Combined pharmacokinetic and pharmacodynamic studies on alprenolol and 4-hydroxy-alprenolol in man
The effects of orally (100 mg) and intravenously (10 mg) administered alprenolol on the heart rate of 4 exercising healthy volunteers were correlated with the plasma concentrations of alprenolol and its metabolite 4-OH-alprenolol. The metabolite was recovered in plasma after both routes of alprenolo...
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| Veröffentlicht in: | Life sciences (1973) 1974-02, Vol.14 (4), p.693-704 |
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| container_issue | 4 |
| container_start_page | 693 |
| container_title | Life sciences (1973) |
| container_volume | 14 |
| creator | Åblad, B. Borg, K.O. Johnsson, G. Regårdh, C-G. Sölvell, L. |
| description | The effects of orally (100 mg) and intravenously (10 mg) administered alprenolol on the heart rate of 4 exercising healthy volunteers were correlated with the plasma concentrations of alprenolol and its metabolite 4-OH-alprenolol. The metabolite was recovered in plasma after both routes of alprenolol administration and was eliminated from the body at the same rate as alprenolol (
t
1
2
≅ 3
h
). Infusion of 4-OH-alprenolol (10 mg) significantly reduced the heart rate during exercise. The results indicate that orally administered alprenolol forms the active metabolite 4-OH-alprenolol in sufficiently large amounts to significantly influence the effect of the parent drug. The “first pass” elimination of the oral alprenolol dose was about 90 per cent. |
| doi_str_mv | 10.1016/0024-3205(74)90452-4 |
| format | Article |
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t
1
2
≅ 3
h
). Infusion of 4-OH-alprenolol (10 mg) significantly reduced the heart rate during exercise. The results indicate that orally administered alprenolol forms the active metabolite 4-OH-alprenolol in sufficiently large amounts to significantly influence the effect of the parent drug. The “first pass” elimination of the oral alprenolol dose was about 90 per cent.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/0024-3205(74)90452-4</identifier><identifier>PMID: 4823626</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>Administration, Oral ; Alprenolol - administration & dosage ; Alprenolol - blood ; Alprenolol - pharmacology ; Dose-Response Relationship, Drug ; Half-Life ; Heart Rate - drug effects ; Humans ; Hydroxylation ; Injections, Intravenous ; Physical Exertion - drug effects ; Regression Analysis ; Structure-Activity Relationship ; Time Factors</subject><ispartof>Life sciences (1973), 1974-02, Vol.14 (4), p.693-704</ispartof><rights>1974</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c357t-2fafb06f67f2c543a1ceb2ea7e2164502401f4eb5c8775742332f0ac8936d14f3</citedby><cites>FETCH-LOGICAL-c357t-2fafb06f67f2c543a1ceb2ea7e2164502401f4eb5c8775742332f0ac8936d14f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0024-3205(74)90452-4$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4823626$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Åblad, B.</creatorcontrib><creatorcontrib>Borg, K.O.</creatorcontrib><creatorcontrib>Johnsson, G.</creatorcontrib><creatorcontrib>Regårdh, C-G.</creatorcontrib><creatorcontrib>Sölvell, L.</creatorcontrib><title>Combined pharmacokinetic and pharmacodynamic studies on alprenolol and 4-hydroxy-alprenolol in man</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>The effects of orally (100 mg) and intravenously (10 mg) administered alprenolol on the heart rate of 4 exercising healthy volunteers were correlated with the plasma concentrations of alprenolol and its metabolite 4-OH-alprenolol. The metabolite was recovered in plasma after both routes of alprenolol administration and was eliminated from the body at the same rate as alprenolol (
t
1
2
≅ 3
h
). Infusion of 4-OH-alprenolol (10 mg) significantly reduced the heart rate during exercise. The results indicate that orally administered alprenolol forms the active metabolite 4-OH-alprenolol in sufficiently large amounts to significantly influence the effect of the parent drug. The “first pass” elimination of the oral alprenolol dose was about 90 per cent.</description><subject>Administration, Oral</subject><subject>Alprenolol - administration & dosage</subject><subject>Alprenolol - blood</subject><subject>Alprenolol - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Half-Life</subject><subject>Heart Rate - drug effects</subject><subject>Humans</subject><subject>Hydroxylation</subject><subject>Injections, Intravenous</subject><subject>Physical Exertion - drug effects</subject><subject>Regression Analysis</subject><subject>Structure-Activity Relationship</subject><subject>Time Factors</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1974</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtLxDAUhYMo4zj6DxS6El1U82w6G0EGXzDgRtchTW-YaJuMSUfsv7fzQF25CrnnnHs5H0KnBF8RTIprjCnPGcXiQvLLKeaC5nwPjUkppzkuGNlH4x_LITpK6Q1jLIRkIzTiJWUFLcaomoW2ch7qbLnQsdUmvA-_zplM-99Z3XvdDrPUrWoHKQs-080ygg9NaDZOni_6OoavPv8jOJ-12h-jA6ubBCe7d4Je7-9eZo_5_PnhaXY7zw0Tssup1bbChS2kpUZwpomBioKWQEnBxdAEE8uhEqaUUkhOGaMWa1NOWVETbtkEnW_3LmP4WEHqVOuSgabRHsIqqaFyKcSQmyC-NZoYUopg1TK6VsdeEazWaNWam1pzU5KrDVrFh9jZbv-qaqH-Ce1YDvrNVoeh5KeDqJJx4A3ULoLpVB3c_we-AcdciOo</recordid><startdate>19740216</startdate><enddate>19740216</enddate><creator>Åblad, B.</creator><creator>Borg, K.O.</creator><creator>Johnsson, G.</creator><creator>Regårdh, C-G.</creator><creator>Sölvell, L.</creator><general>Elsevier Inc</general><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>19740216</creationdate><title>Combined pharmacokinetic and pharmacodynamic studies on alprenolol and 4-hydroxy-alprenolol in man</title><author>Åblad, B. ; Borg, K.O. ; Johnsson, G. ; Regårdh, C-G. ; Sölvell, L.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-2fafb06f67f2c543a1ceb2ea7e2164502401f4eb5c8775742332f0ac8936d14f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1974</creationdate><topic>Administration, Oral</topic><topic>Alprenolol - administration & dosage</topic><topic>Alprenolol - blood</topic><topic>Alprenolol - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>Half-Life</topic><topic>Heart Rate - drug effects</topic><topic>Humans</topic><topic>Hydroxylation</topic><topic>Injections, Intravenous</topic><topic>Physical Exertion - drug effects</topic><topic>Regression Analysis</topic><topic>Structure-Activity Relationship</topic><topic>Time Factors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Åblad, B.</creatorcontrib><creatorcontrib>Borg, K.O.</creatorcontrib><creatorcontrib>Johnsson, G.</creatorcontrib><creatorcontrib>Regårdh, C-G.</creatorcontrib><creatorcontrib>Sölvell, L.</creatorcontrib><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>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Åblad, B.</au><au>Borg, K.O.</au><au>Johnsson, G.</au><au>Regårdh, C-G.</au><au>Sölvell, L.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Combined pharmacokinetic and pharmacodynamic studies on alprenolol and 4-hydroxy-alprenolol in man</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>1974-02-16</date><risdate>1974</risdate><volume>14</volume><issue>4</issue><spage>693</spage><epage>704</epage><pages>693-704</pages><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>The effects of orally (100 mg) and intravenously (10 mg) administered alprenolol on the heart rate of 4 exercising healthy volunteers were correlated with the plasma concentrations of alprenolol and its metabolite 4-OH-alprenolol. The metabolite was recovered in plasma after both routes of alprenolol administration and was eliminated from the body at the same rate as alprenolol (
t
1
2
≅ 3
h
). Infusion of 4-OH-alprenolol (10 mg) significantly reduced the heart rate during exercise. The results indicate that orally administered alprenolol forms the active metabolite 4-OH-alprenolol in sufficiently large amounts to significantly influence the effect of the parent drug. The “first pass” elimination of the oral alprenolol dose was about 90 per cent.</abstract><cop>Netherlands</cop><pub>Elsevier Inc</pub><pmid>4823626</pmid><doi>10.1016/0024-3205(74)90452-4</doi><tpages>12</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0024-3205 |
| ispartof | Life sciences (1973), 1974-02, Vol.14 (4), p.693-704 |
| issn | 0024-3205 1879-0631 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_82385542 |
| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Administration, Oral Alprenolol - administration & dosage Alprenolol - blood Alprenolol - pharmacology Dose-Response Relationship, Drug Half-Life Heart Rate - drug effects Humans Hydroxylation Injections, Intravenous Physical Exertion - drug effects Regression Analysis Structure-Activity Relationship Time Factors |
| title | Combined pharmacokinetic and pharmacodynamic studies on alprenolol and 4-hydroxy-alprenolol in man |
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