Plasma concentrations and bioavailability of propranolol by oral, rectal and intravenous administration in man
Eight normal male volunteers received 80 mg doses of propranolol by the oral and rectal routes and 2·2 mg by intravenous administration in a crossover fashion. Plasma concentrations of propranolol were measured by a gas chromatographic method using an electron capture detector. Individual subject co...
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| Veröffentlicht in: | Biopharmaceutics & drug disposition 1986-11, Vol.7 (6), p.559-566 |
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| container_title | Biopharmaceutics & drug disposition |
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| creator | Cid, Edison Mella, Fernando Lucchini, Leonardo Cárcamo, Martín Monasterio, José |
| description | Eight normal male volunteers received 80 mg doses of propranolol by the oral and rectal routes and 2·2 mg by intravenous administration in a crossover fashion. Plasma concentrations of propranolol were measured by a gas chromatographic method using an electron capture detector. Individual subject concentration–time data were analysed and results indicated that the data fit a two compartment model with first order absorption. An approximately two‐fold higher plasma propranolol concentration was observed after rectal administration as compared with oral dosing. Statistical analysis of the difference in the total AUCs indicates a significantly higher bioavailability of propranolol administered by the rectal route. The reduced bioavailability after oral administration indicates a substantial first pass effect but that it is possible to bypass the liver, at least partially, by giving the drug rectally to man. |
| doi_str_mv | 10.1002/bdd.2510070605 |
| format | Article |
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Plasma concentrations of propranolol were measured by a gas chromatographic method using an electron capture detector. Individual subject concentration–time data were analysed and results indicated that the data fit a two compartment model with first order absorption. An approximately two‐fold higher plasma propranolol concentration was observed after rectal administration as compared with oral dosing. Statistical analysis of the difference in the total AUCs indicates a significantly higher bioavailability of propranolol administered by the rectal route. The reduced bioavailability after oral administration indicates a substantial first pass effect but that it is possible to bypass the liver, at least partially, by giving the drug rectally to man.</description><identifier>ISSN: 0142-2782</identifier><identifier>EISSN: 1099-081X</identifier><identifier>DOI: 10.1002/bdd.2510070605</identifier><identifier>PMID: 3828485</identifier><identifier>CODEN: BDDID8</identifier><language>eng</language><publisher>New York: John Wiley & Sons, Ltd</publisher><subject>Administration, Oral ; Administration, Rectal ; Adult ; Bioavailability ; Biological and medical sciences ; Biological Availability ; Cardiovascular system ; First pass effect ; Humans ; Infusions, Intravenous ; Kinetics ; Male ; Medical sciences ; Miscellaneous ; Pharmacokinetics ; Pharmacology. 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Drug Dispos</addtitle><description>Eight normal male volunteers received 80 mg doses of propranolol by the oral and rectal routes and 2·2 mg by intravenous administration in a crossover fashion. Plasma concentrations of propranolol were measured by a gas chromatographic method using an electron capture detector. Individual subject concentration–time data were analysed and results indicated that the data fit a two compartment model with first order absorption. An approximately two‐fold higher plasma propranolol concentration was observed after rectal administration as compared with oral dosing. Statistical analysis of the difference in the total AUCs indicates a significantly higher bioavailability of propranolol administered by the rectal route. The reduced bioavailability after oral administration indicates a substantial first pass effect but that it is possible to bypass the liver, at least partially, by giving the drug rectally to man.</description><subject>Administration, Oral</subject><subject>Administration, Rectal</subject><subject>Adult</subject><subject>Bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Cardiovascular system</subject><subject>First pass effect</subject><subject>Humans</subject><subject>Infusions, Intravenous</subject><subject>Kinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Propranolol</subject><subject>Propranolol - administration & dosage</subject><subject>Propranolol - blood</subject><subject>Rectal absorption</subject><issn>0142-2782</issn><issn>1099-081X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFUEuPFCEYJEazzo5evZn0wXjaHqGBhj66sw-N6yNRozfyNdAJSsMIPbvOv5dxOmP25IkK9fgqhdAzglcE4-ZVb8yq4QUK3GL-AC0I7roaS_L9IVpgwpq6EbJ5jE5z_oExbgkhJ-iEykYyyRcofPKQR6h0DNqGKcHkYsgVBFP1LsItOA-9827aVXGoNiluEoToo6_68pPAn1XJ6gn8X4vbJ9zaELclwowuuDxHFqoaITxBjwbw2T6d3yX6enX5Zf2mvvl4_Xb9-qbWDAteW2aJoGzQXDYdx4LQQRohMWUCc9IK2RYwaKMFgwIM63trpLRMWqO55nSJXh5yS-NfW5snNbqsrfcQbCmnhGg62pTcJVodhDrFnJMd1Ca5EdJOEaz2A6sysPo3cDE8n5O3_WjNUT4vWvgXMw9Zgx_KXNrlo0wSwoTc3-0Osjvn7e4_R9X5xcW9CvXBW9a1v49eSD9VK6jg6tuHa_Ue88_n8t1aUfoHOlykCQ</recordid><startdate>198611</startdate><enddate>198611</enddate><creator>Cid, Edison</creator><creator>Mella, Fernando</creator><creator>Lucchini, Leonardo</creator><creator>Cárcamo, Martín</creator><creator>Monasterio, José</creator><general>John Wiley & Sons, Ltd</general><general>Wiley</general><scope>BSCLL</scope><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>7X8</scope></search><sort><creationdate>198611</creationdate><title>Plasma concentrations and bioavailability of propranolol by oral, rectal and intravenous administration in man</title><author>Cid, Edison ; Mella, Fernando ; Lucchini, Leonardo ; Cárcamo, Martín ; Monasterio, José</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4075-e4e1734fc582950713f8d7803470516786470fcdc74a70fd4bbed88e48edc5c53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>Administration, Oral</topic><topic>Administration, Rectal</topic><topic>Adult</topic><topic>Bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Cardiovascular system</topic><topic>First pass effect</topic><topic>Humans</topic><topic>Infusions, Intravenous</topic><topic>Kinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Miscellaneous</topic><topic>Pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Propranolol</topic><topic>Propranolol - administration & dosage</topic><topic>Propranolol - blood</topic><topic>Rectal absorption</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cid, Edison</creatorcontrib><creatorcontrib>Mella, Fernando</creatorcontrib><creatorcontrib>Lucchini, Leonardo</creatorcontrib><creatorcontrib>Cárcamo, Martín</creatorcontrib><creatorcontrib>Monasterio, José</creatorcontrib><collection>Istex</collection><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>Biopharmaceutics & drug disposition</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cid, Edison</au><au>Mella, Fernando</au><au>Lucchini, Leonardo</au><au>Cárcamo, Martín</au><au>Monasterio, José</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Plasma concentrations and bioavailability of propranolol by oral, rectal and intravenous administration in man</atitle><jtitle>Biopharmaceutics & drug disposition</jtitle><addtitle>Biopharm. Drug Dispos</addtitle><date>1986-11</date><risdate>1986</risdate><volume>7</volume><issue>6</issue><spage>559</spage><epage>566</epage><pages>559-566</pages><issn>0142-2782</issn><eissn>1099-081X</eissn><coden>BDDID8</coden><abstract>Eight normal male volunteers received 80 mg doses of propranolol by the oral and rectal routes and 2·2 mg by intravenous administration in a crossover fashion. Plasma concentrations of propranolol were measured by a gas chromatographic method using an electron capture detector. Individual subject concentration–time data were analysed and results indicated that the data fit a two compartment model with first order absorption. An approximately two‐fold higher plasma propranolol concentration was observed after rectal administration as compared with oral dosing. Statistical analysis of the difference in the total AUCs indicates a significantly higher bioavailability of propranolol administered by the rectal route. The reduced bioavailability after oral administration indicates a substantial first pass effect but that it is possible to bypass the liver, at least partially, by giving the drug rectally to man.</abstract><cop>New York</cop><pub>John Wiley & Sons, Ltd</pub><pmid>3828485</pmid><doi>10.1002/bdd.2510070605</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0142-2782 |
| ispartof | Biopharmaceutics & drug disposition, 1986-11, Vol.7 (6), p.559-566 |
| issn | 0142-2782 1099-081X |
| language | eng |
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| source | MEDLINE; Wiley Journals |
| subjects | Administration, Oral Administration, Rectal Adult Bioavailability Biological and medical sciences Biological Availability Cardiovascular system First pass effect Humans Infusions, Intravenous Kinetics Male Medical sciences Miscellaneous Pharmacokinetics Pharmacology. Drug treatments Propranolol Propranolol - administration & dosage Propranolol - blood Rectal absorption |
| title | Plasma concentrations and bioavailability of propranolol by oral, rectal and intravenous administration in man |
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