Metabolism of 36Cl-ornidazole after oral application to the male rat in relation to its antifertility activity.

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  • Author(s): Jones AR;Jones AR; Cooper TG
  • Source:
    Xenobiotica; the fate of foreign compounds in biological systems [Xenobiotica] 1997 Jul; Vol. 27 (7), pp. 711-21.
  • Publication Type:
    Journal Article; Research Support, Non-U.S. Gov't
  • Language:
    English
  • Additional Information
    • Source:
      Publisher: Informa Healthcare Country of Publication: England NLM ID: 1306665 Publication Model: Print Cited Medium: Print ISSN: 0049-8254 (Print) Linking ISSN: 00498254 NLM ISO Abbreviation: Xenobiotica Subsets: MEDLINE
    • Publication Information:
      Publication: London : Informa Healthcare
      Original Publication: London, Taylor & Francis.
    • Subject Terms:
      Contraceptive Agents, Male/*metabolism ; Kidney/*metabolism ; Ornidazole/*metabolism; Administration, Oral ; Animals ; Diuresis/drug effects ; Glycosuria/chemically induced ; Male ; Rats ; Rats, Sprague-Dawley ; Tissue Distribution
    • Abstract:
      1. The antimycotic ornidazole (a male antifertility agent in rats) was synthesized incorporating 36Cl in the chloropropyl sidechain and its metabolism was investigated in the male rat after oral ingestion. 2. Blood levels of radioactivity were low over the first 24 h and there was no tissue accumulation of radioactivity over 48 h. 3. Most of the excreted radioactivity (20% of the ingested dose) appeared in the urine within the first 24 h. 4. Three major compounds were detected in 0-24-h urine samples and were characterized as ornidazole (13% of total radioactivity), Cl- (22%) and 3-chlorolactate (30%), the oxidation product of 3-chlorolactaldehyde. 5. No polyuria or glucosuria was observed following the oral administration of ornidazole, suggesting that any (R)-3-chlorolactate produced was insufficient to affect renal metabolism. 6. Conversion of ornidazole initially to (R, S)-alpha-chlorohydrin or ultimately to the glycolytic inhibitor (S)-3-chlorolactaldehyde could explain its antifertility action in the male rat.
    • Accession Number:
      0 (Contraceptive Agents, Male)
      62XCK0G93T (Ornidazole)
    • Publication Date:
      Date Created: 19970701 Date Completed: 19970918 Latest Revision: 20190909
    • Publication Date:
      20221213
    • Accession Number:
      10.1080/004982597240299
    • Accession Number:
      9253147