| Metabolism of nomifensine after oral and intravenous administration. | |
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MedLine Citation:
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PMID: 3956054 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The metabolism of nomifensine was studied after single oral and intravenous administration and after 2 weeks of oral dosing. The three principal metabolites reached maximum plasma concentrations rapidly (in 1 to 1.5 hours) after nomifensine administration. Less than 10% was detected as a free, unconjugated form. All three metabolites were eliminated rapidly (elimination t1/2 values between 6.8 and 9.0 hours). Only very low concentrations of free metabolites were found in plasma after 24 hours of nomifensine administration. AUC values for free metabolites were between 0.27 to 0.46 hr X mumol/L after all nomifensine schedules. Two weeks of dosing had no significant influence on the elimination t1/2 or AUC values of the metabolites, indicating no change in the hydroxylation and methylation reactions. In addition, there were no changes in the conjugation reactions during prolonged nomifensine dosing. Nomifensine has a very short t1/2 and no tendency for accumulation after repeated doses. We conclude that nomifensine's clinical pharmacokinetic profile is not significantly changed by the kinetic behavior of its three main metabolites after the usual maintenance doses. |
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Authors:
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R L Lindberg; E K Syvälahti |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Clinical pharmacology and therapeutics Volume: 39 ISSN: 0009-9236 ISO Abbreviation: Clin. Pharmacol. Ther. Publication Date: 1986 Apr |
Date Detail:
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Created Date: 1986-05-13 Completed Date: 1986-05-13 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 0372741 Medline TA: Clin Pharmacol Ther Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 378-83 Citation Subset: AIM; IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Adult Biotransformation Chromatography, High Pressure Liquid Female Half-Life Humans Injections, Intravenous Kinetics Male Nomifensine / administration & dosage, analogs & derivatives, blood, metabolism*, urine |
| Chemical | |
Reg. No./Substance:
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24526-64-5/Nomifensine; 55774-26-0/4'-hydroxynomifensine; 60520-18-5/3'-hydroxy-4'-methoxynomifensine; 62080-80-2/4'-hydroxy-3'-methoxynomifensine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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