amides - blood ; Amides - metabolism ; Amides - pharmacokinetics ; Amides - urine ; Anesthetics, Local - blood ; Anesthetics, Local - pharmacokinetics ; Anesthetics, Local - urine ; Anesthetics. Neuromuscular blocking agents ; Anti-Infective Agents - pharmacology ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Area Under Curve ; Biological and medical sciences ; Bupivacaine - analogs & derivatives ; Bupivacaine - blood ; Bupivacaine - urine ; Ciprofloxacin - pharmacology ; Cross-Over Studies ; Cytochrome P-450 CYP1A2 - metabolism ; Cytochrome P-450 CYP1A2 Inhibitors ; Cytochrome P-450 CYP3A ; Cytochrome P-450 Enzyme System - metabolism ; Double-Blind Method ; Drug Interactions ; Female ; Humans ; Male ; Medical sciences ; Neuropharmacology ; Pharmacology. Drug treatments ; Ropivacaine ; Stereoisomerism</subject><ispartof>European journal of clinical pharmacology, 2003-02, Vol.58 (10), p.653-657</ispartof><rights>2003 INIST-CNRS</rights><rights>Springer-Verlag 2003</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c354t-f14ff89a2be8e1c1efe6dbcc1560243c201c8b4f3b80a9f9b11bb442d4831a23</citedby><cites>FETCH-LOGICAL-c354t-f14ff89a2be8e1c1efe6dbcc1560243c201c8b4f3b80a9f9b11bb442d4831a23</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,782,786,27933,27934</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14603737$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12610740$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>JOKINEN, Mika J</creatorcontrib><creatorcontrib>OLKKOLA, Klaus T</creatorcontrib><creatorcontrib>AHONEN, Jouni</creatorcontrib><creatorcontrib>NEUVONEN, Pertti J</creatorcontrib><title>Effect of ciprofloxacin on the pharmacokinetics of ropivacaine</title><title>European journal of clinical pharmacology</title><addtitle>Eur J Clin Pharmacol</addtitle><description>To assess the effect of ciprofloxacin on the pharmacokinetics of ropivacaine. METHODS. In a double-blind, randomised, cross-over study, nine healthy volunteers were treated for 2.5 days with 500 mg oral ciprofloxacin or placebo twice daily. On day 3, they received a single dose of 0.6 mg/kg ropivacaine intravenously over 30 min. Ropivacaine, 3-hydroxyropivacaine (3-OH-ropivacaine), and (S)-2',6'-pipecoloxylidide (PPX) in venous plasma and urine were measured for up to 12 h and 24 h, respectively.
Ciprofloxacin decreased the mean clearance (CL) of ropivacaine by 31% (P<0.05), with a considerable inter-individual variation (range from -52% to +39%). It also decreased the area under the plasma concentration-time curve (AUC) of 3-OH-ropivacaine by 38% (P<0.05) and urinary excretion of 3-OH-ropivacaine by 27% (P<0.05). Ciprofloxacin increased the AUC of PPX by 71% (P<0.01) and urinary excretion of PPX by 97% (P<0.01).
Ciprofloxacin modestly decreased the mean ropivacaine CL by inhibiting the CYP1A2-mediated formation of 3-OH-ropivacaine. At the same time, the CYP3A4-mediated formation of PPX was increased. There was a marked inter-individual variation in the extent of the interaction, and, for some individuals, the concomitant use of ciprofloxacin with ropivacaine might produce toxic symptoms.</description><subject>Adult</subject><subject>Amides - blood</subject><subject>Amides - metabolism</subject><subject>Amides - pharmacokinetics</subject><subject>Amides - urine</subject><subject>Anesthetics, Local - blood</subject><subject>Anesthetics, Local - pharmacokinetics</subject><subject>Anesthetics, Local - urine</subject><subject>Anesthetics. Neuromuscular blocking agents</subject><subject>Anti-Infective Agents - pharmacology</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Area Under Curve</subject><subject>Biological and medical sciences</subject><subject>Bupivacaine - analogs & derivatives</subject><subject>Bupivacaine - blood</subject><subject>Bupivacaine - urine</subject><subject>Ciprofloxacin - pharmacology</subject><subject>Cross-Over Studies</subject><subject>Cytochrome P-450 CYP1A2 - metabolism</subject><subject>Cytochrome P-450 CYP1A2 Inhibitors</subject><subject>Cytochrome P-450 CYP3A</subject><subject>Cytochrome P-450 Enzyme System - metabolism</subject><subject>Double-Blind Method</subject><subject>Drug Interactions</subject><subject>Female</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Ropivacaine</subject><subject>Stereoisomerism</subject><issn>0031-6970</issn><issn>1432-1041</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNpFkE9LAzEQxYMotlY_gBdZBI_RmSS7m70IUuofKHjpPSRpQre2m5psRb-9KV0oA29g-L2Z4RFyi_CIAPVTAmBM0qwUSgFUnpExCs4ogsBzMgbgSKumhhG5SmkNgGUD_JKMkFUItYAxeZ5572xfBF_YdheD34RfbduuCF3Rr1yxW-m41TZ8tZ3rW5sOYAy79kdbnUfX5MLrTXI3Q5-QxetsMX2n88-3j-nLnFpeip56FN7LRjPjpEOLzrtqaazFsgImuGWAVhrhuZGgG98YRGOEYEshOWrGJ-T-uDZ_-L13qVfrsI9dvqgYCiGxajBDeIRsDClF59Uutlsd_xSCOuSljnmprOqQl5LZczcs3putW54cQ0AZeBgAnaze-Kg726YTJyrgda5_hZpyLA</recordid><startdate>20030201</startdate><enddate>20030201</enddate><creator>JOKINEN, Mika J</creator><creator>OLKKOLA, Klaus T</creator><creator>AHONEN, Jouni</creator><creator>NEUVONEN, Pertti J</creator><general>Springer</general><general>Springer Nature B.V</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7RV</scope><scope>7TK</scope><scope>7U9</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>H94</scope><scope>K9.</scope><scope>KB0</scope><scope>M0S</scope><scope>M1P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope></search><sort><creationdate>20030201</creationdate><title>Effect of ciprofloxacin on the pharmacokinetics of ropivacaine</title><author>JOKINEN, Mika J ; OLKKOLA, Klaus T ; AHONEN, Jouni ; NEUVONEN, Pertti J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c354t-f14ff89a2be8e1c1efe6dbcc1560243c201c8b4f3b80a9f9b11bb442d4831a23</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Adult</topic><topic>Amides - blood</topic><topic>Amides - metabolism</topic><topic>Amides - pharmacokinetics</topic><topic>Amides - urine</topic><topic>Anesthetics, Local - blood</topic><topic>Anesthetics, Local - pharmacokinetics</topic><topic>Anesthetics, Local - urine</topic><topic>Anesthetics. Neuromuscular blocking agents</topic><topic>Anti-Infective Agents - pharmacology</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Area Under Curve</topic><topic>Biological and medical sciences</topic><topic>Bupivacaine - analogs & derivatives</topic><topic>Bupivacaine - blood</topic><topic>Bupivacaine - urine</topic><topic>Ciprofloxacin - pharmacology</topic><topic>Cross-Over Studies</topic><topic>Cytochrome P-450 CYP1A2 - metabolism</topic><topic>Cytochrome P-450 CYP1A2 Inhibitors</topic><topic>Cytochrome P-450 CYP3A</topic><topic>Cytochrome P-450 Enzyme System - metabolism</topic><topic>Double-Blind Method</topic><topic>Drug Interactions</topic><topic>Female</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Ropivacaine</topic><topic>Stereoisomerism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>JOKINEN, Mika J</creatorcontrib><creatorcontrib>OLKKOLA, Klaus T</creatorcontrib><creatorcontrib>AHONEN, Jouni</creatorcontrib><creatorcontrib>NEUVONEN, Pertti 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>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><jtitle>European journal of clinical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>JOKINEN, Mika J</au><au>OLKKOLA, Klaus T</au><au>AHONEN, Jouni</au><au>NEUVONEN, Pertti J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of ciprofloxacin on the pharmacokinetics of ropivacaine</atitle><jtitle>European journal of clinical pharmacology</jtitle><addtitle>Eur J Clin Pharmacol</addtitle><date>2003-02-01</date><risdate>2003</risdate><volume>58</volume><issue>10</issue><spage>653</spage><epage>657</epage><pages>653-657</pages><issn>0031-6970</issn><eissn>1432-1041</eissn><abstract>To assess the effect of ciprofloxacin on the pharmacokinetics of ropivacaine. METHODS. In a double-blind, randomised, cross-over study, nine healthy volunteers were treated for 2.5 days with 500 mg oral ciprofloxacin or placebo twice daily. On day 3, they received a single dose of 0.6 mg/kg ropivacaine intravenously over 30 min. Ropivacaine, 3-hydroxyropivacaine (3-OH-ropivacaine), and (S)-2',6'-pipecoloxylidide (PPX) in venous plasma and urine were measured for up to 12 h and 24 h, respectively.
Ciprofloxacin decreased the mean clearance (CL) of ropivacaine by 31% (P<0.05), with a considerable inter-individual variation (range from -52% to +39%). It also decreased the area under the plasma concentration-time curve (AUC) of 3-OH-ropivacaine by 38% (P<0.05) and urinary excretion of 3-OH-ropivacaine by 27% (P<0.05). Ciprofloxacin increased the AUC of PPX by 71% (P<0.01) and urinary excretion of PPX by 97% (P<0.01).
Ciprofloxacin modestly decreased the mean ropivacaine CL by inhibiting the CYP1A2-mediated formation of 3-OH-ropivacaine. At the same time, the CYP3A4-mediated formation of PPX was increased. There was a marked inter-individual variation in the extent of the interaction, and, for some individuals, the concomitant use of ciprofloxacin with ropivacaine might produce toxic symptoms.</abstract><cop>Heidelberg</cop><cop>Berlin</cop><pub>Springer</pub><pmid>12610740</pmid><doi>10.1007/s00228-002-0540-8</doi><tpages>5</tpages></addata></record> |
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| ispartof | European journal of clinical pharmacology, 2003-02, Vol.58 (10), p.653-657 |
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| subjects | Adult Amides - blood Amides - metabolism Amides - pharmacokinetics Amides - urine Anesthetics, Local - blood Anesthetics, Local - pharmacokinetics Anesthetics, Local - urine Anesthetics. Neuromuscular blocking agents Anti-Infective Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Area Under Curve Biological and medical sciences Bupivacaine - analogs & derivatives Bupivacaine - blood Bupivacaine - urine Ciprofloxacin - pharmacology Cross-Over Studies Cytochrome P-450 CYP1A2 - metabolism Cytochrome P-450 CYP1A2 Inhibitors Cytochrome P-450 CYP3A Cytochrome P-450 Enzyme System - metabolism Double-Blind Method Drug Interactions Female Humans Male Medical sciences Neuropharmacology Pharmacology. Drug treatments Ropivacaine Stereoisomerism |
| title | Effect of ciprofloxacin on the pharmacokinetics of ropivacaine |
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