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Drug Metabolism and Disposition
ISSN :
0090-9556
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Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro / R. Scott Obach (2006)
Titre : Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro Type de document : texte imprimé Auteurs : R. Scott Obach, Auteur ; Anne E. Reed-Hagen, Auteur ; Suzanne S. Krueger, Auteur ; Beth J. Obach, Auteur Editeur : American Society for Pharmacology and Experimental Therapeutic Année de publication : 2006 Collection : Drug Metabolism and Disposition, ISSN 0090-9556 num. 34:1 Importance : p. 121-130 Présentation : tab., graph. Langues : Anglais (eng) Catégories : [TABAC] étude
[TABAC] sevrage tabagique:méthode de sevrage:méthode individuelle:approche pharmacologique:varéniclineIndex. décimale : TA 6.2.3.2 Autres produits Résumé : he metabolism and disposition of varenicline (7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine), a partial agonist of the nicotinic acetylcholine receptor for the treatment of tobacco addiction, was examined in rats, mice, monkeys, and humans after oral administration of [14C]varenicline. In the circulation of all species, the majority of drug-related material was composed of unchanged varenicline. In all four species, drug-related material was primarily excreted in the urine. A large percentage was excreted as unchanged parent drug (90, 84, 75, and 81% of the dose in mouse, rat, monkey, and human, respectively). Metabolites observed in excreta arose via N-carbamoyl glucuronidation and oxidation. These metabolites were also observed in the circulation, in addition to metabolites that arose via N-formylation and formation of a novel hexose conjugate. Experiments were conducted using in vitro systems to gain an understanding of the enzymes involved in the formation of the N-carbamoylglucuronide metabolite in humans. N-Carbamoyl glucuronidation was catalyzed by UGT2B7 in human liver microsomes when incubations were conducted under a CO2 atmosphere. The straightforward dispositional profile of varenicline should simplify its use in the clinic as an aid in smoking cessation. Permalink : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=8368 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité TA 005999 TA 6.2.3.2 OBA M Article/Périodique Bibliothèque FARES Tabac Consultation sur place
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