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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
|
pubmed:dateCreated |
1984-9-6
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pubmed:abstractText |
Premazepam, a pyrrolodiazepine with potential anxiolytic properties, behaves as a partial antagonist to diazepam in animal tests. Its pharmacokinetics and metabolism were studied in four healthy volunteers. After oral administration of 30 mg [6-14C] premazepam, the plasma levels of total radioactivity reached maximum concentrations 1-4 h (mean 2 h) following administration. The plasma curve was described by an open one-compartment model, and half-life was 11.5 +/- 1.3 h. Levels of the unchanged compound accounted for about 80% of the total radioactivity up to 24 h. Half-life of the unchanged compound was 7.9 +/- 1.2 h. On the average, 89.6% of the administered radioactivity was recovered in the urine and 2.3% in the feces during the 5 days following administration. Unchanged premazepam accounted for about 70% of the total radioactivity excreted in the urine. Of the three metabolites identified in the urine, none was active in vitro in displacing 3H-diazepam from its forebrain receptors in the rat, indicating that only the parent compound has definite pharmacologic activity.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0174-4879
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
22
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
273-7
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:6146571-Adult,
pubmed-meshheading:6146571-Anti-Anxiety Agents,
pubmed-meshheading:6146571-Azepines,
pubmed-meshheading:6146571-Biotransformation,
pubmed-meshheading:6146571-Feces,
pubmed-meshheading:6146571-Half-Life,
pubmed-meshheading:6146571-Humans,
pubmed-meshheading:6146571-Kinetics,
pubmed-meshheading:6146571-Male
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pubmed:year |
1984
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pubmed:articleTitle |
Pharmacokinetics and metabolism of premazepam, a new potential anxiolytic, in humans.
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pubmed:publicationType |
Journal Article
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