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Article: Plasma and biliary disposition of pirenzepine in man

TitlePlasma and biliary disposition of pirenzepine in man
Authors
Issue Date1986
PublisherBlackwell Publishing Asia. The Journal's web site is located at http://www.blackwellpublishing.com/journals/CEP
Citation
Clinical And Experimental Pharmacology And Physiology, 1986, v. 13 n. 3, p. 241-248 How to Cite?
AbstractThe binding of pirenzepine, a selective muscarinic receptor antagonist to plasma and bile, was studied in vitro and in vivo. Plasma and hepatic bile were incubated with 14C-pirenzepine and the bound fraction of 14C-pirenzepine determined by equilibrium dialysis. The bound fractions were 12.6% (s.e.m. = 1.5) and 12.1% (s.e.m. = 1.6) in plasma and bile samples, respectively. After an in vitro incubation, the radioactivity in both plasma and bile was removed by exhaustive dialysis against water for up to 94 h, suggesting that the binding was a noncovalent association. 14C-Pirenzepine was also given intravenously to five postoperative patients with T-tube drainage of hepatic bile. In plasma, 12.6% (s.e.m. = 1.8) of 14C-pirenzepine was reversibly bound to albumin. By contrast, in bile 13.4% (s.e.m. = 3.2) was irreversibly bound, mainly to bilirubin glucuronides (>90%). After an intravenous injection of 14C-pirenzepine, the radioactivity in plasma decreased bi-exponentially with an initial distribution half-life of 0.24 h and an elimination half-life of 10.2 h. The radioactivity reappeared cyclically in bile, suggesting enterohepatic recirculation of 14C-pirenzepine.
Persistent Identifierhttp://hdl.handle.net/10722/175643
ISSN
2012 Impact Factor: 2.16
2015 SCImago Journal Rankings: 0.944
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorLee, SPen_US
dc.contributor.authorPaxton, JWen_US
dc.contributor.authorChoong, YSen_US
dc.date.accessioned2012-11-26T09:00:14Z-
dc.date.available2012-11-26T09:00:14Z-
dc.date.issued1986en_US
dc.identifier.citationClinical And Experimental Pharmacology And Physiology, 1986, v. 13 n. 3, p. 241-248en_US
dc.identifier.issn0305-1870en_US
dc.identifier.urihttp://hdl.handle.net/10722/175643-
dc.description.abstractThe binding of pirenzepine, a selective muscarinic receptor antagonist to plasma and bile, was studied in vitro and in vivo. Plasma and hepatic bile were incubated with 14C-pirenzepine and the bound fraction of 14C-pirenzepine determined by equilibrium dialysis. The bound fractions were 12.6% (s.e.m. = 1.5) and 12.1% (s.e.m. = 1.6) in plasma and bile samples, respectively. After an in vitro incubation, the radioactivity in both plasma and bile was removed by exhaustive dialysis against water for up to 94 h, suggesting that the binding was a noncovalent association. 14C-Pirenzepine was also given intravenously to five postoperative patients with T-tube drainage of hepatic bile. In plasma, 12.6% (s.e.m. = 1.8) of 14C-pirenzepine was reversibly bound to albumin. By contrast, in bile 13.4% (s.e.m. = 3.2) was irreversibly bound, mainly to bilirubin glucuronides (>90%). After an intravenous injection of 14C-pirenzepine, the radioactivity in plasma decreased bi-exponentially with an initial distribution half-life of 0.24 h and an elimination half-life of 10.2 h. The radioactivity reappeared cyclically in bile, suggesting enterohepatic recirculation of 14C-pirenzepine.en_US
dc.languageengen_US
dc.publisherBlackwell Publishing Asia. The Journal's web site is located at http://www.blackwellpublishing.com/journals/CEPen_US
dc.relation.ispartofClinical and Experimental Pharmacology and Physiologyen_US
dc.subject.meshAdulten_US
dc.subject.meshAgeden_US
dc.subject.meshBenzodiazepinones - Blood - Metabolismen_US
dc.subject.meshBile - Metabolismen_US
dc.subject.meshChromatographyen_US
dc.subject.meshElectrophoresis, Agar Gelen_US
dc.subject.meshEnterohepatic Circulationen_US
dc.subject.meshFemaleen_US
dc.subject.meshHalf-Lifeen_US
dc.subject.meshHumansen_US
dc.subject.meshImmunodiffusionen_US
dc.subject.meshMaleen_US
dc.subject.meshMiddle Ageden_US
dc.subject.meshPirenzepineen_US
dc.subject.meshProtein Bindingen_US
dc.titlePlasma and biliary disposition of pirenzepine in manen_US
dc.typeArticleen_US
dc.identifier.emailLee, SP: sumlee@hku.hken_US
dc.identifier.authorityLee, SP=rp01351en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1111/j.1440-1681.1986.tb00342.x-
dc.identifier.pmid3087665-
dc.identifier.scopuseid_2-s2.0-0022871753en_US
dc.identifier.volume13en_US
dc.identifier.issue3en_US
dc.identifier.spage241en_US
dc.identifier.epage248en_US
dc.identifier.isiWOS:A1986C624300008-
dc.publisher.placeAustraliaen_US
dc.identifier.scopusauthoridLee, SP=7601417497en_US
dc.identifier.scopusauthoridPaxton, JW=7005717521en_US
dc.identifier.scopusauthoridChoong, YS=36797593200en_US

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