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. 2011 Jul;6(1):4–16.

TABLE 1.

FDA-Approved and Investigational Smoking-Cessation Medications Targeting Nicotinic Acetylcholine Receptors

MEDICATIONS/COMPOUNDS MECHANISM STATUS REFERENCE
Nicotine replacement therapies* Replace nicotine obtained from tobacco smoke through the use of safer options FDA approved Nides, 2008
Varenicline Partial α4β2 nAChR agonist
Acts as an antagonist in the presence of nicotine to decrease the reinforcing effects of nicotine
Activates nicotinic receptors during abstinence and limits the aversive effects associated with nicotine withdrawal
FDA approved Gonzales et al., 2006
Mecamylamine Nonselective nicotinic receptor antagonist Utility limited due to non-selective action Schnoll and Lerman, 2006
*

Nicotine patch, gum, inhaler, microtab, nasal spray, and lozenge.