Tobacco smoking is widespread and is one of the world’s most prevalent modifiable risk factors for morbidity and mortality. It is important to facilitate smoking cessation better in order to reduce the health consequences of tobacco use. The most effective approach assisting smokers in their quit attempts combines both pharmacotherapy and nonpharmacological interventions. This review summarizes the latest international epidemiological data available on tobacco use, considers the associated effects on health, and reviews existing policies against tobacco use. Among the interventions for smoking cessation, the three major pharmacotherapies (which have demonstrated efficacy when combined with behavioral support) are discussed: nicotine replacement therapy (NRT), bupropion, and varenicline. As the newest pharmacotherapy made available in this area, particular consideration is given to varenicline, and a review of our clinical experience is offered.