Can the use of varenicline improve the efficacy of pharmacotherapy for nicotine addiction?

Rafał Mazur 1 , Sebastian Masternak 1 , Michał Pająk 1 , Nikodem Skoczeń 2 , Ewelina Soroka 2  and Marcin Olajossy 2
  • 1 Student Scientific Association by the II Department of Psychiatry and Psychiatric Rehabilitation, Medical University of Lublin
  • 2 II Department of Psychiatry and Psychiatric Rehabilitation, Medical University of Lublin


Introduction: Smoking is a huge medical and social problem in Poland, with as many as about 24% of Poles being addicted to nicotine. Approximately 6 million people worldwide die every year from conditions that are closely related to tobacco addiction, such as cancer and cardiovascular, metabolic or lung diseases. The difficulty in combatting nicotine dependence is largely due to the complex mechanism of this addiction. The motivation of a patient to quit smoking is of great importance in the difficult withdrawal process. Strengthening this motivation is one of the most important tasks of physicians and addiction therapists.

Overview of literature: Nicotine replacement therapy (NRT) has been the most widely known way to break away from smoking addiction for many years now. It involves delivering nicotine to the body in ways that are less harmful than through tobacco smoke. As a consequence, the cravings for nicotine are reduced, making it easier for the patient to break with the addiction. Clinical trials have shown that the use of NRT is associated with a 50-70% increased chance of maintaining abstinence from smoking compared to placebo. There are many NRT products, including nicotine chewing gum, nicotine patches, lozenges, dissolvable nicotine sticks, or inhalers. Bupropion is a selective dopamine–noradrenaline reuptake inhibitor. This drug is one of the most commonly used in the pharmacotherapy of depression in the United States. At the same time, it has been found to have a positive effect on people trying to break up with the habit of smoking cigarettes. The mechanism of action remains unknown in this case, but studies clearly indicate the efficacy of bupropion, which is comparable to the efficacy of NRT. Varenicline is a partial agonist selective for α4β2 nicotinic acetylcholine receptors. It has a higher affinity for these receptors than nicotine. By stimulating them, it causes an increase in dopamine secretion (but to a lesser extent than cigarette smoking), helping in this way ease withdrawal symptoms.

Conclusions: Varenicline has higher efficacy than bupropion and NRTs. Simultaneous use of two NRT forms increases the effectiveness of this method to a level comparable to varenicline. Contrary to previous reports, it seems that varenicline does not increase self-aggressive behaviour and the risk of suicide. The effectiveness of antinicotinic drugs depends on the sex of the patient. For both sexes, the most effective drug is varenicline. It is slightly more effective in women than in men. By contrast, NRT and bupropion show greater therapeutic potential in men.

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