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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
|
| pubmed:dateCreated |
1994-3-4
|
| pubmed:abstractText |
The disposition of [14C]salmeterol xinafoate, a new inhaled beta 2-adrenoceptor agonist with both bronchodilator and antiinflammatory activity, has been studied in laboratory animals and humans following intravenous and oral administration. [14C]Salmeterol was rapidly absorbed in animal species and humans with Cmax observed within 2 hr. Cmax was similar for normalized oral dose level in mice, rats, and rabbits. In dogs, Cmax was higher and reflected the greater oral bioavailability in this species. The plasma t1/2, after intravenous administration, was 5 hr in rats and 2 hr in dogs. The volume of distribution of salmeterol was significantly greater than total body water in both rats (40 liters/kg) and dogs (6 liters/kg) and indicated high tissue uptake of the compound. Plasma clearance was high in rats (95 ml/min/kg) and dogs (30 ml/min/kg). Radioactive drug-related material was widely distributed throughout body tissues in rats. The highest concentrations were present in kidney, liver, gastrointestinal tract, pituitary, lung, heart, and bone marrow. Transfer of radioactive drug-related material across the placental barrier or into milk, studied in rats, was low. In all species the majority of an oral or intravenous dose (55-75%) was excreted in feces. Biliary excretion in rats and dogs accounted for 53% (0-27 hr) and 40% (0-8 hr) of an oral dose, respectively, indicating good absorption across the gastrointestinal tract. Enterohepatic circulation was significant in rats. Salmeterol was cleared predominantly by metabolism in animals and humans.(ABSTRACT TRUNCATED AT 250 WORDS)
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Albuterol,
http://linkedlifedata.com/resource/pubmed/chemical/Bronchodilator Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Carbon Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/salmeterol
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| pubmed:status |
MEDLINE
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| pubmed:issn |
0090-9556
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
21
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1022-8
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| pubmed:dateRevised |
2004-11-17
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| pubmed:meshHeading |
pubmed-meshheading:7905380-Absorption,
pubmed-meshheading:7905380-Administration, Oral,
pubmed-meshheading:7905380-Adrenergic beta-Agonists,
pubmed-meshheading:7905380-Adult,
pubmed-meshheading:7905380-Albuterol,
pubmed-meshheading:7905380-Animals,
pubmed-meshheading:7905380-Bile,
pubmed-meshheading:7905380-Biological Availability,
pubmed-meshheading:7905380-Bronchodilator Agents,
pubmed-meshheading:7905380-Carbon Radioisotopes,
pubmed-meshheading:7905380-Dogs,
pubmed-meshheading:7905380-Feces,
pubmed-meshheading:7905380-Female,
pubmed-meshheading:7905380-Humans,
pubmed-meshheading:7905380-Injections, Intravenous,
pubmed-meshheading:7905380-Male,
pubmed-meshheading:7905380-Mice,
pubmed-meshheading:7905380-Mice, Inbred Strains,
pubmed-meshheading:7905380-Pregnancy,
pubmed-meshheading:7905380-Rabbits,
pubmed-meshheading:7905380-Rats,
pubmed-meshheading:7905380-Rats, Sprague-Dawley,
pubmed-meshheading:7905380-Tissue Distribution
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| pubmed:articleTitle |
Disposition of salmeterol xinafoate in laboratory animals and humans.
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| pubmed:affiliation |
Glaxo Group Research Ltd., Drug Metabolism III Department, Ware, Herts, UK.
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| pubmed:publicationType |
Journal Article
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