Multiple-dose pharmacokinetics of the selective nicotinic receptor partial antagonist, varenicline, in healthy smokers / Helene Faessel (2006)

Public 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 : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=7930

Exemplaires (1)

Code-barres	Cote	Support	Localisation	Section	Disponibilité
TA 005471	TA 6.2.3.1.4 FAE M	Article/Périodique	Bibliothèque FARES	Tabac	Consultation sur place Exclu du prêt

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Single-dose pharmacokinetics of varenicline, a selective nicotinic receptor partial agonist, in healty smokers and no smokers / Helene Faessel (2006)

Public Titre : Single-dose pharmacokinetics of varenicline, a selective nicotinic receptor partial agonist, in healty smokers and no smokers Type de document : texte imprimé Auteurs : Helene Faessel, Auteur ; Bill J. Smith, Auteur ; Megan A. Gibbs, Auteur Editeur : Wiley Année de publication : 2006 Collection : Journal of Clinical Pharmacology, ISSN 0091-2700 num. Vol 46 Importance : p. 991-998 Présentation : tab., graph. Langues : Anglais (eng) Catégories : [TABAC] étude [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 alpha4beta2 nicotinic receptor partial agonist that is under development for smoking cessation. The primary objectives of this double-blind, placebo-controlled, single-dose, dose-escalation study were to determine the clinical pharmacology of single doses of varenicline in healthy smokers and nonsmokers under fed and fasted conditions and to determine the clinical pharmacology of varenicline administered in the morning and in the evening to smokers. Within each subject group, 4 subjects were randomized to varenicline and 2 subjects to placebo. Subjects received one single oral administration of varenicline or placebo: 6 doses (0.01, 0.03, 0.1, 0.3, 1.0, and 3.0 mg) were investigated in nonsmokers and 7 doses in smokers (0.01, 0.03, 0.1, 0.3, 1.0, 3.0, and 10.0 mg). Varenicline was well tolerated after single doses up to 3.0 mg in smokers and 1.0 mg in nonsmokers. Nausea and vomiting at doses above 3.0 mg in smokers and 1.0 mg in nonsmokers were dose limiting. Systemic exposure to varenicline and pharmacokinetic variability were similar between smokers and nonsmokers. Coadministration with food, smoking restriction, and time-of-day dosing did not affect the pharmacokinetics of varenicline. Permalink : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=7945

Exemplaires (1)

Code-barres	Cote	Support	Localisation	Section	Disponibilité
TA 005486	TA 6.2.3.1.4 FAE S	Article/Périodique	Bibliothèque FARES	Tabac	Consultation sur place Exclu du prêt

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