Identification and human pharmacokinetics of dihydroergotoxine metabolites in man: Preliminary results

dc.creatorBicalho, B
dc.creatorGiolo, JM
dc.creatorLilla, S
dc.creatorDe Nucci, G
dc.date2008
dc.dateJAN
dc.date2014-11-14T23:20:36Z
dc.date2015-11-26T16:08:51Z
dc.date2014-11-14T23:20:36Z
dc.date2015-11-26T16:08:51Z
dc.date.accessioned2018-03-28T22:57:26Z
dc.date.available2018-03-28T22:57:26Z
dc.identifierBiopharmaceutics & Drug Disposition. John Wiley & Sons Ltd, v. 29, n. 1, n. 17, n. 28, 2008.
dc.identifier0142-2782
dc.identifierWOS:000253332800003
dc.identifier10.1002/bdd.585
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/69117
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/69117
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/69117
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1266470
dc.descriptionDihydroergotoxine is a mixture of semi-synthetic ergot alkaloids mainly used for age-related cognitive impairment. In this study, dihydroergotoxine (30 mu M) was added to incubates of rat and bovine liver microsomes, and the resulting major metabolites were identified as hydroxydihydroergocornine, hydroxy-dihydroergocryptine and hydroxy-dihydroergocristine on the basis of molecular mass measurements, determined with a time-of-flight mass spectrometer. The relevance of these to humans was then investigated by simultaneously monitoring dihydroergotoxine and its hydroxy-metabolites in human plasma by LC-MS/MS after oral dosing of dihydroergotoxine mesylate (27 mg) to a healthy volunteer (male, age 45, height 1.93 m, weight 103 kg). In this preliminary approach, the peaks (C-max) of dihydroergocornine, dihydroergocryptine and dihydroergocristine were about 0.04 mu g/l. The peaks (C-max) of their hydroxy-metabolites were 0.98, 0.53 and 0.30 mu g/l, respectively. In conclusion, in this preliminary approach it was found that hydroxy-dihydroergocornine, hydroxydihydroergocryptine and hydroxy-dihydroergocristine were one order of magnitude higher in concentration than their parents in human plasma. Copyright (C) 2007 John Wiley & Sons, Ltd.
dc.description29
dc.description1
dc.description17
dc.description28
dc.languageen
dc.publisherJohn Wiley & Sons Ltd
dc.publisherChichester
dc.publisherInglaterra
dc.relationBiopharmaceutics & Drug Disposition
dc.relationBiopharm. Drug Dispos.
dc.rightsfechado
dc.rightshttp://olabout.wiley.com/WileyCDA/Section/id-406071.html
dc.sourceWeb of Science
dc.subjectdihydroergotoxine
dc.subjectcodergocrine
dc.subjectOH-dihydroergocornine
dc.subjectOH-dihydroergocryptine
dc.subjectOH-dihydroergocristine
dc.subjectAlpha-dihydroergocryptine
dc.subjectMajor Metabolite
dc.subjectHuman Plasma
dc.subjectBromocriptine
dc.subjectRat
dc.subjectCytochrome-p450
dc.subjectBioavailability
dc.subjectBioequivalence
dc.subjectFormulation
dc.titleIdentification and human pharmacokinetics of dihydroergotoxine metabolites in man: Preliminary results
dc.typeArtículos de revistas


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