Document Detail


Metabolism of nomifensine after oral and intravenous administration.
MedLine Citation:
PMID:  3956054     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
R L Lindberg; E K Syvälahti
Related Documents :
7131264 - Species differences in the urinary excretion of the novel primary amine conjugate: toca...
6102854 - Methoxyethylmercury nephrotoxicity: effects on enzymuria and kidney function.
157364 - Metabolism of crufomate (4-tert-butyl-2-chlorophenyl methyl methylphosphoramidate) admi...
1971984 - The metabolic fate of the dopamine agonist 2-(n-propyl-n-2-thienylethylamino)-5-hydroxy...
2340984 - L-methionine suppresses pathological sequelae of cis-platinum in the rat.
3936304 - Organochlorine pesticides and polychlorinated biphenyls in sprats from the southern bal...
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Clinical pharmacology and therapeutics     Volume:  39     ISSN:  0009-9236     ISO Abbreviation:  Clin. Pharmacol. Ther.     Publication Date:  1986 Apr 
Date Detail:
Created Date:  1986-05-13     Completed Date:  1986-05-13     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0372741     Medline TA:  Clin Pharmacol Ther     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  378-83     Citation Subset:  AIM; IM    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
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:
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


Previous Document:  Amitriptyline metabolism: association with debrisoquin hydroxylation in nonsmokers.
Next Document:  Disposition of nomifensine after acute and prolonged dosing.