Multiple-Dose Pharmacokinetics of the Selective Nicotinic Receptor Partial Agonist, Varenicline, in Healthy Smokers

Abstract
Curve from time zero to the end of the dosing interval val- ues 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.