Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse
Horse urine was investigated for metabolites by chromatography and mass spectrometry following the oral administration of the large animal analgesic sedative detomidine to two stallions and intravenous administration of [3H]-detomidine to a mare. Detomidine carboxylic acid and hydroxydetomidine gluc...
Gespeichert in:
| Veröffentlicht in: | European journal of drug metabolism and pharmacokinetics 1992, Vol.17 (1), p.13-20 |
|---|---|
| Hauptverfasser: | , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 20 |
|---|---|
| container_issue | 1 |
| container_start_page | 13 |
| container_title | European journal of drug metabolism and pharmacokinetics |
| container_volume | 17 |
| creator | SALONEN, J. S VUORILEHTO, L GILBERT, M MAYLIN, G. A |
| description | Horse urine was investigated for metabolites by chromatography and mass spectrometry following the oral administration of the large animal analgesic sedative detomidine to two stallions and intravenous administration of [3H]-detomidine to a mare. Detomidine carboxylic acid and hydroxydetomidine glucuronic acid conjugate were identified in the urine after the oral doses. In addition, traces of free hydroxydetomidine were observed. About half of the radioactivity of [3H]-detomidine was excreted in the urine in 12 h after the i.v. dose (80 micrograms/kg). Most of the excretion occurred between 5 and 12 h in contrast to urine output which was highest 2-5 h after the dosing. The major radioactive metabolite in the urine was detomidine carboxylic acid. It comprised more than two thirds of the total metabolites in all the urine fractions collected. Its excretion profile was similar to that of total radioactivity. Hydroxydetomidine glucuronide was also excreted. It contributed 10-20% of the total metabolites in the urine. The free aglycone was only seen in the samples collected during the peak urine flow. A minor metabolite was tentatively characterized as the glucuronide of N-hydroxydetomidine. |
| doi_str_mv | 10.1007/BF03189982 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_73118219</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>73118219</sourcerecordid><originalsourceid>FETCH-LOGICAL-c311t-e5fa86616d1d3918232b5bf870c68e50b22ee717824fa5dcd1f2b004681825613</originalsourceid><addsrcrecordid>eNpdkEtLAzEUhYMoWtSNeyELcSGM5tG8lio-CgU3uh4yyY1NmZnUZAr67x1tseDd3MX57rmcg9AZJdeUEHVz90g41cZotocmjBJVEarJPpoQrnSljJRH6LSUJRmHayOEPESHdGqMMHyC3mce-iGG6OwQU49TwB6G1EUfe8DO5iZ9frXRYeuix7bgYQG4s8uU8TrH3uYv3MFgm9TGAf5dx_6XXqRc4AQdBNsWON3uY_T2-PB6_1zNX55m97fzynFKhwpEsFpKKj313FDNOGtEE7QiTmoQpGEMQFGl2TRY4Z2ngTWETKUeWSEpP0aXG99VTh9rKEPdxeKgbW0PaV1qNb7RjJoRvNqALqdSMoR6lWM35qkpqX-KrXfFjvD51nXddOB36KbGUb_Y6rY424ZsexfLHya4MEZp_g2MVH88</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>73118219</pqid></control><display><type>article</type><title>Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse</title><source>MEDLINE</source><source>SpringerLink Journals</source><creator>SALONEN, J. S ; VUORILEHTO, L ; GILBERT, M ; MAYLIN, G. A</creator><creatorcontrib>SALONEN, J. S ; VUORILEHTO, L ; GILBERT, M ; MAYLIN, G. A</creatorcontrib><description>Horse urine was investigated for metabolites by chromatography and mass spectrometry following the oral administration of the large animal analgesic sedative detomidine to two stallions and intravenous administration of [3H]-detomidine to a mare. Detomidine carboxylic acid and hydroxydetomidine glucuronic acid conjugate were identified in the urine after the oral doses. In addition, traces of free hydroxydetomidine were observed. About half of the radioactivity of [3H]-detomidine was excreted in the urine in 12 h after the i.v. dose (80 micrograms/kg). Most of the excretion occurred between 5 and 12 h in contrast to urine output which was highest 2-5 h after the dosing. The major radioactive metabolite in the urine was detomidine carboxylic acid. It comprised more than two thirds of the total metabolites in all the urine fractions collected. Its excretion profile was similar to that of total radioactivity. Hydroxydetomidine glucuronide was also excreted. It contributed 10-20% of the total metabolites in the urine. The free aglycone was only seen in the samples collected during the peak urine flow. A minor metabolite was tentatively characterized as the glucuronide of N-hydroxydetomidine.</description><identifier>ISSN: 0378-7966</identifier><identifier>EISSN: 2107-0180</identifier><identifier>DOI: 10.1007/BF03189982</identifier><identifier>PMID: 1499593</identifier><language>eng</language><publisher>Genève: Médecine et hygiène</publisher><subject>Analgesics - pharmacokinetics ; Analgesics - urine ; Animals ; Biological and medical sciences ; Biotransformation ; Chromatography, Liquid ; Female ; Horses - urine ; Hypnotics and Sedatives - pharmacokinetics ; Hypnotics and Sedatives - urine ; Hypnotics. Sedatives ; Imidazoles - pharmacokinetics ; Imidazoles - urine ; Male ; Mass Spectrometry ; Medical sciences ; Neuropharmacology ; Pharmacology. Drug treatments ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Tritium</subject><ispartof>European journal of drug metabolism and pharmacokinetics, 1992, Vol.17 (1), p.13-20</ispartof><rights>1992 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c311t-e5fa86616d1d3918232b5bf870c68e50b22ee717824fa5dcd1f2b004681825613</citedby><cites>FETCH-LOGICAL-c311t-e5fa86616d1d3918232b5bf870c68e50b22ee717824fa5dcd1f2b004681825613</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,4010,27900,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=5359978$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1499593$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>SALONEN, J. S</creatorcontrib><creatorcontrib>VUORILEHTO, L</creatorcontrib><creatorcontrib>GILBERT, M</creatorcontrib><creatorcontrib>MAYLIN, G. A</creatorcontrib><title>Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse</title><title>European journal of drug metabolism and pharmacokinetics</title><addtitle>Eur J Drug Metab Pharmacokinet</addtitle><description>Horse urine was investigated for metabolites by chromatography and mass spectrometry following the oral administration of the large animal analgesic sedative detomidine to two stallions and intravenous administration of [3H]-detomidine to a mare. Detomidine carboxylic acid and hydroxydetomidine glucuronic acid conjugate were identified in the urine after the oral doses. In addition, traces of free hydroxydetomidine were observed. About half of the radioactivity of [3H]-detomidine was excreted in the urine in 12 h after the i.v. dose (80 micrograms/kg). Most of the excretion occurred between 5 and 12 h in contrast to urine output which was highest 2-5 h after the dosing. The major radioactive metabolite in the urine was detomidine carboxylic acid. It comprised more than two thirds of the total metabolites in all the urine fractions collected. Its excretion profile was similar to that of total radioactivity. Hydroxydetomidine glucuronide was also excreted. It contributed 10-20% of the total metabolites in the urine. The free aglycone was only seen in the samples collected during the peak urine flow. A minor metabolite was tentatively characterized as the glucuronide of N-hydroxydetomidine.</description><subject>Analgesics - pharmacokinetics</subject><subject>Analgesics - urine</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Biotransformation</subject><subject>Chromatography, Liquid</subject><subject>Female</subject><subject>Horses - urine</subject><subject>Hypnotics and Sedatives - pharmacokinetics</subject><subject>Hypnotics and Sedatives - urine</subject><subject>Hypnotics. Sedatives</subject><subject>Imidazoles - pharmacokinetics</subject><subject>Imidazoles - urine</subject><subject>Male</subject><subject>Mass Spectrometry</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Tritium</subject><issn>0378-7966</issn><issn>2107-0180</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkEtLAzEUhYMoWtSNeyELcSGM5tG8lio-CgU3uh4yyY1NmZnUZAr67x1tseDd3MX57rmcg9AZJdeUEHVz90g41cZotocmjBJVEarJPpoQrnSljJRH6LSUJRmHayOEPESHdGqMMHyC3mce-iGG6OwQU49TwB6G1EUfe8DO5iZ9frXRYeuix7bgYQG4s8uU8TrH3uYv3MFgm9TGAf5dx_6XXqRc4AQdBNsWON3uY_T2-PB6_1zNX55m97fzynFKhwpEsFpKKj313FDNOGtEE7QiTmoQpGEMQFGl2TRY4Z2ngTWETKUeWSEpP0aXG99VTh9rKEPdxeKgbW0PaV1qNb7RjJoRvNqALqdSMoR6lWM35qkpqX-KrXfFjvD51nXddOB36KbGUb_Y6rY424ZsexfLHya4MEZp_g2MVH88</recordid><startdate>1992</startdate><enddate>1992</enddate><creator>SALONEN, J. S</creator><creator>VUORILEHTO, L</creator><creator>GILBERT, M</creator><creator>MAYLIN, G. A</creator><general>Médecine et hygiène</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>7X8</scope></search><sort><creationdate>1992</creationdate><title>Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse</title><author>SALONEN, J. S ; VUORILEHTO, L ; GILBERT, M ; MAYLIN, G. A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c311t-e5fa86616d1d3918232b5bf870c68e50b22ee717824fa5dcd1f2b004681825613</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>Analgesics - pharmacokinetics</topic><topic>Analgesics - urine</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Biotransformation</topic><topic>Chromatography, Liquid</topic><topic>Female</topic><topic>Horses - urine</topic><topic>Hypnotics and Sedatives - pharmacokinetics</topic><topic>Hypnotics and Sedatives - urine</topic><topic>Hypnotics. Sedatives</topic><topic>Imidazoles - pharmacokinetics</topic><topic>Imidazoles - urine</topic><topic>Male</topic><topic>Mass Spectrometry</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Tritium</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SALONEN, J. S</creatorcontrib><creatorcontrib>VUORILEHTO, L</creatorcontrib><creatorcontrib>GILBERT, M</creatorcontrib><creatorcontrib>MAYLIN, G. A</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 drug metabolism and pharmacokinetics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SALONEN, J. S</au><au>VUORILEHTO, L</au><au>GILBERT, M</au><au>MAYLIN, G. A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse</atitle><jtitle>European journal of drug metabolism and pharmacokinetics</jtitle><addtitle>Eur J Drug Metab Pharmacokinet</addtitle><date>1992</date><risdate>1992</risdate><volume>17</volume><issue>1</issue><spage>13</spage><epage>20</epage><pages>13-20</pages><issn>0378-7966</issn><eissn>2107-0180</eissn><abstract>Horse urine was investigated for metabolites by chromatography and mass spectrometry following the oral administration of the large animal analgesic sedative detomidine to two stallions and intravenous administration of [3H]-detomidine to a mare. Detomidine carboxylic acid and hydroxydetomidine glucuronic acid conjugate were identified in the urine after the oral doses. In addition, traces of free hydroxydetomidine were observed. About half of the radioactivity of [3H]-detomidine was excreted in the urine in 12 h after the i.v. dose (80 micrograms/kg). Most of the excretion occurred between 5 and 12 h in contrast to urine output which was highest 2-5 h after the dosing. The major radioactive metabolite in the urine was detomidine carboxylic acid. It comprised more than two thirds of the total metabolites in all the urine fractions collected. Its excretion profile was similar to that of total radioactivity. Hydroxydetomidine glucuronide was also excreted. It contributed 10-20% of the total metabolites in the urine. The free aglycone was only seen in the samples collected during the peak urine flow. A minor metabolite was tentatively characterized as the glucuronide of N-hydroxydetomidine.</abstract><cop>Genève</cop><pub>Médecine et hygiène</pub><pmid>1499593</pmid><doi>10.1007/BF03189982</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0378-7966 |
| ispartof | European journal of drug metabolism and pharmacokinetics, 1992, Vol.17 (1), p.13-20 |
| issn | 0378-7966 2107-0180 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_73118219 |
| source | MEDLINE; SpringerLink Journals |
| subjects | Analgesics - pharmacokinetics Analgesics - urine Animals Biological and medical sciences Biotransformation Chromatography, Liquid Female Horses - urine Hypnotics and Sedatives - pharmacokinetics Hypnotics and Sedatives - urine Hypnotics. Sedatives Imidazoles - pharmacokinetics Imidazoles - urine Male Mass Spectrometry Medical sciences Neuropharmacology Pharmacology. Drug treatments Psychology. Psychoanalysis. Psychiatry Psychopharmacology Tritium |
| title | Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-07T07%3A01%3A47IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Identification%20of%20detomidine%20carboxylic%20acid%20as%20the%20major%20urinary%20metabolite%20of%20detomidine%20in%20the%20horse&rft.jtitle=European%20journal%20of%20drug%20metabolism%20and%20pharmacokinetics&rft.au=SALONEN,%20J.%20S&rft.date=1992&rft.volume=17&rft.issue=1&rft.spage=13&rft.epage=20&rft.pages=13-20&rft.issn=0378-7966&rft.eissn=2107-0180&rft_id=info:doi/10.1007/BF03189982&rft_dat=%3Cproquest_cross%3E73118219%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=73118219&rft_id=info:pmid/1499593&rfr_iscdi=true |