Nicotine Addiction Medication

Updated: Jul 16, 2018
  • Author: R Gregory Lande, DO, FACN; Chief Editor: Glen L Xiong, MD  more...
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Medication

Medication Summary

Two types of pharmacologic therapy are available as part of a smoking cessation program nicotine and antidepressants. The goals of pharmacotherapy are to induce smoking cessation, reduce morbidity, and prevent complications.

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Smoking Cessation Aids

Class Summary

Nicotine replacement therapy (NRT) is available in the form of cutaneous patches, inhaled or nasal delivery, or chewing gum. Nicotine patches are sold under various trade names (see below). For each proprietary system, the dosing schedule involves a graduated decrease of the drug dose over 9-12 weeks.

Nicotine acetylcholine receptor partial agonists are also used as smoking cessation aids. They bind to nicotine receptors and elicit mild central effects to ease nicotine withdrawal symptoms. They also decrease the stimulatory effect of nicotine consumption by blocking nicotine receptors.

Nicotine transdermal system (NicoDerm CQ, Nicorette, Thrive, Nicotrol Inhaler, Nicotrol NS, Nicorelief)

Nicotine stimulates all autonomic ganglia and catecholamine discharge in the adrenal medulla at small doses. At larger doses transmission through autonomic ganglia is blocked and catecholamine discharge from the medulla is inhibited.

Nicotine replacement therapy works best when used in conjunction with a support program, such as counseling, group therapy, or behavioral therapy.

Nicotine chewing gum, if chewed correctly, increases quit rates up to 2-fold. At 1 year, the abstinence rate with the patch is 20%. At 4 years, the abstinence rate is 12.4%, as opposed to 4.5% with placebo. Nicotine patches are sold under various trade names (see below). For each proprietary system, the dosing schedule involves a graduated decrease of the drug dose over 9-12 weeks.

Nicotine gum is marketed in 2 strengths, 2 mg and 4 mg. Individuals who smoke 1 pack per day should use the 4-mg pieces; those who smoke less than 1 pack per day should use the 2-mg pieces. Instruct the patient to chew hourly and for their initial cravings for 2 weeks, then gradually reduce the amount chewed over the next 3 months.

The nicotine nasal spray and the inhaler dosage forms provide nicotine delivery through the nasal and oral mucosa, respectively.

The nicotine in nicotine polacrilex is absorbed through the oral mucosa. Absorption is quick and closely approximates the time course of plasma nicotine levels observed after cigarette smoking.

Intranasal nicotine and nicotine from an oral inhaler may closely approximate the time course of plasma nicotine levels observed after cigarette smoking.

Varenicline (Chantix)

Varenicline is a partial agonist that is selective for alpha-4, beta-2 nicotinic acetylcholine receptors. Its action is thought to result from activity at a nicotinic receptor subtype, where its binding produces agonist activity while simultaneously preventing nicotine binding. Its agonistic activity is significantly lower than that of nicotine. It also elicits moderate affinity for serotonin receptors. Maximum plasma concentrations occur within 3-4 hours after oral administration. With regular dosing, a steady state is reached within 4 days.

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Antidepressants, Other

Class Summary

These medications ameliorate withdrawal symptoms while the smoker deals with behavioral aspects of smoking cessation.

Bupropion is used as a non–nicotine-containing aid to smoking cessation. It acts by enhancing central nervous nonadrenergic function. A 23% sustained cessation rate is achieved with bupropion tablets at 1 year, compared with a 12% sustained cessation rate with placebo. Bupropion also is effective for patients in whom nicotine replacement therapy fails.

Bupropion hydrochloride (Zyban, Aplenzin, Fortivo XL, Wellbutrin XL)

Bupropion is used in conjunction with a support group, behavioral counseling, or both. It may also be used in combination with nicotine replacement therapy. It inhibits neuronal dopamine reuptake, in addition to being a weak blocker of serotonin and norepinephrine reuptake. For any given dosage form use the same total daily dose but adjust frequency as indicated for immediate (3-4 times daily), sustained release (twice daily), or extended release (once daily).

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