title: Biliary excretion of olmesartan, an anigotensin II receptor antagonist, in the rat.
abstract: OBJECTIVE
  Olmesartan (RNH-6270) is a newly developed anigotensin II receptor antagonist, and has been reported to be excreted into feces. To examine the mechanism of the biliary excretion of olmesartan, we studied its biliary excretion in rats.
  
  
  METHODS
  The biliary excretion of olmesartan in Eisai hyperbilirubinemic rats (EHBR), a multidrug resistance protein 2-deficient rat, was compared with control rats, and the effect of organic anions and cation and bile acids on the biliary excretion of olmesartan was studied in control rats.
  
  
  RESULTS
  The biliary excretion of olmesartan was markedly delayed in EHBR. The biliary excretion of olmesartan was inhibited by sulfobromophthalein, cefpiramide and pravastatin, but was not inhibited by taurocholate or tauroursodeoxycholate. Vinblastine inhibited and phenothiazine treatment increased the biliary excretion of olmesartan.
  
  
  CONCLUSIONS
  These findings suggest that olmesartan is excreted into the bile mainly by multidrug resistance protein 2 and partly by P-glycoprotein.
authors.affiliation: Department of Medicine, Teikyo University School of Medicine, Tokyo, Japan.
authors.forename: Motoe
authors.initials: M
authors.lastname: Takayanagi
authors.forename: Naoyo
authors.initials: N
authors.lastname: Sano
authors.forename: Hajime
authors.initials: H
authors.lastname: Takikawa
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000502:physiology; D047228:Angiotensin II Type 1 Receptor Blockers / Q000493:pharmacokinetics*; D000818:Animals; D002511:Cephalosporins / Q000494:pharmacology; D003135:Common Bile Duct / Q000187:drug effects / Q000378:metabolism*; D007093:Imidazoles / Q000493:pharmacokinetics*; D008297:Male; D000068557:Olmesartan Medoxomil; D010640:Phenothiazines / Q000494:pharmacology; D017035:Pravastatin / Q000494:pharmacology; D051381:Rats; D011922:Rats, Mutant Strains; D017207:Rats, Sprague-Dawley; D013448:Sulfobromophthalein / Q000494:pharmacology; D013655:Taurochenodeoxycholic Acid / Q000494:pharmacology; D013656:Taurocholic Acid / Q000494:pharmacology; D013777:Tetrazoles / Q000493:pharmacokinetics*; D014747:Vinblastine / Q000494:pharmacology
chemical_list: D018528:ATP-Binding Cassette Transporters; C423013:Abcc2 protein, rat; D047228:Angiotensin II Type 1 Receptor Blockers; D002511:Cephalosporins; D007093:Imidazoles; D010640:Phenothiazines; D013777:Tetrazoles; D013448:Sulfobromophthalein; D013655:Taurochenodeoxycholic Acid; D013656:Taurocholic Acid; D014747:Vinblastine; C031655:ursodoxicoltaurine; D000068557:Olmesartan Medoxomil; C031637:phenothiazine; D017035:Pravastatin; C036666:cefpiramide