The nicotinic acetylcholine receptor partial agonist varenicline and the treatment of drug dependence: A review

Drug dependence is a chronic brain disease characterized by recurrent episodes of relapse, even when the person is motivated to quit. Relapse is a major problem and new pharmacotherapies are needed to prevent relapse episodes. The nicotinic acetylcholine receptor (nAChR) plays an important rote in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Stimulation of the nAChR has been found to alter and modulate cell firing in brain areas important for the maintenance of drug dependence. Varenicline, an alpha 4 beta 2 nAChR partial agonist and an alpha 7 nAChR full agonist registered for the treatment of nicotine dependence, significantly reduces nicotine craving and prevents relapse. In addition, varenicline reduces alcohol consumption in rats. Based on a review of the available literature, we hypothesize a potential rote for varenicline in the prevention of relapse in patients recovering from drug dependence other than nicotine dependence. (C) 2009 Elsevier B.V. and ECNP. All rights reserved.