Kicking Butts: Using Drugs to Quit Smoking

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Editor's note: People sometimes think of smoking as little more dangerous than countless other bad habits, so the idea of quitting through nicotine replacement therapy or pharmaceuticals that combat nicotine cravings may strike some as counterintuitive as though it were a mere switching from one substance to another. But smoking kills about a third of users and has many other negative health effects (see ACSH's book about Cigarettes), while drugs to aid smoking cessation just might save your life. The most common such drugs are described in this excerpt from ACSH's book Kicking Butts in the Twenty-First Century: What Modern Science Has Learned About Smoking Cessation. TS

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Bupropion SR (sustained-release) was the first non-nicotine medication approved to treat tobacco dependence. This drug, which is also used as an antidepressant, was made available by prescription for smoking cessation purposes in 1997, under the brand name Zyban. Researchers presume that blocking reuptake of the neurotransmitters dopamine and/or norepinephrine is what makes this drug effective; however, this has not been definitively established. Bupropion is considered a first-line therapy because it has been proven effective in helping smokers quit; research shows that using bupropion can nearly double quit rates compared to placebo. This is equivalent to the benefit achieved with nicotine replacement therapy (NRT).

Users are advised to begin taking bupropion approximately 1-2 weeks before they plan to quit, as this is the amount of time required to achieve a steady blood level of the medication. The recommended dose is 150 mg daily for 3 days, then 150 mg twice daily (for a daily total of 300 mg) for up to 12 weeks. For maintenance therapy, bupropion can be used for up to 6 months, which is the FDA-approved duration. However, new research shows that using the medication for up to 12 months is both safe and effective at preventing relapse. Treatment duration should be discussed with a doctor and geared towards the individual's progress. However, those not making significant progress in quitting by the seventh week should consider discontinuing the attempt and stop taking bupropion.

Bupropion offers many benefits to those trying to quit. Because bupropion treatment must be initiated before the quit attempt, it prepares a smoker's body for the actual stress of quitting. Many people like bupropion because it is an alternative to traditional nicotine replacement, or because they have previously tried NRT without success. Further, this therapy comes in the form of a twice-daily pill, which is an easy regimen to follow. Another benefit of bupropion is that the side effects are minimal. The most common side effects are insomnia (in 35-40% of users) and dry mouth (10%). Users can minimize the risk of insomnia by abstaining from a dose near bedtime or by taking it much earlier in the afternoon or evening (though doses should be taken in intervals of at least 8 hours). Less common side effects include shakiness, skin irritations, headaches, and dizziness.

The major drawback of bupropion is that people with a history of seizures or eating disorders and those taking a monoamine oxidase (MAO) inhibitor or another medication containing bupropion (such as Wellbutrin to treat depression) should not use bupropion for smoking cessation purposes. In addition, similar to recommendations for NRTs, pregnant and lactating women should be encouraged to quit first and consider bupropion only when the prospect of quitting without it is minimal. Although there is no evidence of danger to a fetus or nursing infant, women who are pregnant or lactating should check with a physician prior to starting this or any other medication. The average cost of bupropion is approximately $4.00 per day, plus any necessary doctor's or prescribing fee.

Second-Line Medications

There are also two second-line medications that may be helpful to smokers clonidine and nortryptyline in addition to or instead of nicotine replacement therapy. Second-line medications have evidence of being effective in helping smokers to quit; however they are not FDA-approved specifically for tobacco dependence treatment and have an increased potential for side effects compared to first-line therapies. These treatments should be explored on a case-by-case basis and only after first-line medications have been utilized and determined ineffective. As with first-line therapies, pregnant and lactating women should first be encouraged to quit without pharmacologic treatment and to use these medications only if the chances of quitting without them are minimal.

Clonidine (Catapres)

Clonidine is a prescription medication used primarily for treating high blood pressure. However, studies show that clonidine can be effective in treating tobacco dependence and nearly doubles quit rates compared to placebo. Clonidine can be administered orally or via a skin patch, and although an official dosing regimen for smoking cessation has not been established, the preliminary recommendation is 0.10 mg daily, increasing by 0.10 mg/day per week if needed, for 3-10 weeks. Users should begin the medication 3 days prior to quitting. Users should not stop taking clonidine abruptly because side effects such as dry mouth, drowsiness, dizziness, headaches, and sedation may occur. Rebound hypertension (rapid increase in blood pressure) may occur if the medication is stopped abruptly. Instead, users should taper the dose over a period of a few days before discontinuing treatment. The average cost of clonidine is $0.24 per day.

Nortriptyline HCI (Aventyl, Pamelor)

This prescription medication is FDA-approved as an antidepressant. Like bupropion, which is also an antidepressant, it has been shown to be effective in helping smokers quit. Treatment is initiated 10 to 28 days prior to quitting, at a recommended dosage of 25 mg per day initially, increasing to 75-100 mg per day, for a duration of 12 weeks. Common side effects include sedation, dry mouth, blurred vision, urinary retention, lightheadedness, and shaky hands. Because of the sedative effect of nortriptyline, users should take extra caution while driving and operating machinery. Also, because this medication increases the risk of arrhythmias, patients with cardiovascular disease should discuss the use of nortriptyline thoroughly with their doctors. The risk of overdose is high and the drug may produce cardiotoxic effects. The average cost is $0.74 per day.