rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
5
|
pubmed:dateCreated |
1983-12-20
|
pubmed:abstractText |
The biotransformation of N-(6-phenoxyindan-5-yl)methansulphonamide (PMS) and of its 2',4'-difluoro derivative (DF-PMS) were studied in vitro using rat-liver homogenate followed by h.p.l.c. separation and mass-spectrometric identification of metabolites. Both sulphonamides were rapidly oxidized at positions 1 and 3. The pharmacokinetics of DF-PMS and of piroxicam were examined in the rat and monkey (Macaca fascicularis). Considerable concentrations were achieved in the plasma only by the 1-oxo metabolite of DF-PMS but not by the unchanged drug, indicating that the administered compound was a pro-drug of the active principle. 1-Oxo DF-PMS exhibited shorter half-lives, larger volumes of distribution and higher total clearance rates than piroxicam in the animal model studied.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0049-8254
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
13
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
265-72
|
pubmed:dateRevised |
2003-11-14
|
pubmed:meshHeading |
pubmed-meshheading:6636822-Animals,
pubmed-meshheading:6636822-Anti-Inflammatory Agents,
pubmed-meshheading:6636822-Biotransformation,
pubmed-meshheading:6636822-Chromatography, High Pressure Liquid,
pubmed-meshheading:6636822-Female,
pubmed-meshheading:6636822-Half-Life,
pubmed-meshheading:6636822-Indans,
pubmed-meshheading:6636822-Indenes,
pubmed-meshheading:6636822-Kinetics,
pubmed-meshheading:6636822-Liver,
pubmed-meshheading:6636822-Macaca fascicularis,
pubmed-meshheading:6636822-Piroxicam,
pubmed-meshheading:6636822-Rats,
pubmed-meshheading:6636822-Rats, Inbred Strains,
pubmed-meshheading:6636822-Thiazines
|
pubmed:year |
1983
|
pubmed:articleTitle |
Pharmacokinetics and biotransformation of methane sulphonanilides with anti-inflammatory activity in the rat and monkey--comparison with piroxicam.
|
pubmed:publicationType |
Journal Article
|