Health Systems and Tobacco Use

Pharmacotherapy for Smoking Cessation

The Role of Nicotine Receptors

Nicotinic receptors are normal structures in the brain (and elsewhere) of smokers and never smokers. Nicotinic receptors affect neurotransmitters (e.g. dopamine (α4β2), norepinephrine, serotonin, opioid peptides, etc.) in all people. When nicotine is present, it binds to receptors and disrupts normal activity.  Chronic nicotine use results in a permanent increase in the number of receptors in the brain.  The brain gets used to a new, "nicotine normal” level. Quitting smoking disrupts “nicotine normal” receptor activity.  This causes nicotine withdrawal symptoms.1

Without nicotine, receptor activity normalizes again in 3-6 months, but increase in receptors remains indefinitely.The increase in receptors is responsible for difficulty reducing amount smoked and quick relapse to former levels of smoking.2

The most common withdrawal symptoms are irritability and craving. Other symptoms may include depressed mood, sleep disturbance, difficulty concentrating, anxiety, restlessness, decreased heart rate, and increases appetite or weight gain.3

Nicotine Replacement Therapy (NRT)

NRT is used to help smokers get off nicotine slowly. The most commonly used types are nicotine patches, gum, and lozenges.  Less commonly used are the nicotine inhaler and nasal spray.  With these products, nicotine is released into the bloodstream (via the type of NRT) in order to help reduce physical withdrawal symptoms.  NRT works by replacing some of the nicotine from smoking at the receptor sites with nicotine from less harmful sources.3,4

For more information, please see the Clinical Guidelines for prescribing Pharmacotherapy for Smoking Cessation and the Pharmacologic Product Guide: FDA-Approved Medications for Smoking Cessation for usage guidelines and contraindications for NRT

Medications for Smoking Cessation

Bupropion (Zyban) is a non-nicotine prescription drug, the sustained-release form of the antidepressant Wellbutrin.  This “pill” is thought to stimulate dopamine and norepinephrine, brain chemicals that give smokers the sensation of alertness & energy.  It has been shown to help reduce the withdrawal symptoms such as cravings, irritability and depressed mood.3,5

Varenicline (Chantix) is a non-nicotine prescription drug developed specifically for smoking cessation.  It is not an antidepressant.  This “pill” releases dopamine but substantially less than with smoking.  Varenicline specifically targets the alpha-4 beta-2 (α4β2) nicotinic receptors, blocking the binding of nicotine from smoking.  It reduces the urge to smoke and reduces the pleasure derived from smoking.3,5

For more information please see the Pharmacologic Product Guide: FDA-Approved Medications for Smoking Cessation for usage guidelines and contraindications for Zyban & Chantix.

Trends in Pharmacotherapy Use

More and more smokers are using combination therapy (e,g patch & gum) or using NRT pre-cessation, or for longer periods of time. The FDA has acknowledged that this change in use patterns can be helpful for those trying to quit and pose no further risk of adverse health events.6


[1] U.S. Department of Health and Human Services. The Health Consequences of Smoking—50 Years of Progress: A Report of the Surgeon General. Atlanta: U.S. Department of Health and Human Services, Centers for Disease Control and Prevention, National Center for Chronic Disease Prevention and Health Promotion, Office on Smoking and Health, 2014

[2] Benowitz, Neal L. (2010). Nicotine Addiction. New England Journal of Medicine 362 (24): 2295–303. doi:10.1056/NEJMra0809890. PMC 2928221. PMID 20554984

[3] Fiore MC, Jaén CR, Baker TB, Bailey WC, Benowitz NL, Curry SJ, Dorfman SF, Froelicher ES, Goldstein MG, Froelicher ES, Healton CG, et al. Treating Tobacco Use and Dependence: 2008 Update—Clinical Practice Guidelines. Rockville (MD): U.S. Department of Health and Human Services, Public Health Service, Agency for Healthcare Research and Quality, 2008

[4] U.S. Food and Drug Administration (FDA). (2014, April 24). FDA 101: Smoking Cessation Products. Retrieved on 12/18/14 from: http://www.fda.gov/ForConsumers/ConsumerUpdates/ucm198176.htm

[5] U.S. Department of Health and Human Services. Reducing Tobacco Use: A Report of the Surgeon General. Atlanta: U.S. Department of Health and Human Services, Centers for Disease Control and Prevention, National Center for Chronic Disease Prevention and Health Promotion, Office on Smoking and Health, 2000

[6] Guide to Clinical Preventive Services, 2014: Recommendations of the U.S. Preventive Services Task Force. June 2014. Agency for Healthcare Research and Quality, Rockville, MD. Retrieved on 12/18/14 from, http://www.ahrq.gov/professionals/clinicians-providers/guidelines-recommendations/guide/index.html

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