Document Detail


Contribution of cytochrome P450 3A pathway to bromocriptine metabolism and effects of ferrous iron and hypoxia-re-oxygenation on its elimination in the perfused rat liver.
MedLine Citation:
PMID:  9178193     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The contribution of the cytochrome P450 3A pathway to bromocriptine metabolism, and the effects of ferrous iron and hypoxia-re-oxygenation on its elimination, were evaluated with the perfused rat liver. Outflow profiles of bromocriptine after bolus administration were estimated by moment analysis and dispersion model analysis. Kinetic parameters were not significantly changed by troleandomycin, a P450 3A inhibitor. The inhibition of bromocriptine metabolism by troleandomycin was 5.7 +/- 2.4%. These findings indicate that cytochrome P450 3A does not play an important role in bromocriptine elimination with the perfused rat liver. Elimination rate constant (ka) values were significantly increased by ferrous iron perfusion or hypoxia-re-oxygenation. Free-radical generation can, therefore, affect bromocriptine elimination. Our observations suggest that bromocriptine might be eliminated by scavenging of free radicals in the liver.
Authors:
K Matsubayashi; H Matsumoto; Y Fukui
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  49     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  1997 May 
Date Detail:
Created Date:  1997-09-02     Completed Date:  1997-09-02     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  551-7     Citation Subset:  IM    
Affiliation:
Department of Legal Medicine, Kyoto University Faculty of Medicine, Japan.
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MeSH Terms
Descriptor/Qualifier:
Amitrole / pharmacology
Animals
Aryl Hydrocarbon Hydroxylases*
Body Fluid Compartments
Bromocriptine / metabolism*,  pharmacokinetics
Cell Hypoxia
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System / antagonists & inhibitors,  metabolism*
Enzyme Inhibitors / pharmacology
Ferrous Compounds / pharmacology*
Liver / enzymology,  metabolism*
Male
Oxidation-Reduction
Oxidoreductases, N-Demethylating / antagonists & inhibitors,  metabolism*
Oxygen / metabolism,  pharmacology*
Perfusion
Rats
Rats, Wistar
Troleandomycin / pharmacology
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Ferrous Compounds; 25614-03-3/Bromocriptine; 2751-09-9/Troleandomycin; 61-82-5/Amitrole; 7782-44-7/Oxygen; 9035-51-2/Cytochrome P-450 Enzyme System; EC 1.14.14.1/Aryl Hydrocarbon Hydroxylases; EC 1.14.14.1/Cytochrome P-450 CYP3A; EC 1.5.-/Oxidoreductases, N-Demethylating

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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