The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat
The goal of this study was to determine if the co-administration of esmolol (ES), a short acting cardioselective beta-blocker, significantly alters the pharmacokinetics and/or pharmacodynamics of remifentanil (REMI), an ultra short-acting opioid, in the rat. Sprague-Dawley rats (N = 8, Wt. = 325 +/-...
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| Veröffentlicht in: | Pharmaceutical research 1997-12, Vol.14 (12), p.1817-1823 |
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| creator | HAIDAR, S. H MORETON, J. E LIANG, Z HOKE, J. F MUIR, K. T EDDINGTON, N. D |
| description | The goal of this study was to determine if the co-administration of esmolol (ES), a short acting cardioselective beta-blocker, significantly alters the pharmacokinetics and/or pharmacodynamics of remifentanil (REMI), an ultra short-acting opioid, in the rat.
Sprague-Dawley rats (N = 8, Wt. = 325 +/- 15 g) were surgically implanted with stainless steel cerebrocortical EEG electrodes three days before the study. Each rat was dosed with REMI (15 micrograms/kg/min), and REMI & ES (15 micrograms/kg/min and 600 micrograms/kg/min) for 21 minutes in a random crossover design. Six serial blood samples were collected over 25 minutes into test-tubes containing 0.5 ml acetonitrile. Blood samples were extracted with methylene chloride and analyzed by a validated GC-MS assay. EEG was captured and subjected to power spectral analysis (0.1-50 Hz) for spectral edge (97%).
No significant differences (p < 0.05) were found in clearance (REMI = 287 + 73 ml/min/leg vs. REMI & ES = 289 +/- 148 ml/min kg) or Vd (REMI = 286 +/- 49 ml/kg vs REMI & ES = 248 + 40 ml/kg). A linked sigmoid Emax PK-PD model was used and the pharmacodynamic parameters were not statistically different. Mean Emax and EC50 after REMI were 18.0 +/- 6.0 Hz and 32 +/- 12 ng/ml; and after REMI + ES were 19 + 4.8 Hz and 26 + 8.6 ng/ml.
At the doses tested, there is no pharmacokinetic or pharmacodynamic interaction between remifentanil and esmolol in the rat. |
| doi_str_mv | 10.1023/A:1012156502624 |
| format | Article |
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Sprague-Dawley rats (N = 8, Wt. = 325 +/- 15 g) were surgically implanted with stainless steel cerebrocortical EEG electrodes three days before the study. Each rat was dosed with REMI (15 micrograms/kg/min), and REMI & ES (15 micrograms/kg/min and 600 micrograms/kg/min) for 21 minutes in a random crossover design. Six serial blood samples were collected over 25 minutes into test-tubes containing 0.5 ml acetonitrile. Blood samples were extracted with methylene chloride and analyzed by a validated GC-MS assay. EEG was captured and subjected to power spectral analysis (0.1-50 Hz) for spectral edge (97%).
No significant differences (p < 0.05) were found in clearance (REMI = 287 + 73 ml/min/leg vs. REMI & ES = 289 +/- 148 ml/min kg) or Vd (REMI = 286 +/- 49 ml/kg vs REMI & ES = 248 + 40 ml/kg). A linked sigmoid Emax PK-PD model was used and the pharmacodynamic parameters were not statistically different. Mean Emax and EC50 after REMI were 18.0 +/- 6.0 Hz and 32 +/- 12 ng/ml; and after REMI + ES were 19 + 4.8 Hz and 26 + 8.6 ng/ml.
At the doses tested, there is no pharmacokinetic or pharmacodynamic interaction between remifentanil and esmolol in the rat.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1023/A:1012156502624</identifier><identifier>PMID: 9453074</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject>Adrenergic beta-Antagonists - administration & dosage ; Adrenergic beta-Antagonists - pharmacology ; Analgesics ; Analgesics, Opioid - administration & dosage ; Analgesics, Opioid - pharmacokinetics ; Analgesics, Opioid - pharmacology ; Animals ; Biological and medical sciences ; Cross-Over Studies ; Drug Interactions ; Electroencephalography - drug effects ; Half-Life ; Infusions, Intravenous ; Male ; Medical sciences ; Metabolic Clearance Rate ; Neuropharmacology ; Pharmacology. Drug treatments ; Piperidines - administration & dosage ; Piperidines - pharmacokinetics ; Piperidines - pharmacology ; Propanolamines - administration & dosage ; Propanolamines - pharmacology ; Rats ; Rats, Sprague-Dawley ; Remifentanil</subject><ispartof>Pharmaceutical research, 1997-12, Vol.14 (12), p.1817-1823</ispartof><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c281t-eb93beec0bb2c6ad841d166ed0488c812e00f8b50e6f5bbe321edbf57ee657583</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2117740$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9453074$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>HAIDAR, S. H</creatorcontrib><creatorcontrib>MORETON, J. E</creatorcontrib><creatorcontrib>LIANG, Z</creatorcontrib><creatorcontrib>HOKE, J. F</creatorcontrib><creatorcontrib>MUIR, K. T</creatorcontrib><creatorcontrib>EDDINGTON, N. D</creatorcontrib><title>The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><description>The goal of this study was to determine if the co-administration of esmolol (ES), a short acting cardioselective beta-blocker, significantly alters the pharmacokinetics and/or pharmacodynamics of remifentanil (REMI), an ultra short-acting opioid, in the rat.
Sprague-Dawley rats (N = 8, Wt. = 325 +/- 15 g) were surgically implanted with stainless steel cerebrocortical EEG electrodes three days before the study. Each rat was dosed with REMI (15 micrograms/kg/min), and REMI & ES (15 micrograms/kg/min and 600 micrograms/kg/min) for 21 minutes in a random crossover design. Six serial blood samples were collected over 25 minutes into test-tubes containing 0.5 ml acetonitrile. Blood samples were extracted with methylene chloride and analyzed by a validated GC-MS assay. EEG was captured and subjected to power spectral analysis (0.1-50 Hz) for spectral edge (97%).
No significant differences (p < 0.05) were found in clearance (REMI = 287 + 73 ml/min/leg vs. REMI & ES = 289 +/- 148 ml/min kg) or Vd (REMI = 286 +/- 49 ml/kg vs REMI & ES = 248 + 40 ml/kg). A linked sigmoid Emax PK-PD model was used and the pharmacodynamic parameters were not statistically different. Mean Emax and EC50 after REMI were 18.0 +/- 6.0 Hz and 32 +/- 12 ng/ml; and after REMI + ES were 19 + 4.8 Hz and 26 + 8.6 ng/ml.
At the doses tested, there is no pharmacokinetic or pharmacodynamic interaction between remifentanil and esmolol in the rat.</description><subject>Adrenergic beta-Antagonists - administration & dosage</subject><subject>Adrenergic beta-Antagonists - pharmacology</subject><subject>Analgesics</subject><subject>Analgesics, Opioid - administration & dosage</subject><subject>Analgesics, Opioid - pharmacokinetics</subject><subject>Analgesics, Opioid - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cross-Over Studies</subject><subject>Drug Interactions</subject><subject>Electroencephalography - drug effects</subject><subject>Half-Life</subject><subject>Infusions, Intravenous</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Metabolic Clearance Rate</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - administration & dosage</subject><subject>Piperidines - pharmacokinetics</subject><subject>Piperidines - pharmacology</subject><subject>Propanolamines - administration & dosage</subject><subject>Propanolamines - pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Remifentanil</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kE1LxDAQhoMo67p69iTk4LU6SZMm9bYsfsGClxW8LUk6daNtUpKK-O-tuniaged5Z-Al5JzBFQNeXi9vGDDOZCWBV1wckDmTqixqEC-HZA6Ki0IrwY7JSc5vAKBZLWZkVgtZghJz8rnZIR12JvXGxXcfcPQuUxMaih26MUUMDifexddkepowDzFkpLGd9t63GEYTfEcnIeBvzgfqYm99MKOPgX76cUcx97GL3Q8bp3_JjKfkqDVdxrP9XJDnu9vN6qFYP90_rpbrwnHNxgJtXVpEB9ZyV5lGC9awqsIGhNZOM44ArbYSsGqltVhyho1tpUKspJK6XJCLv7vDh-2x2Q7J9yZ9bfcFTPxyz012pmuTCc7nf40zppSA8ht2-20j</recordid><startdate>19971201</startdate><enddate>19971201</enddate><creator>HAIDAR, S. H</creator><creator>MORETON, J. E</creator><creator>LIANG, Z</creator><creator>HOKE, J. F</creator><creator>MUIR, K. T</creator><creator>EDDINGTON, N. D</creator><general>Springer</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>19971201</creationdate><title>The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat</title><author>HAIDAR, S. H ; MORETON, J. E ; LIANG, Z ; HOKE, J. F ; MUIR, K. T ; EDDINGTON, N. D</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c281t-eb93beec0bb2c6ad841d166ed0488c812e00f8b50e6f5bbe321edbf57ee657583</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>Adrenergic beta-Antagonists - administration & dosage</topic><topic>Adrenergic beta-Antagonists - pharmacology</topic><topic>Analgesics</topic><topic>Analgesics, Opioid - administration & dosage</topic><topic>Analgesics, Opioid - pharmacokinetics</topic><topic>Analgesics, Opioid - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cross-Over Studies</topic><topic>Drug Interactions</topic><topic>Electroencephalography - drug effects</topic><topic>Half-Life</topic><topic>Infusions, Intravenous</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Metabolic Clearance Rate</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperidines - administration & dosage</topic><topic>Piperidines - pharmacokinetics</topic><topic>Piperidines - pharmacology</topic><topic>Propanolamines - administration & dosage</topic><topic>Propanolamines - pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Remifentanil</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>HAIDAR, S. H</creatorcontrib><creatorcontrib>MORETON, J. E</creatorcontrib><creatorcontrib>LIANG, Z</creatorcontrib><creatorcontrib>HOKE, J. F</creatorcontrib><creatorcontrib>MUIR, K. T</creatorcontrib><creatorcontrib>EDDINGTON, N. D</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>HAIDAR, S. H</au><au>MORETON, J. E</au><au>LIANG, Z</au><au>HOKE, J. F</au><au>MUIR, K. T</au><au>EDDINGTON, N. D</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat</atitle><jtitle>Pharmaceutical research</jtitle><addtitle>Pharm Res</addtitle><date>1997-12-01</date><risdate>1997</risdate><volume>14</volume><issue>12</issue><spage>1817</spage><epage>1823</epage><pages>1817-1823</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>The goal of this study was to determine if the co-administration of esmolol (ES), a short acting cardioselective beta-blocker, significantly alters the pharmacokinetics and/or pharmacodynamics of remifentanil (REMI), an ultra short-acting opioid, in the rat.
Sprague-Dawley rats (N = 8, Wt. = 325 +/- 15 g) were surgically implanted with stainless steel cerebrocortical EEG electrodes three days before the study. Each rat was dosed with REMI (15 micrograms/kg/min), and REMI & ES (15 micrograms/kg/min and 600 micrograms/kg/min) for 21 minutes in a random crossover design. Six serial blood samples were collected over 25 minutes into test-tubes containing 0.5 ml acetonitrile. Blood samples were extracted with methylene chloride and analyzed by a validated GC-MS assay. EEG was captured and subjected to power spectral analysis (0.1-50 Hz) for spectral edge (97%).
No significant differences (p < 0.05) were found in clearance (REMI = 287 + 73 ml/min/leg vs. REMI & ES = 289 +/- 148 ml/min kg) or Vd (REMI = 286 +/- 49 ml/kg vs REMI & ES = 248 + 40 ml/kg). A linked sigmoid Emax PK-PD model was used and the pharmacodynamic parameters were not statistically different. Mean Emax and EC50 after REMI were 18.0 +/- 6.0 Hz and 32 +/- 12 ng/ml; and after REMI + ES were 19 + 4.8 Hz and 26 + 8.6 ng/ml.
At the doses tested, there is no pharmacokinetic or pharmacodynamic interaction between remifentanil and esmolol in the rat.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>9453074</pmid><doi>10.1023/A:1012156502624</doi><tpages>7</tpages></addata></record> |
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| subjects | Adrenergic beta-Antagonists - administration & dosage Adrenergic beta-Antagonists - pharmacology Analgesics Analgesics, Opioid - administration & dosage Analgesics, Opioid - pharmacokinetics Analgesics, Opioid - pharmacology Animals Biological and medical sciences Cross-Over Studies Drug Interactions Electroencephalography - drug effects Half-Life Infusions, Intravenous Male Medical sciences Metabolic Clearance Rate Neuropharmacology Pharmacology. Drug treatments Piperidines - administration & dosage Piperidines - pharmacokinetics Piperidines - pharmacology Propanolamines - administration & dosage Propanolamines - pharmacology Rats Rats, Sprague-Dawley Remifentanil |
| title | The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat |
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