Stop Smoking Medications to Help You Stay Quit

Editor's Note: This article was originally written by patient expert Carol Southard.

An updated clinical practice guideline released by the U.S. Public Health Service on May 7, 2008, identified new medication treatments that are effective for helping people quit smoking. No matter the level of addiction, anyone attempting to quit should consider trying at least one or more of the effective pharmacotherapies. The goal of cessation pharmacotherapy is to alleviate or diminish the symptoms of withdrawal. The more physically comfortable one is, the more likely the smoker will make a serious quit attempt and succeed in permanently quitting. Currently, the FDA-approved, first-line agents for smoking cessation include five nicotine replacement therapy (NRT) products and two non-nicotine medications. All of these medications were found to be effective first-line medications in the guideline's meta-analyses. There is no question that the odds of a smoker quitting are increased by using a pharmacological treatment.

In addition, multiple combinations of medications were shown to be effective. For the first time, the 2008 guideline update has assessed the relative effectiveness of cessation medications. These comparisons showed that two forms of pharmacotherapy, varenicline (Chantix) used alone and the combination of a long term nicotine patch plus ad lib (i.e., as needed) nicotine nasal spray or gum, produced significantly higher long term quit rates that did the patch by itself. This is "off label" use but now it is definitively medically sanctioned. (I have been encouraging my own clients to use multiple NRT products for years!)

There are five nicotine replacement therapy (NRT) products on the market the United States. The nicotine gum first appeared in 1984 and the nicotine patch was made available in 1994. Between 1995 and 1996 both became available without prescription. This resulted in the largest increase in smoking cessation since the 1964 Surgeon General's report on smoking. Two NRT products are still only attainable through prescription. The Nicotrol Nasal Spray appeared in 1996 and the Nicotrol Inhaler in 1998. The final NRT product to materialize, obtainable without prescription, is the nicotine lozenge which has been on the market since 2002.

Almost all researchers agree that nicotine is not a carcinogen and there is growing consensus that nicotine derived from medications does not promote cardiovascular disease. All of the NRT formulations are associated with slower onset and much lower nicotine levels than are cigarettes and of course they do not produce carbon monoxide, toxins, and carcinogens. The safety and abuse records of NRT have been excellent. The choice of NRT should be individualized - based on preference, past experience, smoking dependence and habits.

The labeling on NRT still instructs tobacco users to consult their clinician if there is a history of heart disease, ulcers, or hypertension or with pregnancy or breast feeding. But the only medical contraindications in the guideline are:

  • Immediate myocardial infarction (< 2 weeks)

  • Serious arrhythmia

  • Serious or worsening angina pectoris

  • Accelerated hypertension

There is a documented lack of an association between NRT and acute cardiovascular events in persons who continue to smoke while on the patch as well as in those who have had past cardiac events! The guideline recommends use of NRT in pregnancy if other therapies have failed. Clearly, the fetus is exposed to significantly less nicotine with NRT than with smoking and most importantly is not exposed to carbon monoxide, carcinogens and toxins from cigarettes.

Light smoking has become more common, perhaps due to smoking restrictions and increases in the price and taxation of tobacco products. Many light smokers have a strong dependence even though they smoke relatively few cigarettes. They are less likely to receive treatment than are heavier smokers but anecdotal evidence shows an increase in success rates for light smokers with use of NRT. At the other end of the spectrum, higher than recommended doses may be indicated in tobacco users with severe addiction. Failure to respond to NRT products may reflect inadequate dosage, incorrect usage, or both.

There are two non-nicotine medications available to tobacco users as well. Buproprion (Zyban), an atypical antidepressant, has been shown to double quit rates. It blocks the reuptake of dopamine and norepinephrine in the central nervous system which modulates the dopamine reward pathway and reduces cravings for nicotine and symptoms of withdrawal. It is effective in those whether or not this is current or past depressive symptoms. Combining bupropion with NRT often increases success rates over buproprion used alone.

The most recent non-nicotine medication is Varenicline (Chantix), a partial agonist selective for a specific nicotine receptor subtype, was approved in 2006. The drug's efficacy is believed to be the result of a sustained, low-level agonist activity at the receptor site, combined with competitive blockade of nicotine binding. The partial agonist activity modestly stimulates receptors, leading to increased dopamine levels that reduce nicotine withdrawal symptoms. By blocking the binding of nicotine to receptors in the central nervous system, Varenicline inhibits the surge of dopamine release that occurs immediately (7 to 10 seconds) following each inhalation of tobacco smoke. This effect may help prevent relapse by reducing or even eliminating the pleasure linked with smoking. Evidence suggests that using Varenicline can increase successful quitting 3 times more when compared to placebo.