| Titre : |
Multiple-dose pharmacokinetics of the selective nicotinic receptor partial antagonist, varenicline, in healthy smokers |
| Type de document : |
texte imprimé |
| Auteurs : |
Helene Faessel, Auteur ; Megan A. Gibbs, Auteur ; David J. Clark, Auteur ; Kevin Rohrbacher, Auteur ; Marilyn Stolar, Auteur ; Aaron H. Burstein, Auteur |
| Editeur : |
Wiley |
| Année de publication : |
2006 |
| Collection : |
Journal of Clinical Pharmacology, ISSN 0091-2700 |
| Importance : |
9 p. |
| Langues : |
Anglais (eng) |
| Catégories : |
[DIVERS] discipline médicale, paramédicale et scientifique:pharmacologie
[TABAC] sevrage tabagique:méthode de sevrage:méthode individuelle:approche pharmacologique:varénicline
|
| Index. décimale : |
TA 6.2.3.1.4 Autres substituts nicotiniques |
| Résumé : |
Varenicline is a novel and selective α4β2 nicotinic acetylcholine receptor partial agonist developed for smoking cessation. The primary objectives of this double-blind, placebo-controlled, dose-escalation study were to determine the pharmacokinetics, safety, and tolerability of multiple oral doses of varenicline given as tablets once (1 mg, 2 mg, and 3 mg) or twice (1 mg) daily to healthy adult smokers. Within each dose level, 8 subjects were randomized to varenicline and 4 subjects to placebo. Varenicline was well tolerated at doses up to and including 2 mg daily. Dose-proportional increases in maximum observed plasma concentrations and area under the plasma concentration-time curve from time zero to the end of the dosing interval values were observed between the 1-mg and 2-mg daily doses of varenicline. Once- and twice-daily dosing resulted, on average, in an approximate 2- and 3-fold increase in varenicline systemic exposure, respectively, compared with single dose. There was no evidence of concentration- or time-dependent changes in the pharmacokinetics of varenicline upon repeat dosing. |
| Permalink : |
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Multiple-dose pharmacokinetics of the selective nicotinic receptor partial antagonist, varenicline, in healthy smokers (2006)
