Document Detail

Biliary excretion of azelnidipine, a calcium antagonist, in rats.
MedLine Citation:
PMID:  15012778     Owner:  NLM     Status:  MEDLINE    
BACKGROUND AND AIMS: Azelnidipine (CS-905) is a novel dihydropyridine calcium antagonist that is known to be excreted in feces. To examine the mechanism of biliary excretion of azelnidipine, the authors studied its biliary excretion in Eisai hyperbilirubinuria rats (EHBR), multidrug resistance protein (Mrp)2-deficient rats, and the effect of cholephilic compounds on the biliary excretion of azelnidipine in rats. METHODS: Radiolabeled azelnidipine was intravenously administered to EHBR and control rats, and the biliary excretion of radiolabeled metabolites was studied. Furthermore, the effect of sulfobromophthalein, taurocholate and vinblastine on the biliary excretion of azelnidipine metabolites was also studied in control rats. RESULTS: The biliary excretion of azelnidipine metabolites was delayed in EHBR. The biliary excretion of azelnidipine metabolites was inhibited by sulfobromophthalein and vinblastine, but was not inhibited by taurocholate or phenothiazine pretreatment. CONCLUSION: These findings suggest that the metabolites of azelnidipine are excreted into the bile partly by Mrp2 and P-glycoprotein.
Naoko Hanawa; Naoyo Sano; Hajime Takikawa
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of gastroenterology and hepatology     Volume:  19     ISSN:  0815-9319     ISO Abbreviation:  J. Gastroenterol. Hepatol.     Publication Date:  2004 Apr 
Date Detail:
Created Date:  2004-03-11     Completed Date:  2004-06-24     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  8607909     Medline TA:  J Gastroenterol Hepatol     Country:  Australia    
Other Details:
Languages:  eng     Pagination:  413-7     Citation Subset:  IM    
Department of Medicine, Teikyo University School of Medicine, Tokyo, Japan.
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MeSH Terms
Azetidinecarboxylic Acid / analogs & derivatives*,  antagonists & inhibitors,  metabolism*
Bile / metabolism*
Calcium Channel Blockers / metabolism*
Cholagogues and Choleretics / pharmacology
Dihydropyridines / antagonists & inhibitors,  metabolism*
Hyperbilirubinemia / metabolism*
Membrane Transport Proteins / deficiency*
Multidrug Resistance-Associated Proteins / deficiency*
Rats, Sprague-Dawley
Sulfobromophthalein / pharmacology
Taurocholic Acid / pharmacology
Vinblastine / pharmacology
Reg. No./Substance:
0/Calcium Channel Blockers; 0/Cholagogues and Choleretics; 0/Dihydropyridines; 0/Membrane Transport Proteins; 0/Multidrug Resistance-Associated Proteins; 0/multidrug resistance-associated protein 2; 123524-52-7/azelnidipine; 2517-04-6/Azetidinecarboxylic Acid; 297-83-6/Sulfobromophthalein; 81-24-3/Taurocholic Acid; 865-21-4/Vinblastine

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