Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2003-12-3
pubmed:abstractText
Verapamil is a widely prescribed calcium antagonist, but suffers from extensive first pass metabolism. Despite its frequent use in drug metabolism a complete understanding of its metabolic pathway is still lacking. We thus investigated verapamil's metabolism in cultures of primary rat hepatocytes and isolated metabolites from cell culture media by solid phase extraction (SPE). In detail, we investigated their structure in multiple liquid chromatography-mass spectrometry (LC-MSn) experiments and found 25 phase I and 14 phase II metabolites. We showed many metabolites to be produced by oxidative dealkylation, and several yet unknown metabolites were identified that stem from hydroxylation and dealkylation reactions. Furthermore, we identified an array of glucuronides and, additionally, a glucoside. Finally, we investigated the enantioselective biotransformation of verapamil and found preferential metabolism of the S-enantiomers. In conclusion, this illustrates again the true complexity of verapamil's disposition.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
1570-0232
pubmed:author
pubmed:issnType
Print
pubmed:day
25
pubmed:volume
798
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
265-74
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2003
pubmed:articleTitle
Metabolism of verapamil: 24 new phase I and phase II metabolites identified in cell cultures of rat hepatocytes by liquid chromatography-tandem mass spectrometry.
pubmed:affiliation
Department of Analytical Chemistry, Fraunhofer Institute of Toxicology and Experimental Medicine, 30625 Hannover, Germany.
pubmed:publicationType
Journal Article