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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1993-4-21
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pubmed:abstractText |
The pharmacokinetics of racemic (rac) felodipine, rac-nitrendipine and nifedipine (all given as an oral dose of 20 mg in solution) have been investigated in a randomised cross-over study in 12 healthy male subjects using stereoselective assays. Both felodipine and nitrendipine exhibited stereoselective pharmacokinetics. On average, the AUCs of the active (S)-enantiomers of felodipine and nitrendipine were 139% and 104% higher than those of their optical antipodes, but the elimination half-lives of the enantiomers of each racemate were not different. The AUCs of nifedipine, rac-felodipine, rac-nitrendipine and of their enantiomers were highly correlated (all r > 0.83), suggesting closely related rate limiting steps in the in vivo first-pass metabolism of these high-clearance drugs. Stereoselectivity was only a minor contributor to inter-individual variability in the oral pharmacokinetics of these compounds in healthy subjects.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Blood Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Felodipine,
http://linkedlifedata.com/resource/pubmed/chemical/Nifedipine,
http://linkedlifedata.com/resource/pubmed/chemical/Nitrendipine,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines
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pubmed:status |
MEDLINE
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pubmed:issn |
0031-6970
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
163-9
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8453961-Administration, Oral,
pubmed-meshheading:8453961-Adult,
pubmed-meshheading:8453961-Blood Proteins,
pubmed-meshheading:8453961-Double-Blind Method,
pubmed-meshheading:8453961-Felodipine,
pubmed-meshheading:8453961-Half-Life,
pubmed-meshheading:8453961-Humans,
pubmed-meshheading:8453961-Male,
pubmed-meshheading:8453961-Nifedipine,
pubmed-meshheading:8453961-Nitrendipine,
pubmed-meshheading:8453961-Pyridines,
pubmed-meshheading:8453961-Stereoisomerism
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pubmed:year |
1993
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pubmed:articleTitle |
Stereoselective pharmacokinetics of oral felodipine and nitrendipine in healthy subjects: correlation with nifedipine pharmacokinetics.
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pubmed:affiliation |
Center for Bio-Pharmaceutical Sciences, University of Leiden, The Netherlands.
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Randomized Controlled Trial,
Research Support, Non-U.S. Gov't
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